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Top Level Index

Gastrointestinal tract / Alimentary system

Antibiotics

Antidiabetic & pcos

Cardiovascular system

Central nervous system

Contraceptive agents

Dermatologicals

Opthalmic

Genito-urinary tract

Hormones

Immunology

Metabolism

Musculo - skeletal disorder

Oncology

Oropharyngeal

Respiratory system & anti- allergics

Supplementation

Surgical & Vaccines

Veterinary list

We manufacture

 

Index / Table of Content

Gastrointestinal tract / Alimentary system
Antacids, Antireflux Agents & Antiulcerants Homatropine Methylbromide
Mesalazine
Rebamipide
Sucralfate
Magaldrate
Constipation & Bowel Cleansers Docusate Sodium
Prucalopride Succinate
Bisacodyl
Dissolution Of Cholestrol - Rich Gallstones Ursodeoxycholic Acid
Drug Modifying Intestinal Motility & Acid Secretions Hyoscine Butylbromide
Metoclopramide
Mosapride citrate
H2 Blockers & Ulcer Healing Drugs Esomeprazole
Lansoprazole
Omeprazole
Pantoprazole
Ranitidine
Rabeprazole sodium
Non Specific Antidiarrhoeal Agents Loperamide
Racecadotril
Rifaximin
Trimethoprim
Probiotics Saccharomyces Boulardii
Prokinetic Agent Cisapride Monohydrate
  Mosapride Citrate
   
Antibiotics
Anthelmintics Albendazole
Febantel
Mebendazole
Nitazoxanide
Antifungals Anidulafungin
Eberconazole
Fluconazole
Ketoconazole
Luliconazole
Micafungin
Sodium Posaconazole
Tavaborole
Itraconazole
Antimalarial Drug Lumefantrine
Antiretroviral Abacavir Sulphate
Atazanavir
Efavirenz
Darunavir (Amorphous / Ethanolate)
Dolutegravir Sodium
Indinavir Sulphate
Oseltamivir
Rilpivirine HCl
Ritonavir
Saquinavir
Simeprevir
Tenofovir
Antivirals Acyclovir
Lamivudine
Valacyclovir
Valganciclovir
Beta-Lactam Faropenem Sodium
Carbapenem Doripenem
Ertapenem
Imipenem with cilastatin (Imipenem/cilastatin)
Meropenem Trihydrate
Drugs used in Ornidazole Protozoal Infections Tinidazole
Metronidazole Benzoate
Glycopeptide Antibacterial Teicoplanin
Macrolides Azithromycin
Erythromycin
Fidaxomici
Oxazolidinones Linezolid
Penicillins Amoxycillin
Ampicillin
Ampicillin with Sulbactam Sodium
Cloxacillin
Pienicillin-G-Amidase Enzyme
Piperacillin with Tazobactam
Quinolones Ciprofloxacin
Garenoxacin
Levofloxacin
Marbofloxacin
Ofloxacin
Sparfloxacin
Tetracyclines Tigecycline
   
Antidiabetic & pcos
Antidiabetic Agents Repaglinide
Metformin HCl
Diabetic Neuropathy Epalrestat
Tapentadol HCl
DPP-4 Inhibitor (Gliptin) Alogliptin
Teneligliptin
Gestational Diabetes Inositol
PCOS D-Chiro-Inositol
SGLT-2 Inhibitor (Gliflozin) Canagliflozin
   
Cardiovascular system
Alpha/Beta Adrenoceptor Agonist Carvedilol HCl / Phosphate
Eplerenone
Fenoterol HBr
Icatibant Acetate
Imiquimod
Isoprenaline HCl
Levosalbutamol HCl / Sulphate
Levosalbutamol Tartrate
Macitentan
Ractopamine HCl
Silodosin
Tizanidine HCl
Tulobuterol Base / HCl
Anti-Anginal Drug Amlodipine
Isosorbide 5 MonoNitrate
Isosorbide DiNitrate / MonoNitrat
Ivabradine
Nifedipine
Pazopanib
Antianemic Agent Ferrous Bisglycinate
Antiarrhythmic Drugs Amiodarone HCl
Diltiazem
Dronedarone
Lidocaine (Lignocaine)
Anticoagulants Dabigatran Etexilate
Enoxaparin
Warfarin Sodium Clathrate
Antihypertensives Cilnidipine
Irbesartan
Losartan Potassium
Moexipril
Sodium Nitroprusside
Atorvastatin Calcium
Rosuvastatin Calcium
Antiparkinsonian Drugs Levodopa
Antiplatelet Drugs Clopidogrel
Attention Deficit Hyperactivity Disorder (ADHD) Clonidine HCl
Beta Blockers Atenolo
Labetalol
Metoprolol
Moxonidine
Nadolol
Propranolol
S - Metoprolol Succinate
Cardiovascular Energizers Coenzyme Q 10
Cerdiac Glycosides Digoxin
Diuretics Frusemide
Hydrochlorothiazide
Indapamide
Telmisartan
Furosemide
Idiopathic Pulmonary Fibrosis Pirfenidone
Peripheral Vasodilators Cinnarizine
Ginkgo Biloba
Papaverine HCl
Vasopressors Phenylephrine
   
Central nervous system
Anti-Emetics & Antinauseants Domperidone
Fosaprepitant
Granisetron
Metoclopramide
Ondansetron Di HCl
Prochlorperazine
Trifluoperazine
Trimethobenzamide
Antiarrhythmic Agent Haloperidol
Anticovulsants Carbamazepine
Divalproex
Felbamate
Fosphenytoin Sodium
Gabapentin
Lamotrigine
Levetiracetam
Phenytoin Sodium
Pregabalin
Retigabine
Sodium Valproate
Topiramate
Valproic Acid
Vigabatrin
Antimanic Drugs Haloperidol
  Quetiapine Fumarate
Antipsychotics Aripiprazole
Iloperidone
Lurasidone
Zotepine
Drugs to control Rigidity & Tremors Selegiline
Drugs used to treat Migraine Flunarizine
Frovatriptan
Sumatriptan
Drugs used in Peripheral Neuropathy Benfotiamine
Mecobalamin / Methylcobalamin
Hepatic Encephalopathy Amino Acids
Insomnia Eszopiclone
Ramelteon
Zolpidem Tartrate
Multiple Sclerosis Fingolimod
Neuroleptic Agent Amisulpride
Neuropathic Pain Carbamazepine
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) Ibuprofen
Nabumetone
Naproxen Sodium
Sedatives & Tranquillisers Alprazolam
Diazepam
Tricyclic & Related Antidepressants Agomelatine
Brexpiprazole
Cinitapride Hydrogen Tartrate
Citalopram
Dothiepin HCl
Escitalopram
Fluoxetine Hydrochloride
Milnacipran
Nortriptyline
Sertraline HCl
Imipramine
Trimipramine Maleate
Vilazodone
Amitriptyline HCl
   
Contraceptive agents
Oral Contraceptives Ulipristal Acetate
   
Dermatologicals
Anti- Infective Skin Preparations Acyclovir
Polymyxin B Sulfate
Silver Sulfadiazine
Selenium Sulphide
Antipruritic Crotamiton
Antipsoriasis Acitretin
Dimethyl Fumarate
Methoxsalen
Corticosteroid Responsive Methylprednisolone & Salts
Drugs for Acne Vulgaris Adapalene
Melanizing Agents Trioxsalen
Topical Antifungals & Anti-Parasitics Sertaconazole Nitrate
Terbinafine
Topical Steroids Betamethasone
Fluticasone Propionate
Mometasone Furoate
   
Opthalmic
Anti- Infective Eye Preparations Acyclovir
Fluconazole
Anti- Inflammatory & Anti Allergic Preparations Ketorolac Tromethamine
Sodium Cromoglycate
   
Glaucoma Bimatoprost
Dorzolamide
Timolol Maleate
Mydriatics & Cycloplegics Phenylephrine
 
Genito-urinary tract
Androgen & Anabolic Steroid (AAS) Stanozolol
Erectile Dysfunction Sildenafil Citrate
Hyperphosphatemia Sevelamer HCl / Carbonate
Sucroferric Oxyhydroxide
Intravenous Pyelogram (IVP) Diatrizoate Sodium / Meglumine
Diatrizoic Acid
Urinary Tract Analgesics & Antispasmodics Adiphenine HCl
Drotaverine HCl
Phenazopyridine
Trospium Chloride
Urinary Tract Infections Fosfomycin Trometamol
Uterine Stimulants Ritodrine Hydrochloride
 
Hormones
Corticosteroids & Related Drugs Deflazacort
Hyper & Hypoglycaemics Glibenclamide
  Glimepiride
Thyroid Hormones Levothyroxine Sodium
Liothyronine Sodium
Vitamin D Analogs Calcitriol
 
Immunology
Immuno-Suppressants Everolimus
Mycophenolic Mofetil / Sodium
Pimecrolimus
Thalidomide
Multiple Sclerosis Teriflunomide
 
Metabolism
Anti- Obesity Cetilistat
Ezetimibe
Drugs used in Gout Colchicine
Febuxostat
Probenecid
Hepatitis C (HCV) Daclatasvir Dihydrochloride
Ledipasvir
Sofosbuvir
Telaprevir
Wilson’s Disease Trientine HCl
 
Musculo - skeletal disorder
Arthritis Celecoxib
Diacerein
Risedronate
Sulfasalazine
Zinc Bisglycinate
Muscular Dystrophy, Duchenne Oxatomide Anhydrouse / Monohydrate
Muscle Relaxants Flavoxate HCl
Meprobamate
Methocarbamol
Thiocolchicoside
Tofisopam
Muscle Spasms Baclofen
Nonopioid Analgesics Carbamazepine
Etodolac
Glucosamine Sulphate
Indomethacin
Ketorolac Tromethamine
Leflunomide
Meloxicam
Nimesulide
Oxcarbazepine
Paracetamol / DC Grade
Piroxicam
Opioid Analgesics Tramadol Hydrochloride
Osteoporosis Alendronate Sodium
  Ambroxol HCl/Base
   
Oncology
Antimucositis Rutoside
Antineoplastic Agents Irinotecan HCl
Mitomycin
Bladder,Kidney & other Urologic Cancers Sunitinib
Brain Cancer, Head and Neck Cancer, Lung Cancer, Ovarian Cancer & Neuroblastoma Carboplatin
Chemotherapeutic Agents Azacitidine
Cisplatin
Dactinomycin
Diminazene Aceturate
Doxorubicin
Epirubicin
Gemcitabine HCl
Palbociclib
Risedronate
Colorectal Cancer Oxaliplatin
Hormone Therapy Letrozole
Leukemias,Lymphomas & other Hematologic Cancers Romidepsin
Multiple Myeloma Bortezomib
Carfilzomib
Prostate Cancer Cabazitaxel
Enzalutamide
Renal Cell Carcinoma (RCC) Temsirolimus
 
Oropharyngeal
Nasal Decongestants Fluticasone Propionate / Furoate
Phenylephrine
 
Respiratory system & anti- allergics
Anti- Allergics Acrivastine
Bilastine
Buclizine
Bupivacaine HCl
Cetirizine Dihydrochloride
Chlorpheniramine Maleate ( Chlorphenamine )
Cloperastine
Desloratadine
Fexofenadine
Hydroxyzine HCl
Levocetirizine HCl
Loratadine
Rupatadine Fumarate
Triprolidine HCl
Anti- Asthma/COPD Acebrophylline
Ciclesonide
Ipratropium Bromide
Ozagrel HCl
Roflumilast
Tiotropium Bromide / Monohydrate
Erdosteine
Terbutaline Sulphate
Bronchodilators & Mast Cell Stabilizers Montelukast Sodium
 
Supplementation
Appetite Suppressant Phentermine HCl
Dietary Supplement Nicotinamide
Phosphorus Supplementation Butaphosphan
 
Surgical & Vaccines
Intravenous & Other Sterile Solutions Hydroxyethyl Starch
Maize Starch
Mucolytics, Proteolytic & Other Enzymes Serratiopeptidase
Trypsin And Chymotrypsin
Non-Ionic Iodinated Iopamidol
Clenbuterol HCl
Cyclobenzaprine HCl
Vecuronium Bromide
Peripherally Acting Muscle Relaxants Lidocaine (Lignocaine)
Myrtecaine
 
Veterinary list
Veterinary Albendazole
Buparvaquone
Butaphosphan
Clorsulon
Diminazene Diaceturate
Quinapyramine Chloride / Sulphate
Triclabendazole
 
We manufacture
  Adenosylcobalamin
  Beclomethasone Dipropionate
  Betamethasone Valerate
  Betamethasone Dipropionate
  Betamethasone Sodium Phosphate
  Clobetasol Propionate
  Deflazacort
  Diacerein
  Hydrocortisone Acetate
  Hydroxycobalamin
  Methyl Prednisolone Acetate
  Methyl Prednisolone Base
 

Summary By Fucntion

 
Gastrointestinal tract / Alimentary system
Antacids, Antireflux Agents & Antiulcerants Homatropine Methylbromide
https://en.wikipedia.org/wiki/Homatropine_methylbromide

Homatropine methylbromide (INN; also known as methylhomatropine bromide) is a quaternary ammonium salt of methylhomatropine. It is a peripherally acting anticholinergic medication that inhibits muscarinic acetylcholine receptors and thus the parasympathetic nervous system. It does not cross the blood–brain barrier. It is used to effectively relieve intestinal spasms and abdominal cramps, without producing the adverse effects of less specific anticholinergics.It is used, in addition to papaverine, as a component of mild drugs that help "flush" the bile.

Certain preparations of drugs such as hydrocodone are mixed with a small, sub-therapeutic amount of homatropine methylbromide to discourage intentional overdose.

 

Mesalazine
https://en.wikipedia.org/wiki/Mesalazine

Mesalazine, also known as mesalamine or 5-aminosalicylic acid (5-ASA), is a medication used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease. It is generally used for mildly to moderately severe disease. It is taken by mouth or rectally.The formulations which are taken by mouth appear to be similarly effective.

It is used to treat inflammatory bowel disease, including ulcerative colitis and Crohn's disease. It is generally used for mildly to moderately severe disease. It is taken by mouth or rectally. Thformulations which are taken by mouth appear to be similarly effective.

 

Rebamipide
https://en.wikipedia.org/wiki/Rebamipide

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis.It works by enhancing mucosal defense, scavenging free radicals and temporarily activating genes encoding cyclooxygenase-2

Studies have shown that rebamipide can fight the damaging effects of NSAIDs on the GIT mucosa and more recently, the small intestine, but not for naproxen-induced gastric damage.
 

Sucralfate
https://en.wikipedia.org/wiki/Sucralfate

Sucralfate, sold under various brand names, is a medication
 used to treat stomach ulcersgastroesophageal reflux disease (GERD), radiation proctitis, and stomach inflammation and to prevent stress ulcers. Its usefulness in people infected by H. pylori is limited. It is used by mouth and rectally

Sucralfate is a locally acting substance that in an acidic environment (pH < 4) reacts with hydrochloric acid in the stomach to form a cross-linking, viscous, paste-like material capable of acting as an acid buffer for as long as 6 to 8 hours after a single dose. It also attaches to proteins on the surface of ulcers, such as albumin and fibrinogen, to form stable insoluble complexes. These complexes serve as protective barriers at the ulcer surface, preventing further damage from acid, pepsin, and bile In addition, sucralfate prevents back diffusion of hydrogen ions, and adsorbs both pepsin and bile acids.

It has been thought that sucralfate also stimulates the production of prostaglandin E2, epidermal growth factors (EGF), bFGF, and gastric mucus

Magaldrate
https://en.wikipedia.org/wiki/Magaldrate

Magaldrate (INN) is a common antacid drug that is used for the treatment of duodenal and gastric ulcers, esophagitis from gastroesophageal reflux.Magaldrate is a hydroxymagnesium aluminate complex that is converted rapidly by gastric acid into Mg(OH)2 and Al(OH)3, which are absorbed poorly and thus provide a sustained antacid effect.
Constipation & Bowel Cleansers Docusate Sodium
https://en.wikipedia.org/wiki/Docusate

Docusate is the common chemical and pharmaceutical name of the anion bis(2-ethylhexyl) sulfosuccinate, also commonly called dioctyl sulfosuccinate (DOSS).

Salts of this anion, especially docusate sodium, are widely used in medicine as laxatives and as stool softeners, by mouth or rectally.Docusate sodium is on the WHO List of Essential Medicines. It is a widely available and relatively inexpensive generic medication, with more than six million prescriptions in the US in 2017.Other docusate salts with medical use include those of calcium, sodium, and potassium.

Docusate salts are also used as food additives, emulsifiers, dispersants, and wetting agents, among other uses

  Prucalopride Succinate
https://en.wikipedia.org/wiki/Prucalopride

Prucalopride, brand name Prudac, among others, is a drug acting as a selective, high affinity 5-HT4 receptor agonist which targets the impaired motility associated with chronic constipation, thus normalizing bowel movements. Prucalopride was approved for use in Europe in 2009,in Canada in 2011 and in Israel in 2014 but has only been recently approved by the Food and Drug Administration for use in the United States. The drug has also been tested for the treatment of chronic intestinal pseudo-obstruction.
  Bisacodyl
https://en.wikipedia.org/wiki/Bisacodyl

Bisacodyl (INN) is an organic compound that is used as a stimulant laxative drug. It works directly on the colon to produce a bowel movement. It is typically prescribed for relief of episodic and chronic constipation and for the management of neurogenic bowel dysfunction, as well as part of bowel preparation before medical examinations, such as for a colonoscopy.

Bisacodyl is a derivative of triphenylmethane. It was first used as a laxative in 1953 because of its structural similarity to phenolphthalein.Bisacodyl works by stimulating enteric nerves to cause peristalsis, i.e., colonic contractions. It is also a contact laxative; it increases fluid and salt secretion. The action of bisacodyl on the small intestine is negligible; stimulant laxatives mainly promote evacuation of the colon.

.
Dissolution Of Cholestrol - Rich Gallstones Ursodeoxycholic Acid
https://en.wikipedia.org/wiki/Ursodeoxycholic_acid

Ursodeoxycholic acid (UDCA), also known as ursodiol, is a secondary bile acid, produced in humans and most other species from metabolism by intestinal bacteria. It is synthesized in the liver in some species, and was first identified in bear bile, which is the derivation of its name Ursus. In purified form, it has been used to treat or prevent several diseases of the liver or bile ducts.
Primary Primary bile acids are produced by the 
liver and stored in the gall bladder. When secreted into the intestine, primary bile acids can be metabolized into secondary bile acids by intestinal bacteria. Primary and secondary bile acids help the body digest fats. Ursodeoxycholic acid helps regulate cholesterol by reducing the rate at which the intestine absorbs cholesterol molecules while breaking up micelles containing cholesterol. The drug reduces cholesterol absorption and is used to dissolve (cholesterol) gallstones in patients who want an alternative to surgery.There are multiple mechanisms involved in cholestatic liver diseases.

Drug Modifying Intestinal Motility & Acid Secretions Hyoscine Butylbromide
https://en.wikipedia.org/wiki/Hyoscine_butylbromide

Hyoscine butylbromide, also known as scopolamine butylbromide and sold under the brandname Buscopan among others,[3] is a medication used to treat crampy abdominal pain, esophageal spasms, renal colic, and bladder spasms.It is also used to improve respiratory secretions at the end of life. Hyoscine butylbromide can be taken by mouth, injection into a muscle, or into a vein.

Hyoscine butylbromide is effective in treating crampy abdominal pain.Hyoscine butylbromide is effective in reducing the duration of the first stage of labour, and it is not associated with any obvious adverse outcomes in mother or neonate.It is also used during abdominal or pelvic MRI or CT scans to improve the quality of pictures.

Metoclopramide
https://en.wikipedia.org/wiki/Metoclopramide

Metoclopramide is a medication used mostly for stomach and esophageal problems It is commonly used to treat and prevent nausea and vomiting, to help with emptying of the stomach in people with delayed stomach emptying, and to help with gastroesophageal reflux disease.It is also used to treat migraine headaches

In 2012, metoclopramide was one of the top 100 most prescribed medications in the United States.It is available as a generic medication.It is on the World Health Organization's List of Essential Medicines In 2017, it was the 253rd most commonly prescribed medication in the United States, with more than one million prescriptions.

Mosapride citrate
https://en.wikipedia.org/wiki/Mosapride

Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. The major active metabolite of mosapride, known as M1, additionally acts as a 5HT3 antagonist, which accelerates gastric emptying throughout the whole of the gastrointestinal tract in humans, and is used for the treatment of gastritis, gastroesophageal reflux disease, functional dyspepsia and irritable bowel syndrome. It is recommended to be taken on an empty stomach (i.e. at least one hour before food or two hours after food).

H2 Blockers & Ulcer Healing Drugs Esomeprazole
https://en.wikipedia.org/wiki/Esomeprazole

Esomeprazole, sold under the brand names Nexium among others,[2] is a medication which reduces stomach acid. It is used to treat gastroesophageal reflux disease, peptic ulcer disease, and Zollinger–Ellison syndrome. Effectiveness is similar to other proton pump inhibitors (PPIs). It is taken by mouth or injection into a vein.

Lansoprazole
https://en.wikipedia.org/wiki/Lansoprazole

Lansoprazole, sold under the brand name Prevacid among others, is a medication which reduces stomach acid. It is used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger–Ellison syndrome. Effectiveness is similar to other proton pump inhibitors (PPIs). It is taken by mouth.Onset is over a few hours and effects last up to a couple of daysIt is a racemic 1:1 mixture of the enantiomers dexlansoprazole and levolansoprazole. Dexlansoprazole is an enantiomerically pure active ingredient of a commercial drug as a result of the enantiomeric shift. Lansoprazole's plasma elimination half-life (1.5 h) is not proportional to the duration of the drug's effects to the person (i.e. gastric acid suppression).

Omeprazole
https://en.wikipedia.org/wiki/Omeprazole

Omeprazole, sold under the brand names Prilosec and Losec among others, is a medication used in the treatment of gastroesophageal reflux disease (GERD), peptic ulcer disease, and Zollinger–Ellison syndrome.It is also used to prevent upper gastrointestinal bleeding in people who are at high risk. Omeprazole is a proton-pump inhibitor (PPI) and its effectiveness is similar to other PPIs. It can be taken by mouth or by injection into a vein.Omeprazole contains a tricoordinated sulfinyl sulfur in a pyramidal structure and therefore can exist as either the (S)- or (R)-enantiomers. Omeprazole is a racemate, an equal mixture of the two. In the acidic conditions of the canaliculi of parietal cells, both enantiomers are converted to achiral products (sulfenic acid and sulfenamide configurations) which react with a cysteine group in H+/K+ ATPase, thereby inhibiting the ability of the parietal cells to produce gastric acid.

Pantoprazole
https://en.wikipedia.org/wiki/Pantoprazole

Pantoprazole, sold under the brand name Protonix among others, is a medication used for the treatment of stomach ulcers, short-term treatment of erosive esophagitis due to gastroesophageal reflux disease (GERD), maintenance of healing of erosive esophagitis, and pathological hypersecretory conditions including Zollinger–Ellison syndrome. It may also be used along with other medications to eliminate Helicobacter pylori. Effectiveness is similar to other proton pump inhibitors (PPIs). It is available by mouth and by injection into a vein.

Rabeprazole sodium
https://en.wikipedia.org/wiki/Rabeprazole

Rabeprazole, sold under the brand name Aciphex, among others, is a medication that decreases stomach acid.It is used to treat peptic ulcer disease, gastroesophageal reflux disease, and excess stomach acid production such as in Zollinger–Ellison syndrome. It may also be used in combination with other medications to treat Helicobacter pylori. Effectiveness is similar to other proton pump inhibitors (PPIs). It is taken by mouth.Rabeprazole is classified as a substituted benzimidazole, like omeprazole, lansoprazole, and pantoprazole. Rabeprazole possess properties of both acids and bases, making it an amphotere.The acid dissociation constant (pKa) of the pyridine nitrogen is about equal to 5.

Ranitidine
https://en.wikipedia.org/wiki/Ranitidine

Ranitidine, sold under the trade name Zantac among others, is a medication that decreases stomach acid production. It is commonly used in treatment of peptic ulcer disease, gastroesophageal reflux disease, and Zollinger–Ellison syndrome. There is also tentative evidence of benefit for hives. It can be given by mouth, by injection into a muscle, or by injection into a veinRanitidine is a competitive, reversible inhibitor of the action of histamine at the histamine H2 receptors found in gastric parietal cells. This results in decreased gastric acid secretion and gastric volume, and reduced hydrogen ion concentration.

Non Specific Antidiarrhoeal Agents Loperamide
https://en.wikipedia.org/wiki/Loperamide

Loperamide, sold under the brand name Imodium, among others, is a medication used to decrease the frequency of diarrhea. It is often used for this purpose in, inflammatory bowel disease, and short bowel syndrome. It is not recommended for those with blood in the stool, mucus in the stool or fevers. The medication is taken by mouth.

Loperamide is an opioid-receptor agonist and acts on the μ-opioid receptors in the myenteric plexus of the large intestine. It works like morphine, decreasing the activity of the myenteric plexus, which decreases the tone of the longitudinal and circular smooth muscles of the intestinal wall. This increases the time material stays in the intestine, allowing more water to be absorbed from the fecal matter. It also decreases colonic mass movements and suppresses the gastrocolic reflex.

Loperamide's circulation in the bloodstream is limited in two ways. Efflux by P-glycoprotein in the intestinal wall reduces passage of loperamide, and the fraction of drug crossing is then further reduced through first-pass metabolism by the liver.Loperamide metabolizes into an MPTP-like compound, but is unlikely to exert neurotoxicity.

Racecadotril
https://en.wikipedia.org/wiki/Racecadotril

Racecadotril, also known as acetorphan, is an antidiarrheal drug which acts as a peripheral enkephalinase inhibitor.Unlike other opioid medications used to treat diarrhea, which reduce intestinal motility, racecadotril has an antisecretory effect — it reduces the secretion of water and electrolytes into the intestine. It is available in France (where it was first introduced in ~1990) and other European countries (including Germany, Italy, the United Kingdom, Spain, Portugal, Russia and the Czech Republic) as well as most of South America and some South East Asian countries (including China, India and Thailand), but not in the United States. It is sold under the tradename Hidrasec, among others. Thiorphan is the active metabolite of racecadotril, which exerts the bulk of its inhibitory actions on enkephalinases.

Enkephalins are peptides produced by the body that act on opioid receptors with preference for the δ subtype.[ Activation of δ receptors inhibits the enzyme adenylyl cyclase, decreasing intracellular levels of the messenger molecule cAMP.

The active metabolite of racecadotril, thiorphan, inhibits enkephalinase enzymes in the intestinal epithelium with an IC50 of 6.1 nM, protecting enkephalins from being broken down by these enzymes. (Racecadotril itself is much less potent at 4500 nM. This reduces diarrhea related hypersecretion in the small intestine without influencing basal secretion. Racecadotril also has no influence on the time substances, bacteria or virus particles stay in the intestine.

Rifaximin
https://en.wikipedia.org/wiki/Rifaximin

Rifaximin, sold under the trade name Xifaxan among others, is an antibiotic used to treat traveler's diarrhea, irritable bowel syndrome, and hepatic encephalopathy. It has poor absorption when taken by mouth.

Rifaximin interferes with transcription by binding to the β-subunit of bacterial RNA polymerase. This results in the blockage of the translocation step that normally follows the formation of the first phosphodiester bond, which occurs in the transcription process.[ This in turn results in a reduction of bacteria populations, including gas producing bacteria, which may reduce mucosal inflammation, epithelial dysfunction and visceral hypersensitivity. Rifaximin has broad spectrum antibacterial properties against both gram positive and gram negative anaerobic and aerobic bacteria. As a result of bile acid solubility, its antibacterial action is limited mostly to the small intestine and less so the colon. A resetting of the bacteria composition has also been suggested as a possible mechanism of action for relief of IBS symptoms.Additionally, rifaximin may have a direct anti-inflammatory effect on gut mucosa via modulation of the pregnane X receptor.

Other mechanisms for its therapeutic properties include inhibition of bacterial translocation across the epithelial lining of the intestine, inhibition of adherence of bacteria to the epithelial cells and a reduction in the expression of proinflammatory cytokines.

Trimethoprim
https://en.wikipedia.org/wiki/Trimethoprim

Trimethoprim (TMP) is an antibiotic used mainly in the treatment of bladder infections.Other uses include for middle ear infections and travelers' diarrhea With sulfamethoxazole or dapsone it may be used for Pneumocystis pneumonia in people with HIV/AIDS It is taken by mouth.Trimethoprim binds to dihydrofolate reductase and inhibits the reduction of dihydrofolic acid (DHF) to tetrahydrofolic acid (THF).THF is an essential precursor in the thymidine synthesis pathway and interference with this pathway inhibits bacterial DNA synthesis.Trimethoprim's affinity for bacterial dihydrofolate reductase is several thousand times greater than its affinity for human dihydrofolate reductase. Sulfamethoxazole inhibits dihydropteroate synthase, an enzyme involved further upstream in the same pathway. Trimethoprim and sulfamethoxazole are commonly used in combination due to possible synergistic effects, and reduced development of resistance.This benefit has been questioned.

Probiotics Saccharomyces Boulardii
https://en.wikipedia.org/wiki/Saccharomyces_boulardii

Saccharomyces boulardii is a tropical species of yeast first isolated from lychee and mangosteen fruit in 1923 by French scientist Henri Boulard. Although early reports described distinct taxonomic, metabolic, and genetic properties S. boulardii is a strain of S. cerevisiae, sharing >99% genomic relatedness, giving the synonym S. cerevisiae var boulardii. A type strain is Hansen CBS 5926.

S. boulardii is sometimes used as a probiotic with the purpose of introducing beneficial microbes into the large and small intestines and conferring protection against pathogens.It grows at 37 °C (98.6 °F).In addition, the popular genome-editing tool CRISPR-Cas9 was proven to be effective in S. boulardii.[9] Boulard first isolated this yeast after he observed natives of Southeast Asia chewing on the skin of lychee and mangosteen in an attempt to control the symptoms of cholera. In healthy patients, S. boulardii has been shown to be nonpathogenic and nonsystemic (it remains in the gastrointestinal tract rather than spreading elsewhere in the body).

 

Prokinetic Agent Cisapride Monohydrate
https://en.wikipedia.org/wiki/Cisapride

Cisapride is a gastroprokinetic agent, a drug that increases motility in the upper gastrointestinal tract. It acts directly as a serotonin 5-HT4 receptor agonist and indirectly as a parasympathomimetic. Stimulation of the serotonin receptors increases acetylcholine release in the enteric nervous system. It has been sold under the trade names Prepulsid (Janssen-Ortho) and Propulsid (in the United States). It was discovered by Janssen Pharmaceutica in 1980. In many countries, it has been either withdrawn from the market or had its indications limited due to incidences of serious cardiac side-effects.

The commercial preparations of this drug are the racemic mixture of both enantiomers of the compound. The (+) enantiomer itself has the major pharmacologic effects and does not induce many of the detrimental side-effects of the mixture.

Mosapride citrate
https://en.wikipedia.org/wiki/Mosapride

Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. The major active metabolite
 of mosapride, known as M1, additionally acts as a 5HT3 antagonist, which accelerates gastric emptying throughout the whole of the gastrointestinal tract in humans, and is used for the treatment of gastritis, gastroesophageal reflux disease, functional dyspepsia and irritable bowel syndrome. It is recommended to be taken on an empty stomach (i.e. at least one hour before food or two hours after food).
   
Antibiotics
Anthelmintics Albendazole
https://en.wikipedia.org/wiki/Albendazole

Albendazole, also known as albendazolum, is a medication used for the treatment of a variety of parasitic worm infestations. It is useful for giardiasis, trichuriasis, filariasis, neurocysticercosis, hydatid disease, pinworm disease, and ascariasis, among other diseases It is taken by mouth.

As a vermicide, albendazole causes degenerative alterations in the intestinal cells of the worm by binding to the colchicine-sensitive site of β-tubulin, thus inhibiting its polymerization or assembly into microtubules (it binds much better to the β-tubulin of parasites than that of mammals). Albendazole leads to impaired uptake of glucose by the larval and adult stages of the susceptible parasites, and depletes their glycogen stores. Albendazole also prevents the formation of spindle fibers needed for cell division, which in turn blocks egg production and development; existing eggs are prevented from hatching.Cell motility, maintenance of cell shape, and intracellular transport are also disrupted. At higher concentrations, it disrupts the helminths' metabolic pathways by inhibiting metabolic enzymes such as malate dehydrogenase and fumarate reductase, with inhibition of the latter leading to less energy produced by the Krebs cycle.Due to diminished ATP production, the parasite is immobilized and eventually dies.

Some parasites have evolved to have some resistance to albendazole by having a different set of acids comprising β-tubulin, decreasing the binding affinity of albendazole.Drosophilia have many of the same mutations, meaning the drug does not affect fruit flies.

 

Febantel
https://en.wikipedia.org/wiki/Fenbendazole

Fenbendazole is a broad spectrum benzimidazole anthelmintic used against gastrointestinal parasites including: giardia, roundworms, hookworms, whipworms, the tapeworm genus Taenia (but not effective against Dipylidium caninum, a common dog tapeworm), pinworms, aelurostrongylus, paragonimiasis, strongyles, and strongyloides that can be administered to sheep, cattle, horses, fish, dogs, cats, rabbits, and seals.Fenbendazole is metabolized in the liver to oxfendazole, which is anthelmintic too; oxfendazole partially gets reduced back to fenbendazole in the liver and rumen.Also, fenbendazole itself is an active metabolite of another anthelmintic drug, febantel.
Mebendazole
https://en.wikipedia.org/wiki/Mebendazole

Mebendazole (MBZ) is a medication used to treat a number of parasitic worm infestations.This includes ascariasis, pinworm disease, hookworm infections, guinea worm infections, hydatid disease, and giardia, among others.It is taken by mouth.

Mebendazole is usually well tolerated.Common side effects include headache, vomiting, and ringing in the ears0">ringing .If used at large doses it may cause bone marrow suppressionone marrow suppression.[3]< It is unclear if it is safe in pregnancy. Mebendazole is a broad-spectrum antihelminthic agent of the benzimidazole type.

Mebendazole works by selectively inhibiting the synthesis ofiting the synthesis of microtubules via binding to colchicine binding site of β-tubulin, thereby blocking polymerisation of tubulin Disruption of cytoplasmic microtubules leads to blocking the uptake of glucose and other nutrients, resulting in the gradual immobilization and eventual death of the helminths. Poor absorption in digestive tract makes mebendazole an efficient drug for treating intestinal parasitic infections with limited adverse effects. However mebendazole has impact on mammalian cells mostly by inhibiting polymeration ofbiting polymeration of tubulin dimers, thereby disrupting essential microtubule structures such as mito. Disassembly of mitotic spindle then leads to apoptosis mediated via dephosphorylation of Bcl-2 which allows pro-apoptotic protein Bax to dimerize and innitiate programmed cell death.

Nitazoxanide
https://en.wikipedia.org/wiki/Nitazoxanide

Nitazoxanide is a broad-spectrum antiparasitic and broad-spectrum antiviral drug that is used in medicine for the treatment of various helminthic, protozoal, and viral infections. It is indicated for the treatment of infection by Cryptosporidium parvum and Giardia lamblia in immunocompetent individuals and has been repurposed for the treatment of influenza. Nitazoxanide has also been shown to have in vitro antiparasitic activity and clinical treatment efficacy for infections caused by other protozoa and helminths; emerging evidence suggests that it possesses efficacy in treating a number of viral infections as well.

Chemically, nitazoxanide is the prototype member of the thiazolides, a class of drugs which are synthetic nitrothiazolyl-salicylamide derivatives with antiparasitic and antiviral activity.Tizoxanide, an active metabolite of nitazoxanide in humans, is also an antiparasitic drug of the thiazolide class.

The anti-protozoal activity of nitazoxanide is believed to be due to interference with the pyruvate:ferredoxin oxidoreductase (PFOR) enzyme-dependent electron transfer reaction which is essential to anaerobic energy metabolism. PFOR inhibition may also contribute to its activity against anaerobic bacteria.

