Nonsteroidal anti-inflammatory drug.
Pharmacology: The mechanism of action of celecoxib is due to inhibition of prostaglandin synthesis, primarily via inhibition of cyclooxygenase-2 (COX-2) and at therapeutic concentrations in humans, celecoxib does not inhibit the cyclooxygenase-1 (COX-1) isoenzyme.
Pharmacokinetics: Absorption: Peak plasma levels of celecoxib occur approximately 3 hrs after an oral dose. Both peak plasma levels and area under the curve are roughly dose proportional across the clinical dose range of 100-200 mg.
Distribution: In healthy subjects, celecoxib is highly protein-bound within the clinical dose range.
Metabolism: Celecoxib metabolism is primarily mediated via cytochrome P-450 2C9. Three metabolites, a primary alcohol, the corresponding carboxylic acid and its glucuronide conjugate, have been identified in human plasma. These metabolites are inactive as COX-1 or -2 inhibitors.
Excretion: Celecoxib is eliminated predominantly by hepatic metabolism with little unchanged drug recovered in the urine and feces.