Name: | valdecoxib |
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PubChem Compound ID: | 119607 |
Molecular formula: | C16H14N2O3S |
Molecular weight: | 314.36 g/mol |
Synonyms: |
KBioGR_001617; Kudeq; Valdyn; Spectrum4_001129; KBio3_001941; KBio2_004795; SC 65872; Valdecoxib (USAN); Spectrum_001747; KBio2_007363.
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Name: | valdecoxib |
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Name (isomeric): | DB00580 |
Drug Type: | small molecule |
Brand: | Bextra |
Category: | Cyclooxygenase Inhibitors, Anti-inflammatory Agents, Nonsteroidal Anti-inflammatory Agents (NSAIAs) |
CAS number: | 181695-72-7 |
Indication: | For the treatment of osteoarthritis and dysmenorrhoea |
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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...
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Mechanism of Action: | Both COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin (PG) H2, the precursor of PGs and thromboxane. Valdecoxib selectively inhibits the cyclooxygenase-2 (COX-2) enzyme, important for the mediation of inflammation and pain. Unlike non-selective NSAIDs, valdecoxib does not inhibit platelet aggregation. |
Absorption: | Oral bioavailability is 83%. |
Protein binding: | 98% |
Biotransformation: | Hepatic (involves CYP3A4 and 2C9) |
Route of 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. |
Half Life: | 8-11 hours |
Clearance: | oral cl=6 L/h 6 – 7 L/h [In patients undergoing hemodialysis] 6 – 7 L/h [healthy elderly subjects] |
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 |
Drug interaction: |
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