It has also been shown to have activity against influenza A virus in vitro. The mechanism appears to be by selectively blocking the maturation of the viral hemagglutinin at a stage preceding resistance to endoglycosidase H digestion. This impairs hemagglutinin intracellular trafficking and insertion of the protein into the host plasma membrane.

Nitazoxanide modulates a variety of other pathways in vitro, including glutathione-S-transferase and glutamate-gated chloride ion channels in nematodes, respiration and other pathways in bacteria and cancer cells, and viral and host transcriptional factors.

Antifungals Anidulafungin
ttps://en.wikipedia.org/wiki/Anidulafungin

Anidulafungin (INN) (trade names Eraxis, Ecalta) is a semisynthetic echinocandin used as an antifungal drug. It was previously known as LY303366.[3][4][5] It may also have application in treating invasive Aspergillus infection when used in combination with Voriconazole.It is a member of the class of antifungal drugs known as the echinocandins; its mechanism of action is by inhibition of (1→3)-β-D-glucan synthase, an enzyme important to the synthesis of the fungal cell wall.Anidulafungin inhibits glucan synthase, an enzyme important in the formation of (1→3)-β-D-glucan, a major fungal cell wall component. Glucan synthase is not present in mammalian cells, so it is an attractive target for antifungal activity.

Eberconazole
https://en.wikipedia.org/wiki/Eberconazole

Eberconazole is an antifungal drug. As a 1% topical cream, it is an effective treatment for dermatophytosis, candidiasis, and pityriasis.It was approved for use in Spain in 2015 and is sold under the trade name Ebernet.

Fluconazole
https://en.wikipedia.org/wiki/Fluconazole

Fluconazole is an antifungal medication used for a number of fungal infections.This includes candidiasis, blastomycosis, coccidiodomycosis, cryptococcosis, histoplasmosis, dermatophytosis, and pityriasis versicolor.It is also used to prevent candidiasis in those who are at high risk such as following organ transplantation, low birth weight babies, and those with low blood neutrophil counts. It is given either by mouth or by injection into a vein.
Like other 
imidazole- and triazole-class antifungals, fluconazole inhibits the fungal cytochrome P450 enzyme 14α-demethylase. Mammalian demethylase activity is much less sensitive to fluconazole than fungal demethylase. This inhibition prevents the conversion of lanosterol to ergosterol, an essential component of the fungal cytoplasmic membrane, and subsequent accumulation of 14α-methyl sterols.Fluconazole is primarily fungistatic; however, it may be fungicidal against certain organisms in a dose-dependent manner, specifically Cryptococcus.

Ketoconazole
https://en.wikipedia.org/wiki/Ketoconazole

Ketoconazole, sold under the brand name Nizoral among others, is an antifungal medication used to treat a number of fungal infections. Applied to the skin it is used for fungal skin infections such as tinea, cutaneous candidiasis, pityriasis versicolor, dandruff, and seborrheic dermatitis.Taken by mouth it is a less preferred option and only recommended for severe infections when other agents cannot be used. Other uses include in the treatment of excessive hair growth and Cushing's syndrome.As an antifungal, ketoconazole is structurally similar to imidazole, and interferes with the fungal synthesis of ergosterol, a constituent of fungal cell membranes, as well as certain enzymes. As with all azole antifungal agents, ketoconazole works principally by inhibiting the enzyme cytochrome P450 14α-demethylase (CYP51A1). This enzyme participates in the sterol biosynthesis pathway that leads from lanosterol to ergosterol.
Luliconazole
https://en.wikipedia.org/wiki/Luliconazole

Luliconazole, trade names Luzu among others, is an imidazole antifungal medication. As a 1% topical cream, It is indicated for the treatment of athlete's foot, jock itch, and ringworm caused y dermatophytes such as Trichophyton rubrum, Microsporum gypseum and Epidermophyton floccosum.

Micafungin
https://en.wikipedia.org/wiki/Micafungin

Micafungin (trade name Mycamine) is an echinocandin antifungal drug used to treat and prevent invasive fungal infections including candidemia, abscesses and esophageal candidiasis. It inhibits the production of beta-1,3-glucan, an essential component of fungal cell walls. Micafungin is administered intravenously. It received final approval from the U.S. Food and Drug Administration on March 16, 2005, and gained approval in the European Union on April 25, 2008.

Sodium Posaconazole
https://en.wikipedia.org/wiki/Posaconazole

Posaconazole, sold under the brand names Noxafil and Posanol is a triazole antifungal medication.

It was approved for medical use in the United States in September 2006, and is available as a generic medication.

Posaconazole works by disrupting the close packing of acyl chains of phospholipids, impairing the functions of certain membrane-bound enzyme systems such as ATPase and enzymes of the electron transport system, thus inhibiting growth of the fungi. It does this by blocking the synthesis of ergosterol by inhibiting of the enzyme lanosterol 14α-demethylase and accumulation of methylated sterol precursors. Posaconazole is significantly more potent at inhibiting 14-alpha demethylase than itraconazole.

Tavaborole
https://en.wikipedia.org/wiki/Tavaborole

Tavaborole, sold under the brand name Kerydin, is a topical antifungal medication for the treatment of onychomycosis, a fungal infection of the nail and nail bed. Tavaborole began phase III clinical trials in December 2010 and was approved by the US FDA in July 2014.The medication inhibits an essential fungal enzyme, leucyl-tRNA synthetase, that is required for protein synthesis. The inhibition of protein synthesis leads to termination of cell growth and then cell death, eliminating the fungal infection.

Tavaborole, when prepared with a 1:1 mixture of ethyl acetate and propylene glycol, has the ability to fully penetrate through the human nail.[citation needed] In studies with cadaver fingernails, a 5% solution of tavaborole penetrated the nail an average of 524.7 mcg/cm2 after two weeks of daily use.

Tavaborole is detectable in the blood at a level of 3.54 ng/mL after a single use of 0.2 mL of the 5% solution. Tavaborole has an elimination half-life of 28.5 hours, a maximum concentration of 5.17 ng/mL after two weeks of daily use, and takes 8 days to reach the maximum concentration.

Itraconazole
https://en.wikipedia.org/wiki/Itraconazole

Itraconazole is an antifungal medication used to treat a number of fungal infections. This includes aspergillosis, blastomycosis, coccidioidomycosis, histoplasmosis, and paracoccidioidomycosis.

The mechanism of action of itraconazole is the same as the other azole antifungals: it inhibits the fungal-mediated synthesis of ergosterol, via inhibition of lanosterol 14α-demethylase. Because of its ability to inhibit cytochrome P450 3A4 CC-3, caution should be used when considering interactions with other medications.

Itraconazole is pharmacologically distinct from other azole antifungal agents in that it is the only inhibitor in this class that has been shown to inhibit both the hedgehog signaling pathway and angiogenesis These distinct activities are unrelated to inhibition of the cytochrome P450 lanosterol 14 alpha-demethylase and the exact molecular targets responsible remain unidentified. Functionally, the antiangiogenic activity of itraconazole has been shown to be linked to inhibition of glycosylation, VEGFR2 phosphorylation, trafficking, and cholesterol biosynthesis pathways. Evidence suggests the structural determinants for inhibition of hedgehog signaling by itraconazole are recognizably different from those associated with antiangiogenic activity.

Antimalarial Drug Lumefantrine
https://en.wikipedia.org/wiki/Lumefantrine

Lumefantrine (or benflumetol) is an antimalarial drug. It is only used in combination with artemether. The term "co-artemether" is sometimes used to describe this combination. Lumefantrine has a much longer half-life compared to artemether, and is therefore thought to clear any residual parasites that remain after combination treatment.

Antiretroviral Abacavir Sulphate
https://en.wikipedia.org/wiki/Abacavir

Abacavir, sold under the brand name Ziagen, is a medication used to prevent and treat HIV/AIDS.[1][2] Similar to other nucleoside analog reverse-transcriptase inhibitors (NRTIs), abacavir is used together with other HIV medications, and is not recommended by itself. It is taken by mouth as a tablet or solution and may be used in children over the age of three months.Abacavir is a nucleoside reverse transcriptase inhibitor that inhibits viral replication. It is a guanosine analogue that is phosphorylated to carbovir triphosphate (CBV-TP). CBV-TP competes with the viral molecules and is incorporated into the viral DNA. Once CBV-TP is integrated into the viral DNA, transcription and HIV reverse transcriptase is inhibited.

Atazanavir
https://en.wikipedia.org/wiki/Atazanavir

Atazanavir, sold under the trade name Reyataz among others, is an antiretroviral medication used to treat and prevent HIV/AIDS. It is generally recommended for use with other antiretrovirals.It may be used for prevention after a needlestick injury or other potential exposure. It is taken by mouth once a day..Atazanavir binds to the active site HIV protease and prevents it from cleaving the pro-form of viral proteins into the working machinery of the virus.If the HIV protease enzyme does not work, the virus is not infectious, and no mature virions are made.The azapeptide drug was designed as an analog of the peptide chain substrate that HIV protease would cleave normally into active viral proteins. More specifically, atazanavir is a structural analog of the transition state during which the bond between a phenylalanine and proline is broken.Humans do not have any enzymes that break bonds between phenylalanine and proline, so this drug will not target human enzymes.

Efavirenz
https://en.wikipedia.org/wiki/Efavirenz

Efavirenz (EFV), sold under the brand names Sustiva among others, is an antiretroviral medication used to treat and prevent HIV/AIDS.It is generally recommended for use with other antiretrovirals.It may be used for prevention after a needlestick injury or other potential exposure.It is sold both by itself and in combination as efavirenz/emtricitabine/tenofovir..

Efavirenz falls in the NNRTI class of antiretrovirals. Both nucleoside and non-nucleoside RTIs inhibit the same target, the reverse transcriptase enzyme, an essential viral enzyme which transcribes viral RNA into DNA. Unlike nucleoside RTIs, which bind at the enzyme's active site, NNRTIs act allosterically by binding to a distinct site away from the active site known as the NNRTI pocket.

Efavirenz is not effective against HIV-2, as the pocket of the HIV-2 reverse transcriptase has a different structure, which confers intrinsic resistance to the NNRTI class.

As most NNRTIs bind within the same pocket, viral strains which are resistant to efavirenz are usually also resistant to the other NNRTIs, nevirapine and delavirdine. The most common mutation observed after efavirenz treatment is K103N, which is also observed with other NNRTIs. Nucleoside reverse-transcriptase inhibitors (NRTIs) and efavirenz have different binding targets, so cross-resistance is unlikely; the same is true with regard to efavirenz and protease inhibitors.

 

 

Darunavir (Amorphous / Ethanolate / Sodium)
https://en.wikipedia.org/wiki/Darunavir

Darunavir (DRV), sold under the brand name Prezista among others, is an antiretroviral medication used to treat and prevent HIV/AIDS.[1] It is generally recommended for use with other antiretrovirals.It is often used with low doses of ritonavir or cobicistat to increase darunavir levels.Darunavir is a nonpeptidic inhibitor of protease (PR) that lodges itself in the active site of PR
 through a number of hydrogen bonds.It was developed to increase interactions with HIV-1 protease and
 to be more resistant against HIV-1 protease mutations. With a K
d (dissociation constant) of 4.5 x
 10
−12 M, darunavir has a much stronger interaction with PR and its dissociation constant is 1/100 to 1/1000 of other protease inhibitors.This strong interaction comes from increased hydrogen bonds between darunavir and the backbone of the PR active site (Figure 2). Darunavir's structure allows it to create more hydrogen bonds with the PR active site than most PIs that have been developed and approved by the FDA Furthermore, the backbone of HIV-1 protease maintains its spatial conformation in the presence of mutations.Because darunavir interacts with this stable portion of the protease, the PR-PI interaction is less likely to be disrupted by a mutation.

Indinavir Sulphate
https://en.wikipedia.org/wiki/Indinavir

Indinavir (IDV; trade name Crixivan, made by Merck) is a protease inhibitor used as a component of highly active antiretroviral therapy to treat HIV/AIDS. It is soluble white powder administered orally in combination with other antiviral drugs. The drug prevents protease from functioning normally. Consequently, HIV viruses cannot reproduce, causing a decrease in the viral load. Commercially sold indinavir is indinavir anhydrous, which is indinavir with an additional amine in the hydroxyethylene backbone. This enhances its solubility and oral bioavailability, making it easier for users to intake. It was synthetically produced for the purpose of inhibiting the protease in the HIV virus.

Oseltamivir
https://en.wikipedia.org/wiki/Oseltamivir

Oseltamivir, sold under the brand name Tamiflu, is an antiviral medication used to treat and prevent influenza A and influenza B (flu).Many medical organizations recommend it in people who have complications or are at high risk of complications within 48 hours of first symptoms of infection.They recommend it to prevent infection in those at high risk, but not the general population.Oseltamivir is a neuraminidase inhibitor, a competitive inhibitor of influenza's neuraminidase enzyme. The enzyme cleaves the sialic acid which is found on glycoproteins on the surface of human cells that helps new virions to exit the cell. Thus oseltamivir prevents new viral particles from being released.

Rilpivirine HCl
https://en.wikipedia.org/wiki/Rilpivirine

Rilpivirine (TMC278, trade name Edurant) is a pharmaceutical drug, developed by Tibotec, for the treatment of HIV infection.It is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with higher potency, longer half-life and reduced side-effect profile compared with older NNRTIs, such as efavirenz.

Ritonavir
https://en.wikipedia.org/wiki/Ritonavir

Ritonavir (RTV), sold under the brand name Norvir, is an antiretroviral medication used along with other medications to treat HIV/AIDS.[1] This combination treatment is known as highly active antiretroviral therapy (HAART).Often a low dose is used with other protease inhibitors.It may also be used in combination with other medications for hepatitis C.It is taken by mouth.The capsules of the medication do not work the same as the tablets.

Ritonavir was originally developed as an inhibitor of HIV protease, one of a family of pseudo-C2-symmetric small molecule inhibitors.[citation needed]

Ritonavir is now rarely used for its own antiviral activity but remains widely used as a booster of other protease inhibitors. More specifically, ritonavir is used to inhibit a particular enzyme, in intestines, liver, and elsewhere, that normally metabolizes protease inhibitors, cytochrome P450-3A4 (CYP3A4).The drug binds to and inhibits CYP3A4, so a low dose can be used to enhance other protease inhibitors. This discovery drastically reduced the adverse effects and improved the efficacy of protease inhibitors and HAART. However, because of the general role of CYP3A4 in xenobiotic metabolism, dosing with ritonavir also affects the efficacy of numerous other medications, adding to the challenge of prescribing drugs concurrently.

 

Saquinavir
https://en.wikipedia.org/wiki/Saquinavir

Saquinavir (SQV), sold under the brand names Invirase and Fortovase, is an antiretroviral drug used together with other medications to treat or prevent HIV/AIDS.Typically it is used with ritonavir or lopinavir/ritonavir to increase its effect.It is taken by mouth.Saquinavir binds to the active site of the viral protease and prevents cleavage of viral polyproteins, preventing maturation of the virus. Saquinavir inhibits both HIV-1 and HIV-2 proteases.

Simeprevir
https://en.wikipedia.org/wiki/Simeprevir

Simeprevir, sold under the trade names Olysio among others, is a medication used in combination with other medications for the treatment of hepatitis C.It is specifically used for hepatitis C genotype 1 and 4.Medications it is used with include sofosbuvir or ribavirin and peginterferon-alfa.Cure rates are in 80s to 90s percent.It may be used in those who also have HIV/AIDS.It is taken by mouth once daily for typically 12 weeks..Simeprevir is a NS3/4A protease inhibitor, thus preventing viral maturation through inhibition of protein synthesis. Simeprevir is administered as one capsule once daily with pegylated interferon and ribavirin for the treatment of genotype 1 or genotype 4 chronic hepatitis C in adult people with compensated liver disease (including cirrhosis), with or without HIV-1 co-infection, who are treatment naive or who have failed previous interferon therapy.Genotype 1 is the most prevalent form of hepatitis C virus (HCV) worldwide.

Tenofovir
https://en.wikipedia.org/wiki/Tenofovir_disoproxil

Tenofovir disoproxil, sold under the trade name Viread among others, is a medication used to treat chronic hepatitis B and to prevent and treat HIV/AIDS.It is generally recommended for use with other antiretrovirals.It may be used for prevention of HIV/AIDS among those at high risk before exposure, and after a needlestick injury or other potential exposure.It is sold both by itself and together as emtricitabine/tenofovir and efavirenz/emtricitabine/tenofovir.It does not cure HIV/AIDS or hepatitis B.It is available by mouth as a tablet or powder.enofovir disoproxil is a nucleotide analog reverse-transcriptase inhibitor (NtRTI).It selectively inhibits viral reverse transcriptase, a crucial enzyme in retroviruses such as human immunodeficiency virus (HIV), while showing limited inhibition of human enzymes, such as DNA polymerases α, β, and mitochondrial DNA polymerase γ.In vivo tenofovir disoproxil fumarate is converted to tenofovir, an acyclic analog of deoxyadenosine 5'-monophosphate (d-AMP). Tenofovir lacks a hydroxyl group in the position corresponding to the 3' carbon of the d-AMP, preventing the formation of the 5′ to 3′ phosphodiester linkage essential for DNA chain elongation.Once incorporated into a growing DNA strand, tenofovir causes premature termination of DNA transcription, preventing viral.

Antivirals Acyclovir

Aciclovir (ACV), also known as acyclovir, is an 
antiviral medication. It is primarily used for the treatment of herpes simplex virus infections, chickenpox, and shingles. Other uses include prevention of cytomegalovirus infections following transplant and severe complications of Epstein-Barr virus infection.It can be taken by mouth, applied as a cream, or injected.Aciclovir is converted by viral thymidine kinase to aciclovir monophosphate, which is then converted by host cell kinases to aciclovir triphosphate (ACV-TP). ACV-TP, in turn, competitively inhibits and inactivates HSV-specified DNA polymerases preventing further viral DNA synthesis without affecting the normal cellular processes.

Lamivudine
https://en.wikipedia.org/wiki/Lamivudine

Lamivudine, commonly called 3TC, is an antiretroviral medication used to prevent and treat HIV/AIDS. It is also used to treat chronic hepatitis B when other options are not possible. It is effective against both HIV-1 and HIV-2. It is typically used in combination with other antiretrovirals such as zidovudine and abacavir. Lamivudine may be included as part of post-exposure prevention in those who have been potentially exposed to HIV. Lamivudine is taken by mouth as a liquid or tablet.

Lamivudine is an analogue of cytidine. It can inhibit both types (1 and 2) of HIV reverse transcriptase and also the reverse transcriptase of hepatitis B virus. It is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated.

Lamivudine is administered by mouth, and it is rapidly absorbed with a bio-availability of over 80%. Some research suggests that lamivudine can cross the blood–brain barrier. Lamivudine is often given in combination with zidovudine, with which it is highly synergistic. Lamivudine treatment has been shown to restore zidovudine sensitivity of previously resistant HIV. Lamivudine showed no evidence of carcinogenicity or mutagenicity in in vivo studies in mice and rats at doses from 10 to 58 times those used in humans.

Valacyclovir
https://en.wikipedia.org/wiki/Valaciclovir

Valaciclovir, also spelled valacyclovir, is an antiviral medication used to treat outbreaks of herpes simplex or herpes zoster (shingles).It is also used to prevent cytomegalovirus following a kidney transplant in high risk cases. It is taken by mouth.

Aciclo-GTP, the active triphosphate metabolite of aciclovir, is a very potent inhibitor of viral DNA replication. Aciclo-GTP competitively inhibits and inactivates the viral DNA polymerase.Its monophosphate form also incorporates into the viral DNA, resulting in chain termination. It has also been shown that the viral enzymes cannot remove aciclo-GMP from the chain, which results in inhibition of further activity of DNA polymerase. Aciclo-GTP is fairly rapidly metabolized within the cell, possibly by cellular phosphatases.Aciclovir is active against most species in the herpesvirus family.

 

Valganciclovir
https://en.wikipedia.org/wiki/Valganciclovir

Valganciclovir, sold under the brandname Valcyte among others, is an antiviral medication used to treat cytomegalovirus (CMV) infection in those with HIV/AIDS or following organ transplant.[1] It is often used long term as it only suppresses rather than cures the infection. Valganciclovir is taken by mouth.[

Valganciclovir is a prodrug for ganciclovir, which is a synthetic analog of 2′-deoxy-guanosine. Its structure is the same as ganciclovir, except for the addition of a L-valyl ester at the 5' end of the incomplete deoxyribose ring. The valine increases both the absorption of the drug in the intestines, as well as the bioavailability of the drug once it is absorbed. The L-valyl ester is cleaved by esterases in the intestines and the liver, leaving ganciclovir to be absorbed by the virus-infected cells.

Ganciclovir is first phosphorylated to ganciclovir monophosphate by a viral thymidine kinase encoded by the cytomegalovirus (CMV) upon infection. Human cellular kinases further phosphorylate the molecule to create ganciclovir diphosphate, then ganciclovir triphosphate. These kinases are present in 10-fold greater concentrations in CMV or herpes simplex virus (HSV)-infected cells compared to uninfected human cells, allowing ganciclovir triphosphate to concentrate in infected cells.

Ganciclovir triphosphate is a competitive inhibitor of deoxyguanosine triphosphate (dGTP). It is incorporated into viral DNA and preferentially inhibits viral DNA polymerases more than cellular DNA polymerases. Ganciclovir triphosphate serves as a poor substrate for chain elongation. Once incorporated into viral DNA due to its structure similarity to dGTP, chain termination occurs once a single nucleotide is added to the distal hydroxyl group of the incomplete deoxyribose ring of ganciclovir.

 

Beta-Lactam Faropenem Sodium
https://en.wikipedia.org/wiki/Faropenem

Faropenem is an orally active beta-lactam antibiotic belonging to the penem group. It is resistant to some forms of extended-spectrum beta-lactamase. It is available for oral use.
Carbapenem Doripenem
https://en.wikipedia.org/wiki/Doripenem

Doripenem (Doribax, Finibax) is an antibiotic drug in the carbapenem class. It is a beta-lactam antibiotic drug able to kill Pseudomonas aeruginosa.

Doripenem can be used for bacterial infections such as: complex abdominal infections, pneumonia within the setting of a hospital, and complicated infections of the urinary tract including kidney infections with sepsis.

The greater stability of doripenem in aqueous solution compared to earlier members of the carbapenem class allows it to be administered as an infusion over 4 hours or more, which may be advantageous in the treatment of certain difficult-to-treat infections. It may present a lower risk of inducing seizures than other carbapenems.

 

Ertapenem
https://en.wikipedia.org/wiki/Ertapenem

Ertapenem (trade name Invanz) is a carbapenem antibiotic medication for the treatment of infections of the abdomen, the lungs, the upper part of the female reproductive system, and diabetic foot, used in the form of infusions or injections.Like all beta-lactam antibiotics, ertapenem is bactericidal. It inhibits cross-linking of the peptidoglycan layer of bacterial cell walls by blocking a type of enzymes called penicillin-binding proteins (PBPs). When a bacterial cell tries to synthesize new cell wall in order to grow and divide, the attempt fails, rendering the cell vulnerable to osmotic disruption. Additionally, the surplus of peptidoglycan precursors triggers autolytic enzymes of the bacterium, which disintegrate the existing wall.

Imipenem with cilastatin (Imipenem/cilastatin)
https://en.wikipedia.org/wiki/Imipenem/cilastatin

Imipenem/cilastatin, sold under the brand name Primaxin among others, is an antibiotic useful for the treatment of a number of bacterial infections. It is made from a combination of imipenem and cilastatin. Specifically it is used for pneumonia, sepsis, endocarditis, joint infections, intra-abdominal infections, and urinary tract infections. It is given by injection into a vein or muscle.

Imipenem/cilastatin has the ability to kill a wide variety of bacteria. Imipenem is the active antibiotic agent and works by interfering with their ability to form cell walls, so the bacteria break up and die.

Imipenem is rapidly degraded by the renal enzyme dehydropeptidase if administered alone (making it less effective); the metabolites can cause kidney damage. Imipenem is a broad-spectrum betalactam antibiotic used for severe bacterial infections caused by susceptible organisms. Because imipenem is rapidly inactivated by renal dehydropeptidase I, it is given in combination with cilastatin, a DHP-I inhibitor which increases half-life and tissue penetration of imipenem.

 

Meropenem Trihydrate
https://en.wikipedia.org/wiki/Meropenem

Meropenem, sold under the brandname Merrem among others, is a broad-spectrum antibiotic used to treat a variety of bacterial infections. Some of these include meningitis, intra-abdominal infection, pneumonia, sepsis, and anthrax. It is given by injection into a vein.

Meropenem is bactericidal except against Listeria monocytogenes, where it is bacteriostatic. It inhibits bacterial cell wall synthesis like other β-lactam antibiotics. In contrast to other beta-lactams, it is highly resistant to degradation by β-lactamases or cephalosporinases. In general, resistance arises due to mutations in penicillin-binding proteins, production of metallo-β-lactamases, or resistance to diffusion across the bacterial outer membrane. Unlike imipenem, it is stable to dehydropeptidase-1, so can be given without cilastatin.

In 2016, a synthetic peptide-conjugated PMO (PPMO) was found to inhibit the expression of New Delhi metallo-beta-lactamase, an enzyme that many drug-resistant bacteria use to destroy carbapenems.

Drugs used in Ornidazole Protozoal Infections Tinidazole
https://en.wikipedia.org/wiki/Tinidazole

Tinidazole is a drug used against protozoan infections. It is widely known throughout Europe and the developing world as a treatment for a variety of amoebic and parasitic infections. It was developed in 1972 and is a prominent member of the nitroimidazole antibiotic class.A large body of clinical data exists to support use of tinidazole for infections from amoebae, giardia, and trichomonas, just like metronidazole. Tinidazole may be a therapeutic alternative in the setting of metronidazole intolerance. Tinidazole may also be used to treat a variety of other bacterial infections (e.g., as part of combination therapy for Helicobacter pylori eradication protocols).
Metronidazole Benzoate
https://en.wikipedia.org/wiki/Metronidazole

Metronidazole, marketed under the brand name Flagyl among others, is an antibiotic and antiprotozoal medication. It is used either alone or with other antibiotics to treat pelvic inflammatory disease, endocarditis, and bacterial vaginosis. It is effective for dracunculiasis, giardiasis, trichomoniasis, and amebiasis. It is an option for a first episode of mild-to-moderate Clostridium difficile colitis if vancomycin or fidaxomicin is unavailable.
Metronidazole is of the nitroimidazole class. It inhibits nucleic acid synthesis by forming nitroso radicals, which disrupt the DNA of microbial cells. This function only occurs when metronidazole is partially reduced, and because this reduction usually happens only in anaerobic bacteria and protozoans, it has relatively little effect upon human cells or aerobic bacteria.
Glycopeptide Antibacterial Teicoplanin
https://en.wikipedia.org/wiki/Teicoplanin

Teicoplanin is an antibiotic used in the prophylaxis and treatment of serious infections caused by Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus and Enterococcus faecalis. It is a semisynthetic glycopeptide antibiotic with a spectrum of activity similar to vancomycin. Its mechanism of action is to inhibit bacterial cell wall synthesis.Teicoplanin (TARGOCID, marketed by Sanofi Aventis Ltd) is actually a mixture of several compounds, five major (named teicoplanin A2-1 through A2-5) and four minor (named teicoplanin RS-1 through RS-4). All teicoplanins share a same glycopeptide core,

termed teicoplanin A3-1 — a fused ring structure to which two carbohydrates (mannose and N-acetylglucosamine) are attached. The major and minor components also contain a third carbohydrate moiety  
β-D-glucosamine
 — and differ only by the length and conformation of a side-chain attached to it.

Macrolides Azithromycin
https://en.wikipedia.org/wiki/Azithromycin

Azithromycin is an antibiotic used for the treatment of a number of bacterial infections. This includes middle ear infections, strep throat, pneumonia, traveler's diarrhea, and certain other intestinal infections. It can also be used for a number of sexually transmitted infections, including chlamydia and gonorrhea infections. Along with other medications, it may also be used for malaria. It can be taken by mouth or intravenously with doses once per day.Azithromycin prevents bacteria from growing by interfering with their protein synthesis. It binds to the 50S subunit of the bacterial ribosome, thus inhibiting translation of mRNA. Nucleic acid synthesis is not affected.

Erythromycin
https://en.wikipedia.org/wiki/Erythromycin

Erythromycin is an antibiotic used for the treatment of a number of bacterial infections. This includes respiratory tract infections, skin infections, chlamydia infections, pelvic inflammatory disease, and syphilis. It may also be used during pregnancy to prevent Group B streptococcal infection in the newborn, as well as to improve delayed stomach emptying. It can be given intravenously and by mouth. An eye ointment is routinely recommended after delivery to prevent eye infections in the newborn.

Erythromycin displays bacteriostatic activity or inhibits growth of bacteria, especially at higher concentrations. By binding to the 50s subunit of the bacterial rRNA complex, protein synthesis and subsequent structure and function processes critical for life or replication are inhibited. Erythromycin interferes with aminoacyl translocation, preventing the transfer of the tRNA bound at the A site of the rRNA complex to the P site of the rRNA complex. Without this translocation, the A site remains occupied, thus the addition of an incoming tRNA and its attached amino acid to the nascent polypeptide chain is inhibited. This interferes with the production of functionally useful proteins, which is the basis of this antimicrobial action.

Erythromycin increases gut motility by binding to Motillin, thus it is a Motillin receptor agonist in addition to its antimicrobial properties.

Fidaxomicin
https://en.wikipedia.org/wiki/Fidaxomicin

Fidaxomicin, sold under the brand name Dificid among others, is the first member of a class of narrow spectrum macrocyclic antibiotic drugs called tiacumicins.[2] It is a fermentation product obtained from the actinomycete Dactylosporangium aurantiacum subspecies hamdenesis. Fidaxomicin is minimally absorbed into the bloodstream when taken orally, is bactericidal, and selectively eradicates pathogenic Clostridium difficile with relatively little disruption to the multiple species of bacteria that make up the normal, healthy intestinal flora. The maintenance of normal physiological conditions in the colon may reduce the probability of recurrence of Clostridium difficile infection.Fidaxomicin binds to and prevents movement of the "switch regions" of bacterial RNA polymerase. Switch motion occurs during the opening and closing of the DNA:RNA clamp, a process that occurs throughout RNA transcription but is especially important in the opening of double-stranded DNA during the initiation of transcription. It has minimal systemic absorption and a narrow spectrum of activity; it is active against Gram positive bacteria, especially clostridia. The minimal inhibitory concentration (MIC) range for C. difficile (ATCC 700057) is 0.03–0.25 μg/mL

Oxazolidinones Linezolid
https://en.wikipedia.org/wiki/Linezolid

Linezolid is an antibiotic used for the treatment of infections caused by Gram-positive bacteria that are resistant to other antibiotics. Linezolid is active against most Gram-positive bacteria that cause disease, including streptococci, vancomycin-resistant enterococci (VRE), and methicillin-resistant Staphylococcus aureus (MRSA). The main uses are infections of the skin and pneumonia although it may be used for a variety of other infections including drug-resistant tuberculosis.It is used either by injection into a vein or by mouth.

When given for short periods, linezolid is a relatively safe antibiotic. It can be used in people of all ages and in people with liver disease or poor kidney function.

Linezolid, like other oxazolidinones, is a bacterial protein synthesis inhibitor and a weak, non-selective, reversible monoamine oxidase inhibitor. As a protein synthesis inhibitor, linezolid stops the growth and reproduction of bacteria by disrupting translation of messenger RNA (mRNA) into proteins in bacterial ribosomes. Linezolid inhibits translation at the first step of protein synthesis, initiation unlike most other protein synthesis inhibitors, which inhibit elongation. It does so by preventing the formation of the initiation complex, composed of the 30S and 50S subunits of the ribosome, tRNA, and mRNA. Linezolid binds to the 23S portion of the 50S subunit (the center of peptidyl transferase activity), close to the binding sites of chloramphenicol, lincomycin, and other antibiotics. Due to this unique mechanism of action, cross-resistance between linezolid and other protein synthesis inhibitors is highly infrequent or nonexistent.

Penicillins Amoxycillin
https://en.wikipedia.org/wiki/Amoxicillin

Amoxicillin is an antibiotic used to treat a number of bacterial infections. These include middle ear infection, strep throat, pneumonia, skin infections, and urinary tract infections among others. It is taken by mouth, or less commonly by injection.As a derivative of ampicillin, amoxicillin is a member of the penicillin family and, like penicillins, is a β-lactam antibiotic. It inhibits cross-linkage between the linear peptidoglycan polymer chains that make up a major component of the bacterial cell wall. It has two ionizable groups in the physiological range (the amino group in alpha-position to the amide carbonyl group and the carboxyl group).
Ampicillin
https://en.wikipedia.org/wiki/Ampicillin

Ampicillin is an antibiotic used to prevent and treat a number of bacterial infections, such as respiratory tract infections, urinary tract infections, meningitis, salmonellosis, and endocarditis. It may also be used to prevent group B streptococcal infection in newborns. It is used by mouth, by injection into a muscle, or intravenously.Like all antibiotics, it is not useful for the treatment of viral infections.

Ampicillin is in the penicillin group of beta-lactam antibiotics and is part of the aminopenicillin family. It is roughly equivalent to amoxicillin in terms of activity.[3] Ampicillin is able to penetrate Gram-positive and some Gram-negative bacteria. It differs from penicillin G, or benzylpenicillin, only by the presence of an amino group. This amino group, present on both ampicillin and amoxicillin, helps these antibiotics pass through the pores of the outer membrane of Gram-negative bacteria, such as E. coli, Proteus mirabilis, Salmonella enterica, and Shigella.

Ampicillin acts as an irreversible inhibitor of the enzyme transpeptidase, which is needed by bacteria to make the cell wall. It inhibits the third and final stage of bacterial cell wall synthesis in binary fission, which ultimately leads to cell lysis; therefore, ampicillin is usually bacteriolytic.

 

Ampicillin with Sulbactam Sodium
https://en.wikipedia.org/wiki/Sulbactam

Sulbactam is a β-lactamase inhibitor. This drug is given in combination with β-lactam antibiotics to inhibit β-lactamase, an enzyme produced by bacteria that destroys the antibiotics.Sulbactam is an irreversible inhibitor of β-lactamase; it binds to the enzyme and does not allow it to degrade the antibiotic

Cloxacillin
https://en.wikipedia.org/wiki/Cloxacillin

Cloxacillin is an antibiotic useful for the treatment of a number of bacterial infections. This includes impetigo, cellulitis, pneumonia, septic arthritis, and otitis externa. It is not effective for methicillin-resistant Staphylococcus aureus (MRSA). It is used by mouth and by injection.It is It is semisynthetic and in the same class as penicillin. Cloxacillin is used against staphylococci that produce beta-lactamase, due to its large R chain, which does not allow the beta-lactamases to bind. This drug has a weaker antibacterial activity than benzylpenicillin, and is devoid of serious toxicity except for allergic reactions.

Pienicillin-G-Amidase Enzyme
https://en.wikipedia.org/wiki/Amidase

In enzymology, an amidase (EC 3.5.1.4, acylamidase, acylase (misleading), amidohydrolase (ambiguous), deaminase (ambiguous), fatty acylamidase, N-acetylaminohydrolase (ambiguous)) is an enzyme that catalyzes the hydrolysis of an amide.
Piperacillin with Tazobactam
https://en.wikipedia.org/wiki/Piperacillin

Piperacillin is a broad-spectrum β-lactam antibiotic of the ureidopenicillin class. The chemical structure of piperacillin and other ureidopenicillins incorporates a polar side chain that enhances penetration into gram-negative bacteria and reduces susceptibility to cleavage by gram-negative beta lactamase enzymes. These properties confer activity against the important hospital pathogen Pseudomonas aeruginosa. Thus piperacillin is sometimes referred to as an "anti-pseudomonal penicillin".

