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Pharmacology: Pharmacodynamics: Etoricoxib, an NSAID, is a selective cyclo-oxygenase-2 (COX-2) inhibitor. Its anti-inflammatory and analgesic action is exhibited by inhibition of prostaglandin synthesis via inhibition of COX-2.
Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract, food delays rate of absorption.
Absolute bioavailability: Approx 100%.
Time to peak plasma concentrations: Approx 1 hour (without food), 2 hours (with food).
Distribution: Volume of distribution: 120 L.
Plasma protein binding: Approx 92%.
Metabolism: Extensively metabolised via CYP3A4 isoenzyme to form 6'-hydroxymethyl derivative of etoricoxib, then oxidised to 6'-carboxylic acid derivative (major metabolite).
Excretion: Mainly via urine (70%), 20% in faeces, <2% as unchanged drug.
Elimination half-life: Approx 22 hours.
