Prasugrel hydrochloride (PCR 4099 hydrochloride), a thienopyridine and proagent, inhibits platelet function. Prasugrel hydrochloride is an orally active and potent P2Y12 receptor antagonist and inhibits ADP-induced platelet aggregation.
A novel antiplatelet agent; it is a third-generation thienopyridine. Antiplatelet agent Prasugrel showed greater platelet inhibition and decreased incidence of ischemic events than Clopidogrel but may induce increased incidence of bleeding in patient with acute coronary syndrome
In rat platelets, Prasugrel hydrochloride active metabolite inhibits in vitro platelet aggregation induced by adenosine ADP (10μM) with an IC50 value of 1.8 μM.
Prasugrel hydrochloride acts faster and is significantly more potent than Clopidogrel in vivo. Prasugrel hydrochloride is an inactive prodrug that requires metabolic processing in vivo to generate the active antiplatelet metabolite. Prasugrel hydrochloride is rapidly absorbed from the gut. After oral administration of standard-loading doses of 60 mg, maximum plasma levels of the active metabolite are achieved within 1 h, effective, maximum inhibition of platelet aggregation at 1-2 h.