When used alone, piperacillin lacks strong activity against the gram-positive pathogens such as Staphylococcus aureus, as the beta-lactam ring is hydrolyzed by the bacteria's beta-lactamase.

https://en.wikipedia.org/wiki/Tazobactam

Tazobactam is a pharmaceutical drug that inhibits the action of bacterial β-lactamases, especially those belonging to the SHV-1 and TEM groups. It is commonly used as its sodium salt, tazobactam sodium. In simple terms, it is an ingredient that can be added to certain antibiotics to make them less vulnerable to bacteria's antimicrobial resistance.

Tazobactam is combined with the extended spectrum β-lactam antibiotic piperacillin in the drug piperacillin/tazobactam, used in infections due to Pseudomonas aeruginosa. Tazobactam broadens the spectrum of piperacillin by making it effective against organisms that express β-lactamase and would normally degrade piperacillin.

Tazobactam is a heavily modified penicillin and a sulfone

 

Quinolones Ciprofloxacin
https://en.wikipedia.org/wiki/Ciprofloxacin

Ciprofloxacin is an antibiotic used to treat a number of bacterial infections.This includes bone and joint infections, intra abdominal infections, certain type of infectious diarrhea, respiratory tract infections, skin infections, typhoid fever, and urinary tract infections, among others. For some infections it is used in addition to other antibiotics. It can be taken by mouth, as eye drops, as ear drops, or  intravenously.Ciprofloxacin is a broad-spectrum antibiotic of the fluoroquinolone class. It is active against some Gram-positive and many Gram-negative bacteria. It functions by inhibiting a type
 II topoisomerase 
(DNA gyrase) and topoisomerase IV, necessary to separate bacterial DNA, thereby inhibiting cell division.

Garenoxacin
https://en.wikipedia.org/wiki/Garenoxacin

Garenoxacin (INN) is a quinolone antibiotic for the treatment of Gram-positive and Gram-negative bacterial infections.Garenoxacin was discovered by Toyama Chemical Co., Ltd. of Tokyo, Japan, and is currently being marketed in Japan under the tradename Geninax.

Levofloxacin
https://en.wikipedia.org/wiki/Levofloxacin
Levofloxacin, sold under the trade names Levaquin among others, is an antibiotic. It is used to treat a number of bacterial infections including acute bacterial sinusitis, pneumonia, H. pylori (in combination with other medications), urinary tract infections, chronic prostatitis, and some types of gastroenteritis.Along with other antibiotics it may be used to treat tuberculosis, meningitis, or pelvic inflammatory disease.Use is generally recommended only when other options are not available.It is available by mouth, intravenously,and in eye drop form.

Levofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. Like all quinolones, it functions by inhibiting the DNA gyrase and topoisomerase IV, two bacterial type II topoisomerases. Topoisomerase IV is necessary to separate DNA that has been replicated (doubled) prior to bacterial cell division. With the DNA not being separated, the process is stopped, and the bacterium cannot divide. DNA gyrase, on the other hand, is responsible for supercoiling the DNA, so that it will fit in the newly formed cells. Both mechanisms amount to killing the bacterium. Levofloxacin acts as a bactericide.

As of 2011 the mechanism of action for the drug's musculoskeletal complications were not clear.

Marbofloxacin
https://en.wikipedia.org/wiki/Marbofloxacin

Marbofloxacin is a carboxylic acid derivative third generation fluoroquinolone antibiotic. It is used in veterinary medicine under the trade names Marbocyl, Forcyl, Marbo vet and Zeniquin. A formulation of marbofloxacin combined with clotrimazole and dexamethasone is available under the name Aurizon (CAS number 115550-35-1).Its mechanism of action is not thoroughly understood, but it is believed to be similar to the other fluoroquinolones by impairing the bacterial DNA gyrase which results in rapid bactericidal activity.[1] The other proposed mechanisms include that it acts against nondividing bacteria and does not require protein and RNA synthesis, which block protein and RNA synthesis respectively.

Ofloxacin
https://en.wikipedia.org/wiki/Ofloxacin

Ofloxacin is an antibiotic useful for the treatment of a number of bacterial infections. When taken by mouth or injection into a vein, these include pneumonia, cellulitis, urinary tract infections, prostatitis, plague, and certain types of infectious diarrhea. Other uses, along with other medications, include treating multidrug resistant tuberculosis.[3] An eye drop may be used for a superficial bacterial infection of the eye and an ear drop may be used for otitis media when a hole in the ear drum is present.Ofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It functions by inhibiting two bacterial type II topoisomerases, DNA gyrase and topoisomerase IV. Topo IV is an enzyme necessary to separate (mostly in prokaryotes, in bacteria in particular) replicated DNA, thereby inhibiting bacterial cell division.

Sparfloxacin
https://en.wikipedia.org/wiki/Sparfloxacin

.Sparfloxacin is a fluoroquinolone antibiotic used in the treatment of bacterial infections. It has a controversial safety profile.Sparfloxacin, like other quinolones and fluoroquinolones, are bactericidal drugs, actively killing bacteria. Quinolones inhibit the bacterial DNA gyrase or the topoisomerase IV enzyme, thereby inhibiting DNA replication and transcription. Quinolones can enter cells easily and therefore are often used to treat intracellular pathogens such as Legionella pneumophila and Mycoplasma pneumoniae. For many gram-negative bacteria DNA gyrase is the target, whereas topoisomerase IV is the target for many gram-positive bacteria. Eukaryotic cells do not contain DNA gyrase or topoisomerase IV.

Tetracyclines Tigecycline
https://en.wikipedia.org/wiki/Tigecycline

Tigecycline is an antibiotic for a number of bacterial infections. It is a glycylcycline administered intravenously. It was developed in response to the growing rate of antibiotic resistant bacteria such as Staphylococcus aureus, Acinetobacter baumannii, and E. coli. As a tetracycline derivative antibiotic, its structural modifications has expanded its therapeutic activity to include Gram-positive and Gram-negative organisms, including those of multi-drug resistance.

Tigecycline is broad-spectrum antibiotic that acts as a protein synthesis inhibitor. It exhibits bacteriostatic activity by binding to the 30S ribosomal subunit of bacteria and thereby blocking the interaction of aminoacyl-tRNA with the A site of the ribosome. In addition, tigecycline has demonstrated bactericidal activity against isolates of S. pneumoniae and L. pneumophila.

It is a third generation tetracycline derivative within a class called glycylcyclines which carry a N,N-dimethyglycylamido (DMG) moiety attached to the 9-position of tetracycline ring D. With structural modifications as a 9-DMG derivative of minocycline, tigecycline has been found to improve minimal inhibitory concentrations against Gram-negative and Gram-positive organisms, when compared to tetracyclines.

   
Antidiabetic & pcos
Antidiabetic Agents Repaglinide
https://en.wikipedia.org/wiki/Repaglinide

Repaglinide is an antidiabetic drug in the class of medications known as meglitinides, and was invented in 1983. Repaglinide is an oral medication used in addition to diet and exercise for blood sugar control in type 2 diabetes mellitus. The mechanism of action of repaglinide involves promoting insulin release from β-islet cells of the pancreasRepaglinide lowers blood glucose by stimulating the release of insulin from the beta islet cells of the pancreas. It achieves this by closing ATP-dependent potassium channels in the membrane of the beta cells. This depolarizes the beta cells, opening the cells' calcium channels, and the resulting calcium influx induces insulin secretion.
Metformin HCl
https://en.wikipedia.org/wiki/Metformin

Metformin, marketed under the trade name Glucophage among others, is the first-line medication for the treatment of type 2 diabetes, particularly in people who are overweight. It is also used in the treatment of polycystic ovary syndrome. It is not associated with weight gain.Metformin is the most widely used medication for diabetes taken by mouth. It is available as a generic medication. In 2017, it was the fourth-most commonly prescribed medication in the United States, with more than 78 million prescriptions.
The molecular mechanism of metformin is not completely understood. Multiple potential mechanisms of action have been proposed: inhibition of the mitochondrial respiratory chain (complex I), activation of AMP-activated protein kinase (AMPK), inhibition of glucagon-induced elevation of cyclic adenosine monophosphate (cAMP) with reduced activation of protein kinase A (PKA), inhibition of mitochondrial glycerophosphate dehydrogenase, and an effect on gut microbiota. Metformin also exerts an anorexiant effect in most people, decreasing caloric intake. Ultimately, it decreases gluconeogenesis (glucose production) in the liver. It also has an insulin-sensitizing effect with multiple actions on tissues including the liver, skeletal muscle, endothelium, adipose tissue, and the ovary. The average patient with type 2 diabetes has three times the normal rate of gluconeogenesis; metformin treatment reduces this by over one-third.
Diabetic Neuropathy Epalrestat
https://en.wikipedia.org/wiki/Epalrestat

Epalrestat is a carboxylic acid derivative[1] and a noncompetitive and reversible aldose reductase inhibitor used for the treatment of diabetic neuropathy, which is one of the most common long-term complications in patients with diabetes mellitus. It reduces the accumulation of intracellular sorbitol which is believed to be the cause of diabetic neuropathy, retinopathy and nephropathyIt has been proven in animal experiments that there is an improvement in sorbitol levels and Na+/K+ ATPase activity leading to improved nerve conduction velocity. Diabetic rats treated with epalrestat showed improvement in morphological abnormalities of nerves.

Tapentadol HCl
https://en.wikipedia.org/wiki/Tapentadol

Tapentadol, brand names Nucynta among others, is a centrally acting opioid analgesic of the benzenoid class with a dual mode of action as an agonist of the μ-opioid receptor and as a norepinephrine reuptake inhibitor (NRI). Analgesia occurs within 32 minutes of oral administration, and lasts for 4–6 hours.

It is similar to tramadol in its dual mechanism of action; namely, its ability to activate the mu opioid receptor and inhibit the reuptake of norepinephrine. Unlike tramadol, it has only weak effects on the reuptake of serotonin and is a significantly more potent opioid with no known active metabolites Tapentadol is not a pro-drug and therefore does not rely on metabolism to produce its therapeutic effects; this makes it a useful moderate-potency analgesic option for patients who do not respond adequately to more commonly used opioids due to genetic disposition (poor metabolizers of CYP3A4 and CYP2D6), as well as providing a more consistent dosage-response range among the patient population.

The potency of tapentadol is somewhere between that of tramadol and morphine, with an analgesic efficacy comparable to that of oxycodone despite a lower incidence of side effects. It is generally regarded as a weak-moderate strength opioid (a category shared by many better-known opioids such as hydrocodone and pethidine).

 

DPP-4 Inhibitor (Gliptin) Alogliptin
https://en.wikipedia.org/wiki/Alogliptin

.Alogliptin (trade name Nesina and Vipidia is an oral anti-diabetic drug in the DPP-4 inhibitor (gliptin) class. Alogliptin does not decrease the risk of heart attack and stroke. Like other members of the gliptin class, it causes little or no weight gain, exhibits relatively little risk of hypoglycemia, and has relatively modest glucose-lowering activity. Alogliptin and other gliptins are commonly used in combination with metformin in people whose diabetes cannot adequately be controlled with metformin alone.Alogliptin is a dipeptidyl peptidase-4 inhibitor that decreases blood sugar similar to the other.

Teneligliptin
https://en.wikipedia.org/wiki/Teneligliptin

Teneligliptin (INN; trade name Tenelia) is a pharmaceutical drug for the treatment of type 2 diabetes mellitus. It belongs to the class of anti-diabetic drugs known as dipeptidyl peptidase-4 inhibitors or "gliptins".

Gestational Diabetes Inositol
https://en.wikipedia.org/wiki/Inositol

Inositol, or more precisely myo-inositol, is a carbocyclic sugar that is abundant in brain and other mammalian tissues, mediates cell signal transduction in response to a variety of hormones, neurotransmitters and growth factors and participates in osmoregulation. It is a sugar alcohol with half the sweetness of sucrose (table sugar). It is made naturally in humans from glucose. A human kidney makes about two grams per day. Other tissues synthesize it too, and the highest concentration is in the brain where it plays an important role making other neurotransmitters and some steroid hormones bind to their receptors. Since about 2008 myo-inositol gained importance in the management of polycystic ovary syndrome (PCOS) due to its efficacy, safety profile and worldwide availability.

PCOS D-Chiro-Inositol
https://en.wikipedia.org/wiki/1D-chiro-Inositol

1D-chiro-Inositol (formerly D-chiro-inositol, commonly abbreviated DCI) is a member of a family of related substances often referred to collectively as "inositol", although that term encompasses several isomers of questionable biological relevance, including 1L-chiro-inositol. myo-Inositol is converted into DCI by an insulin dependent NAD/NADH epimerase enzyme.It is known to be an important secondary messenger in insulin signal transduction. DCI accelerates the dephosphorylation of glycogen synthase and pyruvate dehydrogenase, rate limiting enzymes of non-oxidative and oxidative glucose disposal. DCI may act to bypass defective normal epimerization of myo-inositol to DCI associated with insulin resistance and at least partially restore insulin sensitivity and glucose disposal.

SGLT-2 Inhibitor (Gliflozin) Canagliflozin
https://en.wikipedia.org/wiki/Canagliflozin

Canagliflozin, sold under the brand name Invokana
 among others, is a medication used to treat type 2 diabetes. It is a third-line medication to metformin. It is used together with exercise and diet. It is not recommended in type 1 diabetes. It is taken by mouth.

Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of renal glucose reabsorption (the remaining 10% is done by SGLT1). Blocking this transporter causes up to 119 grams of blood glucose per day to be eliminated through the urine, corresponding to 476 kilocalories. Additional water is eliminated by osmotic diuresis, resulting in a lowering of blood pressure.

This mechanism is associated with a low risk of hypoglycaemia (too low blood glucose) compared to other types of anti-diabetic drugs such as sulfonylurea derivatives and insulin.

   
Cardiovascular system
Alpha/Beta Adrenoceptor Agonist Carvedilol HCl / Phosphate
https://en.wikipedia.org/wiki/Carvedilol

Carvedilol, sold under the brand name Coreg among others, is a medication used to treat high blood pressure, congestive heart failure (CHF), and left ventricular dysfunction in people who are otherwise stable. For high blood pressure, it is generally a second-line treatment. It is taken by mouth.[

Carvedilol is both a non-selective beta adrenergic receptor blocker (β1, β2) and an alpha adrenergic receptor blocker (α1). The S(-) enantiomer accounts for the beta blocking activity whereas the S(-) and R(+) enantiomer have alpha blocking activity.

Carvedilol reversibly binds to beta adrenergic receptors on cardiac myocytes. Inhibition of these receptors prevents a response to the sympathetic nervous system, leading to decreased heart rate and contractility. This action is beneficial in heart failure patients where the sympathetic nervous system is activated as a compensatory mechanism.

Carvedilol blockade of α1 receptors causes vasodilation of blood vessels. This inhibition leads to decreased peripheral vascular resistance and an antihypertensive effect. There is no reflex tachycardia response due to carvedilol blockade of β1 receptors on the heart.

Eplerenone
https://en.wikipedia.org/wiki/Eplerenone

Eplerenone, sold under the brand name Inspra, is a steroidal antimineralocorticoid of the spirolactone group that is used as an adjunct in the management of chronic heart failure and high blood pressure, particularly for patients with resistant hypertension due to elevated aldosterone. Classed as a selective aldosterone receptor antagonist (SARA), it is similar to the diuretic spironolactone, though it is much more selective for the mineralocorticoid receptor in comparison (i.e., does not possess any antiandrogen, progestogen, glucocorticoid, or estrogenic effects), and is specifically marketed for educing cardiovascular risk in patients following myocardial infarction. Eplerenone is a potassium-sparing diuretic, meaning that it helps the body get rid of water but still keep potassium.

Fenoterol HBr
https://en.wikipedia.org/wiki/Fenoterol

Fenoterol is a β adrenoreceptor agonist. It is classed as sympathomimetic β2 agonist and an inhaled bronchodilator asthma medication.5-(1-Hydroxy-2-{[2-(4-hydroxyphenyl)-1-methylethyl]amino}ethyl)benzene-1,3-diol is a molecule with two different stereogenic centers. Thus, four stereoisomers may exist, the (R,R)-, (R,S)-, (S,R)- and (S,S)-stereoisomers (see the figure below). Fenoterol is a racemate of the (R,R)- and the (S,S)-enantiomers. This racemate is 9 to 20 times more effective, as compared to the racemate of the (R,S)- and (S,R)-enantiomers.
Icatibant Acetate
https://en.wikipedia.org/wiki/Icatibant

Icatibant, sold under the brand name Firazyr, is a medication for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in adults with C1-esterase-inhibitor deficiency.It is not effective in angioedema caused by medication from the ACE inhibitor class.

It is a peptidomimetic consisting of ten amino acids, which is a selective and specific antagonist of bradykinin B2 receptors. It cost about US$8,000 to 9,000 per dose as of 2014.

Imiquimod
https://en.wikipedia.org/wiki/Imiquimod

Imiquimod (INN) is a prescription medication that acts as an immune response modifier that is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis. 

miquimod yields profound antitumoral activity by acting on several immunological levels synergistically.[9] Imiquimod stimulates the innate immune system by activating toll-like receptor 7 (TLR7), commonly involved in pathogen recognition.Cells activated by imiquimod via TLR-7 secrete cytokines (primarily interferon-α (IFN-α), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α)).There is evidence that imiquimod, when applied to skin, can lead to the activation of Langerhans cells, which subsequently migrate to local lymph nodes to activate the adaptive immune system. Other cell types activated by imiquimod include natural killer cells, macrophages and B-lymphocytes.

Imiquimod exerts its effect by increasing levels of the opioid growth factor receptor (OGFr). In experiments, blocking OGFr function with siRNA technology resulted in loss of any antiproliferative effect of imiquimod.

Isoprenaline HCl
https://en.wikipedia.org/wiki/Isoprenaline

Isoprenaline, or isoproterenol, is a medication used for the treatment of bradycardia (slow heart rate) heart block, and rarely for asthma. It is a non-selective β adrenoreceptor agonist that is the isopropylamine analog of epinephrine (adrenaline).Isoprenaline is a β1 and β2 adrenoreceptor agonist and has almost no activity on alpha adrenergic receptors. Its agonist effects at TAAR1 provide it with a pharmacodynamic effects that resemble those of the endogenous trace amines, like tyramine.The isopropylamine group in isoprenaline makes it selective for β receptors. The free catechol hydroxyl groups keep it susceptible to enzymatic metabolism.

Levosalbutamol HCl / Sulphate / Tartrate
https://en.wikipedia.org/wiki/Levosalbutamol

Levosalbutamol, also known as levalbuterol, is a short-acting β2 adrenergic receptor agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). Evidence does not show that levosalbutamol works better than salbutamol; thus there may not be sufficient justification for prescribing it.

The drug is the (R)-(−)-enantiomer of its prototype drug salbutamol.

Activation of β2 adrenergic receptors on airway smooth muscle leads to the activation of adenylate cyclase and to an increase in the intracellular concentration of 3',5'-cyclic adenosine monophosphate (cyclic AMP). The increase in cyclic AMP is associated with the activation of protein kinase A, which in turn, inhibits the phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in muscle relaxation.

Levosalbutamol relaxes the smooth muscles of all airways, from the trachea to the terminal bronchioles. Increased cyclic AMP concentrations are also associated with the inhibition of the release of mediators from mast cells in the airways. Levosalbutamol acts as a functional agonist that relaxes the airway irrespective of the spasmogen involved, thereby protecting against all bronchoconstrictor challenges.

While it is recognized that β2 adrenergic receptors are the predominant receptors on bronchial smooth muscle, data indicate that there are beta receptors in the human heart, 10–50% of which are β2 adrenergic receptors. The precise function of these receptors has not been established. However, all β adrenergic agonist drugs can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, and restlessness symptoms, and/or electrocardiographic (ECG).

Macitentan
https://en.wikipedia.org/wiki/Macitentan

Macitentan (trade name Opsumit) is an endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH). The other two ERAs marketed as of 2014 are bosentan and ambrisentan. Macitentan is a dual ERA, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype..Endothelin (ET) is an extremely potent blood vessel constricting substance that is secreted by endothelial cells. In the lungs, the most common ET form released is ET-1. ET-1 release can occur through both constitutive and non-constitutive pathways. Upon release, ET-1 can bind to the ET receptors that are expressed on arterial smooth muscle cells and fibroblasts in the lungs. ET receptors are G protein coupled receptors and, when activated, lead to an increase in intracellular calcium levels via the Gαq signaling pathway. The rise in intracellular calcium leads to contraction of the arterial smooth muscle, as well as vascular remodelling due to cell proliferation. Prolonged constriction and fibrosis are factors in the pathogenesis of PAH.

Ractopamine HCl
https://en.wikipedia.org/wiki/Ractopamine

Ractopamine is an animal feed additive used to promote leanness and increase food conversion efficiency in livestock in some countries, but banned in others. Pharmacologically, it is a phenol-based TAAR1 agonist and β adrenoreceptor agonist that stimulates β1 and β2 adrenergic receptors.It is most commonly administered to animals for meat production as ractopamine hydrochloride.It is the active ingredient in products marketed in the US as Paylean for swine, Optaflexx for cattle, and Topmax for turkeys.It was developed by Elanco Animal Health, a division of Eli Lilly and Company.

As of 2014 the use of ractopamine was banned in 160 countries, including the European Union, mainland China and Russia, while 27 other countries, such as Japan, the United States, South Korea, and New Zealand have deemed meat from livestock fed ractopamine safe for human consumption.

Commercial ractopamine is a mixture of all four possible stereoisomers.It is also a positional isomer of dobutamine, a related drug.

Silodosin
https://en.wikipedia.org/wiki/Silodosin

Silodosin (trade names Urief in Japan, Rapaflo in the US, and Silodyx in Europe) is a medication for the symptomatic treatment of benign prostatic hyperplasia (BPH). It acts as an α1-adrenoceptor antagonist with high uroselectivity (selectivity for the prostate).Silodosin has high affinity for the α1A adrenergic receptor in the prostate, the bladder, and the prostatic urethra. By this mechanism it
 relaxes the smooth muscle in these organs, easing urinary flow and other symptoms of BPH.

Tizanidine HCl
https://en.wikipedia.org/wiki/Tizanidine

Tizanidine, sold under the brand name Zanaflex among others, is a medication that is used to treat muscle spasticity due to spinal cord injury or multiple sclerosis. Effectiveness appears similar to baclofen or diazepam.It is taken by mouth.[Tizanidine is an α2 receptor agonist closely related to clonidine. It has approximately one tenth to one fifteenth of the pressure lowering effect of clonidine. The relation between the α2 receptor agonism and the spasmolytic action is still not fully understood.

Tulobuterol Base / HCl
https://en.wikipedia.org/wiki/Tulobuterol

Tulobuterol (INN) is a long-acting beta2-adrenergic receptor agonist, marketed in Japan as a transdermal patch under the name Hokunalin tape (ホクナリンテープ).

Currently, it is only legal in 7 countries: Japan, Germany, China, South Korea, Bangladesh, Pakistan, and Venezuela. It is available in India also.

 
Anti-Anginal Drug Amlodipine
https://en.wikipedia.org/wiki/Amlodipine

Amlodipine, sold under the brand name Norvasc among others, is a medication used to treat high blood pressure and coronary artery disease.[6] While not typically recommended in heart failure, amlodipine may be used if other medications are not sufficient for treating high blood pressure or heart-related chest pain. It is taken by mouth and has an effect that lasts for at least a day.In 2017, it was the fifth most commonly prescribed medication in the United States, with more than 72 million prescriptions.

Amlodipine is an angioselective calcium channel blocker and inhibits the movement of calcium ions into vascular smooth muscle cells and cardiac muscle cells which inhibits the contraction of cardiac muscle and vascular smooth muscle cells. Amlodipine inhibits calcium ion influx across cell membranes, with a greater effect on vascular smooth muscle cells. This causes vasodilation and a reduction in peripheral vascular resistance, thus lowering blood pressure. Its effects on cardiac muscle also prevent excessive constriction in the coronary arteries.

Negative inotropic effects can be detected in vitro, but such effects have not been seen in intact animals at therapeutic doses. Among the two stereoisomers [R(+), S(–)], the (–) isomer has been reported to be more active than the (+) isomer.[36] Serum calcium concentration is not affected by amlodipine. And it specifically inhibits the currents of L-type Cav1.3 channels in the zona glomerulosa of the adrenal gland.

Isosorbide 5 MonoNitrate
https://en.wikipedia.org/wiki/Isosorbide_mononitrate

Isosorbide mononitrate, sold under many brand names, is a medication used for heart-related chest pain (angina), heart failure, and esophageal spasms. It can be used both to treat and to prevent eart-related chest pain; however, it is generally less preferred than beta blockers or calcium channel blockers. It is taken by mouth.

Isosorbide Dinitrate
https://en.wikipedia.org/wiki/Isosorbide_dinitrate

Isosorbide dinitrate (ISDN) is a medication used for heart failure, esophageal spasms, and to treat and prevent chest pain from not enough blood flow to the heart. It has been found to be particularly useful in heart failure due to systolic dysfunction together with hydralazine in black people. It is taken by mouth or under the tongue.
Similar to other nitrites and organic nitrates, isosorbide dinitrate is converted to nitric oxide (NO), an active intermediate compound which activates the enzyme guanylate cyclase (atrial natriuretic peptide receptor A). This stimulates the synthesis of cyclic guanosine 3',5'-monophosphate (cGMP) which then activates a series of protein kinase-dependent phosphorylations in the smooth muscle cells, eventually resulting in the dephosphorylation of the myosin light chain of the smooth muscle fiber. The subsequent sequestration of calcium ions results in the relaxation of the smooth muscle cells and vasodilation.


Ivabradine
https://en.wikipedia.org/wiki/Ivabradine

Ivabradine, marketed under trade names including Coralan, Corlentor, Procoralan, Coraxan, and many more,is a medication used for the symptomatic management of stable heart-related chest pain and heart failure not fully managed by beta blockers.

Ivabradine acts by reducing the heart rate via specific inhibition of the pacemaker current, a mechanism different from that of beta blockers and calcium channel blockers, two commonly prescribed antianginal drugs. Ivabradine is a cardiotonic agent.

Ivabradine acts on the If (f is for "funny", so called because it had unusual properties compared with other current systems known at the time of its discovery) ion current, which is highly expressed in the sinoatrial node. If is a mixed Na+–K+ inward current activated by hyperpolarization and modulated by the autonomic nervous system. It is one of the most important ionic currents for regulating pacemaker activity in the sinoatrial (SA) node. Ivabradine selectively inhibits the pacemaker If current in a dose-dependent manner. Blocking this channel reduces cardiac pacemaker activity, selectively slowing the heart rate and allowing more time for blood to flow to the myocardium. This is in contrast to other commonly used rate-reducing medications, such as beta-blockers and calcium channel blockers, which not only reduce heart rate, but also the cardiac contractility. Given the selective decrease in rate without loss of contractility, ivabradine may prove efficacious for treatment of congestive heart failure with reduced ejection fraction.

Ivabradine binds to HCN4 receptors (Potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel 4), utilizing Y506, F509 and I510 residues.

Nifedipine
https://en.wikipedia.org/wiki/Nifedipine

Nifedipine, sold under the brand name Adalat among others, is a medication used to manage angina, high blood pressure, Raynaud's phenomenon, and premature labor. It is one of the treatments of choice for Prinzmetal angina. It may be used to treat severe high blood pressure in pregnancy.Its use in preterm labor may allow more time for steroids to improve the baby's lung function and provide time for transfer of the mother to a well qualified medical facility before delivery. It is a calcium channel blocker of the dihydropyridine type. Nifedipine is taken by mouth and comes in fast and slow release formulations..

Nifedipine is a calcium channel blocker. Although nifedipine and other dihydropyridines are commonly regarded as specific to the L-type calcium channel, they also possess nonspecific activity towards other voltage-dependent calcium channels.

Nifedipine has additionally been found to act as an antagonist of the mineralocorticoid receptor, or as an antimineralocorticoid
.

Pazopanib
https://en.wikipedia.org/wiki/Pazopanib

Pazopanib (trade name Votrient) is an anti-cancer drug. It is a potent and selective multi-targeted receptor tyrosine kinase inhibitor that blocks tumour growth and inhibits angiogenesis. It has been approved for renal cell carcinoma and soft tissue sarcoma by numerous regulatory administrations worldwide..Pazopanib is a multiple kinase inhibitor that limits tumor growth by targeting angiogenesis via inhibition of enzymes including vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), c-KIT and FGFR.

Antianemic Agent Ferrous Bisglycinate
https://en.wikipedia.org/wiki/List_of_combined_sex-hormonal_preparations

.Glycine (symbol Gly or G; /ˈɡlsn/) is an amino acid that has a single hydrogen atom as its side chain. It is the simplest amino acid (since carbamic acid is unstable), with the chemical formula NH2CH2COOH. Glycine is one of the proteinogenic amino acids. It is encoded by all the codons starting with GG (GGU, GGC, GGA, GGG). Glycine is not widely used in foods for its nutrional value, except in infusions. Instead glycine's role in food chemistry is as a flavorant. It is mildly sweet, and it counters the aftertaste of saccharine. It also has preservative properties, perhaps owing to its complexation to metal ions. Metal glycinate complexes, e.g. copper(II) glycinate are used as supplements for animal feeds..

Antiarrhythmic Drugs Amiodarone HCl
https://en.wikipedia.org/wiki/Tramadol

Tramadol, sold under the brand name Ultram among others, is an opioid pain medication used to treat moderate to moderately severe pain. When taken by mouth in an immediate-release formulation, the onset of pain relief usually begins within an hour. It is also available by injection. It may be sold in combination with paracetamol (acetaminophen) or as longer-acting formulations.Tramadol induces analgesic effects through a variety of different targets on the noradrenergic system, serotoninergic system and opioid receptors system. Tramadol exists as a racemic mixture, the positive enantiomer inhibits serotonin reuptake while the negative enantiomer inhibits noradrenaline re-uptake, by binding to and blocking the transporters. Tramadol has also been shown to act as a serotonin releasing agent. Both enantiomers of tramadol are agonists of the μ-opioid receptor and its M1 metabolite, O-demethylate, is also a μ-opioid receptor agonist but is 6 times more potent than tramadol itself. All these effects work synergistically to induce analgesia..

Diltiazem
https://en.wikipedia.org/wiki/Diltiazem

Diltiazem
, sold under the brand name Cardizem among others, is a calcium channel blocker medication used to treat high blood pressure, angina, and certain heart arrhythmias. It may also be used in hyperthyroidism if beta blockers cannot be used. It is taken by mouth or injection into a vein.When given by injection, effects typically begin within a few minutes and last a few hours.Diltiazem, also known as (2S,3S)-3-acetoxy-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one hydrochlorid has a vasodilating activity attributed to the (2S,3S)-isomer. Diltiazem is a potent vasodilator, increasing blood flow and variably decreasing the heart rate via strong depression of A-V node conduction. Its pharmacological activity is somewhat similar to verapamil, another nondihydropyridine (non-DHP) calcium channel blocker. Chemically, it is based upon a 1,4-thiazepine ring, making it a benzothiazepine-type calcium channel blocker..

Dronedarone
https://en.wikipedia.org/wiki/Dronedarone

Dronedarone
 (development codename SR33589 and marketed as Multaq) is a drug by Sanofi-Aventis, mainly for the indication of cardiac arrhythmias. It was approved by the FDA on July 2, 2009. It was recommended as an alternative to amiodarone for the treatment of atrial fibrillation and atrial flutter in people whose hearts have either returned to normal rhythm or who undergo drug therapy or electric shock treatment i.e. direct current cardioversion (DCCV) to maintain normal rhythm..Dronedarone has been termed a “multichannel blocker” however it is unclear which channel(s) play a pivotal role in its success. Thus, dronedarone's actions at the cellular level are controversial with most studies suggesting an inhibition in multiple outward potassium currents including rapid delayed rectifier, slow delayed rectifier and ACh-activated inward rectifier. It is also believed to reduce inward rapid Na current and L-type Ca channels. 

Lidocaine (Lignocaine)
https://en.wikipedia.org/wiki/Lidocaine

.Lidocaine, also known as lignocaine, is a medication used to numb tissue in a specific area (local anesthetic) It is also used to treat ventricular tachycardia and to perform nerve blocks. Lidocaine mixed with a small amount of adrenaline (epinephrine) is available to allow larger doses for numbing, to decrease bleeding, and to make the numbing effect last longer.[4] When used as an injectable, lidocaine typically begins working within four minutes and lasts for half an hour to three hours. Lidocaine mixtures may also be applied directly to the skin or mucous membranes to numb the area.

Lidocaine alters signal conduction in neurons by prolonging the inactivation of the fast voltage-gated Na+ channels in the neuronal cell membrane responsible for action potential propagation. With sufficient blockage, the voltage-gated sodium channels will not open and an action potential will not be generated. Careful titration allows for a high degree of selectivity in the blockage of sensory neurons, whereas higher concentrations also affect other types of neurons.

The same principle applies for this drug's actions in the heart. Blocking sodium channels in the conduction system, as well as the muscle cells of the heart, raises the depolarization threshold, making the heart less likely to initiate or conduct early action potentials that may cause an arrhythmia.

Anticoagulants Dabigatran Etexilate
https://en.wikipedia.org/wiki/Dabigatran

.Dabigatran, sold under the brand name Pradaxa among others, is an anticoagulant used to treat and prevent blood clots and to prevent stroke in people with atrial fibrillation. Specifically it is used to prevent blood clots following hip or knee replacement and in those with a history of prior clots. It is used as an alternative to warfarin and does not require monitoring by blood tests. It is taken by mouth.Dabigatran reversibly binds to the active site on the thrombin molecule, preventing thrombin-mediated activation of coagulation factors. Furthermore, dabigatran can inactivate thrombin even when thrombin is fibrin-bound; it reduces thrombin-mediated inhibition of fibrinolysis and, therefore, may enhance fibrinolysis.

Enoxaparin
https://en.wikipedia.org/wiki/Enoxaparin_sodium 

Enoxaparin sodium is an anticoagulant medication (blood thinner). It is used to treat and prevent deep vein thrombosis (DVT) and pulmonary embolism (PE) including during pregnancy and following certain types of surgery. It is also used in those with acute coronary syndrome (ACS) and heart attacks. It is given by injection just under the skin or into a vein. Other uses include inside kidney dialysis machines.Enoxaparin binds to and potentiates antithrombin (a circulating anticoagulant) to form a complex that irreversibly inactivates clotting factor Xa. It has less activity against factor IIa (thrombin) compared to unfractionated heparin (UFH) due to its low molecular weight.
Warfarin Sodium Clathrate
https://en.wikipedia.org/wiki/Warfarin

Warfarin, sold under the brand name Coumadin among others,is a medication that is used as an anticoagulant (blood thinner). It is commonly used to treat blood clots such as deep vein thrombosis and pulmonary embolism, and to prevent stroke in people who have atrial fibrillation, valvular heart disease or artificial heart valves. Less commonly it is used following ST-segment elevation myocardial infarction (STEMI) and orthopedic surgery.

Warfarin decreases blood clotting by blocking an enzyme called vitamin K epoxide reductase that reactivates vitamin K1. Without sufficient active vitamin K1, clotting factors II, VII, IX, and X have decreased clotting ability. The anticlotting protein C and protein S are also inhibited, but to a lesser degree. A few days are required for full effect to occur, and these effects can last for up to five days.

Warfarin first came into commercial use in 1948 as a rat poison. In 1954 it was approved for medical use in the United States.

Antihypertensives Cilnidipine
https://en.wikipedia.org/wiki/Cilnidipine

Cilnidipine is a calcium channel blocker. Cilnidipine is approved for use in Japan, China, India, Korea, and some European countries to treat hypertension.

It is a calcium antagonist accompanied with L-type and N-type calcium channel blocking functions. Unlike other calcium antagonists, cilnidipine can act on the N-type calcium channel in addition to acting on the L-type calcium channel.

