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Pharmacology: Pharmacodynamics: Etoricoxib decreases synthesis of prostaglandins due to selective dose-dependent inhibition of cyclooxygenase-2 (COX-2) enzyme within the clinical dose range; has antipyretic, analgesic and anti-inflammatory properties. Etoricoxib does not inhibit cyclooxygenase-1 (COX-1) at therapeutic concentrations.
Pharmacokinetics: Absorption: Etoricoxib is well absorbed from gastrointestinal tract after oral doses. The absolute bioavailability is approximately 100%. Peak plasma concentrations occur in about 1 hour in fasted adults; food delays absorption by about 2 hours, although it has no effect on the extent of absorption.
Distribution: Plasma protein binding is about 92%. The volume of distribution at steady state (Vd) is approximately 120 L.
Metabolism: Etoricoxib is extensively metabolized with less than 2% of a dose recovered in the urine as the parent drug. The major route of metabolism is via cytochrome P450 isoenzymes including CYP3A4 to form the 6'-hydroxymethyl derivative of Etoricoxib, which is then oxidized to the 6'-carboxylic acid derivative, the major metabolite. Both are inactive or only weak cyclooxygenase-2 (COX-2) inhibitors.
Excretion: At steady state the half-life of Etoricoxib is about 22 hours. Excretion is mainly via the urine (70%) with only 20% of a dose appearing in the feces.
