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PHARMACOLOGY: Pharmacodynamics: Etoricoxib is a member of a class of
Non-Steroid Anti-Inflammatory Drugs which is highly selective cyclo-oxygenase-2
(COX-2) inhibitor with anti-inflammatory and analgesic properties.
Pharmacokinetics: Absorption: Etoricoxib is well absorbed from the
gastrointestinal tract after oral doses. The bioavailability is approximately
100%. Peak plasma concentrations are reached in about 1 hour in fasted adults.
Dosing with food has no effect on the extent of absorption of etoricoxib. Food delays
absorption, resulting peak plasma concentrations by about 2 hours.
Distribution: Etoricoxib
is approximately 92% bound to plasma protein. At steady state the half-life of
etoricoxib is about 22 hours. The volume of distribution (Vd) is
approximately 120 l.
Metabolism: The major route of metabolism is via cytochrome
P450 isoenzymes including CYP3A4 to from 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 cyclo-oxygenase-2 (COX-2)
inhibitors.
Excretion: Etoricoxib is excretion mainly via the urine 70% with only 20% of a dose
appearing in the faeces. Less than 2% was recovered as
unchanged drug.