Cilnidipine decreases blood pressure and is used to treat hypertension and its comorbidities. Due to its blocking action at the N-type and L-type calcium channel, cilnidipine dilates both arterioles and venules, reducing the pressure in the capillary bed. Cilnidipine is vasoselective and has a weak direct dromotropic effect, a strong vasodepressor effect, and an arrhythmia-inhibiting effect. 
Irbesartan
https://en.wikipedia.org/wiki/Irbesartan

Irbesartan, sold under the brand name Avapro among others, is a medication used to treat high blood pressure, heart failure, and diabetic kidney disease. It is a reasonable initial treatment for high blood pressure.[2] It is taken by mouth.[2] Versions are available as the combination irbesartan/hydrochlorothiazide.As with all angiotensin II receptor antagonists, irbesartan is used for the treatment of hypertension. It may also delay progression of diabetic nephropathy and is also indicated for the reduction of renal disease progression in patients with type 2 diabetes, hypertension and microalbuminuria (>30 mg/24 h) or proteinuria (>900 mg/24 h)..

Losartan Potassium
https://en.wikipedia.org/wiki/Losartan

All of the physiological effects of angiotensin II, including release of aldosterone, are antagonized in the presence of losartan. Reduction in blood pressure occurs independently of the status of the renin–angiotensin system. As a result of losartan dosing, plasma renin
 activity increases due to removal of the angiotensin II feedback. Renin is released from the kidneys when there is reduced renal arterial pressure, sympathetic activation, or increased sodium delivery to the distal renal tubule. Renin then acts by converting angiotensinogen to angiotensin I; angiotensin converting enzyme (ACE) converts angiotensin I to angiotensin II; angiotensin II causes vasoconstriction and aldosterone release. Aldosterone serves to retain sodium from the distal renal tubule. Sodium retention ultimately results in increased blood pressure. Therefore, the use of angiotensin II receptor antagonists like losartan result in blocking the downstream effect of renin, angiotensin II, and ultimately decreasing blood pressure.

Moexipril
https://en.wikipedia.org/wiki/Moexipril

Moexipril an angiotensin converting enzyme inhibitor (ACE inhibitor) used for the treatment of hypertension and congestive heart failure. Moexipril can be administered alone or with other antihypertensives or diuretics.

It works by inhibiting the conversion of angiotensin I to angiotensin II.As an ACE inhibitor, moexipril causes a decrease in ACE. This blocks the conversion of angiotensin I to angiotensin II. Blockage of angiotensin II limits hypertension within the vasculature. Additionally, moexipril has been found to possess cardioprotective properties.

Sodium Nitroprusside
https://en.wikipedia.org/wiki/Sodium_nitroprusside

Sodium nitroprusside (SNP), sold under the brand name Nitropress among others, is a medication used to lower blood pressure. This may be done if the blood pressure is very high and resulting in symptoms, in certain types of heart failure, and during surgery to decrease bleeding. It is used by continuous injection into a vein.Onset is typically immediate and effects last for up to ten minutes..

As a result of its breakdown to nitric oxide (NO), sodium nitroprusside has potent vasodilating effects on arterioles and venules (veins more than arteries) but this selectivity is much less marked than that of nitroglycerin.

Sodium nitroprusside breaks down in circulation to release nitric oxide (NO). It does this by binding to oxyhaemoglobin to release cyanide, methaemoglobin and nitric oxide. NO activates guanylate cyclase in vascular smooth muscle and increases intracellular production of cGMP. cGMP activates protein kinase G which activates phosphatases which inactivate myosin light chains.[28] Myosin light chains are involved in muscle contraction. The end result is vascular smooth muscle relaxation, which allow vessels to dilate.[This mechanism is similar to that of phosphodiesterase 5 (PDE5) inhibitors such as sildenafil (Viagra) and tadalafil (Cialis), which elevate cGMP concentration by inhibiting its degradation by PDE5.

Atorvastatin Calcium
https://en.wikipedia.org/wiki/Atorvastatin

Atorvastatin, sold under the brand name Lipitor among others, is a statin medication used to prevent cardiovascular disease in those at high risk and treat abnormal lipid levels. For the prevention of cardiovascular disease, statins are a first-line treatment.[
As with other statins, atorvastatin is a competitive inhibitor of HMG-CoA reductase. Unlike most others, however, it is a completely synthetic compound. HMG-CoA reductase catalyzes the reduction of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, which is the rate-limiting step in hepatic cholesterol biosynthesis. Inhibition of the enzyme decreases de novo cholesterol synthesis, increasing expression of low-density lipoprotein receptors (LDL receptors) on hepatocytes. This increases LDL uptake by the hepatocytes, decreasing the amount of LDL-cholesterol in the blood. Like other statins, atorvastatin also reduces blood levels of triglycerides and slightly increases levels of HDL-cholesterol.
Antiparkinsonian Drugs Levodopa
https://en.wikipedia.org/wiki/L-DOPA

l-DOPA crosses the protective blood-brain barrier, whereas dopamine itself cannot. Thus, l-DOPA is used to increase dopamine concentrations in the treatment of Parkinson's disease and dopamine-responsive dystonia. Once l-DOPA has entered the central nervous system, it is converted into dopamine by the enzyme aromatic l-amino acid decarboxylase, also known as DOPA decarboxylase. Pyridoxal phosphate (vitamin B6) is a required cofactor in this reaction, and may occasionally be administered along with l-DOPA, usually in the form of pyridoxine.Herbal extracts containing l-DOPA are available; high-yielding sources include Mucuna pruriens (velvet bean), and Vicia faba (broad bean), while other sources include the genera Phanera, Piliostigma, Cassia, Canavalia, and Dalbergia.

Rosuvastatin Calcium
https://en.wikipedia.org/wiki/Rosuvastatin

Rosuvastatin, sold under the trade name Crestor among others, is a statin medication, used to prevent cardiovascular disease in those at high risk and treat abnormal lipids. It is recommended to be used together with dietary changes, exercise, and weight loss. It is taken by mouth.

Rosuvastatin is a competitive inhibitor of the enzyme HMG-CoA reductase, having a mechanism of action similar to that of other statins.

Putative beneficial effects of rosuvastatin therapy on chronic heart failure may be negated by increases in collagen turnover markers as well as a reduction in plasma coenzyme Q10 levels in patients with chronic heart failure.

   
Antiplatelet Drugs Clopidogrel
https://en.wikipedia.org/wiki/Clopidogrel

Clopidogrel, sold under the trade name Plavix among others, is an antiplatelet medication used to reduce the risk of heart disease and stroke in those at high risk. It is also used together with aspirin in heart attacks and following the placement of a coronary artery stent (dual antiplatelet therapy). It is taken by mouth.[4] Onset of effects is about two hours and lasts for five days.Clopidogrel is a prodrug, which is activated in two steps, first by CYP2C19, CYP1A2 and CYP2B6, then by CYP2C19, CYP2C9, CYP2B6 and CYP3A. The active metabolite then specifically and irreversibly inhibits the P2Y12 subtype of ADP receptor, which is important in activation of platelets and eventual cross-linking by the protein fibrin. Platelet inhibition can be demonstrated two hours after a single dose of oral clopidogrel, but the onset of action is slow, so a loading dose of either 600 or 300 mg is administered when a rapid effect is needed.

Attention Deficit Hyperactivity Disorder (ADHD) Clonidine HCl
https://en.wikipedia.org/wiki/Clonidine

Clonidine, sold as the brand name Catapres among others, is a medication used to treat high blood pressure, attention deficit hyperactivity disorder, drug withdrawal (alcohol, opioids, or smoking), menopausal flushing, diarrhea, and certain pain conditions.[7] It is used by mouth, by injection, or as a skin patch.

Clonidine crosses the blood-brain barrier.

Clonidine treats high blood pressure by stimulating α2 receptors in the brain stem, which decreases peripheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic α2 receptors in the vasomotor center in the brainstem. This binding has a sympatholytic effect, suppresses release of norepinephrine, ATP, renin, and neuropeptide Y which if released would increase vascular resistance.

Beta Blockers Atenolol
https://en.wikipedia.org/wiki/Atenolol

.Atenolol is a beta blocker medication primarily used to treat high blood pressure and heart-associated chest pain.Atenolol, however, does not seem to improve mortality in those with high blood pressure. Other uses include the prevention of migraines and treatment of certain irregular heart beats.

Atenolol is used for a number of conditions including hypertension, angina, long QT syndrome, acute myocardial infarction, supraventricular tachycardia, ventricular tachycardia, and the symptoms of alcohol withdrawal.

The role for β-blockers in general in hypertension was downgraded in June 2006 in the United Kingdom, and later in the United States, as they are less appropriate than other agents such as ACE inhibitors, calcium channel blockers, thiazide diuretics and angiotensin receptor blockers, particularly in the elderly.

Labetalol
https://en.wikipedia.org/wiki/Labetalol

Labetalol is a medication used to treat high blood pressure and in long term management of angina. This includes essential hypertension, hypertensive emergencies, and hypertension of pregnancy. In essential hypertension it is generally less preferred than a number of other blood pressure medications.

Labetalol's dual alpha and beta adrenergic antagonism has different physiological effects in short- and long-term situations. In short-term, acute situations, labetalol decreases blood pressure by decreasing systemic vascular resistance with little effect on stroke volume, heart rate and cardiac output.During long-term use, labetalol can reduce heart rate during exercise while maintaining cardiac output by an increase in stroke volume.

Labetalol is a dual alpha (α1) and beta (β1/β2) adrenergic receptor blocker and competes with other Catecholamines for binding to these sites. Its action on these receptors are potent and reversible Labetalol is highly selective for postsynaptic alpha1- adrenergic, and non-selective for beta-adrenergic receptors. It is about equipotent in blocking beta1- and beta2- receptors.

Metoprolol
https://en.wikipedia.org/wiki/Metoprolol

Metoprolol, marketed under the tradename Lopressor among others, is a selective β1 receptor blocker medication. It is used to treat high blood pressure, chest pain due to poor blood flow to the heart, and a number of conditions involving an abnormally fast heart rate. It is also used to prevent further heart problems after myocardial infarction and to prevent headaches in those with migraines.Metoprolol blocks β1 adrenergic receptors in heart muscle cells, thereby decreasing the slope of phase 4 in the
 nodal action potential (reducing Na+ uptake) and prolonging repolarization of phase 3 (slowing down
 K+ release).It also suppresses the norepinephrine-induced increase in the sarcoplasmic reticulum (SR)
Ca2+ leak and the spontaneous SR Ca2+ release, which are the major triggers for atrial fibrillation.


Moxonidine
https://en.wikipedia.org/wiki/Moxonidine

Moxonidine (INN) is a new-generation alpha-2/imidazoline receptor agonist antihypertensive drug licensed for the treatment of mild to moderate essential hypertension. It may have a role when thiazides, beta-blockers, ACE inhibitors, and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction. It is also a growth hormone releaser.

Moxonidine is a selective agonist at the imidazoline receptor subtype 1 (I1). This receptor subtype is found in both the rostral ventro-lateral pressor and ventromedial depressor areas of the medulla oblongata. Moxonidine therefore causes a decrease in sympathetic nervous system activity and, therefore, a decrease in blood pressure.

Compared to the older central-acting antihypertensives, moxonidine binds with much greater affinity to the imidazoline I1-receptor than to the α2-receptor. In contrast, clonidine binds to both receptors with near equal affinity. Moxonidine has an affinity for I1 that is 33 times greater than α2, compared to clonidine which is only four times greater.

In addition, moxonidine may also promote sodium excretion, improve insulin resistance and glucose tolerance and protect against hypertensive target organ damage, such as kidney disease and cardiac hypertrophy.

Nadolol
https://en.wikipedia.org/wiki/Nadolol

Nadolol, sold under the brand name Corgard among others, is a medication used to treat high blood pressure, heart pain, and atrial fibrillation. It has also been used to prevent migraine headaches and complications of cirrhosis It is taken by mouth.

Nadolol is a non-selective beta blocker; that is, it non-selectively blocks both beta-1 and beta-2 receptors. It has a preference for beta-1 receptors, which are predominantly located in the heart, thereby inhibiting the effects of catecholamines and causing a decrease in heart rate and blood pressure. Its inhibition of beta-2 receptors, which are mainly located in the bronchial smooth muscle of the airways, leads to airway constriction similar to that seen in asthma. Inhibition of beta-1 receptors in the juxtaglomerular apparatus of the kidney inhibits the renin–angiotensin system, causing a decrease in vasoconstriction and a decrease in water retention. Nadolol's inhibition of beta-1 receptors in the heart and kidney leads to its effects on lowering blood pressure.

The drug impairs AV node conduction and decreases sinus rate.

Nadolol may also increase plasma triglycerides and decrease HDL-cholesterol levels.

Propranolol
https://en.wikipedia.org/wiki/Propranolol

Propranolol, sold under the brand name Inderal among others, is a medication of the beta blocker class. It is used to treat high blood pressure, a number of types of irregular heart rate, thyrotoxicosis, capillary hemangiomas, performance anxiety, and essential tremors.[1][2][3] It is used to prevent migraine headaches, and to prevent further heart problems in those with angina or previous heart attacks.Propranolol is a non-selective beta receptor antagonist. It competes with sympathomimetic neurotransmitters for binding to receptors, which inhibits sympathetic stimulation of the heart. Blockage of neurotransmitter binding to beta 1 receptors on cardiac myocytes inhibits activation of adenylate cyclase, which in turn inhibits cAMP synthesis leading to reduced PKA activation. This results in less calcium influx to cardiac myocytes through voltage gated L-type calcium channels meaning there is a decreased sympathetic effect on cardiac cells, resulting in antihypertensive effects including reduced heart rate and lower arterial blood pressure..

S - Metoprolol Succinate
https://en.wikipedia.org/wiki/Metoprolol

Metoprolol, marketed under the tradename Lopressor among others, is a selective β1 receptor blocker medication.[3] It is used to treat high blood pressure, chest pain due to poor blood flow to the heart, and a number of conditions involving an abnormally fast heart rate.[3] It is also used to prevent further heart problems after myocardial infarction and to prevent headaches in those with migraines.Metoprolol blocks β1 adrenergic receptors in heart muscle cells, thereby decreasing the slope of phase 4 in the nodal action potential (reducing Na+ uptake) and prolonging repolarization of phase 3 (slowing down K+ release). It also suppresses the norepinephrine-induced increase in
the sarcoplasmic reticulum (SR) Ca2+ leak and the spontaneous SR Ca2+ release, which are the major
 triggers for atrial fibrillation.
Cardiovascular Energizers Coenzyme Q 10
https://en.wikipedia.org/wiki/Coenzyme_Q10

Coenzyme Q, also known as ubiquinone, is a coenzyme family that is ubiquitous in animals and most bacteria (hence the name ubiquinone). In humans, the most common form is Coenzyme Q10 or ubiquinone-10. CoQ10 is not approved by the U.S. Food and Drug Administration (FDA) for the treatment of any medical condition; however, it is sold as a dietary supplement and is an ingredient in some cosmetics.

It is a 1,4-benzoquinone, where Q refers to the quinone chemical group and 10 refers to the number of isoprenyl chemical subunits in its tail. In natural ubiquinones, the number can be anywhere from 6 to 10. This family of fat-soluble substances, which resemble vitamins, is present in all respiring eukaryotic cells, primarily in the mitochondria. It is a component of the electron transport chain and participates in aerobic cellular respiration, which generates energy in the form of ATP. Ninety-five percent of the human body's energy is generated this way.Organs with the highest energy requirements—such as the heart, liver, and kidney—have the highest CoQ10 concentrations.

There are three redox states of CoQ: fully oxidized (ubiquinone), semiquinone (ubisemiquinone), and fully reduced (ubiquinol). The capacity of this molecule to act as a two-electron carrier (moving between the quinone and quinol form) and a one-electron carrier (moving between the semiquinone and one of these other forms) is central to its role in the electron transport chain due to the iron–sulfur clusters that can only accept one electron at a time, and as a free-radical–scavenging antioxidant.

Cerdiac Glycosides Digoxin
https://en.wikipedia.org/wiki/Digoxin

Digoxin, sold under the brand name Lanoxin among others, is a medication used to treat various heart conditions. Most frequently it is used for atrial fibrillation, atrial flutter, and heart failure.Digoxin's primary mechanism of action involves inhibition of the sodium potassium adenosine triphosphatase (Na+/K+ ATPase), mainly in the myocardium. This inhibition causes an increase in intracellular sodium levels, resulting in decreased activity of the sodium-calcium exchanger, which normally imports three extracellular sodium ions into the cell and transports one intracellular calcium ion out of the cell.
Diuretics Frusemide
https://en.wikipedia.org/wiki/Furosemide

Furosemide, sold under the brand name Lasix among others, is a medication used to treat fluid build-up due to heart failure, liver scarring, or kidney disease. It may also be used for the treatment of high blood pressure. It can be taken by injection into a vein or by mouth. When taken by mouth, it typically begins working within an hour, while intravenously, it typically begins working within five minutes..Furosemide, like other loop diuretics, acts by inhibiting the luminal Na-K-Cl cotransporter in the thick ascending limb of the loop of Henle, by binding to the chloride transport channel, thus causing sodium, chloride, and potassium loss in urine.

Hydrochlorothiazide
https://en.wikipedia.org/wiki/Hydrochlorothiazide

Hydrochlorothiazide (HCTZ or HCT) is a diuretic medication often used to treat high blood pressure and swelling due to fluid build up. Other uses include treating diabetes insipidus and renal tubular acidosis and to decrease the risk of kidney stones in those with a high calcium level in the urine. For high blood pressure it is sometimes considered as a first-line treatment. HCTZ is taken by mouth and may be combined with other blood pressure medications as a single pill to increase effectiveness.Hydrochlorothiazide belongs to thiazide class of diuretics. It reduces blood volume by acting on the kidneys to reduce sodium (Na+) reabsorption in the distal convoluted tubule. The major site of action in the nephron appears on an electroneutral NaCl co-transporter by competing for the chloride site on the transporter. By impairing Na+ transport in the distal convoluted tubule, hydrochlorothiazide induces a natriuresis and concomitant water loss. Thiazides increase the reabsorption of calcium in this segment in a manner unrelated to sodium transport. Additionally, by other mechanisms, HCTZ is believed to lower peripheral vascular resistance.

Indapamide
https://en.wikipedia.org/wiki/Indapamide

Indapamide is a thiazide-like diuretic drug generally used in the treatment of hypertension, as well as decompensated heart failure. Combination preparations with perindopril (an ACE inhibitor antihypertensive) are also available. Thiazide-like diuretics (indapamide and chlorthalidone) appear to be more effective than the thiazide-type diuretics (hydrochlorothiazide) in reducing risk of major cardiovascular events and heart failure in persons with high blood pressure. In terms of risk of stroke, both thiazide-type and thiazide-like diuretic are effective in reducing it.Both drug classes also appear to have similar rates of adverse effects when compared to other classes of anti-hypertensives.

Telmisartan
https://en.wikipedia.org/wiki/Telmisartan

Telmisartan, sold under the trade name Micardis among others, is a medication used to treat high blood pressure, heart failure, and diabetic kidney disease. It is a reasonable initial treatment for high blood press. It is taken by mouth. Versions are available as the combination telmisartan/hydrochlorothiazide and telmisartan/amlodipine..

elmisartan is an angiotensin II receptor blocker that shows high affinity for the angiotensin II receptor type 1 (AT1), with a binding affinity 3000 times greater for AT1 than AT2.

In addition to blocking the RAS, telmisartan acts as a selective modulator of peroxisome proliferator-activated receptor gamma (PPAR-γ), a central regulator of insulin and glucose metabolism. It is believed that telmisartan's dual mode of action may provide protective benefits against the vascular and renal damage caused by diabetes and cardiovascular disease (CVD).

Telmisartan's activity at the peroxisome proliferator-activated receptor delta (PPAR-δ) receptor has prompted speculation around its potential as a sport doping agent as an alternative to GW 501516. Telmisartan activates PPAR-δ receptors in several tissues.

Also, Telmisartan has a PPARγ agonist activity.

Furosemide
https://en.wikipedia.org/wiki/Furosemide

Furosemide, sold under the brand name Lasix among others, is a medication used to treat fluid build-up due to heart failure, liver scarring, or kidney disease.It may also be used for the treatment of high blood pressure.Furosemide is primarily used for the treatment of edema, but also in some cases of hypertension (where there is also kidney or heart impairment).It is often viewed as a first-line agent in most people with edema caused by congestive heart failure.

Furosemide, like other loop diuretics, acts by inhibiting the luminal Na-K-Cl cotransporter in the thick ascending limb of the loop of Henle, by binding to the chloride transport channel, thus causing sodium, chloride, and potassium loss in urine.

The action on the distal tubules is independent of any inhibitory effect on carbonic anhydrase or aldosterone; it also abolishes the corticomedullary osmotic gradient and blocks negative, as well as positive, free water clearance. Because of the large NaCl absorptive capacity of the loop of Henle, diuresis is not limited by development of acidosis, as it is with the carbonic anhydrase inhibitors.

Additionally, furosemide is a noncompetitive subtype-specific blocker of GABA-A receptors. Furosemide has been reported to reversibly antagonize GABA-evoked currents of α6β2γ2 receptors at μM concentrations, but not α1β2γ2 receptors. During development, the α6β2γ2 receptor increases in expression in cerebellar granule neurons, corresponding to increased sensitivity to furosemide.

Idiopathic Pulmonary Fibrosis Pirfenidone
https://en.wikipedia.org/wiki/Pirfenidone

Pirfenidone is a medication used for the treatment of idiopathic pulmonary fibrosis. It works by reducing lung fibrosis through downregulation of the production of growth factors and procollagens I and II.Pirfenidone has well-established antifibrotic and anti-inflammatory properties in various in vitro systems and animal models of fibrosis.A number of cell-based studies have shown that pirfenidone reduces fibroblast proliferation,inhibits transforming growth factor beta stimulated collagen production and reduces the production of fibrogenic mediators such as transforming growth factor beta. Pirfenidone has also been shown to reduce production of inflammatory mediators such as tumor necrosis factor alpha and IL-1β in both cultured cells and isolated human peripheral blood mononuclear cells.These activities are consistent with the broader antifibrotic and anti-inflammatory activities observed in animal models of fibrosis..

Peripheral Vasodilators Cinnarizine
https://en.wikipedia.org/wiki/Cinnarizine

.Cinnarizine is an antihistamine and calcium channel blocker of the diphenylmethylpiperazine group. It is prescribed for nausea and vomiting due to motion sickness or other sources such as chemotherapy, vertigo, or Ménière's disease.Cinnarizine is classified as a selective antagonist of T-type voltage-operated calcium ion channels, because its binding blocks the channels and keeps them inert. It has a Ki (inhibitory constant) value of 22nM.[ It is also known to have antihistaminic, antiserotoninergic and antidopaminergic effects, binding to H1 histamine receptors, and dopaminergic (D2) receptors.

Ginkgo Biloba
https://en.wikipedia.org/wiki/Ginkgo_biloba

Ginkgo biloba, conly known as ginkgo or gingko (both pronounced /ˈɡɪŋk/), also known as the maidenhair tree, is the only living species in the division Ginkgophyta, all others being extinct. It is a very old species, with some fossils dating back 270 million years. Native to China, the tree is widely cultivated, and was cultivated early in human history. It has various uses in traditional medicine and as a source of food.

Papaverine HCl
https://en.wikipedia.org/wiki/Papaverine

Papaverine (Latin papaver, "poppy") is an opium alkaloid antispasmodic drug, used primarily in the treatment of visceral spasm and vasospasm (especially those involving the intestines, heart, or brain), and occasionally in the treatment of erectile dysfunction. It is used in the treatment of acute mesenteric ischemia. While it is found in the opium poppy, papaverine differs in both structure and pharmacological action from the analgesic morphine-like compounds.

The in vivo mechanism of action is not entirely clear, but an inhibition of the enzyme phosphodiesterase causing elevation of cyclic AMP and cyclic GMP[clarification needed] levels is significant. It may also alter mitochondrial respiration.

Papaverine has also been demonstrated to be a selective phosphodiesterase inhibitor for the PDE10A subtype found mainly in the striatum of the brain. When administered chronically to mice, it produced motor and cognitive deficits and increased anxiety, but conversely may produce an antipsychotic effect, although not all studies support this view.

Vasopressors Phenylephrine
https://en.wikipedia.org/wiki/Phenylephrine

Phenylephrine is a medication primarily used as a decongestant, to dilate the pupil, to increase blood pressure, and to relieve hemorrhoids. While marketed as a decongestant, taken by mouth at recommended doses it is of unclear benefit for hay fever..

Phenylephrine is a sympathomimetic drug, which means that it mimics the actions of epinephrine (commonly known as adrenaline) or norepinephrine. Phenylephrine selectively binds to alpha-1 receptors which cause blood vessels to constrict.

Whereas pseudoephedrine causes both vasoconstriction and increase of mucociliary clearance through its nonspecific adrenergic activity, phenylephrine's selective α-adrenergic agonism causes vasoconstriction alone, creating a difference in their methods of action.

   
Central Nervous System
Anti-Emetics & Antinauseants Domperidone
https://en.wikipedia.org/wiki/Domperidone

Domperidone, sold under the brand name Motilium among others, is a medication used as an antiemetic, gastric prokinetic agent, and galactagogue. It may be taken by mouth or rectally, and is available as a tablet, orally disintegrating tablets, suspension, and suppositories.[The drug is used to relieve nausea and vomiting; to increase the transit of food through the stomach (by increasing gastrointestinal peristalsis); and to promote lactation (breast milk production) by release of prolactin.

It is a peripherally selective dopamine D2 receptor antagonist

Domperidone is a peripherally selective dopamine D2 and D3 receptor antagonist. It has no clinically significant interaction with the D1 receptor, unlike metoclopramideThe medication provides relief from nausea by blocking D receptors. It blocks dopamine receptors in the anterior pituitary gland increasing release of prolactin which in turn increases lactation. Domperidone may be more useful in some patients and cause harm in others by way of the genetics of the person, such as polymorphisms in the drug transporter gene ABCB1 (which encodes P-glycoprotein), the voltage-gated potassium channel KCNH2 gene (hERG/Kv11.1), and the α1D—adrenoceptor ADRA1D gene.
Fosaprepitant
https://en.wikipedia.org/wiki/Fosaprepitant

Fosaprepitant (Emend for Injection (US), Ivemend (EU)) is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant.

Fosaprepitant was developed by Merck & Co. and was approved by the United States Food and Drug Administration (FDA) on January 25, 2008 and by the European Medicines Agency (EMA) on January 11 of the same year.

Granisetron
https://en.wikipedia.org/wiki/Granisetron

Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors..

Metoclopramide
https://en.wikipedia.org/wiki/Metoclopramide

Metoclopramide is a medication used mostly for stomach and esophageal problems. It is commonly used to treat and prevent nausea and vomiting, to help with emptying of the stomach in people with delayed stomach emptying, and to help with gastroesophageal reflux disease. It is also used to treat migraine headaches.

The antiemetic action of metoclopramide is due to its antagonist activity at D2 receptors in the chemoreceptor trigger zone in the central nervous system — this action prevents nausea and vomiting triggered by most stimuli. At higher doses, 5-HT3 antagonist activity may also contribute to the antiemetic effect.

The gastroprokinetic activity of metoclopramide is mediated by muscarinic activity, D2 receptor antagonist activity, and 5-HT4 receptor agonist activity. The gastroprokinetic effect itself may also contribute to the antiemetic effect. Metoclopramide also increases the tone of the lower esophageal sphincter.

Metoclopramide might influence on mood because of its blockade action on 5-HT4 and 5-HT3.

Ondansetron Di HCl
https://en.wikipedia.org/wiki/Ondansetron

Ondansetron, sold under the brand name Zofran, is a medication used to prevent nausea and vomiting caused by cancer chemotherapy, radiation therapy, or surgery. It is also effective for treating gastroenteritis. It is ineffective for treating vomiting caused by motion
 sickness.Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist, with low
 affinity for dopamine receptors. The 5-HT3 receptors are present both peripherally on vagal
 nerve terminals and centrally in the chemoreceptor trigger zone of the area postrema in the medulla. Serotonin is released by the enterochromaffin cells of the small intestine in response to chemotherapeutic agents and may stimulate vagal afferents (via 5-HT3 receptors) to initiate the vomiting reflex. It is thought that ondansetron's antiemetic action is mediated mostly via antagonism of vagal afferents with a minor contribution from antagonism of central receptors.


Prochlorperazine
https://en.wikipedia.org/wiki/Prochlorperazine

Prochlorperazine, sold under the brand name Compazine among others, is

Prochlorperazine is thought to exert its antipsychotic effects by blocking dopamine receptors.

Prochlorperazine is analogous to chlorpromazine; both of these agents antagonize dopaminergic D2 receptors in various pathways of the central nervous system. This D2 blockade results in antipsychotic, antiemetic and other effects. Hyperprolactinemia is a side effect of dopamine antagonists as blockade of D2 receptors within the tuberoinfundibular pathway results in increased plasma levels of prolactin due to increased secretion by lactotrophs in the anterior pituitary.

a medication used to treat nausea, schizophrenia, migraines, and anxiety.It is a less preferred medication for anxiety. It may be taken by mouth, rectally, injection into a vein, or injection into a muscle..
Trifluoperazine
https://en.wikipedia.org/wiki/Trifluoperazine

Trifluoperazine, sold under a number of brand names, is a typical antipsychotic primarily used to treat schizophrenia. It may also be used short term in those with generalized anxiety disorder but is less preferred to benzodiazepines. It is of the phenothiazine chemical class.Trifluoperazine has central antiadrenergic,[antidopaminergic, and minimal anticholinergic effects. It is believed to work by

blockading dopamine D1 and D2 receptors in the mesocortical and mesolimbic pathways, relieving or
 minimizing such symptoms of schizophrenia as hallucinations, delusions, and disorganized thought and speech.


Trimethobenzamide
https://en.wikipedia.org/wiki/Trimethobenzamide

Trimethobenzamide (trade names Tebamide, Tigan) is an antiemetic used to prevent nausea and vomiting.Trimethobenzamide is an antagonist of the D2 receptor. It is believed to affect the chemoreceptor trigger zone (CTZ) of the medulla oblongata to suppress nausea and vomiting.
Antiarrhythmic Agent Haloperidol
https://en.wikipedia.org/wiki/Haloperidol

Haloperidol, sold under the brand name Haldol among others, is a typical antipsychotic medication.[4] Haloperidol is used in the treatment of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, nausea and vomiting, delirium, agitation, acute psychosis, and hallucinations in alcohol withdrawal.Haloperidol is heavily protein bound in human plasma, with a free fraction of only 7.5 to 11.6%. It is also extensively metabolized in the liver with only about 1% of the administered dose excreted unchanged in the urine. The greatest proportion of the hepatic clearance is by glucuronidation, followed by reduction and CYP-mediated oxidation, primarily by CYP3A4.

Anticovulsants Carbamazepine
https://en.wikipedia.org/wiki/Carbamazepine

Carbamazepine (CBZ), sold under the trade name Tegretol among others, is an anticonvulsant medication used primarily in the treatment of epilepsy and neuropathic pain. It is used in schizophrenia along with other medications and as a second-line agent in bipolar disorder. Carbamazepine appears to work as well as phenytoin and valproate for focal and generalized seizures. It is not effective for absence or myoclonic seizures..Carbamazepine is a sodium channel blocker. It binds preferentially to voltage-gated sodium channels in their inactive conformation, which prevents repetitive and sustained firing of an action potential. Carbamazepine has effects on serotonin systems but the relevance to its antiseizure effects is uncertain. There is evidence that it is a serotonin releasing agent and possibly even a serotonin reuptake inhibitor.

Divalproex
https://en.wikipedia.org/wiki/Valproate

Valproate (VPA) and its valproic acid, sodium valproate, and valproate semisodium forms are medications primarily used to treat epilepsy and bipolar disorder and prevent migraine headaches. They are useful for the prevention of seizures in those with absence seizures, partial seizures, and generalized seizures.Although the mechanism of action of valproate is not fully understood,[50] traditionally, its anticonvulsant effect has been attributed to the blockade of voltage-gated sodium channels and increased brain levels of gamma-aminobutyric acid (GABA). The GABAergic effect is also believed to contribute towards the anti-manic properties of valproate.[50] In animals, sodium valproate raises cerebral and cerebellar levels of the inhibitory synaptic neurotransmitter, GABA, possibly by inhibiting GABA degradative enzymes, such as GABA transaminase, succinate-semialdehyde dehydrogenase and by inhibiting the re-uptake of GABA by neuronal cells.

Felbamate
https://en.wikipedia.org/wiki/Felbamate

Felbamate (marketed under the brand name Felbatol by MedPointe) is an anticonvulsant used in the treatment of epilepsy. It is used to treat partial seizures (with and without generalization) in adults and partial and generalized seizures associated with Lennox–Gastaut syndrome in children. However, an increased risk of potentially fatal aplastic anemia and/or liver failure limit the drug's usage to severe refractory epilepsy.Felbamate has been proposed to a unique dual mechanism of action as a positive modulator of GABAA receptors and as a blocker of NMDA receptors, particularly isoforms containing the NR2B subunit. Although it is clear that felbamate does cause pharmacological inhibition of NMDA receptors, the relevance of NMDA receptor blockade as a strategy for the treatment of human epilepsy has been questioned. Therefore, the importance of the effects of felbamate on NMDA receptors to its therapeutic action in epilepsy is uncertain.


Fosphenytoin Sodium
https://en.wikipedia.org/wiki/Fosphenytoin

Fosphenytoin (fosphenytoin sodium, trade names Cerebyx, Parke-Davis; Prodilantin, Pfizer Holding France) is a water-soluble phenytoin prodrug that is administered intravenously to deliver phenytoin, potentially more safely than intravenous phenytoin. It is most commonly used in the acute treatment of convulsive status epilepticus.One millimole of phenytoin is produced for every millimole of fosphenytoin administered; the hydrolysis of fosphenytoin also yields phosphate and formaldehyde, the latter of which is subsequently metabolized to formate, which is in turn metabolized by a folate dependent mechanism.

Gabapentin
https://en.wikipedia.org/wiki/Gabapentin

Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication used to treat partial seizures, neuropathic pain, hot flashes, and restless legs syndrome. It is recommended as one of a number of first-line medications for the treatment of neuropathic pain caused by diabetic neuropathy, postherpetic neuralgia, and central neuropathic pain.About 15% of those given gabapentin for diabetic neuropathy or postherpetic neuralgia have a measurable benefit. Gabapentin is taken by mouth.Gabapentin is a gabapentinoid, or a ligand of the auxiliary α2δ subunit site of
certain voltage-dependent calcium channels (VDCCs), and thereby acts as an inhibitor of α2δ subunit-containing VDCCs.There are two drug-binding α2δ subunits, α
2δ-1
 and α2δ-2
, and gabapentin shows similar affinity for (and hence lack of selectivity between) these two sites. Gabapentin is selective in its binding to the α2δ VDCC subunit. Despite the fact that gabapentin is a GABA analogue, and in spite of its name, it does not bind to the GABA receptors, does not convert into GABA or another GABA receptor agonist in vivo, and does not modulate GABA transport or metabolism.There is currently no evidence that the effects of gabapentin are mediated by any mechanism other than inhibition of α2δ-containing
 VDCCs.In accordance, inhibition of α2δ-1-containing VDCCs by gabapentin appears to be responsible for its anticonvulsant, analgesic, and anxiolytic effects.

Lamotrigine
https://en.wikipedia.org/wiki/Lamotrigine

Lamotrigine, sold as the brand name Lamictal among others, is an anticonvulsant medication used to treat epilepsy and to delay or prevent the recurrence of depressive episodes in bipolar disorder. For epilepsy, this includes focal seizures, tonic-clonic seizures, and seizures in Lennox-Gastaut syndrome. In bipolar disorder, lamotrigine has not been shown to reliably treat acute depression; but for patients with bipolar disorder who are not currently symptomatic, it appears to be effective in reducing the risk of future episodes of depression.It is a triazine derivate that inhibits voltage-sensitive sodium channels, leading to stabilization of neuronal membranes. It also blocks L-, N-, and P-type calcium channels and weakly inhibits the serotonin 5-HT3 receptor. These actions are thought to inhibit release of glutamate at cortical projections in the ventral striatum limbic areas, and its neuroprotective and antiglutamatergic effects have been pointed out as promising contributors to its mood stabilizing activity. Observations that lamotrigine reduced γ-aminobutyric acid (GABA) A receptor-mediated neurotransmission in rat amygdala, suggest that a GABAergic mechanism may also be involved. It appears that lamotrigine does not increase GABA blood levels in humans.

