Sikstop Mechanism of Action

Pharmacology: Mechanism of action: Etoricoxib is a nonsteroidal anti inflammatory drug (NSAID) that exhibits anti inflammatory, analgesic, and antipyretic activities in animal models. Etoricoxib is a potent, orally active highly selective cyclooxygenase-2 (COX-2) inhibitor within and above the clinical dose range. Two isoforms of cyclooxygenase have been identified: cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). COX-1 is responsible for prostaglandin-mediated normal physiologic functions such as gastric cytoprotection and platelet aggregation. Inhibition of COX-1 by nonselective NSAIDs has been associated with gastric damage and platelet inhibition. COX-2 has been shown to be primarily responsible for the synthesis of prostanoid mediators of pain, inflammation, and fever. Selective inhibition of COX- by etoricoxib decreases these clinical signs and symptoms with decreased GI toxicity and without effects on platelet function.
Etoricoxib produced dose - dependent inhibition of COX-2 without inhibition of COX-1 at doses up to 150 mg daily.
Platelet Function: Multiple doses of etoricoxib up to 150 mg administered daily up to nine days had no effect on bleeding time relative to placebo. Similarly, bleeding time was not altered in a single-dose study with etoricoxib 250 or 500 mg. There was no inhibition of ex vivo arachidonic acid-or collagen-induced platelet aggregation at steady state with doses of Etoricoxib up to 150 mg. These findings are consistent with the COX-2 selectivity of Etoricoxib.