Sign Out
Pharmacology: Pharmacodynamics: Etoricoxib decreases synthesis of prostaglandins due to selective inhibition of cyclooxygenase-2 (COX-2) enzyme; 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 the gastrointestinal tract after oral dose. Peak plasma concentrations occur in about 1 hour in fasted adults; food delays absorption by about 2 hours, it has no affect on the extent of absorption.
Bioavailability is about 100%.
Distribution: Volume of distribution is about 120 L. Plasma protein binding is about 92%.
Metabolism: Etoricoxib is extensively metabolized via hepatic. 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 derivative, the major metabolite. Both are inactive or only weak cyclooxygenase-2 (COX-2) inhibitors and no inhibition of cyclooxygenase-1 (COX-1).
Excretion: Excretion is mainly via the urine 70% with the only 20% of a dose appearing in the faeces. The half-life of etoricoxib is about 22 hours.