Levetiracetam
https://en.wikipedia.org/wiki/Levetiracetam

Levetiracetam, sold under the brand name Keppra among others, is a medication used to treat epilepsy. It is used for partial-onset, myoclonic, or tonic–clonic seizures and is taken either by mouth as an immediate or extended release formulation or by injection into a vein.The exact mechanism by which levetiracetam acts to treat epilepsy is unknown. Levetiracetam does not exhibit pharmacologic actions similar to that of classical anticonvulsants. It does not inhibit voltage-dependent Na+ channels, does not affect GABAergic transmission, and does not bind to GABAergic or glutamatergic receptors. However, the drug binds to SV2A, a synaptic vesicle glycoprotein, and inhibits presynaptic calcium channels, reducing neurotransmitter release and acting as a neuromodulator. This is believed to impede impulse conduction across synapses.

Phenytoin
https://en.wikipedia.org/wiki/Phenytoin

Phenytoin (PHT), sold under the brand name Dilantin among others, is an anti-seizure medication. It is useful for the prevention of tonic-clonic seizures and focal seizures, but not absence seizures. The intravenous form is used for statusPhenytoin is believed to protect against seizures by causing voltage-dependent block of voltage gated sodium channels. This blocks sustained high frequency repetitive firing of action potentials. This is accomplished by reducing the amplitude of sodium-dependent action potentials through enhancing steady state inactivation. Sodium channels exist in three main conformations: the resting state, the open state, and the inactive state. epilepticus that does not improve with benzodiazepines. It may also be used for certain heart arrhythmias or neuropathic pain.

Pregabalin
https://en.wikipedia.org/wiki/Pregabalin

Pregabalin, marketed under the brand name Lyrica among others, is a medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless leg syndrome, and generalized anxiety disorder. Its use in epilepsy is as an add-on therapy for partial seizures.Pregabalin is a gabapentinoid
 and acts by inhibiting certain calcium channels. Specifically it is a ligand of the auxiliary α2δ subunit site of certain voltage-dependent calcium channels (VDCCs), and thereby acts as an inhibitor of α2δ subunit-containing VDCCs.
Retigabine
https://en.wikipedia.org/wiki/Retigabine

Retigabine (INN) or ezogabine (USAN) is an anticonvulsant used as an adjunctive treatment for partial epilepsies in treatment-experienced adult patients.Retigabine acts as a neuronal KCNQ/Kv7 potassium channel opener, a mechanism of action markedly different from that of any current anticonvulsants. This mechanism of action is similar to that of the chemically-similar flupirtine, which is used mainly for its analgesic properties.


Sodium Valproate
https://en.wikipedia.org/wiki/Valproate

Valproate (VPA) and its valproic acid, sodium valproate, and valproate semisodium forms are medications primarily used to treat epilepsy and bipolar disorder and prevent migraine headaches..Valproate's precise mechanism of action is unclear. Proposed mechanisms include affecting GABA levels, blocking voltage-gated sodium channels, and inhibiting histone deacetylases. Valproic acid is a branched short-chain fatty acid (SCFA) made from valeric acid.

Topiramate
https://en.wikipedia.org/wiki/Topiramate

Topiramate, sold under the brand name Topamax among others, is a medication used to treat epilepsy and prevent migraines. It has also been used in alcohol dependence. For epilepsy this includes treatment for generalized or focalSeveral cellular targets have been proposed to be relevant to the therapeutic activity of topiramate. These include (1) voltage-gated sodium channels; (2) high-voltage-activated calcium channels; (3) GABA-A receptors; (4) AMPA/kainate receptors; and (5) carbonic anhydrase isoenzymes. There is evidence that topiramate may alter the activity of its targets by modifying their phosphorylation state instead of by a direct action.[42] The effect on sodium channels could be of particular relevance for seizure protection. Although topiramate does inhibit high-voltage-activated calcium channels, the relevance to clinical activity is uncertain. Effects on specific GABA-A receptor isoforms could also contribute to the antiseizure activity of the drug. Topiramate selectively inhibits cytosolic (type II) and membrane associated (type IV) forms of carbonic anhydrase. The action on carbonic anhydrase isoenzymes may contribute to the drug's side-effects, including its propensity to cause metabolic acidosis and calcium phosphate kidney stones. seizures. It is taken by mouth.

Valproic Acid
https://en.wikipedia.org/wiki/Valproate

Valproate (VPA) and its valproic acid, sodium valproate, and valproate semisodium forms are medications primarily used to treat epilepsy and bipolar disorder and prevent migraine headaches..Valproate's precise mechanism of action is unclear. Proposed mechanisms include affecting GABA levels, blocking voltage-gated sodium channels, and inhibiting histone deacetylases. Valproic acid is a branched short-chain fatty acid (SCFA) made from valeric acid.


Vigabatrin
https://en.wikipedia.org/wiki/Vigabatrin

Vigabatrin, brand name Sabril, is a medication used to treat epilepsy. It became available as a generic medication in 2019.

It works by inhibiting the breakdown of γ-aminobutyric acid (GABA). It is also known as γ-vinyl-GABA, and is a structural analogue of GABA, but does not bind to GABA receptors.Vigabatrin is an irreversible mechanism-based inhibitor of gamma-aminobutyric acid aminotransferase (GABA-AT), the enzyme responsible for the catabolism of GABA. Inhibition of GABA-AT results in increased levels of GABA in the brain. Vigabatrin is a racemic compound, and its [S]-enantiomer is pharmacologically active.

Antimanic Drugs Haloperidol
https://en.wikipedia.org/wiki/Haloperidol

Haloperidol is a typical 
butyrophenone type antipsychotic that exhibits high affinity dopamine D2 receptor antagonism and slow receptor dissociation kinetics. It has effects similar to the phenothiazines.Haloperidol, sold under the brand name Haldol among others, is a typical antipsychotic medication. Haloperidol is used in the treatment of schizophrenia, tics in Tourette syndrome, mania in bipolar disorder, nausea and vomiting, delirium, agitation, acute psychosis, and hallucinations in alcohol withdrawal.

  Quetiapine Fumarate
https://en.wikipedia.org/wiki/Quetiapine

Quetiapine, sold under the brand name Seroquel among others, is an atypical antipsychotic medication used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder. Despite being widely used as a sleep aid due its sedating effect, the benefits of such use do not appear to generally outweigh the side effects.

Quetiapine has the following pharmacological actions:

 

Antipsychotics Aripiprazole
https://en.wikipedia.org/wiki/Aripiprazole

Aripiprazole, sold under the brand name Abilify among others, is an atypical antipsychotic. It is primarily used in the treatment of schizophrenia and bipolar disorder. Other uses include as an add-on treatment in major depressive disorder, tic disorders and irritability associated with autism..
Aripiprazole's mechanism of action is different from those of the other FDA-approved atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine, ziprasidone, and risperidone). It shows differential engagement at the dopamine receptor (D2). It appears to show
predominantly antagonist activity on postsynaptic D
2 receptors and partial agonist activity on
 presynaptic D
2 receptors, D3 and partially D4
) and is a partial activator of serotonin (5-
HT1A, 5-HT2A, 5-HT2B, 5-HT6
, and 5-HT7).

Iloperidone
https://en.wikipedia.org/wiki/Iloperidone

Iloperidone, commonly known as Fanapt and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia.Iloperidone is a monoamine directed towards acting upon and antagonizing specific neurotransmitters, particularly multiple dopamine and serotonin receptor subtypes. It is considered an ‘atypical’ antipsychotic because it displays serotonin receptor antagonism, similar to other atypical antipsychotics. The older typical antipsychotics are primarily dopamine antagonists.


Lurasidone
https://en.wikipedia.org/wiki/Lurasidone


Lurasidone, sold under the trade name Latuda among others, is an antipsychotic medication used to treat schizophrenia and bipolar disorder In bipolar it may be used together with a mood stabilizer such as lithium or valproate. It is taken by mouth.Lurasidone acts as an antagonist of the dopamine D2 and D3 receptors, the serotonin 5-HT2A and 5-HT7 receptors, and the α2C-adrenergic receptor, and as a partial agonist of the serotonin 5-HT1A receptor. It has only low and likely clinically unimportant affinity for the serotonin 5-HT2C receptor, which may underlie its low propensity for appetite stimulation and weight gain. The drug also has negligible affinity for the histamine H1 receptor and the muscarinic acetylcholine receptors, and hence has no antihistamine or anticholinergic effects.


Zotepine
https://en.wikipedia.org/wiki/Zotepine

Zotepine is an atypical antipsychotic drug indicated for acute and chronic schizophrenia. The antipsychotic effect of zotepine is thought to be mediated through antagonist activity at dopamine and serotonin receptors. Zotepine has a high affinity for the D1 and D2 receptors. It also affects the 5-HT2A, 5-HT2C, 5-HT6, and 5-HT7 receptors. In addition, its active metabolite, norzotepine, serves as a potent norepinephrine reuptake inhibitor..

Drugs to control Rigidity & Tremors Selegiline
https://en.wikipedia.org/wiki/Selegiline

Selegiline, also known as L-deprenyl and sold under the brand names Eldepryl and Emsam among others, is a medication which is used in the treatment of Parkinson's disease and major depressive disorder.It is provided in the form of a capsule or tablet taken by mouth for Parkinson's disease and as a patch applied to skin for depression.

Selegiline acts as a monoamine oxidase inhibitor, and increases levels of monoamine neurotransmitters in the brain. At typical clinical doses, selegiline is a selective and irreversible inhibitor of monoamine oxidase B (MAO-B), increasing levels of dopamine in the brain. In larger doses, it loses its specificity and also inhibits MAO-A, increasing levels of serotonin, norepinephrine, and dopamine in the brain.


Drugs used to treat Migraine Flunarizine
https://en.wikipedia.org/wiki/Flunarizine

Flunarizine, sold under the brand name Sibelium among others, is a drug classified as a calcium antagonist which is used for various indications.Flunarizine is a selective calcium antagonist with moderate other actions including antihistamine, serotonin receptor blocking and dopamine D2 blocking activity. Compared to other calcium channel blockers such as dihydropyridine derivatives, verapamil and diltiazem, flunarizine has low affinity to voltage-dependent calcium channels. It has been theorised that it may act not by inhibiting calcium entry into cells, but rather by an intracellular mechanism such as antagonising calmodulin, a calcium binding protein.
Frovatriptan
https://en.wikipedia.org/wiki/Frovatriptan

Frovatriptan (trade name Frova) is a triptan drug developed by Vernalis for the treatment of migraine headaches and for short term prevention of menstrual miraine.Frovatriptan is a 5HT receptor agonist, with high affinity for the 5-HT1B/1D receptors. It has no significant effects on the GABAA mediated channel activity and benzodiazepine binding sites
.

Sumatriptan
https://en.wikipedia.org/wiki/Sumatriptan

Sumatriptan, sold under the brand name Imitrex among others, is a medication used to treat migraine headaches and cluster headaches.

Sumatriptan is structurally similar to serotonin (5-HT), and is a 5-HT receptor (types 5-HT1D and 5-HT1B) agonist. Sumatriptan's primary therapeutic effect, however, is in its inhibition of the release of Calcitonin gene-related peptide (CGRP), likely through its 5-HT1D/1B receptor-agonist action. This is substantiated by the efficacy of newly developed CGRP antagonists and antibodies in the preventative treatment of migraine. However, how agonism of the 5-HT1D/1B receptors inhibits CGRP release is not fully understood. CGRP is believed to cause sensitization of trigeminal nociceptive neurons, contributing to the pain experienced in migraine.

Sumatriptan is also shown to decrease the activity of the trigeminal nerve, which presumably accounts for sumatriptan's efficacy in treating cluster headaches. The injectable form of the drug has been shown to abort a cluster headache within 30 minutes in 77% of cases.


Drugs used in Peripheral Neuropathy Benfotiamine
https://en.wikipedia.org/wiki/Benfotiamine

Benfotiamine (rINN, or S-benzoylthiamine O-monophosphate) is a synthetic S-acyl derivative of thiamine (vitamin B1) that sold as a medication or dietary supplement to treat diabetic neuropathy. Combination drugs with pyridoxine or cyanocobalamin are also marketed.

Benfotiamine is more bioavailable than thiamine salts, providing higher levels of thiamine in muscle, brain, liver, and kidney.

Benfotiamine is dephosphorylated to S-benzoylthiamine by ecto-alkaline phosphatases present in the intestinal mucosa, and is then hydrolyzed to thiamine by thioesterases in the liver.

Benfotiamine mainly acts on peripheral tissues through an increase in transketolase activity.


Mecobalamin / Methylcobalamin
https://en.wikipedia.org/wiki/Methylcobalamin

Methylcobalamin (mecobalamin, MeCbl, or MeB12) is a cobalamin, a form of vitamin B12. It differs from cyanocobalamin in that the cyano group at the cobalt is replaced with a methyl group. Methylcobalamin features an octahedral cobalt(III) centre and can be obtained as bright red crystals. From the perspective of coordination chemistry, methylcobalamin is notable as a rare example of a compound that contains metal–alkyl bonds. Nickel–methyl intermediates have been proposed for the final step of methanogenesis.

Methylcobalamin is equivalent physiologically to vitamin B12,and can be used to prevent or treat pathology arising from a lack of vitamin B12 intake (vitamin B12 deficiency).

Methylcobalamin is also used in the treatment of peripheral neuropathy, diabetic neuropathy, and as a preliminary treatment for amyotrophic lateral sclerosis.

Methylcobalamin that is ingested is not used directly as a cofactor, but is first converted by MMACHC into cob(II)alamin. Cob(II)alamin is then later converted into the other 2 forms, adenosylcobalamin and methylcobalamin for use as cofactors. That is, methylcobalamin is first dealkylated and then regenerated.

According to one author, it is important to treat vitamin B12 deficiency with hydroxocobalamin or cyanocobalamin or a combination of adenosylcobalamin and methylcobalamin, and not methylcobalamin alone.


Hepatic Encephalopathy Amino Acids
https://en.wikipedia.org/wiki/Amino_acid

Amino acids are organic compounds that contain amine (–NH2) and carboxyl (–COOH) functional groups, along with a side chain (R group) specific to each amino acid. The key elements of an amino acid are carbon (C), hydrogen (H), oxygen (O), and nitrogen (N), although other elements are found in the side chains of certain amino acids. About 500 naturally occurring amino acids are known (though only 20 appear in the genetic code) and can be classified in many ways.When taken up into the human body from the diet, the 20 standard amino acids either are used to synthesize proteins, other biomolecules, or are oxidized to urea and carbon dioxide as a source of energy. The oxidation pathway starts with the removal of the amino group by a transaminase; the amino group is then fed into the urea cycle. The other product of transamidation is a keto acid that enters the citric acid cycle. Glucogenic amino acids can also be converted into glucose, through gluconeogenesis..


Insomnia Eszopiclone
https://en.wikipedia.org/wiki/Eszopiclone

Eszopiclone, sold under the brand-name Lunesta among others, is a medication used in the treatment of insomnia. Evidence supports slight to moderate benefit up to six months. It is taken by mouth.Eszopiclone acts on benzodiazepine binding site situated on GABAA neurons as a positive allosteric modulator.


Ramelteon
https://en.wikipedia.org/wiki/Ramelteon

Ramelteon, sold under the brand name Rozerem among others, is a sleep agent medication that selectively binds to the MT1 and MT2 receptors in the suprachiasmatic nucleus (SCN), instead of binding to GABAA receptors, such as with drugs like zolpidem.

Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 and MT2 receptors and selectivity over the MT3 receptor. Ramelteon demonstrates full agonist activity in vitro in cells expressing human MT1 or MT2 receptors, and high selectivity for human MT1 and MT2 receptors compared to the MT3 receptor.

The activity of ramelteon at the MT1 and MT2 receptors is believed to contribute to its sleep-promoting properties, as these receptors, acted upon by endogenous melatonin, are thought to be involved in the maintenance of the circadian rhythm underlying the normal sleep-wake cycle. Ramelteon has no appreciable affinity for the GABA receptor complex or for receptors that bind neuropeptides, cytokines, serotonin, dopamine, noradrenaline, acetylcholine, and opioids. Ramelteon also does not interfere with the activity of a number of selected enzymes in a standard panel.


Zolpidem Tartrate
https://en.wikipedia.org/wiki/Zolpidem

Zolpidem, sold under the brand name Ambien, among others, is a medication primarily used for the short-term treatment of sleeping problems.Zolpidem is a ligand of high-affinity positive modulator sites of GABAA receptors, which enhances GABAergic inhibition of neurotransmission in the central nervous system. It selectively binds to α1 subunits of this pentameric ion channel. Accordingly, it has strong hypnotic properties and weak anxiolytic, myorelaxant, and anticonvulsant properties. Opposed to diazepam, zolpidem is able to bind to binary αβ GABA receptors, where it was shown to bind to the α1–α1 subunit interface.

Multiple Sclerosis Fingolimod
https://en.wikipedia.org/wiki/Fingolimod

Fingolimod (INN, trade name Gilenya, Novartis) is an immunomodulating drug, mostly used for treating multiple sclerosis (MS).Fingolimod is a sphingosine-1-phosphate receptor modulator, which sequesters lymphocytes in lymph nodes, preventing them from contributing to an autoimmune reaction. It has been reported to reduce the rate of relapses in relapsing-remitting multiple sclerosis by approximately one-half over a two-year period.The molecular biology of phospho-fingolimod is thought to lie in its activity at one of the five sphingosine-1-phosphate receptors, S1PR1. Phospho-fingolimod causes the internalization of S1P receptors, which sequesters lymphocytes in lymph nodes, preventing them from moving to the central nervous system and causing a relapse of multiple sclerosis.


Neuroleptic Agent Amisulpride
https://en.wikipedia.org/wiki/Amisulpride

Amisulpride is an antiemetic and antipsychotic medication used at lower doses intravenously to prevent and treat postoperative nausea and vomiting; and at higher doses orally and intramuscularly to treat schizophrenia and acute psychotic episodes.Amisulpride

 functions primarily as a dopamine D2 and D3 receptor antagonist. It has high affinity for these

receptors with dissociation constants of 3.0 and 3.5 nM, respectively. Although standard doses used to treat psychosis inhibit dopaminergic neurotransmission, low doses preferentially block inhibitory presynaptic autoreceptors.


Neuropathic Pain Carbamazepine
https://en.wikipedia.org/wiki/Carbamazepine

Carbamazepine (CBZ), sold under the trade name Tegretol among others, is an anticonvulsant medication used primarily in the treatment of epilepsy and neuropathic pain. It is used in schizophrenia along with other medications and as a second-line agent in bipolar disorder.Carbamazepine is a sodium channel blocker. It binds preferentially to voltage-gated sodium channels in their inactive conformation, which prevents repetitive and sustained firing of an action potential. Carbamazepine has effects on serotonin systems but the relevance to its antiseizure effects is uncertain. There is evidence that it is a serotonin releasing agent and possibly even a serotonin reuptake inhibitor..

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) Ibuprofen
https://en.wikipedia.org/wiki/Ibuprofen

Ibuprofen is a medication in the nonsteroidal anti-inflammatory drug (NSAID) class that is used for treating pain, fever, and inflammation. This includes painful menstrual periods, migraines,

NSAIDs such as ibuprofen work by inhibiting the cyclooxygenase (COX) enzymes, which convert arachidonic acid to prostaglandin H2 (PGH2). PGH2, in turn, is converted by other enzymes to several other prostaglandins (which are mediators of pain, inflammation, and fever) and to thromboxane A2 (which stimulates platelet aggregation, leading to the formation of blood clots).

Like aspirin and indomethacin, ibuprofen is a nonselective COX inhibitor, in that it inhibits two isoforms of cyclooxygenase, COX-1 and COX-2.

 and rheumatoid arthritis. It may also be used to close a patent ductus arteriosus in a premature baby.It can be used by mouth or intravenously.

Nabumetone
https://en.wikipedia.org/wiki/Nabumetone

Nabumetone is a nonacidic NSAID that is rapidly metabolized in the liver to a major active metabolite, 6-methoxy-2-naphthyl acetic acid. As found with previous NSAIDs, nabumetone's active metabolite inhibits the cyclooxygenase enzyme and preferentially blocks COX-2 activity (which is indirectly responsible for the production of inflammation and pain during arthritis). The active metabolite of nabumetone is felt to be the compound primarily responsible for therapeutic effect. Comparatively, the parent drug is a poor inhibitor of COX-2 byproducts, particularly prostaglandins. It may be less nephrotoxic than indomethacin. There are two known polymorphs of the compound.


Naproxen Sodium
https://en.wikipedia.org/wiki/Naproxen

Naproxen, sold under the brand name Aleve among others, is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain, menstrual cramps, inflammatory diseases such as rheumatoid arthritis, and fever. It is taken orally. It is available in immediate and delayed release formulations.Naproxen works by reversibly inhibiting both the COX-1 and COX-2 enzymes as a non-selective coxib. This results in the inhibition of prostaglandin synthesis. Prostaglandins act as signaling molecules in the body, inducing inflammation. Thus, by inhibiting COX-1/2, naproxen induces an anti-inflammatory effect.


Sedatives & Tranquillisers Alprazolam
https://en.wikipedia.org/wiki/Alprazolam

Alprazolam, sold under the brand name Xanax, among others, is a short-acting tranquilizer of the triazolobenzodiazepine (TBZD) class, which are benzodiazepines (BZDs) fused with a triazole ring. It is most commonly used in short-term management of anxiety disorders, specifically panic disorder or generalized anxiety disorder (GAD).

Alprazolam is classed as a high-potency triazolobenzodiazepine: a benzodiazepine with a triazole ring attached to its structure. As a benzodiazepine, alprazolam produces a variety of therapeutic and adverse effects by binding to the GABAA benzodiazepine receptor site and modulating its function; GABA receptors are the most prolific inhibitory receptor within the brain.The GABA chemical and receptor system mediates inhibitory or calming effects of alprazolam on the nervous system. Binding of alprazolam to the GABAA receptor, a chloride ion channel, enhances the effects of GABA, a neurotransmitter. When GABA binds the GABAA receptor the channel opens and chloride enters the cell which makes it more resistant to depolarisation. Therefore, alprazolam has a depressant effect on synaptic transmission to reduce anxiety.

Diazepam
ttps://en.wikipedia.org/wiki/Diazepam

Diazepam, first marketed as Valium, is a medicine of the benzodiazepine family that typically produces a calming effect. It is commonly used to treat a range of conditions, including anxiety, seizures, alcohol withdrawal syndrome, benzodiazepine withdrawal syndrome, muscle spasms, trouble sleeping, and restless legs syndrome..enzodiazepines are positive allosteric modulators of the GABA type A receptors (GABAA). The GABAA receptors are ligand-gated chloride-selective ion channels that are activated by GABA, the major inhibitory neurotransmitter in the brain. Binding of benzodiazepines to this receptor complex promotes the binding of GABA, which in turn increases the total conduction of chloride ions across the neuronal cell membrane. This increased chloride ion influx hyperpolarizes the neuron's membrane potential. As a result, the difference between resting potential and threshold potential is increased and firing is less likely. As a result, the arousal of the cortical and limbic systems in the central nervous system is reduced.


Tricyclic & Related Antidepressants Agomelatine
https://en.wikipedia.org/wiki/Agomelatine

Agomelatine is an atypical antidepressant used to treat major depressive disorder. One review found that it is as effective as other antidepressants with similar discontinuation rates overall but less

Agomelatine is a melatonin receptor agonist (MT1 (Ki 0.1 nM) and MT2 (Ki = 0.12 nM)) and serotonin 5-HT2C (Ki = 631 nM) and 5-HT2B receptor (Ki = 660 nM) antagonist. Binding studies indicate that it has no effect on monoamine uptake and no affinity for adrenergic, histamine, cholinergic, dopamine, and benzodiazepine receptors, nor other serotonin receptors.

Agomelatine resynchronizes circadian rhythms in animal models of delayed sleep phase syndrome. By antagonizing 5-HT2C, it disinhibits/increases noradrenaline and dopamine release specifically in the frontal cortex. Therefore, it is sometimes classified as a norepinephrine–dopamine disinhibitor.

 discontinuations due to side effects. Another review also found it was similarly effective to many other antidepressants.


Brexpiprazole
https://en.wikipedia.org/wiki/Brexpiprazole

Brexpiprazole, sold under the brand name Rexulti among others, is an atypical antipsychotic. It is a dopamine D2 receptor partial agonist and has been described as a "serotonin–dopamine activity modulator" (SDAM). The drug was approved by the U.S. Food and Drug Administration (FDA) on July 10, 2015, for the treatment of schizophrenia, and as an adjunctive treatment for depression. It has been designed to provide improved efficacy and tolerability (e.g., less akathisia, restlessness and/or insomnia) over established adjunctive treatments for major depressive disorder (MDD).Brexpiprazole acts as a partial agonist of the serotonin 5-HT1A receptor and the dopamine D2 and D3 receptors. Partial agonists have both blocking properties and stimulating properties at the receptor they bind to. The ratio of blocking activity to stimulating activity determines a portion of its clinical effects.


Cinitapride Hydrogen Tartrate
https://en.wikipedia.org/wiki/Cinitapride

Cinitapride (trade names Cintapro, Pemix) is a gastroprokinetic agent and antiulcer agent of the benzamide class which is marketed in India, Mexico, Pakistan and Spain. It acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors.

It is indicated for the treatment of gastrointestinal disorders associated with motility disturbances such as gastroesophageal reflux disease, non-ulcer dyspepsia and delayed gastric emptying


 
Citalopram
https://en.wikipedia.org/wiki/Citalopram

Citalopram, sold under the brand name Celexa among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class.[2] It is used to treat major depressive disorder, obsessive compulsive disorder, panic disorder, and social phobia.Citalopram was first synthesized in 1972 by chemist Klaus Bøgesø and his research group at the pharmaceutical company Lundbeck and was first marketed in 1989 in Denmark. It was first marketed in the US in 1998.[66] The patent expired in 2003, allowing other companies to legally produce generic versions.

Dothiepin HCl
https://en.wikipedia.org/wiki/Dosulepin

Dosulepin, also known as dothiepin and sold under the brand name Prothiaden among others, is a tricyclic antidepressant (TCA) which is used in the treatment of depression. Dosulepin was once the most frequently prescribed antidepressant in the United Kingdom, but it is no longer widely used due to its relatively high toxicity in overdose without therapeutic advantages over other TCAs. It acts as a serotonin–norepinephrine reuptake inhibitor (SNRI) and also has other activities including antihistamine, antiadrenergic, antiserotonergic, anticholinergic, and sodium channel-blocking effects.Dosulepin is a transporter blocker of the serotonin transporter (SERT) and the norepinephrine transporter (NET), thereby acting as an SNRI. It is also an antagonist of the histamine H1 receptor, α1-adrenergic receptor, serotonin 5-HT2 receptors, and muscarinic acetylcholine receptors (mACh), as well as a blocker of voltage-gated sodium channels (VGSCs). The antidepressant effects of dosulepin are thought to be due to inhibition of the reuptake of norepinephrine and possibly also of serotonin..

Escitalopram
https://en.wikipedia.org/wiki/Escitalopram

Escitalopram, sold under the brand names Cipralex and Lexapro, among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. Escitalopram is mainly used to treat major depressive disorder or generalized anxiety disorder. It is taken by mouth.
Escitalopram increases intrasynaptic levels of the neurotransmitter serotonin by blocking the reuptake of the neurotransmitter into the presynaptic neuron. Of the SSRIs currently available, escitalopram has the highest selectivity for the serotonin transporter (SERT) compared to the norepinephrine transporter (NET), making the side-effect profile relatively mild in comparison to less-selective SSRIs.

Fluoxetine Hydrochloride
https://en.wikipedia.org/wiki/Fluoxetine

Fluoxetine, sold under the brand names Prozac and Sarafem among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used for the treatment of major depressive disorder, obsessive–compulsive disorder (OCD), bulimia nervosa, panic disorder, and premenstrual dysphoric disorder. It may decrease the risk of suicide in those over the age of 65. It has also been used to treat premature ejaculation.Fluoxetine elicits antidepressant effect by inhibiting serotonin re-uptake in the synapse by binding to the re-uptake pump on the neuronal membrane to increase its availability and enhance neurotransmission. Norfluoxetine and desmethylfluoxetine are metabolites of fluoxetine and also act as serotonin re-uptake inhibitors, so increase the duration of action of the drug.

Milnacipran
https://en.wikipedia.org/wiki/Milnacipran

Milnacipran (trade names Ixel, Savella, Dalcipran, Toledomin) is a serotonin–norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia. It is not approved for the clinical treatment of major depressive disorder in the US, but it is in other countries.

Milnacipran inhibits the reuptake of serotonin and norepinephrine in an approximately 1:3 ratio, respectively. Milnacipran exerts no significant actions on H1, α1, D1, D2, and mACh receptors, nor on benzodiazepine and opioid binding sites.

Recently, levomilnacipran, the levorotatory enantiomer of milnacipran, has been found to act as an inhibitor of beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1), which is responsible for β-amyloid plaque formation, and hence may be a potentially useful drug in the treatment of Alzheimer's disease Other BACE-1 inhibitors, such as CTS-21166 (ASP1720), MK-8931, and AZD3293 are currently in clinical trials for the treatment of Alzheimer's disease.

Nortriptyline
https://en.wikipedia.org/wiki/Nortriptyline

Nortriptyline, sold under the brand name Pamelor, among others, is a medication used to treat depression, neuropathic pain, attention deficit hyperactivity disorder (ADHD), stopping smoking and anxiety.

Nortriptyline is an active metabolite of amitriptyline by demethylation in the liver. Its pharmacologic profile is as the table to the right shows (inhibition or antagonism of all sites).

Chemically, it is a secondary amine dibenzocycloheptene and pharmacologically it is classed as a first-generation antidepressant.

Sertraline HCl
https://en.wikipedia.org/wiki/Sertraline

Sertraline, sold under the brand name Zoloft among others, is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class. It is used to treat major depressive disorder, obsessive–compulsive disorder, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, and social anxiety disorder.Sertraline acts as a potent serotonin reuptake inhibitor (SRI), with an affinity (Ki) for the serotonin transporter (SERT) of 0.4 nM and an IC50 value of 2.8 nM, according to a couple of studies. It is highly selective in its inhibition of serotonin reuptake. By inhibiting the reuptake of serotonin, sertraline increases extracellular levels of serotonin and thereby increases serotonergic neurotransmission in the brain. It is this action that is thought to be responsible for the antidepressant, anxiolytic, and antiobsessional effects of sertraline.
Imipramine
https://en.wikipedia.org/wiki/Imipramine

Imipramine, sold under the brand name Tofranil, among others, is a tricyclic antidepressant (TCA) mainly used in the treatment of depression. It is also effective in treating anxiety and panic disorder. The drug is also used to treat bedwetting.. It was the first TCA to be marketed. Imipramine and the other TCAs have decreased in use in recent decades, due to the introduction of the selective serotonin reuptake inhibitors (SSRIs), which have fewer side effects and are safer in overdose.

Trimipramine Maleate
https://en.wikipedia.org/wiki/Imipramine

Imipramine, sold under the brand name Tofranil, among others, is a tricyclic antidepressant (TCA) mainly used in the treatment of depression. It is also effective in treating anxiety and panic disorder. The drug is also used to treat bedwetting..The mechanisms of imipramine's actions include, but are not limited to, effects on:


Vilazodone
https://en.wikipedia.org/wiki/Vilazodone

Vilazodone, sold under the brand name Viibryd among others, is a medication used to treat major depressive disorder.[1] While it was being studied for generalized anxiety disorder, such research had stopped as of 2017..Vilazodone acts as a serotonin reuptake inhibitor (IC50 = 2.1 nM; Ki = 0.1 nM) and 5-HT1A receptor partial agonist (IC50 = 0.2 nM; IA = ~60–70%).It has negligible affinity for other serotonin receptors such as 5-HT1D, 5-HT2A, and 5-HT2C. It also exhibits clinically unimportant inhibitory activity at the norepinephrine and dopamine transporters (Ki = 56 nM for NET and 37 nM for DAT).

Amitriptyline HCl
https://en.wikipedia.org/wiki/Amitriptyline

Amitriptyline inhibits neuronal reuptake of serotonin and noradrenaline from the synapse in the central nervous system; this increases their availability in the synapse to cause neurotransmission on the post-synaptic neurone.
Amitriptyline is metabolised by cytochrome P450 enzymes in the liver to nortriptyline, which also acts as a noradrenaline reuptake inhibitor; this potentiates the antidepressant effects of amitriptyline.
Contraceptive agents
Oral Contraceptives Ulipristal Acetate
https://en.wikipedia.org/wiki/Ulipristal_acetate

Ulipristal acetate, sold under the brand name Ella among others, is a medication used for emergency contraception (birth control) and uterine fibroids.[1][2][3] As emergency contraception it should be used within 120 hours of sex. For fibroids it may be taken for up to six months. It is taken by mouth.As an SPRM, ulipristal acetate has partial agonistic as well as antagonistic effects on the progesterone receptor. Ulipristal acetate exhibits similar potency to antagonize progesterone receptor as mifepristone in vitro. It also binds to the androgen receptor and the glucocorticoid receptor, but is only a weak antiandrogen and antiglucocorticoid relative to flutamide and mifepristone, respectively.

Dermatologicals
Anti- Infective Skin Preparations Acyclovir
https://en.wikipedia.org/wiki/Aciclovir

Aciclovir (ACV), also known as acyclovir, is an antiviral medication. It is primarily used for the treatment of herpes simplex virus infections, chickenpox, and shingles.Other uses include prevention of cytomegalovirus infections following transplant and severe complications of Epstein-Barr virus infection.Aciclovir is converted by viral thymidine kinase to aciclovir monophosphate, which is then converted by host cell kinases to aciclovir triphosphate (ACV-TP). ACV-TP, in turn, competitively inhibits and inactivates HSV-specified DNA polymerases preventing further viral DNA synthesis without affecting the normal cellular processes.

Polymyxin B Sulfate
https://en.wikipedia.org/wiki/Polymyxin_B

Polymyxin B, sold under the brand name Poly-Rx among others, is an antibiotic used to treat meningitis, pneumonia, sepsis, and urinary tract infections. While it is useful for many Gram negative infections, it is not useful for Gram positive infections..
  1. Alters bacterial outer membrane permeability by binding to a negatively charged site in the lipopolysaccharide layer, which has an electrostatic attraction for the positively charged amino groups in the cyclic peptide portion  (this site normally is a binding site for calcium and magnesium counter ions); the result is a destabilized outer membrane
  2. Fatty acid portion dissolves in hydrophobic region of cytoplasmic membrane and disrupts membrane integrity
  3. Leakage of cellular molecules, inhibition of cellular respiration
  4. Binds and inactivates endotoxin
  5. Relative absence of selective toxicity: nonspecific for cell membranes of any type, highly toxic.
Silver Sulfadiazine
https://en.wikipedia.org/wiki/Silver_sulfadiazine

Silver sulfadiazine, sold under the brand Silvadene among others, is a topical antibiotic used in partial thickness and full thickness burns to prevent infection. Tentative evidence has found other antibiotics to be more effective and therefore it is no longer generally recommended.The chemical is poorly soluble, and has only very limited penetration through intact skin. However, contact with body fluids produces free sulfadiazine which can then be systemically absorbed and distributed; it undergoes glucuronidation in the liver and is also excreted unaltered in urine. Only when applied to large-area (especially second- and third-degree) burns or other lesions is absorption into the body a problem.
Selenium Sulphide
https://en.wikipedia.org/wiki/Selenium_disulfide

Selenium disulfide, also known as selenium sulfide, is a chemical compound and medication used to treat pityriasis versicolor, seborrhoeic dermatitis, and dandruff. It is applied to the affected area as a lotion or shampoo. Dandruff frequently returns if treatment is stopped.Selenium disulfide is sold as an antifungal agent in shampoos for the treatment of dandruff and seborrheic dermatitis associated in the scalp with fungi of genus Malassezia. In the United States, a 1% strength is available over-the-counter, and a 2.5% strength is also available with a prescription. In Canada, the 2.5% strength is available over-the-counter. At the 2.5% strength, selenium disulfide is also used on the body to treat Tinea versicolor, a type of fungal skin infection caused by a different species of Malassezia. It has been suggested to be effective as a treatment for hyperkeratosis..

