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Home / Drugs / Starting with V / Valdecoxib

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.
CategoriesAnti-inflammatory Agents
Cyclooxygenase Inhibitors
Nonsteroidal Anti-inflammatory Agents (NSAIAs)
ManufacturersGd searle llc
PackagersCardinal Health
GD Searle LLC
Murfreesboro Pharmaceutical Nursing Supply
PD-Rx Pharmaceuticals Inc.
Pfizer Inc.
Physicians Total Care Inc.


For the treatment of osteoarthritis and dysmenorrhoea


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.

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.


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.


Hepatic (involves CYP3A4 and 2C9)


Oral bioavailability is 83%.

half life

8-11 hours

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.

drug interactions

Fluconazole: Fluconazole may increase the effect and toxicity of valdecoxib.

Ketoconazole: Ketoconazole may increase the effect and toxicity of valdecoxib.

Lithium: The COX-2 inhibitor increases serum levels of lithium