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QuickView for Valdecoxib (compound)


PubChem
Name: valdecoxib
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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DrugBank
Identification
Name: valdecoxib
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
Pharmacology
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...
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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
Interactions
Drug interaction:
KetoconazoleKetoconazole may increase the effect and toxicity of valdecoxib.
FluconazoleFluconazole may increase the effect and toxicity of valdecoxib.
LithiumThe COX-2 inhibitor increases serum levels of lithium

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Enzymes