Antipruritic Crotamiton
https://en.wikipedia.org/wiki/Crotamiton

Crotamiton is a drug that is used both as a scabicidal (for treating scabies) and as a general antipruritic (anti-itching drug). It is a prescription, lotion-based medicine that is applied to the whole body to get rid of the scabies parasite that burrows under the skin and causes itching.
Crotamiton is toxic to the scabies mite,
 The mechanism of action of crotamiton as a general antipruritic was reported, in which crotamiton inhibits TRPV4 (transient receptor potential vanilloid 4) channel that is expressed in the skin, primary sensory neurons, and so on.

Antipsoriasis Acitretin
https://en.wikipedia.org/wiki/Acitretin

Acitretin (trade names Soriatane and Neotigason) is a second-generation retinoid. It is taken orally, and is typically used for psoriasis.

Acitretin is an oral retinoid used in the treatment of severe resistant psoriasis. Because of the potential for problems and severe side effects it is generally used in only very severe cases of psoriasis that have been unresponsive to other treatments. It binds to nuclear receptors that regulates gene transcription. They induce keratinocyte differentiation and reduce epidermal hyperplasia, leading to the slowing of cell reproduction.

Dimethyl Fumarate
https://en.wikipedia.org/wiki/Dimethyl_fumarate

Dimethyl fumarate (DMF) is the methyl ester of fumaric acid and is named after the earth smoke plant (Fumaria officinalis). DMF combined with three other fumaric acid esters (FAEs) is solely licensed in Germany as an oral therapy for psoriasis (trade name Fumaderm). Since 2013, it has been approved by the U.S. Food and Drug Administration as a treatment option for adults with relapsing multiple sclerosis (trade name Tecfidera).DMF has also been applied as a biocide in furniture or shoes to prevent growths of mold during storage or transport in a humid climates. However, due to cases of allergic reactions after skin contact, DMF-containing consumer products are no longer authorised to be manufactured (since 1998) or imported (since 2009) in the European Union..
Methoxsalen
https://en.wikipedia.org/wiki/Methoxsalen

Methoxsalen (also called xanthotoxin), sold under the brand name Oxsoralen among others, is a drug used to treat psoriasis, eczema, vitiligo, and some cutaneous lymphomas in conjunction with exposing the skin to UVA light from lamps or sunlight. Methoxsalen modifies the way skin cells receive the UVA radiation, allegedly clearing up the disease. The dosage comes in 10 mg tablets, which are taken in the amount of 30 mg 75 minutes before a PUVA (psoralen + UVA) light treatment. Levels of individual patient PUVA exposure were originally determined using the Fitzpatrick scale. The scale was developed after patients demonstrated symptoms of phototoxicity after oral ingestion of Methoxsalen followed by PUVA therapy. Chemically, methoxsalen belongs to a class of organic natural molecules known as furanocoumarins. They consist of coumarin annulated with furan.

Corticosteroid Responsive Methylprednisolone & Salts
https://en.wikipedia.org/wiki/Methylprednisolone

Methylprednisolone, sold under the brand name Medrol among others, is a corticosteroid medication used to suppress the immune system and decrease inflammation. Conditions in which it is used include skin diseases, rheumatic disorders, allergies, asthma, croup, COPD, certain cancers, multiple sclerosis, and as add-on therapy for tuberculosis or radiculopathyUnbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors, modifying transcription and protein synthesis. By this mechanism, glucocorticoids can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The anti-inflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Drugs for Acne Vulgaris Adapalene
https://en.wikipedia.org/wiki/Adapalene

Adapalene is a third-generation topical retinoid primarily used in the treatment of mild-moderate acne, and is also used off-label to treat keratosis pilaris as well as other skin conditions.[1] It is effective against acne conditions where comedones are predominant.Unlike the retinoid tretinoin (Retin-A), adapalene has also been shown to retain its efficacy when applied at the same time as benzoyl peroxide due to its more stable chemical structure.[14] Furthermore, photodegradation of the molecule is less of a concern in comparison to tretinoin and tazarotene.

Melanizing Agents Trioxsalen
https://en.wikipedia.org/wiki/Trioxsalen

Trioxsalen (trimethylpsoralen, trioxysalen (INN) or Trisoralen) is a furanocoumarin and a psoralen derivative. It is obtained from several plants, mainly Psoralea corylifolia. Like other psoralens it causes photosensitization of the skin. It is administered either topically or orally in conjunction with UV-A (the least damaging form of ultraviolet light) for phototherapy treatment of vitiligo and hand eczema. After photoactivation it creates interstrand cross-links in DNA, which can cause programmed cell death unless repaired by cellular mechanisms. In research it can be conjugated to dyes for confocal microscopy and used to visualize sites of DNA damage. The compound is also being explored for development of antisense oligonucleotides that can be cross-linked specifically to a mutant mRNA sequence without affecting normal transcripts differing at even a single base pair.

Topical Antifungals & Anti-Parasitics Sertaconazole Nitrate
https://en.wikipedia.org/wiki/Sertaconazole

Sertaconazole, sold under the brand names Ertaczo, Dermofix, Konzert, and Zalain, is an antifungal medication of the imidazole class. It is available as a cream to treat skin infections such as athlete's foot.

It is also available in a vaginal tablet form. The most popular of these is Gyno-Dermofix.

Like other imidazole antifungals, sertaconazole blocks the synthesis of ergosterol by inhibiting the 14α-demethylase enzyme. Ergosterol is a critical component of the fungal cell membrane. Inhibition of ergosterol synthesis prevents fungal cells from multiplying and impairs hyphae growth.
Terbinafine
https://en.wikipedia.org/wiki/Terbinafine

Terbinafine, sold under the brand name Lamisil among others, is an antifungal medication used to treat pityriasis versicolor, fungal nail infections, and ringworm including jock itch and athlete's foot.

Like other allylamines, terbinafine inhibits ergosterol synthesis by inhibiting squalene epoxidase, an enzyme that catalyzes the conversion of squalene to lanosterol. In fungi, lanosterol is then converted to ergosterol; in humans, lanosterol becomes cholesterol. However, there is sufficient genetic divergence between fungal and human squalene epoxidases that terbinafine preferentially binds fungal squalene epoxidase, making it selective for inhibiting ergosterol production in fungi without significantly affecting cholesterol production in humans. This is thought to change cell membrane permeability, causing fungal cell lysis.

Terbinafine is highly lipophilic and tends to accumulate in hair, skin, nails, and fatty tissue.

Topical Steroids
Betamethasone
https://en.wikipedia.org/wiki/Betamethasone

Betamethasone is a steroid medication. It is used for a number of diseases including rheumatic disorders such as rheumatoid arthritis and systemic lupus erythematosus, skin diseases such as dermatitis and psoriasis, allergic conditions such as asthma and angioedema, preterm labor to speed the development of the baby's lungs, Crohn's disease, cancers such as leukemia, and along with fludrocortisone for adrenocortical insufficiency, among others.

Fluticasone Propionate
https://en.wikipedia.org/wiki/Fluticasone_propionate

Fluticasone propionate, sold under the brand names Flovent and Flonase among others, is a steroid medication.[6] When inhaled it is used for the long term management of asthma and COPD.[6] In the nose it is used for hay fever and nasal polyps.[7][8] It can also be used for mouth ulcers..Fluticasone propionate is a highly selective agonist at the glucocorticoid receptor with negligible activity at androgen, estrogen, or mineralocorticoid receptors, thereby producing anti-inflammatory and vasoconstriction effects. It has been shown to have a wide range of inhibitory effects on multiple cell types (e.g. mast cell, eosinophil, neutrophil, macrophages, and lymphocytes) and mediators (e.g. histamine, eicosanoids, leukotrienes, and cytokines) involved in inflammation. Fluticasone propionate is stated to exert a topical effect on the lungs without significant systemic effects at usual doses, due to its low systemic bioavailability.

Mometasone Furoate
https://en.wikipedia.org/wiki/Mometasone

Mometasone, also known as mometasone furoate, is a steroid medication used to treat certain skin conditions, hay fever, and asthma. Specifically it is used to prevent rather than treat asthma attacks. It can be applied to the skin, inhaled, or used in the nose. Mometasone furoate, not mometasone is used in medical products.

Mometasone, like other corticosteroids, possesses anti-inflammatory, antipruritic, and vasoconstrictive properties. For allergies, corticosteroids reduce the allergic reactions in various types of cells (mastocytes and eosinophils) that are responsible for allergic reactions. Mometasone and other corticosteroids circulate in the blood easily, crossing cellular membranes and binding with cytoplasmic receptors, resulting in the transcription and synthesis of proteins. It also inhibits the actions of the enzyme cytochrome P450 2C8 which participates in the activity of monooxygenase.

The inflammation is reduced in decreasing the liberation of hydrolase acids of leukocytes, the prevention of the accumulation macrophages in the sites of inflammation, the interference with adhesion of leukocytes to capillary walls, the reduction of the permeability of the capillary membranes and consequently edema, the reduction of complementary components, inhibition of histamine and kinin liberation, and interference with scar tissue formation.

   
Opthalmic
Anti- Infective Eye Preparations Acyclovir
https://en.wikipedia.org/wiki/Aciclovir

Aciclovir (ACV), also known as acyclovir, is an antiviral medication. It is primarily used for the treatment of herpes simplex virus infections, chickenpox, and shingles. Other uses include prevention of cytomegalovirus infections following transplant and severe complications of Epstein-Barr virus infection.Aciclovir is converted by viral thymidine kinase to aciclovir monophosphate, which is then converted by host cell kinases to aciclovir triphosphate (ACV-TP). ACV-TP, in turn, competitively inhibits and inactivates HSV-specified DNA polymerases preventing further viral DNA synthesis without affecting the normal cellular processes.

Fluconazole
https://en.wikipedia.org/wiki/Fluconazole

Fluconazole is an antifungal medication used for a number of fungal infections. This includes candidiasis, blastomycosis, coccidiodomycosis, cryptococcosis, histoplasmosis, dermatophytosis, and pityriasis versicolor. It is also used to prevent candidiasis in those who are at high risk such as following organ transplantation, low birth weight babies, and those with low blood neutrophil counts.Like other imidazole- and triazole-class antifungals, fluconazole inhibits the fungal cytochrome P450 enzyme 14α-demethylase. Mammalian demethylase activity is much less sensitive to fluconazole than fungal demethylase. This inhibition prevents the conversion of lanosterol to ergosterol, an essential component of the fungal cytoplasmic membrane, and subsequent accumulation of 14α-methyl sterols.[22] Fluconazole is primarily fungistatic; however, it may be fungicidal against certain organisms in a dose-dependent manner, specifically Cryptococcus.

Anti- Inflammatory & Anti Allergic Preparations Ketorolac Tromethamine
https://en.wikipedia.org/wiki/Ketorolac

Ketorolac, sold under the brand name Toradol among others, is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain..Chemically ketorolac functions as a carboxylic acid derivative serving non-selectively to block the prostaglandin synthesis by inhibition of prostaglandin G/H synthesis one and two. Prostaglandin functions in the body as a messenger for contraction/relaxation of smooth muscle and modulation of inflammation. Resultant, inhibition of prostaglandin synthesis prevents inflammation. The primary mechanism of action responsible for ketorolac's anti-inflammatory, antipyretic, and analgesic effects is the inhibition of prostaglandin synthesis by competitive blocking of the enzyme cyclooxygenase (COX). Ketorolac is a non-selective COX inhibitor. It is considered a first-generation NSAID.[

Sodium Cromoglycate
https://en.wikipedia.org/wiki/Cromoglicic_acid

Cromoglicic acid (INN) (also referred to as cromolyn (USAN), cromoglycate (former BAN), or cromoglicate) is traditionally described as a mast cell stabilizer, and is commonly marketed as the sodium salt sodium cromoglicate or cromolyn sodium. This drug prevents the release of inflammatory chemicals such as histamine from mast cells.Cromolyn works because it prevents the release of mediators that would normally attract inflammatory cells and because it stabilizes the inflammatory cells. MCT mast cells found in the mucosa are stabilised." Nedocromil is another mast cell stabilizer that also works in controlling asthma. The underlying mechanism of action is not fully understood; for while cromoglicate stabilizes mast cells, this mechanism is probably not why it works in asthma.

   
Glaucoma Bimatoprost
https://en.wikipedia.org/wiki/Bimatoprost

Bimatoprost, sold under the trade name Lumigan among others, is a medication used to treat high pressure inside the eye including glaucoma. Specifically it is used for open angle glaucoma when other agents are not sufficient. It may also be used to increase the size of the eyelashes.Bimatoprost is a structural analog of prostaglandin F (PGF). Like other PGF analogs such as travoprost, latanoprost and tafluprost, it increases the outflow of aqueous fluid from the eye and lowers intraocular pressure. However, in contrast to these it does not act on the prostaglandin F receptor, nor on any other known prostaglandin receptor. It is thought that bimatoprost mimics the human body's own prostamides (which are chemically similar), a class of substances related to prostaglandins, but with an unknown mechanism of action. No prostamide receptor has been identified as of 2015; the search is ongoing.As of 2019 it was thought that bimatoprost worked via the trabecular meshwork and uveoscleral pathways..

Dorzolamide
https://en.wikipedia.org/wiki/Dorzolamide

Dorzolamide, sold under the brand name Trusopt among others, is medications used to treat high pressure inside the eye including glaucoma.It lowers IOP by about 20%. Carbonic Anhydrase can convert H2CO3 into HCO3 (bicarbonate) and H+. The H+ is then exchanged for sodium (Na) which allows you to make aqueous humor. By blocking carbonic anhydrase, the Na/H exchanger can't work, which will decrease Na in the cell and prevent aqueous humor production.

Timolol Maleate
https://en.wikipedia.org/wiki/Timolol

Timolol is a medication used either by mouth or as eye drops. As eye drops it is used to treat increased pressure inside the eye such as in ocular hypertension and glaucoma. By mouth it is used for high blood pressure, chest pain due to insufficient blood flow to the heart, to prevent further complications after a heart attack, and to prevent migraines.Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors, of the sympathetic nervous system, which mediates the fight-or-flight response. Some block activation of all types of β-adrenergic receptors and others are selective for one of the three known types of beta receptors, designated β1, β2 and β3 receptors β1-adrenergic receptors are located mainly in the heart and in the kidneys.

Mydriatics & Cycloplegics Phenylephrine
https://en.wikipedia.org/wiki/Phenylephrine 

Phenylephrine is a medication primarily used as a decongestant, to dilate the pupil, to increase blood pressure, and to relieve hemorrhoids. While marketed as a decongestant, taken by mouth at recommended doses it is of unclear benefit for hay fever.

Phenylephrine is a sympathomimetic drug, which means that it mimics the actions of epinephrine (commonly known as adrenaline) or norepinephrine. Phenylephrine selectively binds to alpha-1 receptors which cause blood vessels to constrict.

Whereas pseudoephedrine causes both vasoconstriction and increase of mucociliary clearance through its nonspecific adrenergic activity, phenylephrine's selective α-adrenergic agonism causes vasoconstriction alone, creating a difference in their methods of action.

 
Genito-urinary tract
Androgen & Anabolic Steroid (AAS) Stanozolol
https://en.wikipedia.org/wiki/Stanozolol

Stanozolol (abbrev. Stz), sold under many brand names, is an androgen and anabolic steroid (AAS) medication derived from dihydrotestosterone (DHT). It is used to treat hereditary angioedema..Stanozolol is one of the AAS commonly used as performance-enhancing drugs and is banned from use in sports competition under the auspices of the International Association of Athletics Federations (IAAF) and many other sporting bodies. Additionally, stanozolol has been used in US horse racing.As an AAS, stanozolol is an agonist of the androgen receptor (AR), similarly to androgens like testosterone and DHT. Its affinity for the androgen receptor is about 22% of that of dihydrotestosterone. Stanozolol is not a substrate for 5α-reductase as it is already 5α-reduced, and so is not potentiated in so-called "androgenic" tissues like the skin, hair follicles, and prostate gland. This results in a greater ratio of anabolic to androgenic activity compared to testosterone. In addition, due to its 5α-reduced nature, stanozolol is non-aromatizable, and hence has no propensity for producing estrogenic effects such as gynecomastia or fluid retention. Stanozolol also does not possess any progestogenic activity of significance. Because of the presence of its 17α-methyl group, the metabolism of stanozolol is sterically hindered, resulting in it being orally active, although also hepatotoxic.

Erectile Dysfunction Sildenafil Citrate
https://en.wikipedia.org/wiki/Sildenafil

Sildenafil, sold under the brand name Viagra among others, is a medication used to treat erectile dysfunction and pulmonary arterial hypertension. It is unclear if it is effective for treating sexual dysfunction in women.Sildenafil protects cyclic guanosine monophosphate (cGMP) from degradation by cGMP-specific phosphodiesterase type 5 (PDE5) in the corpus cavernosum. Nitric oxide (NO) in the corpus cavernosum of the penis binds to guanylate cyclase receptors, which results in increased levels of cGMP, leading to smooth muscle relaxation (vasodilation) of the intimal cushions of the helicine arteries. This smooth muscle relaxation leads to vasodilation and increased inflow of blood into the spongy tissue of the penis, causing an erection. Robert F. Furchgott, Ferid Murad, and Louis Ignarro won the Nobel Prize in Physiology or Medicine in 1998 for their independent study of the metabolic pathway of nitric oxide in smooth muscle vasodilation.

Hyperphosphatemia Sevelamer HCl / Carbonate
https://en.wikipedia.org/wiki/Sevelamer

Sevelamer (rINN) (/sɛˈvɛləmər/ or /sɛˈvɛləmɪər/) is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease. When taken with meals, it binds to dietary phosphate and prevents its absorption.Sevelamer consists of polyallylamine that is crosslinked with epichlorohydrin. The marketed form sevelamer hydrochloride is a partial hydrochloride salt being present as approximately 40% amine hydrochloride and 60% sevelamer base. The amine groups of sevelamer become partially protonated in the intestine and interact with phosphate ions through ionic and hydrogen bonding..

Sucroferric Oxyhydroxide
https://en.wikipedia.org/wiki/Sucroferric_oxyhydroxide

Sucroferric oxyhydroxide (trade name Velphoro) is a non-calcium, iron-based phosphate binder used for the control of serum phosphorus levels in adult patients with chronic kidney disease (CKD) on haemodialysis (HD) or peritoneal dialysis (PD). It is used in form of chewable tablets.

Sucroferric oxyhydroxide is also known as a mixture of polynuclear iron(III)-oxyhydroxide, sucrose and starches.


Intravenous Pyelogram (IVP) Diatrizoate Sodium Diatrizoic Acid
https://en.wikipedia.org/wiki/Diatrizoate


Meglumine is an amino sugar derived from glucose. It is often used as an excipient in pharmaceuticals and in conjunction with iodinated compounds in contrast media such as diatrizoate meglumine, iothalamate meglumine and iodipamide meglumine..

Meglumine
https://en.wikipedia.org/wiki/Meglumine

Meglumine is an amino sugar derived from glucose. It is often used as an excipient in pharmaceuticals and in conjunction with iodinated compounds in contrast media such as diatrizoate meglumine, iothalamate meglumine and iodipamide meglumine..

Urinary Tract Analgesics & Antispasmodics Adiphenine HCl
https://en.wikipedia.org/wiki/Adiphenine

Adiphenine is an inhibitor of nicotinic receptors.

Drotaverine HCl
https://en.wikipedia.org/wiki/Drotaverine

Drotaverine (INN, also known as drotaverin) is an antispasmodic drug, used to enhance cervical dilation during childbirth.

It is structurally related to papaverine, is a selective inhibitor of phosphodiesterase 4, and has no anticholinergic effects.

Phenazopyridine
https://en.wikipedia.org/wiki/Phenazopyridine

Phenazopyridine is a medication which, when excreted into the urine, has a local analgesic effect. It is often used to help with the pain, irritation, or urgency caused by urinary tract infections, surgery, or injury to the urinary tract.Phenazopyridine's mechanism of action is not well known, and only basic information on its interaction with the body is available. It is known that the chemical has a direct topical analgesic effect on the mucosa lining of the urinary tract. It is rapidly excreted by the kidneys directly into the urine.[20] Hydroxylation is the major form of metabolism in humans,[20] and the azo bond is usually not cleaved. On the order of 65% of an oral dose will be secreted directly into the urine chemically unchanged.

Trospium Chloride
https://en.wikipedia.org/wiki/Trospium_chloride

Trospium chloride is used to treat overactive bladder..Chemically it is a quaternary ammonium cation which causes it to stay in periphery rather than crossing the blood-brain barrier.[5] It works by causing the smooth muscle in the bladder to relax.Trospium chloride is a muscarinic antagonist. Trospium chloride blocks the effect of acetylcholine on muscarinic receptors organs that are responsive to the compounds, including the bladder.[2] Its parasympatholytic action relaxes the smooth muscle in the bladder.[3] Receptor assays showed that trospium chloride has negligible affinity for nicotinic receptors as compared to muscarinic receptors at concentrations obtained from therapeutic doses.

Urinary Tract Infections Fosfomycin Trometamol
https://en.wikipedia.org/wiki/Fosfomycin

Fosfomycin, sold under the brand name Monurol among others, is an antibiotic primarily used to treat bladder infections. It is not recommended for kidney infections.Fosfomycin is bactericidal and inhibits bacterial cell wall biogenesis by inactivating the enzyme UDP-N-acetylglucosamine-3-enolpyruvyltransferase, also known as MurA. This enzyme catalyzes the committed step in peptidoglycan biosynthesis, namely the ligation of phosphoenolpyruvate (PEP) to the 3'-hydroxyl group of UDP-N-acetylglucosamine. This pyruvate moiety provides the linker that bridges the glycan and peptide portion of peptidoglycan. Fosfomycin is a PEP analog that inhibits MurA by alkylating an active site cysteine residue (Cys 115 in the Escherichia coli enzyme)..

Uterine Stimulants Ritodrine Hydrochloride
https://en.wikipedia.org/wiki/Ritodrine

Ritodrine (trade name Yutopar) is a tocolytic drug used to stop premature labor.This drug has been removed from the US market, according to FDA Orange Book.Ritodrine is a short-acting β2 adrenoreceptor agonist — a class of medication used for smooth muscle relaxation (other similar drugs are used in asthma or other pulmonary diseases such as salbutamol (albuterol)). Since ritodrine has a bulky N-substituent, it has high β2 selectivity. Also, the 4-hydroxy group on the benzene ring is important for activity as it is needed to form hydrogen bonds. However, the 4-hydroxy group makes it susceptible to metabolism by catechol-O-methyl transferase (COMT). Since it is β2-selective it is used for premature labor..

 
Hormones
Corticosteroids & Related Drugs Deflazacort
https://en.wikipedia.org/wiki/Deflazacort

Deflazacort (trade name Calcort among others) is a glucocorticoid used as an anti-inflammatory and immunosuppressant.Deflazacort is an inactive prodrug which is metabolized rapidly to the active drug 21-desacetyldeflazacort.

Hyper & Hypoglycaemics Glibenclamide
https://en.wikipedia.org/wiki/Glibenclamide

Glibenclamide, also known as glyburide, is a medication used to treat diabetes mellitus type 2. It is recommended that it be taken together with diet and exercise.[1] It may be used with other antidiabetic medication.[1] It is not recommended for use by itself in diabetes mellitus type 1.

The medication works by binding to and inhibiting the ATP-sensitive potassium channels (KATP) inhibitory regulatory subunit sulfonylurea receptor 1 (SUR1)[10] in pancreatic beta cells. This inhibition causes cell membrane depolarization, opening voltage-dependent calcium channels. This results in an increase in intracellular calcium in the pancreatic beta cell and subsequent stimulation of insulin release.

After a cerebral ischemic insult, the blood–brain barrier is broken and glibenclamide can reach the central nervous system. Glibenclamide has been shown to bind more efficiently to the ischemic hemisphere.

Glimepiride
https://en.wikipedia.org/wiki/Glimepiride

Glimepiride, sold under the trade name Amaryl among others, is a medication used to treat diabetes mellitus type 2. It is less preferred than metformin. Use is recommended together with diet and exercise.

Like all sulfonylureas, glimepiride acts as an insulin secretagogue. It lowers blood sugar by stimulating the release of insulin by pancreatic beta cells and by inducing increased activity of intracellular insulin receptors.

Not all secondary sulfonylureas have the same risk of hypoglycemia. Glibenclamide (glyburide) is associated with an incidence of hypoglycemia of up to 20–30%, compared to as low as 2% to 4% with glimepiride. Glibenclamide also interferes with the normal homeostatic suppression of insulin secretion in reaction to hypoglycemia, whereas glimepiride does not. Also, glibenclamide diminishes glucagon secretion in reaction to hypoglycemia, whereas glimepiride does not.

Thyroid Hormones Levothyroxine Sodium
https://en.wikipedia.org/wiki/Levothyroxine

Levothyroxine, also known as L-thyroxine, is a manufactured form of the thyroid hormone thyroxine (T4). It is used to treat thyroid hormone deficiency, including the severe form known as myxedema coma. It may also be used to treat and prevent certain types of thyroid tumors. It is not indicated for weight loss.Levothyroxine is a synthetic form of thyroxine (T4), an endogenous hormone secreted by the thyroid gland, which is converted to its active metabolite, L-triiodothyronine (T3). T4 and T3 bind to thyroid receptor proteins in the cell nucleus and cause metabolic effects through the control of DNA transcription and protein synthesis. Like its naturally secreted counterpart, levothyroxine is a chiral compound in the L-form.

Liothyronine Sodium
https://en.wikipedia.org/wiki/Liothyronine

Liothyronine is a manufactured form of the thyroid hormone triiodothyronine (T3). It is most commonly used to treat hypothyroidism and myxedema coma.Liothyronine is the most potent form of thyroid hormone. As a salt of triiodothyronine (T3), it is chemically similar and pharmacologically equivalent to T3. As such, it acts on the body to increase the basal metabolic rate, affect protein synthesis and increase the body's sensitivity to catecholamines (such as adrenaline) by permissiveness.

Vitamin D Analogs Calcitriol
https://en.wikipedia.org/wiki/Calcitriol

Calcitriol is the active form of vitamin D, normally made in the kidney A manufactured form is used to treat kidney disease with low blood calcium, hyperparathyroidism due to kidney disease, low blood calcium due to hypoparathyroidism, osteoporosis, osteomalacia, and familial hypophosphatemia.

Many of the effects of calcitriol are mediated by its interaction with the calcitriol receptor, also called the vitamin D receptor or VDR. For instance, the unbound inactive form of the calcitriol receptor in intestinal epithelial cells resides in the cytoplasm. When calcitriol binds to the receptor, the ligand-receptor complex translocates to the cell nucleus, where it acts as a transcription factor promoting the expression of a gene encoding a calcium binding protein. The levels of the calcium binding protein increase enabling the cells to actively transport more calcium (Ca2+
) from the intestine across the intestinal mucosa into the blood.

The maintenance of electroneutrality requires that the transport of Ca2+
 ions catalyzed by the intestinal epithelial cells be accompanied by counterions, primarily inorganic phosphate. Thus calcitriol also stimulates the intestinal absorption of phosphate.

 
Immunology
Immuno-Suppressants Everolimus
https://en.wikipedia.org/wiki/Everolimus

Everolimus is a medication used as an immunosuppressant to prevent rejection of organ transplants and in the treatment of renal cell cancer and other tumours.

Compared with the parent compound rapamycin, everolimus is more selective for the mTORC1 protein complex, with little impact on the mTORC2 complex. This can lead to a hyper-activation of the kinase AKT via inhibition on the mTORC1 negative feedback loop, while not inhibiting the mTORC2 positive feedback to AKT. This AKT elevation can lead to longer survival in some cell types. Thus, everolimus has important effects on cell growth, cell proliferation and cell survival.

Additionally, mTORC2 is believed to play an important role in glucose metabolism and the immune system, suggesting that selective inhibition of mTORC1 by drugs such as everolimus could achieve many of the benefits of rapamycin without the associated glucose intolerance and immunosuppression.

Mycophenolic Mofetil / Sodium
https://en.wikipedia.org/wiki/Mycophenolic_acid
https://en.wikipedia.org/wiki/Morpholino


Mycophenolic acid (MPA) is an immunosuppressant medication used to prevent rejection following organ transplantation and to treat Crohn's disease.[4] Specifically it is used following kidney, heart, and liver transplantation.Purines (including the nucleotides guanosine and adenosine) can either be synthesized de novo using ribose 5-phosphate or they can be salvaged from free nucleotides. Mycophenolic acid is potent, reversible, non-competitive inhibitor of inosine-5′-monophosphate dehydrogenase (IMPDH), an enzyme essential to the de novo synthesis of guanosine-5'-monophosphate (GMP) from inosine-5'-monophosphate (IMP). IMPDH inhibition particularly affects lymphocytes since they rely almost exclusively on de novo purine synthesis. In contrast, many other cell types use both pathways, and some cells, such as terminally differentiated neurons, depend completely on purine nucleotide salvage. Thus, use of mycophenolic acid leads to a relatively selective inhibition of DNA replication in T cells and B cells..

Pimecrolimus
https://en.wikipedia.org/wiki/Pimecrolimus

Pimecrolimus is an immunomodulating agent of the calcineurin inhibitor class used in the treatment of atopic dermatitis (eczema). .

Pimecrolimus is an ascomycin macrolactam derivative. It has been shown in vitro that pimecrolimus binds to FKBP1A and also inhibits calcineurin Thus pimecrolimus inhibits T-cell activation by inhibiting the synthesis and release of cytokines from T-cells. Pimecrolimus also prevents the release of inflammatory cytokines and mediators from mast cells.

Pimecrolimus, like tacrolimus, belongs to the ascomycin class of macrolactam immunosuppressives, acting by the inhibition of T-cell activation by the calcineurin pathway and inhibition of the release of numerous inflammatory cytokines, thereby preventing the cascade of immune and inflammatory signals. Pimecrolimus has a similar mode of action to that of tacrolimus but is more selective, with no effect on dendritic (Langerhans) cells. It has lower permeation through the skin than topical steroids or topical tacrolimus although they have not been compared with each other for their permeation ability through mucosa. In addition, in contrast with topical steroids, pimecrolimus does not produce skin atrophy.

Thalidomide
https://en.wikipedia.org/wiki/Thalidomide

Thalidomide, sold under the brand name Thalomid among others, is a medication used to treat a number of cancers including multiple myeloma, graft-versus-host disease, and a number of skin conditions including complications of leprosy. While it has been used in a number of HIV associated conditions, such use is associated with increased levels of the virus.The precise mechanism of action for thalidomide is not known, although efforts to identify thalidomide's teratogenic action generated 2,000 research papers and the proposal of 15 or 16 plausible mechanisms by the year 2000. As of 2015, the main theories were inhibition of the process of angiogenesis, its inhibition of cereblon, a ubiquitin ligase, and its ability to generate reactive oxygen species which in turn kills cells.

Multiple Sclerosis Teriflunomide
https://en.wikipedia.org/wiki/Teriflunomide

Teriflunomide, sold under the brand name Aubagio, is the active metabolite of leflunomide.

Teriflunomide is an immunomodulatory drug inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase. It is uncertain whether this explains its effect on MS lesions.

Teriflunomide inhibits rapidly dividing cells, including activated T cells, which are thought to drive the disease process in MS. Teriflunomide may decrease the risk of infections compared to chemotherapy-like drugs because of its more-limited effects on the immune system.

 
Metabolism
Anti- Obesity Cetilistat
https://en.wikipedia.org/wiki/Cetilistat

Cetilistat is a drug designed to treat obesity. It acts in the same way as the older drug orlistat (Xenical) by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine. Without this enzyme, triglycerides from the diet are prevented from being hydrolyzed into absorbable free fatty acids and are excreted undigested.

Ezetimibe
https://en.wikipedia.org/wiki/Ezetimibe 

Ezetimibe is a medication used to treat high blood cholesterol and certain other lipid abnormalities. Generally it is used together with dietary changes and a statin.Ezetimibe inhibits the absorption of cholesterol from the small intestine and decreases the amount of cholesterol normally available to liver cells. This leads them to absorb more cholesterol from circulation and thus causes lowering levels of circulating cholesterol. It blocks the critical mediator of cholesterol absorption, the Niemann-Pick C1-like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells, as well as in hepatocytes; it blocks aminopeptidase N and interrupts a caveolin 1annexin A2 complex involved in trafficking cholesterol.

Drugs used in Gout Colchicine
https://en.wikipedia.org/wiki/Colchicine

Colchicine is a medication used to treat gout and Behçet's disease. In gout, it is less preferred to NSAIDs or steroids. Other uses for colchicine include the prevention of pericarditis and familial Mediterranean fever.In gout, inflammation in joints results from the precipitation of circulating uric acid, exceeding its solubility in blood and depositing as crystals of monosodium urate in and around synovial fluid and soft tissues of joints.These crystal deposits cause inflammatory arthritis, which is initiated and sustained by mechanisms involving various proinflammatory mediators, such as cytokines. Colchicine accumulates in white blood cells and affects them in a variety of ways: decreasing motility, mobilization (especially chemotaxis) and adhesion.

Febuxostat
https://en.wikipedia.org/wiki/Febuxostat

Febuxostat, sold under the brand names Uloric and Adenuric among others, is a medication used long-term to treat gout due to high uric acid levels.Febuxostat is a non-purine-selective inhibitor of xanthine oxidase. It works by non-competitively blocking the molybdenum pterin center, which is the active site of xanthine oxidase. Xanthine oxidase is needed to oxidize successively hypoxanthine and xanthine to uric acid. Thus, febuxostat inhibits xanthine oxidase, thereby reducing production of uric acid. Febuxostat inhibits both the oxidized and the reduced forms of xanthine oxidase by virtue of its tight binding to the molybdenum pterin site.

Probenecid
https://en.wikipedia.org/wiki/Probenecid

Probenecid, also sold under the brand name Probalan, is a medication that increases uric acid excretion in the urine. It is primarily used in treating gout and hyperuricemia.

Probenecid was developed as an alternative to caronamide to competitively inhibit renal excretion of some drugs, thereby increasing their plasma concentration and prolonging their effects.Probenecid probably has several pharmacological targets, including blocking pannexins. Probenecid is also useful in the treatment of gout where the mechanism of action is believed to be focused on the kidney. Probenecid interferes with the kidneys' organic anion transporter (OAT), which reclaims uric acid from the urine and returns it to the plasma. If probenecid (an organic acid) is present, the OAT binds preferentially to it (instead of to uric acid), preventing reabsorption of the uric acid. Hence, the urine retains more uric acid, lowering uric acid concentration in the plasma. This is a good example of a medical usage for competition between substrates transported across cell membranes. This same effect, however, alters excretion of acidic drugs by the kidney, leading to the many drug interactions noted above.

Hepatitis C (HCV) Daclatasvir Dihydrochloride
https://en.wikipedia.org/wiki/Daclatasvir

Daclatasvir, sold under the trade name Daklinza, is a medication used in combination with other medications to treat hepatitis C (HCV). The other medications used in combination include sofosbuvir, ribavirin, and interferon, vary depending on the virus type and whether the person has cirrhosis.Daclatasvir stops HCV viral RNA replication and protein translation by directly inhibiting HCV protein NS5A. NS5A is critical for HCV viral transcription and translation, and as of 2014 it appeared that resistance can arise to daclatasvir fairly swiftly.

Ledipasvir
https://en.wikipedia.org/wiki/Ledipasvir

Ledipasvir is a drug for the treatment of hepatitis C that was developed by Gilead Sciences.

Ledipasvir inhibits an important viral phosphoprotein, NS5A, which is involved in viral replication, assembly, and secretion.

Sofosbuvir, on the other hand, is metabolized to a uridine triphosphate mimic, which acts as a RNA chain terminator when incorporated into RNA by NS5B polymerase.

