Metabolism and disposition of the thienopyridine antiplatelet drugs ticlopidine, clopidogrel, and prasugrel in humans

• Published in: Journal of clinical pharmacology Vol. 50; no. 2; p. 126
• Main Authors: Farid, Nagy A, Kurihara, Atsushi, Wrighton, Steven A
• Format: Journal Article
• Language: English
• Published: England 01.02.2010
• Subjects: Acute Coronary Syndrome - drug therapy; Aryl Hydrocarbon Hydroxylases - genetics; Aryl Hydrocarbon Hydroxylases - metabolism; Blood Platelets - drug effects; Cytochrome P-450 CYP2C19; Drug Interactions; Humans; Piperazines - metabolism; Piperazines - therapeutic use; Platelet Aggregation - drug effects; Platelet Aggregation Inhibitors - metabolism; Platelet Aggregation Inhibitors - therapeutic use; Polymorphism, Genetic; Prasugrel Hydrochloride; Pyridines - metabolism; Pyridines - therapeutic use; Thiophenes - metabolism; Thiophenes - therapeutic use; Ticlopidine - analogs & derivatives; Ticlopidine - metabolism; Ticlopidine - therapeutic use

Ticlopidine, clopidogrel, and prasugrel are thienopyridine prodrugs that inhibit adenosine-5'-diphosphate (ADP)-mediated platelet aggregation in vivo. These compounds are converted to thiol-containing active metabolites through a corresponding thiolactone. The 3 compounds differ in their metabo...