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

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Showing 21 - 25 of 25 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Toluene is a colorless, water-insoluble liquid with the smell associated with paint thinners. It is a mono-substituted benzene derivative, consisting of a CH3 group attached to a phenyl group. The major use of toluene is as a mixture added to gasoline to improve octane ratings. Toluene is also usedto produce benzene and as a solvent in paints, coatings, synthetic fragrances, adhesives, inks, and cleaningagents. Toluene is also used in the production of polymers used to make nylon, plastic soda bottles, andpolyurethanes and for pharmaceuticals, dyes, cosmetic nail products, and the synthesis of organicchemicals. The CNS is the primary target organ for toluene toxicity in both humans and animals for acute and chronicexposures. CNS dysfunction (which is often reversible) and narcosis have been frequently observed inhumans acutely exposed to low or moderate levels of toluene by inhalation; symptoms include fatigue,sleepiness, headaches, and nausea. CNS depression and death have occurred at higher levels of exposure. Toluene is used in veterinary medicine as a treatment for various parasites in dogs and cats. It is used for the removal of ascarids (Toxocara canis and Toxascaris leonina) and hookworms (Ancylostoma caninum and Uncinaria stenocephala) and as an aid in removing tapeworms (Taenia pisiformis, Dipylidium caninum, and Echinococcus granulosus) from dogs and cats.
Tenivastatin (well known as simvastatin acid or simvastatin hydroxy acid) is a pharmacologically active metabolite, which is formed in the mammalian organism from lactone prodrug, simvastatin. Tenivastatin is a potent reversible inhibitor of HMGCR (HMG-CoA reductase), reduces cholesterol synthesis and increases low-density lipoprotein (LDL) receptors on cell membranes of liver and extrahepatic tissues. It is also a substrate of organic anion transporting polypeptide 1B1 (OATP1B1/Oatp2), an influx transporter expressed on the sinusoidal membrane of hepatocytes. Recent studies have shown that OATP1B1 plays a clinically important role in the hepatic elimination of several drugs including statins, via mediating the hepatic uptake. In addition, was discovered, that the tenivastatin was a substrate of another transporter protein, human organic anion transporting polypeptide 3A1 (OATP3A1), which is predominately expressed in the heart. Presence of OATP3A1 in cardiomyocytes suggested that transporter could modulate the exposure of cardiac tissue to simvastatin acid due to its enrichment in cardiomyocytes. Increases in the uptake of simvastatin acid by OATP3A1 when combined with OATP substrates suggest the potential for drug-drug interactions that could influence clinical outcomes.
Status:
US Approved OTC
Source:
21 CFR 343.13(b) internal analgesic:rheumatologic aspirin (buffered)
Source URL:
First marketed in 1899
Source:
Aspirin by Friedr. Bayer & Co., Elberfeld, Germany
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Aspirin is a nonsteroidal anti-inflammatory drug. Aspirin is unique in this class of drugs because it irreversibly inhibits both COX-1 and COX-2 activity by acetylating a serine residue (Ser529 and Ser516, respectively) positioned in the arachidonic acid-binding channel, thus inhibiting the synthesis of prostaglandins and reducing the inflammatory response. The drug is used either alone or in combination with other compounds for the treatment of pain, headache, as well as for reducing the risk of stroke and heart attacks in patients with brain ischemia and cardiovascular diseases.