Sofosbuvir
https://en.wikipedia.org/wiki/Sofosbuvir 

Sofosbuvir, sold under the brand name Sovaldi among others, is a medication used to treat hepatitis C. It is only recommended with some combination of ribavirin, peginterferon-alfa, simeprevir, ledipasvir, daclatasvir, or velpatasvir. Cure rates are 30 to 97% depending on the type of hepatitis C virus involved.

Sofosbuvir inhibits the hepatitis C NS5B protein. Sofosbuvir appears to have a high barrier to the development of resistance.

Sofosbuvir is a prodrug of the Protide type, whereby the active phosphorylated nucleotide is granted cell permeability and oral bioavailability. It is metabolized to the active antiviral agent GS-461203 (2'-deoxy-2'-α-fluoro-β-C-methyluridine-5'-triphosphate). GS-461203 serves as a defective substrate for the NS5B protein, which is the viral RNA polymerase, thus acts as an inhibitor of viral RNA synthesis. Although sofosbuvir has a 3' hydroxyl group to act as a nucleophile for an incoming NTP, a similar nucleotide analogue, 2'-deoxy-2'-α-fluoro-β-C-methylcytidine, is proposed to act as a chain terminator because the 2' methyl group of the nucleotide analogue causes a steric clash with an incoming NTP. Sofosbuvir would act in a similar way.

Telaprevir
https://en.wikipedia.org/wiki/Telaprevir

Telaprevir (VX-950), marketed under the brand names Incivek and Incivo, is a pharmaceutical drug for the treatment of hepatitis C co-developed by Vertex Pharmaceuticals and Johnson & Johnson. It is a member of a class of antiviral drugs known as protease inhibitors. Specifically, telaprevir inhibits the hepatitis C viral enzyme NS3/4A serine protease. Telaprevir is only indicated for use against hepatitis C genotype 1 viral infections and has not been proven to have an effect on or being safe when used for other genotypes of the virus. The standard therapy of pegylated interferon and ribavirin is less effective than telaprevir in those with genotype 1.

Wilson’s Disease Trientine HCl
https://en.wikipedia.org/wiki/Triethylenetetramine

Triethylenetetramine (TETA and trien), also called trientine (INN), is an organic compound with the formula [CH2NHCH2CH2NH2]2. This oily liquid is colorless but, like many amines, assumes a yellowish color due to impurities resulting from air-oxidation. It is soluble in polar solvents. The branched isomer tris(2-aminoethyl)amine and piperazine derivatives may also be present in commercial samples of TETA.The hydrochloride salt of TETA, referred to as trientine hydrochloride, is a chelating agent that is used to bind and remove copper in the body to treat Wilson's disease, particularly in those who are intolerant to penicillamine.

 
Musculo - skeletal disorder
Arthritis Celecoxib
https://en.wikipedia.org/wiki/Celecoxib

Celecoxib, sold under the brand name Celebrex among others, is a COX-2 inhibitor and nonsteroidal anti-inflammatory drug (NSAID). It is used to treat the pain and inflammation in osteoarthritis, acute pain in adults, rheumatoid arthritis, ankylosing spondylitis, painful menstruation, and juvenile rheumatoid arthritis. It may also be used to decrease the risk of colorectal adenomas in people with familial adenomatous polyposis.A highly selective reversible inhibitor of the COX-2 isoform of cyclooxygenase, celecoxib inhibits the transformation of arachidonic acid to prostaglandin precursors. Therefore, it has analgesic and anti-inflammatory properties.

For its use in reducing colon polyps, celecoxib affects genes and pathways involved in inflammation and malignant transformation in tumors, but not normal tissues.

Celecoxib binds to Cadherin-11 (which may explain the reduction in cancer progression).

Diacerein
https://en.wikipedia.org/wiki/Diacerein

Diacerein (INN), also known as diacetylrhein, is a slow-acting medicine of the class anthraquinone used to treat joint diseases such as osteoarthritis (swelling and pain in the joints). It works by inhibiting interleukin-1 beta.Diacerein works by blocking the actions of interleukin-1 beta, a protein involved in the inflammation and destruction of cartilage that play a role in the development of symptoms of degenerative joint diseases such as osteoarthritis. Due to its specific mode of action, which does not involve the inhibition of prostaglandin synthesis, diacerein has been shown to have anti-osteoarthritis and cartilage stimulating properties in vitro and animal models.

Risedronate
https://en.wikipedia.org/wiki/Risedronic_acid

Risedronic acid, often used as its sodium salt risedronate sodium, is a bisphosphonate used to strengthen bone, treat or prevent osteoporosis, and treat Paget's disease of bone. 
Sulfasalazine
https://en.wikipedia.org/wiki/Sulfasalazine

Sulfasalazine (SSZ), sold under the trade name Azulfidine among others, is a medication used to treat rheumatoid arthritis, ulcerative colitis, and Crohn's disease. It is considered by some to be a first line treatment in rheumatoid arthritis.Sulfasalazine is in the disease-modifying antirheumatic drugs (DMARDs) family of medications. It is unclear exactly how it works. One proposed mechanism is the inhibition of prostaglandins, resulting in local anti-inflammatory effects in the colon. The medication is broken down by intestinal bacteria into sulfapyridine and 5-aminosalicylic acid. That which is absorbed is excreted by the kidneys and in the bile.

Zinc Bisglycinate
https://en.wikipedia.org/wiki/Magnesium_glycinate
https://pubchem.ncbi.nlm.nih.gov/compound/151910#section=Uses

Magnesium glycinate, also known as magnesium diglycinate or magnesium bisglycinate, is the magnesium salt of glycine (one magnesium and two glycine molecules), and is sold as a dietary supplement.Drug, dietary_supplement, Pharmaceutical related Food_additive, Includes spices, extracts, colorings, flavors, etc added to food for human consumption Personal care, including cosmetics, shampoos, perfumes, soaps, lotions, toothpastes, etc.

Muscular Dystrophy, Duchenne Oxatomide Anhydrouse / Monohydrate
https://en.wikipedia.org/wiki/Oxatomide

Oxatomide, sold under the brand name Tinset among others, is a first-generation antihistamine of the diphenylmethylpiperazine family which is marketed in Europe, Japan, and a number of other countries. It was discovered at Janssen Pharmaceutica in 1975. Oxatomide lacks any anticholinergic effects. In addition to its H1 receptor antagonism, it also possesses antiserotonergic activity similarly to hydroxyzine.

Muscle Relaxants Flavoxate HCl
https://en.wikipedia.org/wiki/Flavoxate

Flavoxate is an anticholinergic with antimuscarinic effects. Its muscle relaxant properties may be due to a direct action on the smooth muscle rather than by antagonizing muscarinic receptors.
Meprobamate
https://en.wikipedia.org/wiki/Meprobamate

Meprobamate—marketed as Miltown by Wallace Laboratories and Equanil by Wyeth, among others—is a carbamate derivative used as an anxiolytic drug. Meprobamate's mechanism of action is not completely known. It has been shown in animal studies to have effects at multiple sites in the central nervous system, including the thalamus and limbic system. Meprobamate binds to GABAA receptors which interrupts neuronal communication in the reticular formation and spinal cord, causing sedation and altered perception of pain. Meprobamate has the ability to activate currents even in the absence of GABA. This relatively unique property makes meprobamate exceptionally dangerous when used in combination with other GABA-mediated drugs (including alcohol). It is also a potent adenosine reuptake inhibitor.
Methocarbamol
https://en.wikipedia.org/wiki/Methocarbamol

Methocarbamol, sold under the brand name Robaxin among others, is a medication used for short-term musculoskeletal pain.The mechanism of action of methocarbamol has not currently been established. Its effect is thought to be localized to the central nervous system rather than a direct effect on skeletal muscles. It has no effect on the motor end plate or the peripheral nerve fiber. The efficacy of the medication is likely related to its sedative effect. Alternatively, methocarbamol may act via inhibition of acetylcholinesterase, similarly to carbamate..

Thiocolchicoside
https://en.wikipedia.org/wiki/Thiocolchicoside

Thiocolchicoside (Muscoril, Myoril, Neoflax) is a muscle relaxant with anti-inflammatory and analgesic effects. It acts as a competitive GABAA receptor antagonist and also glycine receptor antagonist with similar potency and nicotinic acetylcholine receptors to a much lesser extent. It has powerful convulsant activity and should not be used in seizure-prone individuals.
Tofisopam
https://en.wikipedia.org/wiki/Tofisopam

Tofisopam (Emandaxin, Grandaxin, Sériel) is an anxiolytic that is marketed in several European countries. Chemically, it is a 2,3-benzodiazepine. Unlike other anxiolytic benzodiazepines (which are generally 1,4- or 1,5-substituted) however, tofisopam does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties. While it may not be an anticonvulsant in and of itself, it has been shown to enhance the anticonvulsant action of classical 1,4-benzodiazepines (such as diazepam) and muscimol, but not sodium valproate, carbamazepine, phenobarbital, or phenytoin.Tofisopam is indicated for the treatment of anxiety and alcohol withdrawal, and is prescribed in a dosage of 50–300 mg per day divided into three doses.

Muscle Spasms Baclofen
https://en.wikipedia.org/wiki/Baclofen

Baclofen, sold under the brand name Lioresal among others, is a medication used to treat muscle spasticity such as from a spinal cord injury or multiple sclerosis. It may also be used for hiccups and muscle spasms near the end of life.Chemically, baclofen is a derivative of the neurotransmitter γ-aminobutyric acid (GABA). It is believed to work by activating (or agonizing) GABA receptors, specifically the GABAB receptors. Its beneficial effects in spasticity result from its actions in the brain and spinal cord.
Nonopioid Analgesics Carbamazepine
https://en.wikipedia.org/wiki/Carbamazepine

Carbamazepine (CBZ), sold under the trade name Tegretol among others, is an anticonvulsant medication used primarily in the treatment of epilepsy and neuropathic pain. It is used in schizophrenia along with other medications and as a second-line agent in bipolar disorder. Carbamazepine appears to work as well as phenytoin and valproate for focal and generalized seizures It is not effective for absence or myoclonic seizures.Carbamazepine is a sodium channel blocker. It binds preferentially to voltage-gated sodium channels in their inactive conformation, which prevents repetitive and sustained firing of an action potential. Carbamazepine has effects on serotonin systems but the relevance to its antiseizure effects is uncertain. There is evidence that it is a serotonin releasing agent and possibly even a serotonin reuptake inhibitor.

Etodolac
https://en.wikipedia.org/wiki/Etodolac

Etodolac is a nonsteroidal anti-inflammatory drug (NSAID).NSAIDs are used for the management of mild to moderate pain, fever, and inflammation. They work by reducing the levels of prostaglandins, which are chemicals that are responsible for pain and the fever and tenderness that occur with inflammation. Etodolac blocks the cyclooxygenase (abbrev. COX) enzymes which form prostanoids, resulting in lower concentrations of prostaglandins. As a consequence, inflammation, pain and fever are reduced.

Glucosamine Sulphate
https://en.wikipedia.org/wiki/Glucosamine

Glucosamine (C6H13NO5) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. Glucosamine is part of the structure of the polysaccharides, chitosan, and chitin. Glucosamine is one of the most abundant monosaccharides. Produced commercially by the hydrolysis of shellfish exoskeletons or, less commonly, by fermentation of a grain such as corn or wheat, glucosamine has many names depending on country.

Although a common dietary supplement, there is little evidence that it is effective for relief of arthritis or pain, and is not an approved prescription drug..

Indomethacin
https://en.wikipedia.org/wiki/Indometacin

Indometacin, also known as indomethacin, is a nonsteroidal anti-inflammatory drug (NSAID) commonly used as a prescription medication to reduce fever, pain, stiffness, and swelling from inflammation. It works by inhibiting the production of prostaglandins, endogenous signaling molecules known to cause these symptoms. It does this by inhibiting cyclooxygenase, an enzyme that catalyzes the production of prostaglandins.Indometacin, a non-steroidal anti-inflammatory drug (NSAID), has similar mode of action when compared to other drugs in this group. Its is a nonselective inhibitor of cyclooxygenase (COX) 1 and 2, the enzymes that participate in prostaglandin synthesis from arachidonic acid. Prostaglandins are hormone-like molecules normally found in the body, where they have a wide variety of effects, some of which lead to pain, fever, and inflammation. By inhibiting the synthesis of prostaglandins, indometacin can reduce pain, fever, and inflammation. Indometacin mechanism of action, along with several other NSAIDs that inhibit COX, was described in 1971.
Ketorolac Tromethamine
https://en.wikipedia.org/wiki/Ketorolac
https://en.wikipedia.org/wiki/Tris .



Ketorolac, sold under the brand name Toradol among others, is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain. Specifically it is recommended for moderate to severe pain.
Tris (usually known as THAM in this context) is used as alternative to 
sodium bicarbonate in the treatment of metabolic acidosis.
Leflunomide
https://en.wikipedia.org/wiki/Leflunomide

Leflunomide, sold under the brand name Arava among others, is an immunosuppressive disease-modifying antirheumatic drug (DMARD), used in active moderate-to-severe rheumatoid arthritis and psoriatic arthritis. It is a pyrimidine synthesis inhibitor that works by inhibiting dihydroorotate dehydrogenase.

Leflunomide is an immunomodulatory drug that achieves its effects by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH), which plays a key role in the de novo synthesis of uridine monophosphate (rUMP), which is required for the synthesis of DNA and RNA. Hence, leflunomide inhibits the reproduction of rapidly dividing cells, especially lymphocytes.

The inhibition of human DHODH by teriflunomide, the active metabolite of leflunomide, occurs at levels (approximately 600 nM) that are achieved during treatment of rheumatoid arthritis (RA).

Meloxicam
https://en.wikipedia.org/wiki/Meloxicam

Meloxicam, sold under the brand name Mobic among others, is a nonsteroidal anti-inflammatory drug (NSAID) used to treat pain and inflammation in rheumatic diseases and osteoarthritis.Meloxicam blocks cyclooxygenase (COX), the enzyme responsible for converting arachidonic acid into prostaglandin H2—the first step in the synthesis of prostaglandins, which are mediators of inflammation. Meloxicam has been shown, especially at its low therapeutic doses, selectively to inhibit COX-2 over COX-1..

Nimesulide
https://en.wikipedia.org/wiki/Nimesulide

Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID) with pain medication and fever reducing properties. Its approved indications are the treatment of acute pain, the symptomatic treatment of osteoarthritis, and primary dysmenorrhoea in adolescents and adults above 12 years old.

Oxcarbazepine
https://en.wikipedia.org/wiki/Oxcarbazepine

Oxcarbazepine, sold under the brand name Trileptal among others, is a medication used to treat epilepsy and bipolar disorder. For epilepsy it is used for both focal seizures and generalized seizures. It has been used both alone and as add-on therapy in people with bipolar who have had no success with other treatments. It is taken by mouth.Oxcarbazepine is a prodrug, which is largely metabolised to its pharmacologically active 10-monohydroxy derivative licarbazepine (sometimes abbreviated MHD). Oxcarbazepine and MHD exert their action by blocking voltage-sensitive sodium channels, thus leading to the stabilization of hyper-excited neural membranes, suppression of repetitive neuronal firing and diminishment propagation of synaptic impulses. Furthermore, anticonvulsant effects of these compounds could be attributed to enhanced potassium conductance and modulation of high-voltage activated calcium channels.

Paracetamol / DC Grade
https://en.wikipedia.org/wiki/Paracetamol

Paracetamol, also known as acetaminophen, is a medication used to treat pain and fever. It is typically used for mild to moderate pain relief. Evidence is mixed for its use to relieve fever in children. It is often sold in combination with other medications, such as in many cold medications. Paracetamol is also used for severe pain, such as cancer pain and pain after surgery, in combination with opioid pain medication.Despite its common use, the mechanism of action of paracetamol is not completely understood. Unlike NSAIDs such as aspirin, paracetamol does not appear to inhibit the function of any cyclooxygenase (COX) enzyme outside the central nervous system, and this appears to be the reason why it is not useful as an anti-inflammatory. It does appear to selectively inhibit COX activities in the brain, which may contribute to its ability to treat fever and pain. This activity does not appear to be direct inhibition by blocking an active site, but rather by reducing COX, which must be oxidized in order to function.
Piroxicam
https://en.wikipedia.org/wiki/Piroxicam

Piroxicam is a nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class used to relieve the symptoms of painful inflammatory conditions like arthritis. Piroxicam works by preventing the production of endogenous prostaglandins which are involved in the mediation of pain, stiffness, tenderness and swelling.Piroxicam is an NSAID and, as such, is a non-selective COX inhibitor possessing both analgesic and antipyretic properties.
Opioid Analgesics Tramadol Hydrochloride
https://en.wikipedia.org/wiki/Tramadol

Tramadol, sold under the brand name Ultram among others, is an opioid pain medication used to treat moderate to moderately severe pain.Tramadol induces analgesic effects through a variety of different targets on the noradrenergic system, serotoninergic system and opioid receptors system. Tramadol exists as a racemic mixture, the positive enantiomer inhibits serotonin reuptake while the negative enantiomer inhibits noradrenaline re-uptake, by binding to and blocking the transporters. Tramadol has also been shown to act as a serotonin releasing agent. Both enantiomers of tramadol are agonists of the μ-opioid receptor and its M1 metabolite, O-demethylate, is also a μ-opioid receptor agonist but is 6 times more potent than tramadol itself. All these effects work synergistically to induce analgesia.
Osteoporosis Alendronate Sodium
https://en.wikipedia.org/wiki/Alendronic_acid

Alendronic acid, sold under the brand name Fosamax among others, is a bisphosphonate medication used to treat osteoporosis and Paget's disease of bone. It is taken by mouth. Use is often recommended together with vitamin D, calcium supplementation, and lifestyle changes.

Alendronate inhibits osteoclast-mediated bone-resorption. Like all bisphosphonates, it is chemically related to inorganic pyrophosphate, the endogenous regulator of bone turnover. But while pyrophosphate inhibits both osteoclastic bone resorption and the mineralization of the bone newly formed by osteoblasts, alendronate specifically inhibits bone resorption without any effect on mineralization at pharmacologically achievable doses. Its inhibition of bone-resorption is dose-dependent and approximately 1,000 times stronger than the equimolar effect of the first bisphosphonate drug, etidronate. Under therapy, normal bone tissue develops, and alendronate is deposited in the bone-matrix in a pharmacologically inactive form. For optimal action, enough calcium and vitamin D are needed in the body in order to promote normal bone development. Hypocalcemia should, therefore, be corrected before starting therapy.

Etidronate has the same disadvantage as pyrophosphate in inhibiting mineralization, but all of the potent N-containing bisphosphonates, including alendronate, risedronate, ibandronate, and zoledronate, do not.

Ambroxol HCl/Base
https://en.wikipedia.org/wiki/Ambroxol

Ambroxol is a drug that breaks up phlegm, used in the treatment of respiratory diseases associated with viscid or excessive mucus. Recently, a hypothesis suggested that it may have a potential role in treatment of Paget's disease of bone, Parkinsonism, and other common diseases of aging-associated diseases involving dysfunction of autophagy. Ambroxol is often administered as an active ingredient in cough syrup.

The substance acts on mucus membranes, restoring the physiological clearance mechanisms of the respiratory tract (which play an important role in the body’s natural defence mechanisms) through several mechanisms, including breaking up phlegm, stimulating mucus production, and stimulating synthesis and release of surfactant by type II pneumocytes. Surfactant acts as an anti-glue factor by reducing the adhesion of mucus to the bronchial wall, in improving its transport and in providing protection against infection and irritating agents.

Ambroxol is a potent inhibitor of the neuronal Na+ channels. This property led to the development of a lozenge containing 20 mg of ambroxol. Many state-of-the-art clinical studies have demonstrated the efficacy of ambroxol in relieving pain in acute sore throat, with a rapid onset of action, with its effect lasting at least three hours. Ambroxol is also anti-inflammatory, reducing redness in a sore throat.

Ambroxol has recently been shown to increase activity of the lysosomal enzyme glucocerebrosidase. Because of this it may be a useful therapeutic agent for both Gaucher disease and Parkinson's disease.

It was also recently shown that ambroxol triggers exocytosis of lysosomes by releasing calcium from acidic cellular calcium stores. This occurs by diffusion of ambroxol into lysosomes and lysosomal pH neutralization. This mechanism is most likely responsible for the mucolytic effects of the drug, but may also explain the reported activity in Gaucher and Parkinson's disease.

Both ambroxol and its parent drug bromhexine have been shown to induce autophagy in several cell types, and ambroxol was shown to potentiate rifampicin therapy in a model of tuberculosis through host directed effects. Ambroxol also enhances lung levels of a wide range of antibiotics. Ambroxol also had activity against SARS CoV2 in Vero E6 cells, although the mechanism of action is not yet known.

   
Oncology
Antimucositis Rutoside
https://en.wikipedia.org/wiki/Rutin

Rutin, also called rutoside, quercetin-3-O-rutinoside and sophorin, is the glycoside combining the flavonol quercetin and the disaccharide rutinose (α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranose). It is a citrus flavonoid found in a wide variety of plants including citrus.Rutin is a citrus flavonoid glycoside found in many plants including buckwheat, the leaves and petioles of Rheum species, and asparagus. Tartary buckwheat seeds have been found to contain more rutin (about 0.8–1.7% dry weight) than common buckwheat seeds (0.01% dry weight). Rutin is one of the primary flavonols found in 'clingstone' peaches. It is also found in green tea infusions.
Antineoplastic Agents Irinotecan HCl
https://en.wikipedia.org/wiki/Irinotecan

Irinotecan, sold under the brand name Camptosar among others, is a medication used to treat colon cancer, and small cell lung cancer. For colon cancer it is used either alone or with fluorouracil.For small cell lung cancer it is used with cisplatin.

Camptothecin, one of the four major structural classifications of plant-derived anti-cancerous compounds, is a cytotoxic alkaloid which consists of a pentacyclic ring structure containing a pyrrole (3, 4 β) quinoline moiety, an S-configured lactone form, and a carboxylate form. Irinotecan is activated by hydrolysis to SN-38, an inhibitor of topoisomerase I. This is then inactivated by glucuronidation by uridine diphosphate glucuronosyltransferase 1A1 (UGT1A1). The inhibition of topoisomerase I by the active metabolite SN-38 eventually leads to inhibition of both DNA replication and transcription.

The molecular action of irinotecan occurs by trapping a subset of topoisomerase-1-DNA cleavage complexes, those with a guanine +1 in the DNA sequence. One irinotecan molecule stacks against the base pairs flanking the topoisomerase-induced cleavage site and poisons (inactivates) the topoisomerase 1 enzyme.

Mitomycin
https://en.wikipedia.org/wiki/Mitomycins

The mitomycins are a family of aziridine-containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae. They include mitomycin A, mitomycin B, and mitomycin C. When the name mitomycin occurs alone, it usually refers to mitomycin C, its international nonproprietary name. Mitomycin C is used as a medicine for treating various disorders associated with the growth and spread of cells.Mitomycin C has been shown to have activity against stationary phase persisters caused by Borrelia burgdorferi, a factor in lyme disease. Mitomycin C is used to treat symptoms of pancreatic and stomach cancer, and is under clinical research for its potential to treat gastrointestinal strictures, wound healing from glaucoma surgery, corneal excimer laser surgery and endoscopic dacryocystorhinostomy.

Bladder,Kidney & other Urologic Cancers Sunitinib
https://en.wikipedia.org/wiki/Sunitinib

Sunitinib (marketed as Sutent by Pfizer, and previously known as SU11248) is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib was the first cancer drug simultaneously approved for two different indications.

Sunitinib inhibits cellular signaling by targeting multiple receptor tyrosine kinases (RTKs).

These include all receptors for platelet-derived growth factor (PDGF-Rs) and vascular endothelial growth factor receptors (VEGFRs), which play a role in both tumor angiogenesis and tumor cell proliferation. The simultaneous inhibition of these targets therefore reduces tumor vascularization and triggers cancer cell apoptosis and thus results in tumor shrinkage.

Sunitinib also inhibits CD117 (c-KIT), the receptor tyrosine kinase that (when improperly activated by mutation) drives the majority of gastrointestinal stromal cell tumors.

Brain Cancer, Head and Neck Cancer, Lung Cancer, Ovarian Cancer & Neuroblastoma Carboplatin
https://en.wikipedia.org/wiki/Carboplatin

Carboplatin, sold under the trade name Paraplatin among others, is a chemotherapy medication used to treat a number of forms of cancer. This includes ovarian cancer, lung cancer, head and neck cancer, brain cancer, and neuroblastoma.

Two theories exist to explain the molecular mechanism of action of carboplatin with DNA:

  • Aquation, or the like-cisplatin hypothesis.
  • Activation, or the unlike-cisplatin hypothesis.

The former is more accepted owing to the similarity of the leaving groups with its predecessor cisplatin, while the latter hypothesis envisages a biological activation mechanism to release the active Pt2+ species.

Chemotherapeutic Agents Azacitidine
https://en.wikipedia.org/wiki/Azacitidine

Azacitidine, sold under the brand name Vidaza among others, is a chemical analog of cytidine, a nucleoside in DNA and RNA. Azacitidine and its deoxy derivative, decitabine (also known as 5-aza-2′-deoxycytidine), are used in the treatment of myelodysplastic syndrome.

Azacitidine is a chemical analogue of the nucleoside cytosine, which is present in DNA and RNA. It is thought to have antineoplastic activity via two mechanisms – at low doses, by inhibiting of DNA methyltransferase, causing hypomethylation of DNA, and at high doses, by its direct cytotoxicity to abnormal hematopoietic cells in the bone marrow through its incorporation into DNA and RNA, resulting in cell death.

Cisplatin
https://en.wikipedia.org/wiki/Cisplatin

Cisplatin is a chemotherapy medication used to treat a number of cancers.Cisplatin is in the platinum-based antineoplastic family of medications. It works in part by binding to DNA and inhibiting its replication.Cisplatin interferes with DNA replication, which kills the fastest proliferating cells, which in theory are cancerous. Following administration, one chloride ion is slowly displaced by water to give the aquo complex cis-[PtCl(NH3)2(H2O)]+, in a process termed aquation. Dissociation of the chloride is favored inside the cell because the intracellular chloride concentration is only 3–20% of the approximately 100 mM chloride concentration in the extracellular fluid.

Dactinomycin
https://en.wikipedia.org/wiki/Dactinomycin

Dactinomycin, also known as actinomycin D, is a chemotherapy medication used to treat a number of types of cancer.

Because actinomycin can bind DNA duplexes, it can also interfere with DNA replication, although other chemicals such as hydroxyurea are better suited for use in the laboratory as inhibitors of DNA synthesis.

In cell biology, actinomycin D is shown to have the ability to inhibit transcription. Actinomycin D does this by binding DNA at the transcription initiation complex and preventing elongation of RNA chain by RNA polymerase.Actinomycin D and its fluorescent derivative, 7-aminoactinomycin D (7-AAD), are used as stains in microscopy and flow cytometry applications. The affinity of these stains/compounds for GC-rich regions of DNA strands makes them excellent markers for DNA. 7-AAD binds to single stranded DNA; therefore it is a useful tool in determining apoptosis and distinguishing between dead cells and live ones.

Diminazene Aceturate
https://en.wikipedia.org/wiki/Diminazene

Diminazene (INN; also known as diminazen) is an anti-infective medication for animals that is sold under a variety of brand names. It is effective against certain protozoa such as Babesia, Trypanosoma, and Cytauxzoon. The drug may also be effective against certain bacteria including Brucella and Streptococcus.

Chemically it is a di-amidine and it is formulated as its aceturate salt, diminazene aceturate.

The mechanism is not well understood; it probably inhibits DNA replication, but also has affinity to RNA.

Doxorubicin
https://en.wikipedia.org/wiki/Doxorubicin

Doxorubicin, sold under the brand name Adriamycin among others, is a chemotherapy medication used to treat cancer.[3] This includes breast cancer, bladder cancer, Kaposi's sarcoma, lymphoma, and acute lymphocytic leukemia. It is often used together with other chemotherapy agents.

Doxorubicin interacts with DNA by intercalation and inhibition of macromolecular biosynthesis. This inhibits the progression of topoisomerase II, an enzyme which relaxes supercoils in DNA for transcription. Doxorubicin stabilizes the topoisomerase II complex after it has broken the DNA chain for replication, preventing the DNA double helix from being resealed and thereby stopping the process of replication.[4] It may also increase quinone type free radical production, hence contributing to its cytotoxicity.

The planar aromatic chromophore portion of the molecule intercalates between two base pairs of the DNA, while the six-membered daunosamine sugar sits in the minor groove and interacts with flanking base pairs immediately adjacent to the intercalation site, as evidenced by several crystal structures.

By intercalation, doxorubicin can also induce histone eviction from transcriptionally active chromatin. As a result, DNA damage response, epigenome and transcriptome are deregulated in doxorubicin-exposed cells.

Epirubicin
https://en.wikipedia.org/wiki/Epirubicin

Epirubicin is an anthracycline drug used for chemotherapy. It can be used in combination with other medications to treat breast cancer in patients who have had surgery to remove the tumor. It is marketed by Pfizer under the trade name Ellence in the US and Pharmorubicin or Epirubicin Ebewe elsewhere.

Similarly to other anthracyclines, epirubicin acts by intercalating DNA strands. Intercalation results in complex formation which inhibits DNA and RNA synthesis. It also triggers DNA cleavage by topoisomerase II, resulting in mechanisms that lead to cell death. Binding to cell membranes and plasma proteins may be involved in the compound's cytotoxic effects. Epirubicin also generates free radicals that cause cell and DNA damage.

Gemcitabine HCl
https://en.wikipedia.org/wiki/Gemcitabine

Gemcitabine, sold under the brand name Gemzar, among others,[1] is a chemotherapy medication used to treat a number of types of cancer.

Gemcitabine is hydrophilic and must be transported into cells via molecular transporters for nucleosides (the most common transporters for gemcitabine are SLC29A1 SLC28A1, and SLC28A3). After entering the cell, gemcitabine is first modified by attaching a phosphate to it, and so it becomes gemcitabine monophosphate (dFdCMP).This is the rate-determining step that is catalyzed by the enzyme deoxycytidine kinase (DCK). Two more phosphates are added by other enzymes. After the attachment of the three phosphates gemcitabine is finally pharmacologically active as gemcitabine triphosphate (dFdCTP).

After being thrice phosphorylated, gemcitabine can masquerade as deoxycytidine triphosphate and is incorporated into new DNA strands being synthesized as the cell replicates.

Palbociclib
https://en.wikipedia.org/wiki/Palbociclib

Palbociclib, sold under the brand name Ibrance among others, is a medication developed by Pfizer for the treatment of HR-positive and HER2-negative breast cancer. It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6. Palbociclib was the first CDK4/6 inhibitor to be approved as a cancer therapy.

It is a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6.

In the G1 phase of the cell cycle, mammalian cells must pass a checkpoint, known as the restriction point "R", in order to complete the cell cycle and divide. CDK4 and CDK6 complex with cyclin D drive the phosphorylation of the retinoblastoma protein, Rb, which allows the cell to pass R and commit to division. Regulation of one or more proteins involved in this checkpoint is lost in many cancers. However, by inhibiting CDK4/6, palbociclib ensures that the cyclin D-CDK4/6 complex cannot aid in phosphorylating Rb. This prevents the cell from passing R and exiting G1, and in turn from proceeding through the cell cycle.

Risedronate
ttps://en.wikipedia.org/wiki/Risedronic_acid

Risedronic acid, often used as its sodium salt risedronate sodium, is a bisphosphonate used to strengthen bone, treat or prevent osteoporosis, and treat Paget's disease of bone.

Colorectal Cancer Oxaliplatin
https://en.wikipedia.org/wiki/Oxaliplatin

Oxaliplatin, sold under the brand name Eloxatin, is a cancer medication used to treat colorectal cancer. Often it is used together with fluorouracil and folinic acid (leucovorin) in advanced cancer.According to in vivo studies, oxaliplatin fights carcinoma of the colon through non-targeted cytotoxic effects. Like other platinum compounds, its cytotoxicity is thought to result from inhibition of DNA synthesis in cells. In particular, oxaliplatin forms both inter- and intra-strand cross links in DNA, which prevent DNA replication and transcription, causing cell death..
Hormone Therapy Letrozole
https://en.wikipedia.org/wiki/Letrozole

Letrozole, sold under the brand name Femara among others, is an aromatase inhibitor which is used in the treatment of hormonally-responsive breast cancer after surgery.Letrozole is an orally active, nonsteroidal, selective aromatase inhibitor and hence an antiestrogen. It prevents aromatase from producing estrogens by competitive, reversible binding to the heme of its cytochrome P450 unit. The action is specific, and letrozole does not reduce production of corticosteroids.

Leukemias,Lymphomas & other Hematologic Cancers Romidepsin
https://en.wikipedia.org/wiki/Romidepsin

Romidepsin, also known as Istodax, is an anticancer agent used in cutaneous T-cell lymphoma (CTCL) and other peripheral T-cell lymphomas (PTCLs). Romidepsin is a natural product obtained from the bacterium Chromobacterium violaceum, and works by blocking enzymes known as histone deacetylases, thus inducing apoptosis. It is sometimes referred to as depsipeptide, after the class of molecules to which it belongs.Romidepsin acts as a prodrug with the disulfide bond undergoing reduction within the cell to release a zinc-binding thiol. The thiol binds to a zinc atom in the binding pocket of Zn-dependent histone deacetylase to block its activity. Thus it is an HDAC inhibitor. Many HDAC inhibitors are potential treatments for cancer through the ability to epigenetically restore normal expression of tumor suppressor genes, which may result in cell cycle arrest, differentiation, and apoptosis.

Multiple Myeloma Bortezomib
https://en.wikipedia.org/wiki/Bortezomib

Bortezomib, sold under the brand name Velcade among others, is an anti-cancer medication used to treat multiple myeloma and mantle cell lymphoma. This includes multiple myeloma in those who have and have not previously received treatment.The boron atom in bortezomib binds the catalytic site of the 26S proteasome with high affinity and specificity. In normal cells, the proteasome regulates protein expression and function by degradation of ubiquitylated proteins, and also rids the cell of abnormal or misfolded proteins. Clinical and preclinical data support a role for the proteasome in maintaining the immortal phenotype of myeloma cells, and cell-culture and xenograft data support a similar function in solid tumor cancers. While multiple mechanisms are likely to be involved, proteasome inhibition may prevent degradation of pro-apoptotic factors, thereby triggering programmed cell death in neoplastic cells. Recently, it was found that bortezomib caused a rapid and dramatic change in the levels of intracellular peptides that are produced by the proteasome. Some intracellular peptides have been shown to be biologically active, and so the effect of bortezomib on the levels of intracellular peptides may contribute to the biological and/or side effects of the drug.

Carfilzomib
https://en.wikipedia.org/wiki/Carfilzomib

Carfilzomib (marketed under the trade name Kyprolis, developed by Onyx Pharmaceuticals) is an anti-cancer drug acting as a selective proteasome inhibitor. Chemically, it is a tetrapeptide epoxyketone and an analog of epoxomicin.Carfilzomib covalently  irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S proteasome, an enzyme that degrades unwanted cellular proteins. Carfilzomib displays minimal interactions with non-proteasomal targets, thereby improving safety profiles over bortezomib. Inhibition of proteasome-mediated proteolysis results in a build-up of polyubiquitinated proteins, which may cause cell cycle arrest, apoptosis, and inhibition of tumor growth.

Prostate Cancer Cabazitaxel
https://en.wikipedia.org/wiki/Cabazitaxel

Cabazitaxel (previously XRP-6258, trade name Jevtana) is a semi-synthetic derivative of a natural taxoid. It was developed by Sanofi-Aventis and was approved by the U.S. FDA for the treatment of hormone-refractory prostate cancer on June 17, 2010. It is a microtubule inhibitor, and the fourth taxane to be approved as a cancer therapy.

Cabazitaxel in combination with prednisone is a treatment option for hormone-refractory prostate cancer following docetaxel-based treatment.

