U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 2291 - 2300 of 8583 results

Status:
Possibly Marketed Outside US
Source:
NCT02107144: Phase 4 Interventional Completed Coronary Artery Disease
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Trimetazidine is a medicine, which is used for the treatment of angina pectoris. The drug mechanism of action is explained by its ability to selectively inhibit long-chain 3-ketoacyl coenzyme A thiolase, an enzyme responsible for mitochondrial beta-oxidation of long chain fatty acids. Trimetazidine also increases pyruvate dehydrogenase activity, binds to the mitochondrial membrane, directly inhibits cardiac fibrosis and improves mechanical resistance of the sarcolemma.
Status:
Possibly Marketed Outside US
Source:
GLITISOL by Sterling Winthrop
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Thiamphenicol is a broad-spectrum antibiotic, which is active against gram-positive and gram-negative organisms. The drug is marketed in Asia and Latin America for the treatment of various infections, including sexually transmitted diseases. As many phenicols, thiamphenicol inhibits the protein synthesis in bacterias by binding to 23S ribosomal subunit. In Europe and USA the drug is used in a veterinary practice.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Nitroscanate (trade name Lopatol) is a medium-spectrum anthelmintic used on dogs and cats. It is available in the form of tablets for oral administration. It is not used on livestock. Nitroscanate is effective against the major gastrointestinal roundworms (nematodes) of dogs and cats (e.g.Toxocara canis, Toxocara cati, Ancylostoma spp, Uncinaria stenocephala) and tapeworms (e.g. Dipylidium caninum, Echinococcus granulosus, Taenia spp, etc.). The molecular mode of action of nitroscanate has not been elucidated. It is assumed that it acts as an uncoupler of the oxidative phosphorylation in the cell mitochondria, which disturbs the production of ATP, the cellular "fuel". This impairs the parasites motility and probably other processes as well.
Status:
Possibly Marketed Outside US
Source:
NCT02741947: Phase 4 Interventional Completed Parkinson Disease
(2014)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Benserazide is a peripherally-acting aromatic L-amino acid decarboxylase (AADC) or DOPA decarboxylase inhibitor. Benserazide is only used in conjunction with L-dopa for the treatment of Parkinson's disease under the brand name Madopar in the UK. Madopar HBS (125 mg) is a controlled-release dosage form with 100 mg L-dopa and 25 mg benserazide.
Status:
Possibly Marketed Outside US
Source:
NCT02807922: Phase 4 Interventional Completed Sleep
(2016)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Zopiclone (brand names Zimovane and Imovane) is a nonbenzodiazepine hypnotic agent used in the treatment of insomnia. The therapeutic pharmacological properties of zopiclone include hypnotic, anxiolytic, anticonvulsant, and myorelaxant properties. Zopiclone and benzodiazepines bind to different sites on GABAA-containing receptors, causing an enhancement of the actions of GABA to produce the therapeutic and adverse effects of zopiclone. The metabolite of zopiclone called desmethylzopiclone is also pharmacologically active, although it has predominately anxiolytic properties. One study found some slight selectivity for zopiclone on α1 and α5 subunits, although it is regarded as being unselective in its binding to α1, α2, α3, and α5 GABAA benzodiazepine receptor complexes. Desmethylzopiclone has been found to have partial agonist properties, unlike the parent drug zopiclone, which is a full agonist. The mechanism of action of zopiclone is similar to benzodiazepines, with similar effects on locomotor activity and on dopamine and serotonin turnover. A meta-analysis of randomised controlled clinical trials that compared benzodiazepines to zopiclone or other Z drugs such as zolpidem and zaleplon has found few clear and consistent differences between zopiclone and the benzodiazepines in sleep onset latency, total sleep duration, number of awakenings, quality of sleep, adverse events, tolerance, rebound insomnia, and daytime alertness. After oral administration, zopiclone is rapidly absorbed, with a bioavailability around 75–80%. Time to peak plasma concentration is 1–2 hours. High-fat meal preceding zopiclone administration does not change absorption (as measured by AUC), but reduces peak plasma levels and delays its occurrence, thus may delay the onset of therapeutic effects. The pharmacokinetics of zopiclone in humans are stereoselective. After oral administration of the racemic mixture, Cmax (time to maximum plasma concentration), area under the plasma time-concentration curve (AUC) and terminal elimination half-life values are higher for the dextrorotatory enantiomers, owing to the slower total clearance and smaller volume of distribution (corrected by the bioavailability), compared with the levorotatory enantiomer. In urine, the concentrations of the dextrorotatory enantiomers of the N-dimethyl and N-oxide metabolites are higher than those of the respective antipodes. Zopiclone is sometimes used as a method of suicide. It has a similar fatality index to that of benzodiazepine drugs, apart from temazepam, which is particularly toxic in overdose.
Nifuratel is a furane-derivative provided with a strong trichomonicidal activity; it has a broad antibacterial spectrum of action, including both Gram-negative and Gram-positive organisms. It is active against Chlamydia trachomatis and Mycoplasma spp. and has also some degree of activity against Candida spp. and mycetes. The action mechanism of nitrofurans has not been fully elucidated, and it may be the inhibiting of acetyl coenzyme A interfere with the early stages of bacterial glucose metabolism. Nifuratel alone or in complex with nystatin is indicated for the treatment of vulvovaginal and urinary tract infections. The drug is not approved by FDA.
Status:
Possibly Marketed Outside US
Source:
VIRULEX FORTE by Kabi
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Moroxydine is an antiviral drug discovered in the 1950’s which was shown to be active against DNA and RNA viruses. Moroxydine analogues are potent anti-hepatitis C virus (HCV) agents.
Status:
Possibly Marketed Outside US
Source:
GASTROZEPIN by Boehringer Ingelheim
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Pirenzepine is a M1 muscarinic receptor antagonist, which is prescribed for the treatment of gastric and duodenal ulcer in Europe. The drug preferentially acts on the gastric mucosa to inhibit secretion of both gastric acid and pepsin. Experiment with healthy volunteers demonstrated that pirenzepine passes the blood-brain barrier, but only to a small extent.
Status:
Possibly Marketed Outside US
Source:
BECANTEX by Horner
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Dibunate (also known as Becantex, Becantyl, Linctussal, L-1633, and described as the 2,6-isomer or the 2,7-isomer) is an antitussive oral medication that was used in many counties all over the world. The current marketing status of the drug is unknown and is supposed to be "discontinued".
Ttioxidazole has broad spectrum activity against gastrointestinal nematodes. Tiox (tioxidazole) Paste is indicated for removal of mature large strongyles (Strongylus edentatus, S.equinus , and S.vulgaris ), mature ascarids (Parascaris equorum and immature (4th larval stage) pinworms (Oxyuris equi), and mature small strongyles (Triodontophorus spp). Ttioxidazole is a tubulin polymerization inhibitor.

Showing 2291 - 2300 of 8583 results