Vaxol Mechanism of Action

Pharmacology: Pharmacodynamics: Mechanism of Action: Cilostazol is a quinolinone-derivative selective phosphodiesterase (PDE) inhibitor. Although its mechanism of action has not been fully elucidated, the drug appears to inhibit activation of cellular PDE type III (PDE III) resulting in suppressed degradation, and thus increased concentrations, of cyclic AMP (cAMP) in platelets and blood vessels. Cilostazol reversibly inhibits platelet aggregation induced by a wide range of stimuli, including thrombin, adenosine diphosphate (ADP), collagen, arachidonic acid, epinephrine and stress related clinical events.
Pharmacokinetics: Cilostazol is absorbed after oral doses; absorption is increased when administered with a high fat meal. It undergoes extensive hepatic metabolism via cytochrome P450 isoenzymes, mainly CYP3A4 and to a lesser extent CYP2C19, to both active and inactive metabolites which are predominantly excreted in the urine (74%) with the remainder in the feces (20%). Its active metabolites have apparent elimination half-lives of 11 to 13 hours. Cilostazol is 95 to 98% bound to protein.