Valdecoxib was removed from the Canadian, U.S., and E.U. markets in 2005 due to concerns about possible increased risk of heart attack and stroke.
Indication
For the treatment of osteoarthritis and dysmenorrhoea
Pharmacology
Valdecoxib, a selective cyclooxygenase-2 (COX-2) inhibitor, is classified as a nonsteroidal anti-inflammatory drug (NSAID). Valdecoxib is used for its anti-inflammatory, analgesic, and antipyretic activities in the management of osteoarthritis (OA) and for the treatment of dysmenorrhea or acute pain. Unlike celecoxib, valdecoxib lacks a sulfonamide chain and does not require CYP450 enzymes for metabolism.
Toxicity
Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression and coma may occur, but are rare.
Affected Organisms
Humans and other mammals
Biotransformation
Hepatic (involves CYP3A4 and 2C9)
Absorption
Oral bioavailability is 83%.
Half Life
8-11 hours
Protein Binding
98%
Elimination
Valdecoxib is eliminated predominantly via hepatic metabolism with less than 5% of the dose excreted unchanged in the urine and feces. About 70% of the dose is excreted in the urine as metabolites, and about 20% as valdecoxib N-glucuronide.
Biochem/physiol Actions Valdecoxib is a non-steroidal anti-inflammatory drug (NSAID), a cyclooxygenase-2 (COX-2) selective inhibitor. Legal Information Sold for research purposes under agreement from Pfizer Inc.
A nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic and antipyretic properties in animal models. An inhibitor of prostaglandin synthesis primarily through inhibition of COX-2.
参考文献
PubChem文献
数据源提供
• Yuan, J., et al.: Drug Metab. Dispos., 30, 1013 (2002)
• Mahadik, K., et al.: J. Pharm. Biomed. Anal., 33, 545 (2002)
• Kaul, N., et al.: J. Pharm. Biomed. Anal., 37, 27 (2002)
有害性 (Xn)
环境危害性 (N)