Taxanes enhance the microtubules stabilization and inhibit the cellular mitosis and division. Moreover, taxanes prevent androgen receptor (AR) signaling by binding cellular microtubules and the microtubule-associated motor protein dynein, thus averting AR nuclear translocation.
Enzalutamide
https://en.wikipedia.org/wiki/Enzalutamide 

Enzalutamide, sold under the brand name Xtandi, is a nonsteroidal antiandrogen (NSAA) medication which is used in the treatment of prostate cancer. It is indicated for use in conjunction with castration in the treatment of metastatic castration-resistant prostate cancer (mCRPC),[2] nonmetastatic castration-resistant prostate cancer, and metastatic castration-sensitive prostate cancer (mCSPC).Enzalutamide acts as a selective silent antagonist of the androgen receptor (AR), the biological target of androgens like testosterone and dihydrotestosterone (DHT). Unlike the first-generation NSAA bicalutamide, enzalutamide does not promote translocation of AR to the cell nucleus and in addition prevents binding of AR to deoxyribonucleic acid (DNA) and AR to coactivator proteins. As such, it has been described as an AR signaling inhibitor in addition to antagonist.The drug is described as a "second-generation" NSAA because it has greatly increased efficacy as an antiandrogen relative to so-called "first-generation" NSAAs like flutamide and bicalutamide. The drug has only 2-fold lower affinity for the AR than DHT, the endogenous ligand of the AR in the prostate gland.

Renal Cell Carcinoma (RCC) Temsirolimus
https://en.wikipedia.org/wiki/Temsirolimus

Temsirolimus (codenamed CCI-779) is an intravenous drug for the treatment of renal cell carcinoma (RCC)Temsirolimus is a specific inhibitor of mTOR and interferes with the synthesis of proteins that regulate proliferation, growth, and survival of tumor cells. Though temsirolimus shows activity on its own, it is also known to be converted to sirolimus (rapamycin) in vivo; therefore, its activity may be more attributed to its metabolite rather than the prodrug itself (despite claims to the contrary by the manufacturer). Treatment with temsirolimus leads to cell cycle arrest in the G1 phase, and also inhibits tumor angiogenesis by reducing synthesis of VEGF.

 
Oropharyngeal
Nasal Decongestants Fluticasone Propionate / Furoate
https://en.wikipedia.org/wiki/Fluticasone_propionate

Fluticasone propionate, sold under the brand names Flovent and Flonase among others, is a steroid medication. When inhaled it is used for the long term management of asthma and COPD. In the nose it is used for hay fever and nasal polyps. It can also be used for mouth ulcers.Fluticasone propionate is a highly selective agonist at the glucocorticoid receptor with negligible activity at androgen, estrogen, or mineralocorticoid receptors, thereby producing anti-inflammatory and vasoconstriction effects. It has been shown to have a wide range of inhibitory effects on multiple cell types (e.g. mast cell, eosinophil, neutrophil, macrophages, and lymphocytes) and mediators (e.g. histamine, eicosanoids, leukotrienes, and cytokines) involved in inflammation. Fluticasone propionate is stated to exert a topical effect on the lungs without significant systemic effects at usual doses, due to its low systemic bioavailability.
Phenylephrine
https://en.wikipedia.org/wiki/Phenylephrine

Phenylephrine is a medication primarily used as a decongestant, to dilate the pupil, to increase blood pressure, and to relieve hemorrhoids.

Phenylephrine is a sympathomimetic drug, which means that it mimics the actions of epinephrine (commonly known as adrenaline) or norepinephrine. Phenylephrine selectively binds to alpha-1 receptors which cause blood vessels to constrict.[21]

Whereas pseudoephedrine causes both vasoconstriction and increase of mucociliary clearance through its nonspecific adrenergic activity, phenylephrine's selective α-adrenergic agonism causes vasoconstriction alone, creating a difference in their methods of action.

 
Respiratory system & anti- allergics
Anti- Allergics Acrivastine
https://en.wikipedia.org/wiki/Acrivastine

Acrivastine is a medication used for the treatment of allergies and hay fever. It is a second-generation H1-receptor antagonist antihistamine (like its base molecule triprolidine) and works by blocking histamine H1 receptors.Unlike cetirizine or loratadine, for which the standard dose is one tablet per day, a single acrivastine tablet may be taken up to three times a day. It is not to be taken by people over the age of 65, pregnant women, or people with compromised liver or kidney function.

Bilastine
https://en.wikipedia.org/wiki/Bilastine

Bilastine, sold under the brand name BILLASI among others, is a second-generation antihistamine medication which is used in the treatment of allergic rhinoconjunctivitis and urticaria (hives).

It exerts its effect as a selective histamine H1 receptor antagonist, and has an effectiveness similar to cetirizine, fexofenadine, and desloratadine.Bilastine binds to guinea-pig cerebellar histamine H1-receptors (Ki=44 nM) and to human recombinant histamine H1-receptors (Ki=64 nM) with an affinity comparable to that of astemizole and diphenhydramine, and superior than that of cetirizine by three-fold and fexofenadine by five-fold (Corcóstegui). In different murine models, bilastine by oral route, antagonizes the effects of histamine in a dose-dependent manner, with potency similar to that of cetirizine and between 5.5 and 10 times greater than that of fexofenadine.

Buclizine
https://en.wikipedia.org/wiki/Buclizine

Buclizine is an antihistamine and anticholinergic of the diphenylmethylpiperazine group. It is considered to be an antiemetic, similar to meclizine.

Bupivacaine HCl
https://en.wikipedia.org/wiki/Bupivacaine

Bupivacaine, marketed under the brand name Marcaine among others, is a medication used to decrease feeling in a specific area..Bupivacaine binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, which prevents depolarization. Without depolarization, no initiation or conduction of a pain signal can occur.

Cetirizine Dihydrochloride
https://en.wikipedia.org/wiki/Cetirizine

Cetirizine, sold under the brand name Zyrtec among others, is a second-generation antihistamine used to treat allergic rhinitis (hay fever), dermatitis, and urticaria.Cetirizine acts as a highly selective antagonist of the histamine H1 receptor.[3] The Ki values for the H1 receptor are approximately 6 nM for cetirizine, 3 nM for levocetirizine, and 100 nM for dextrocetirizine, indicating that the levorotatory enantiomer is the main active form. Cetirizine has 600-fold or greater selectivity for the H1 receptor over a wide variety of other sites, including muscarinic acetylcholine, serotonin, dopamine, and α-adrenergic receptors, among many others.
Chlorpheniramine Maleate (Chlorphenamine)
https://en.wikipedia.org/wiki/Chlorphenamine

Chlorphenamine (CP, CPM), also known as chlorpheniramine, is an antihistamine used to treat the symptoms of allergic conditions such as allergic rhinitis (hay fever).

Chlorphenamine acts primarily as a potent H1 antihistamine. It is specifically a potent inverse agonist of the histamine H1 receptor.The drug is also commonly described as possessing weak anticholinergic activity by acting as an antagonist of the muscarinic acetylcholine receptors. The dextrorotatory stereoisomer, dexchlorpheniramine, has been reported to possess Kd values of 15 nM for the H1 receptor and 1,300 nM for the muscarinic acetylcholine receptors in human brain tissue. The smaller the Kd value, the greater the binding affinity of the ligand for its target.

In addition to acting as an inverse agonist at the H1 receptor, chlorphenamine has been found to act as a serotonin reuptake inhibitor (Kd = 15.2 nM for the serotonin transporter).

Cloperastine
https://en.wikipedia.org/wiki/Cloperastine

Cloperastine (INN) or cloperastin, also known as cloperastine hydrochloride (JAN) (brand names Hustazol, Nitossil, Seki) and cloperastine fendizoate (or hybenzoate), is an antitussive and antihistamine that is marketed as a cough suppressant in Japan, Hong Kong, and in some European countries.It was first introduced in 1972 in Japan, and then in Italy in 1981. The precise mechanism of action of cloperastine is not fully clear, but several different biological activities have been identified for the drug, of which include: ligand of the σ1 receptor (Ki = 20 nM) (likely an agonist)GIRK channel blocker (described as "potent"),antihistamine (Ki = 3.8 nM for the H1 receptor), and anticholinergic. It is thought that the latter two properties contribute to side effects, such as sedation and somnolence, while the former two may be involved in or responsible for the antitussive efficacy of cloperastine.
Desloratadine
https://en.wikipedia.org/wiki/Desloratadine

Desloratadine (trade name Clarinex and Aerius) is a tricyclic H1 antagonist that is used to treat allergies. It is an active metabolite of loratadine

Desloratadine is a selective H1-antihistamine which functions as an inverse agonist at the histamine H1 receptor.

At very high doses, is also an antagonist at various subtypes of the muscarinic acetylcholine receptors. This effect is not relevant for the drug's action at therapeutic doses.

Fexofenadine
https://en.wikipedia.org/wiki/Fexofenadine

Fexofenadine, sold under the brand name Allegra among others, is an antihistamine pharmaceutical drug used in the treatment of allergy symptoms, such as hay fever and urticaria. Therapeutically, fexofenadine is a selective peripheral H1-blocker.

Fexofenadine is a selectively peripheral H1-blocker. Blockage prevents the activation of the H1 receptors by histamine, preventing the symptoms associated with allergies from occurring. Fexofenadine does not readily cross the blood–brain barrier and is therefore less likely to cause drowsiness in comparison to other antihistamines that readily cross the blood-brain barrier (i.e. first-generation antihistamines like diphenhydramine). In general, fexofenadine takes about one hour to take effect, though this may be affected by the choice of dosage form and the presence/absence of certain foods.

Fexofenadine also exhibits no anticholinergic, antidopaminergic, alpha1-adrenergic, or beta-adrenergic-receptor-blocking effects.

Hydroxyzine HCl
https://en.wikipedia.org/wiki/Hydroxyzine

Hydroxyzine, sold under the brand names Atarax and others, is a medication of the antihistamine type. It is used in the treatment of itchiness, anxiety, and nausea, including that due to motion sickness.Hydroxyzine's predominant mechanism of action is as a potent and selective histamine H1 receptor inverse agonist.[32][33] This action is responsible for its antihistamine and sedative effects. Unlike many other first-generation antihistamines, hydroxyzine has very low affinity for the muscarinic acetylcholine receptors, and in accordance, has low or no propensity for producing anticholinergic side effects..

Levocetirizine HCl
https://en.wikipedia.org/wiki/Levocetirizine

Levocetirizine, sold under the brand name Xyzal among others, is an antihistamine used for the treatment of allergic rhinitis (hay fever) and long term hives of unclear cause. It is less sedating than older antihistamines.Levocetirizine is an antihistamine. It acts as an inverse agonist that decreases activity at histamine H1 receptors. This in turn prevents the release of other allergy chemicals and increase the blood supply to the area, and provides relief from the typical symptoms of hay fever.
Loratadine
https://en.wikipedia.org/wiki/Loratadine

Loratadine, sold under the brand name Claritin among others, is a medication used to treat allergies. This includes allergic rhinitis (hay fever) and hives. It is also available in combination with pseudoephedrine, a decongestant, known as loratadine/pseudoephedrine.Loratadine is a tricyclic antihistamine, which acts as a selective inverse agonist of peripheral histamine H1 receptors. The potency of second generation histamine antagonists is (from strongest to weakest) desloratadine (Ki 0.4 nM) > levocetirizine (Ki 3 nM) > cetirizine (Ki 6 nM) > fexofenadine (Ki 10 nM) > terfenadine > loratadine. However, the onset of action varies significantly and clinical efficacy is not always directly related to only the H1 receptor potency, as concentration of free drug at the receptor must also be considered.

Rupatadine Fumarate
https://en.wikipedia.org/wiki/Rupatadine

Rupatadine is a second generation antihistamine and PAF antagonist used to treat allergies. 

Rupatadine is a second generation, non-sedating, long-acting histamine antagonist with selective peripheral H1 receptor antagonist activity. It further blocks the receptors of the platelet-activating factor (PAF) according to in vitro and in vivo studies.

Rupatadine possesses anti-allergic properties such as the inhibition of the degranulation of mast cells induced by immunological and non-immunological stimuli, and inhibition of the release of cytokines, particularly of the tumor necrosis factors (TNF) in human mast cells and monocytes.

Triprolidine HCl
https://en.wikipedia.org/wiki/Triprolidine

riprolidine is an over-the-counter antihistamine with anticholinergic properties. It is used to combat the symptoms associated with allergies and is sometimes combined with other cold medications designed to provide general relief for flu-like symptoms. As with many antihistamines, the most common side effect is drowsiness.
Anti- Asthma/COPD Acebrophylline
https://pharmeasy.in/molecules/acebrophylline-8210#:~:text=Acebrophylline%20is%20a%20Xanthine%20derivative,read%20more

Acebrophylline is a Xanthine derivative. It is used in obstructive airway diseases such as asthma and COPD (Chronic Obstructive Pulmonary Disease) as a bronchodilator to improve difficulty in breathing.

Ciclesonide
https://en.wikipedia.org/wiki/Ciclesonide

Ciclesonide is a glucocorticoid used to treat asthma and allergic rhinitis

Ciclesonide is a glucocorticoid used to treat asthma and allergic rhinitis. It is marketed under the brand names Alvesco for asthma and Omnaris, Omniair, Zetonna, and Alvesco for hay fever in the US and Canada.

Side effects of the medication include headache, nosebleeds, and inflammation of the nose and throat linings.

Ipratropium Bromide
https://en.wikipedia.org/wiki/Ipratropium_bromide

Ipratropium bromide, sold under the trade name Atrovent among others, is a medication which opens up the medium and large airways in the lungs. It is used to treat the symptoms of chronic obstructive pulmonary disease and asthma. It is used by inhaler or nebulizer.

Chemically, ipratropium bromide is a quaternary ammonium compound (which is indicated by the -ium per the BAN and the USAN)  obtained by treating atropine with isopropyl bromide, thus the name: isopropyl + atropine.[citation needed] It is chemically related to components of the plant Datura stramonium, which was used in ancient India for asthma.

Ipratropium exhibits broncholytic action by reducing cholinergic influence on the bronchial musculature. It blocks muscarinic acetylcholine receptors, without specificity for subtypes, and therefore promotes the degradation of cyclic guanosine monophosphate (cGMP), resulting in a decreased intracellular concentration of cGMP. Most likely due to actions of cGMP on intracellular calcium, this results in decreased contractility of smooth muscle in the lung, inhibiting bronchoconstriction and mucus secretion. It is a nonselective muscarinic antagonist, and does not diffuse into the blood, which prevents systemic side effects. Ipratropium is a derivative of atropine but is a quaternary amine and therefore does not cross the blood–brain barrier, which prevents central side effects (anticholinergic syndrome). Ipratropium should never be used in place of salbutamol (albuterol) as a rescue medication.

Ozagrel HCl
https://en.wikipedia.org/wiki/Ozagrel

Ozagrel (INN) is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor.

Roflumilast
https://en.wikipedia.org/wiki/Roflumilast

Roflumilast, sold under the trade name Daxas among others, is a drug that acts as a selective, long-acting inhibitor of the enzyme phosphodiesterase-4 (PDE-4). It has anti-inflammatory effects and is used as an orally administered drug for the treatment of inflammatory conditions of the lungs such as chronic obstructive pulmonary disease (COPD).Its primary clinical use is in the prevention of exacerbations (lung attacks) in severe chronic obstructive pulmonary disease (COPD).

Tiotropium Bromide / Monohydrate
https://en.wikipedia.org/wiki/Tiotropium_bromide

Tiotropium bromide, sold under the brand name Spiriva among others, is a long-acting bronchodilator used in the management of chronic obstructive pulmonary disease (COPD) and asthma. Specifically it is used to try to prevent periods of worsening rather than for those periods themselves.Tiotropium is a muscarinic receptor antagonist, often referred to as an antimuscarinic or anticholinergic agent. Although it does not display selectivity for specific muscarinic receptors, when topically applied it acts mainly on M3 muscarinic receptors located on smooth muscle cells and submucosal glands. This leads to a reduction in smooth muscle contraction and mucus secretion and thus produces a bronchodilatory effect.

Erdosteine
https://en.wikipedia.org/wiki/Erdosteine

Erdosteine is a molecule with mucolytic activity. Structurally is a thiol derivative characterized by the presence of two thiol groups. These two functional sulfhydryl groups contained in the molecule are released following first-pass metabolism with the conversion of erdosteine into its pharmacologically active metabolite Met-I.
Terbutaline Sulphate
https://en.wikipedia.org/wiki/Terbutaline

Terbutaline, sold under the brand name Bricanyl among others, is a β2 adrenergic receptor agonist, used as a "reliever" inhaler in the management of asthma symptoms and as a tocolytic (anti-contraction medication) to delay preterm labor for up to 48 hours. This time can then be used to administer steroid injections to the mother which help fetal lung maturity and reduce complications of prematurity.[1] It should not be used to prevent preterm labor or delay labor more than 48–72 hours.The tertiary butyl group in terbutaline makes it more selective for β2 receptors. Since there is no hydroxy group on position 4 of the benzene ring, the molecule is less susceptible to metabolism by the enzyme catechol-O-methyl transferase.

Bronchodilators & Mast Cell Stabilizers Montelukast Sodium
https://en.wikipedia.org/wiki/Montelukast

Montelukast, sold under the brand name Singulair among others, is a medication used in the maintenance treatment of asthma.

Montelukast is in the leukotriene receptor antagonist family of medications. It works by blocking the action of leukotriene D4 in the lungs resulting in decreased inflammation and relaxation of smooth muscle.

Montelukast functions as a leukotriene receptor antagonist (cysteinyl leukotriene receptors) and consequently opposes the function of these inflammatory mediators; leukotrienes are produced by the immune system and serve to promote bronchoconstriction, inflammation, microvascular permeability, and mucus secretion in asthma and COPD. Leukotriene receptor antagonists are sometimes colloquially referred to as leukasts.

Two genes of interest are ALOX5 and LTC4S, which catalyze two major steps in the biosynthetic pathway of leukotrienes.

 
Supplementation
Appetite Suppressant Phentermine HCl
https://en.wikipedia.org/wiki/Phentermine

Phentermine (phenyl-tertiary-butylamine), sold under the brand name Ionamin among others, is a medication used together with diet and exercise to treat obesity. It is taken by mouth for up to a few weeks. After a few weeks the beneficial effects no longer occur. It is also available as the combination phentermine/topiramate.Phentermine has some similarity in its pharmacodynamics with its parent compound, amphetamine, as they both are TAAR1 agonists, where the activation of TAAR1 in monoamine neurons facilitates the efflux, or release into the synapse, of these neurochemicals.

Dietary Supplement Nicotinamide
https://en.wikipedia.org/wiki/Nicotinamide

Nicotinamide (NAM) is a form of vitamin B3 found in food and used as a dietary supplement and medication.As a supplement, it is used by mouth to prevent and treat pellagra (niacin deficiency).While nicotinic acid (niacin) may be used for this purpose, nicotinamide has the benefit of not causing skin flushing. As a cream, it is used to treat acne.Side effects are minimal.At high doses liver problems may occur. Normal amounts are safe for use during pregnancy. Nicotinamide is in the vitamin B family of medications, specifically the vitamin B3 complex. It is an amide of nicotinic acid. Foods that contain nicotinamide include yeast, meat, milk, and green vegetables.

Phosphorus Supplementation Butaphosphan
https://www.trc-canada.com/product-detail/?CatNum=B689410

Butafosfan, a component of Catosal, is licensed for the treatment of metabolic disorders or as a tonic in swine. It reduces the stress-induced cortisol (C696302, d4 labelled) response after mixing of unfamiliar pigs. It can also increase milk production in Holstein cows in combination with cyanocobalamin.

 
Surgical & Vaccines
Intravenous & Other Sterile Solutions Hydroxyethyl Starch
https://en.wikipedia.org/wiki/Hydroxyethyl_starch

Hydroxyethyl starch (HES/HAES), sold under the brand name Voluven among others, is a nonionic starch derivative, used as a volume expander in intravenous therapy. The use of HES on critically ill patients is associated with an increased risk of death and kidney problems.HES is a general term and can be sub-classified according to average molecular weight, molar substitution, concentration, C2/C6 ratio and Maximum Daily Dose.

Maize Starch
https://en.wikipedia.org/wiki/Corn_starch

Corn starch, maize starch, or corn flour (British English) is the starch derived from corn (maize) grain. The starch is obtained from the endosperm of the kernel. Corn starch is a common food ingredient, often used to thicken sauces or soups, and to make corn syrup and other sugars Corn starch is versatile, easily modified, and finds many uses in industry such as adhesives, in paper products, as an anti-sticking agent, and textile manufacturing It has medical uses as well, such as to supply glucose for people with glycogen storage disease

Like many products in dust form, it can be hazardous in large quantities due to its flammability. When mixed with a fluid, corn starch can rearrange itself into a non-Newtonian fluid. For example, adding water transforms corn starch into a material commonly known as oobleck while adding oil transforms corn starch into an electrorheological (ER) fluid. The concept can be explained through the mixture termed "cornflour slime".

Corn starch is the preferred anti-stick agent on medical products made from natural latex, including condoms, diaphragms, and medical gloves.

Corn starch has properties enabling supply of glucose to maintain blood sugar levels for people with glycogen storage disease. Corn starch can be used starting at age 6–12 months allowing glucose fluctuations to be deterred.

Mucolytics, Proteolytic & Other Enzymes Serratiopeptidase
https://en.wikipedia.org/wiki/Serratiopeptidase

Serratiopeptidase (Serratia E-15 protease, also known as serralysin, serrapeptase, serratiapeptase, serratia peptidase, serratio peptidase, or serrapeptidase), is a proteolytic enzyme (protease) produced by non-pathogenic enterobacterium Serratia sp. E-15, now known as Serratia marcescens ATCC 21074. This microorganism was originally isolated in the late 1960s from silkworm Bombyx mori L. (intestine), Serratiopeptidase is present in the silkworm intestine and allows the emerging moth to dissolve its cocoon. Serratiopeptase is produced by purification from culture of Serratia E-15 bacteria. It is a member of the Peptitase M10B (Matrixin) family.

Trypsin And Chymotrypsin
https://en.wikipedia.org/wiki/Trypsin
https://en.wikipedia.org/wiki/Chymotrypsin


Trypsin (EC 3.4.21.4) is a serine protease from the PA clan superfamily, found in the digestive system of many vertebrates, where it hydrolyzes proteins. Trypsin is formed in the small intestine when its proenzyme form, the trypsinogen produced by the pancreas, is activated. Trypsin cuts peptide chains mainly at the carboxyl side of the amino acids lysine or arginine. It is used for numerous biotechnological processes. The process is commonly referred to as trypsin proteolysis or trypsinisation, and proteins that have been digested/treated with trypsin are said to have been trypsinized.Chymotrypsin (EC 3.4.21.1, chymotrypsins A and B, alpha-chymar ophth, avazyme, chymar, chymotest, enzeon, quimar, quimotrase, alpha-chymar, alpha-chymotrypsin A, alpha-chymotrypsin) is a digestive enzyme component of pancreatic juice acting in the duodenum, where it performs proteolysis, the breakdown of proteins and polypeptides.

Non-Ionic Iodinated Iopamidol
https://en.wikipedia.org/wiki/Iopamidol

Iopamidol (INN), sold under the brand name Isovue among others, is a nonionic, low-osmolar iodinated contrast agent, developed by Bracco Diagnostics.Iopamidol is indicated for angiography throughout the cardiovascular systemIt is also indicated for intrathecal administration in adult neuroradiology including myelography (lumbar, thoracic, cervical, total columnar), and for contrast enhancement of computed tomographic (CECT) cisternography and ventriculography. Isovue-M 200 (lopamidol Injection) is indicated for thoraco-lumbar myelography in children over the age of two years.

Clenbuterol HCl
https://en.wikipedia.org/wiki/Clenbuterol

Clenbuterol is a sympathomimetic amine used by sufferers of breathing disorders as a decongestant and bronchodilator. People with chronic breathing disorders such as asthma use this as a bronchodilator to make breathing easier. It is most commonly available as the hydrochloride salt, clenbuterol hydrochloride.

Clenbuterol is approved for use in some countries as a bronchodilator for asthma.

Clenbuterol is a β2 agonist with some structural and pharmacological similarities to epinephrine and salbutamol, but its effects are more potent and longer-lasting as a stimulant and thermogenic drug.[ It is commonly used for smooth muscle-relaxant properties as a bronchodilator and tocolytic.

It is classified by the World Anti-Doping Association as an anabolic agent, not as a β2 agonist.

Clenbuterol is prescribed for treatment of respiratory diseases for horses, and as an obstetrical aid in cattle. It is illegal in some countries to use in livestock used for food.

Cyclobenzaprine HCl
https://en.wikipedia.org/wiki/Cyclobenzaprine

Cyclobenzaprine, sold under the brand name Flexeril among others, is a medication used for muscle spasms from musculoskeletal conditions of sudden onset. It is not useful in cerebral palsy.Cyclobenzaprine is a centrally acting muscle relaxant. Cyclobenzaprine is a 5-HT2 receptor antagonist; it relieves muscle spasm through action on the central nervous system at the brain stem, rather than targeting the peripheral nervous system or muscles themselves.

Vecuronium Bromide
https://en.wikipedia.org/wiki/Vecuronium_bromide

Vecuronium bromide, sold under the brand name Norcuron among others, is a medication used as part of general anesthesia to provide skeletal muscle relaxation during surgery or mechanical ventilation.Vecuronium operates by competing for the cholinoceptors at the motor end plate, thereby exerting its muscle-relaxing properties

Peripherally Acting Muscle Relaxants Lidocaine (Lignocaine)
ttps://en.wikipedia.org/wiki/Lidocaine

Lidocaine, also known as lignocaine, is a medication used to numb tissue in a specific area (local anesthetic). It is also used to treat ventricular tachycardia and to perform nerve blocks.

Lidocaine alters signal conduction in neurons by prolonging the inactivation of the fast voltage-gated Na+ channels in the neuronal cell membrane responsible for action potential propagation. With sufficient blockage, the voltage-gated sodium channels will not open and an action potential will not be generated. Careful titration allows for a high degree of selectivity in the blockage of sensory neurons, whereas higher concentrations also affect other types of neurons.

The same principle applies for this drug's actions in the heart. Blocking sodium channels in the conduction system, as well as the muscle cells of the heart, raises the depolarization threshold, making the heart less likely to initiate or conduct early action potentials that may cause an arrhythmia.

Myrtecaine
ttps://en.wikipedia.org/wiki/Myrtecaine

Myrtecaine (Nopoxamine), sold as a combination product with diethylamine salicylate under the trade name Algesal and Algésal Suractivé among others, is a local anaesthetic in the form of a topical cream, or with laurilsulfate in rubefacient preparations. It is used to treat muscle strains, tendinitis or ligament sprains and joint pain. It is a surface anaesthetic, adds to the analgesic and anti-inflammatory actions of diethylamine salicylate by facilitating its penetration. Also myrtecaine has a muscle relaxant effect.
 
Veterinary list
Veterinary Albendazole
https://en.wikipedia.org/wiki/Albendazole

Albendazole, also known as albendazolum, is a medication used for the treatment of a variety of parasitic worm infestations.

As a vermicide, albendazole causes degenerative alterations in the intestinal cells of the worm by binding to the colchicine-sensitive site of β-tubulin, thus inhibiting its polymerization or assembly into microtubules (it binds much better to the β-tubulin of parasites than that of mammals). Albendazole leads to impaired uptake of glucose by the larval and adult stages of the susceptible parasites, and depletes their glycogen stores. Albendazole also prevents the formation of spindle fibers needed for cell division, which in turn blocks egg production and development; existing eggs are prevented from hatching. Cell motility, maintenance of cell shape, and intracellular transport are also disrupted.At higher concentrations, it disrupts the helminths' metabolic pathways by inhibiting metabolic enzymes such as malate dehydrogenase and fumarate reductase, with inhibition of the latter leading to less energy produced by the Krebs cycle. Due to diminished ATP production, the parasite is immobilized and eventually dies.

Some parasites have evolved to have some resistance to albendazole by having a different set of acids comprising β-tubulin, decreasing the binding affinity of albendazole. Drosophilia have many of the same mutations, meaning the drug does not affect fruit flies.

Buparvaquone
https://en.wikipedia.org/wiki/Buparvaquone

Buparvaquone is a hydroxynaphthoquinone antiprotozoal drug related to parvaquone and atovaquone. It is a promising compound for the therapy and prophylaxis of all forms of theileriosis. Buparvaquone has been shown to have anti-leishmanial activity in vitro. It can be used to treat bovine East Coast fever protozoa in vitro, along with the only other substance known – Peganum harmala.[ It is the only really effective commercial therapeutic product against bovine theileriosis, where it has been used since the late 1980s.
Butaphosphan
https://www.trc-canada.com/product-detail/?CatNum=B689410

Butafosfan, a component of Catosal, is licensed for the treatment of metabolic disorders or as a tonic in swine. It reduces the stress-induced cortisol (C696302, d4 labelled) response after mixing of unfamiliar pigs. It can also increase milk production in Holstein cows in combination with cyanocobalamin.


Clorsulon
ttps://www.trc-canada.com/product-detail/?C587380

A benzenedisulfonamide derivative with fasciolicidal activity. Anthelmintic (Trematodes).

Diminazene Diaceturate
https://en.wikipedia.org/wiki/Diminazene

Diminazene (INN; also known as diminazen) is an anti-infective medication for animals that is sold under a variety of brand names. It is effective against certain protozoa such as Babesia, Trypanosoma, and Cytauxzoon. The drug may also be effective against certain bacteria including Brucella and Streptococcus.

Chemically it is a di-amidine and it is formulated as its aceturate salt, diminazene aceturate.

The mechanism is not well understood; it probably inhibits DNA replication, but also has affinity to RNA.

Quinapyramine Chloride / Sulphate
https://en.wikipedia.org/wiki/Quinapyramine

Quinapyramine is a trypanocidal agent for veterinary use.

Triclabendazole
https://en.wikipedia.org/wiki/Triclabendazole

Triclabendazole, sold under the brand name Egaten among others, is a medication used to treat fascioliasis and paragonimiasis. It is very effective for both conditions. Treatment in hospital may be required..It is a member of the benzimidazole family of anthelmintics. The benzimidazole drugs share a common molecular structure, triclabendazole being the exception in having a chlorinated benzene ring but no carbamate group. Benzimidazoles such as triclabendazole are generally accepted to bind to beta-tubulin therefore preventing the polymerization of microtubules.
 
We manufacture
  Adenosylcobalamin
https://en.wikipedia.org/wiki/Adenosylcobalamin

.

Adenosylcobalamin (AdoCbl), also known as coenzyme B12, cobamamide, and dibencozide, is, along with methylcobalamin (MeCbl), one of the biologically active forms of vitamin B12.

Adenosylcobalamin participates as a cofactor in radical-mediated 1,2-carbon skeleton rearrangements. These processes require the formation of the deoxyadenosyl radical through homolytic dissociation of the carbon-cobalt bond. This bond is exceptionally weak, with a bond dissociation energy of 31 kcal/mol, which is further lowered in the chemical environment of an enzyme active site. An enzyme that uses adenosylcobalamin as a cofactor is methylmalonyl-CoA mutase (MCM).

  Beclomethasone Dipropionate
https://en.wikipedia.org/wiki/Beclometasone

Beclometasone, also known as beclometasone dipropionate, and sold under the brand name Qvar among others, is a steroid medication. It is available as an inhaler, cream, pills, and nasal spray. The inhaled form is used in the long-term management of asthma. The cream may be used for dermatitis and psoriasis. The pills have been used to treat ulcerative colitis. The nasal spray is used to treat allergic rhinitis and nasal polyps.

Beclometasone is mainly a glucocorticoid. Glucocorticoids are corticosteroids that bind to the glucocorticoid receptor that is present in almost every vertebrate animal cell. The activated glucocorticoid receptor-glucocorticoid complex up-regulates the expression of anti-inflammatory proteins in the nucleus (a process known as transactivation) and represses the expression of proinflammatory proteins in the cytosol by preventing the translocation of other transcription factors from the cytosol into the nucleus (transrepression).

Glucocorticoids are part of the feedback mechanism in the immune system which reduces certain aspects of immune function, such as inflammation.

  Betamethasone Valerate
https://en.wikipedia.org/wiki/Betamethasone_valerate

Betamethasone valerate is a synthetic glucocorticoid ester. It is the 17-valerate ester of betamethasone.

  Betamethasone Dipropionate
ttps://en.wikipedia.org/wiki/Betamethasone_dipropionate

Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities. It is applied as a topical cream, ointment, lotion or gel (Diprolene) to treat itching and other minor skin conditions such as eczema.

Minor side effects include dry skin and mild, temporary stinging when applied.

Betamethasone dipropionate is a "super high potency" corticosteroid used to treat inflammatory skin conditions such as dermatitis, eczema and psoriasis. It is a synthetic analog of the adrenal corticosteroids. Although its exact mechanism of action is not known, it is effective when applied topically to cortico-responsive inflammatory dermatoses.

  Betamethasone Sodium Phosphate
https://en.wikipedia.org/wiki/Betamethasone_phosphate

Betamethasone sodium phosphate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester.

  Clobetasol Propionate
https://en.wikipedia.org/wiki/Clobetasol_propionate

Clobetasol propionate is a corticosteroid used to treat skin conditions such as eczema, contact dermatitis, seborrheic dermatitis, and psoriasis. It is applied to the skin as a cream, ointment, or shampoo. Use should be short term and only if other weaker corticosteroids are not effective. Use is not recommended in rosacea or perioral dermatitis.
  Deflazacort
https://en.wikipedia.org/wiki/Deflazacort

Deflazacort (trade name Calcort among others) is a glucocorticoid used as an anti-inflammatory and immunosuppressant.

Deflazacort is an inactive prodrug which is metabolized rapidly to the active drug 21-desacetyldeflazacort.

  Diacerein
https://en.wikipedia.org/wiki/Diacerein

Diacerein (INN), also known as diacetylrhein, is a slow-acting medicine of the class anthraquinone used to treat joint diseases such as osteoarthritis (swelling and pain in the joints).Diacerein works by blocking the actions of interleukin-1 beta, a protein involved in the inflammation and destruction of cartilage that play a role in the development of symptoms of degenerative joint diseases such as osteoarthritis. Due to its specific mode of action, which does not involve the inhibition of prostaglandin synthesis, diacerein has been shown to have anti-osteoarthritis and cartilage stimulating properties in vitro and animal models.
  Hydrocortisone Acetate
https://en.wikipedia.org/wiki/Hydrocortisone_acetate

Hydrocortisone acetate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester.

  Hydroxycobalamin
https://en.wikipedia.org/wiki/Hydroxocobalamin

Hydroxocobalamin, also known as vitamin B12a and hydroxycobalamin, is a vitamin found in food and used as a dietary supplement. As a supplement it is used to treat vitamin B12 deficiency including pernicious anemia. Other uses include treatment for cyanide poisoning, Leber's optic atrophy, and toxic amblyopia.

Vitamin B12 refers to a group of compounds called cobalamins that are available in the human body in a variety of mostly interconvertible forms. Together with folate, cobalamins are essential cofactors required for DNA synthesis in cells where chromosomal replication and division are occurring—most notably the bone marrow and myeloid cells. As a cofactor, cobalamins are essential for two cellular reactions:

  Methyl Prednisolone Acetate

Methylprednisolone acetate, sold under the brand names Depo-Medrol among others, is a synthetic glucocorticoid corticosteroid and a corticosteroid ester—specifically the C21 acetate ester of methylprednisolone—which is used in clinical and veterinary medicine. It has been formulated as an aqueous suspension for intramuscular, intra-articular, soft tissue, and intralesional injection alone and in combination with lidocaine, a local anesthetic. Methylprednisolone acetate was previously suspended with polyethylene glycol but is no longer formulated with this excipient due to concerns about possible toxicity.

  Methyl Prednisolone Base
https://en.wikipedia.org/wiki/Methylprednisolone

Methylprednisolone, sold under the brand name Medrol among others, is a corticosteroid medication used to suppress the immune system and decrease inflammation. Conditions in which it is used include skin diseases, rheumatic disorders, allergies, asthma, croup, COPD, certain cancers, multiple sclerosis, and as add-on therapy for tuberculosis or radiculopathyUnbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors, modifying transcription and protein synthesis. By this mechanism, glucocorticoids can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The anti-inflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.



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