Global Pharmaceutical API Products
全球原料藥廠生產品項
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
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.
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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.
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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.
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Sucralfate https://en.wikipedia.org/wiki/Sucralfate
Sucralfate, sold under various brand names, is
a medication used
to treat stomach ulcers, gastroesophageal
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
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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
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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. |
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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.
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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.
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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.
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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.
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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).
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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.
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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).
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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).
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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.
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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). |
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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 Kd (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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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).
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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. | |