| Item |
Information |
|
Drug Groups
|
withdrawn; investigational |
|
Description
|
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. |
| Distribution |
* 86 L |
| Clearance |
* oral cl=6 L/h
* 6 – 7 L/h [In patients undergoing hemodialysis]
* 6 – 7 L/h [healthy elderly subjects] |
| External Links |
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