Absorption, distribution and excretion of the new thienopyridine agent prasugrel in rats.

Abstract

Prasugrel is converted to the pharmacologically active metabolite after oral dosing in vivo. In this study, (14)C-prasugrel or prasugrel was administered to rats at a dose of 5 mg kg(-1). After oral and intravenous dosing, the values of AUC(0-infinity) of total radioactivity were 36.2 and 47.1 microg eqx h ml(-1), respectively. Oral dosing of unlabeled prasugrel showed the second highest AUC(0-8) of the active metabolite of six metabolites analyzed. Quantitative whole body autoradiography showed high radioactivity concentrations in tissues for absorption and excretion at 1 h after oral administration, and were low at 72 h. The excretion of radioactivity in the urine and feces were 20.2% and 78.7%, respectively, after oral dosing. Most radioactivity after oral dosing was excreted in bile (90.1%), which was reabsorbed moderately (62.4%). The results showed that orally administered prasugrel was rapidly and fully absorbed and efficiently converted to the active metabolite with no marked distribution in a particular tissue.

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@article{Hagihara2007AbsorptionDA, title={Absorption, distribution and excretion of the new thienopyridine agent prasugrel in rats.}, author={K Hagihara and A Kurihara and K Kawai and M Kazui and M Takahashi and K Kawabata and N A Farid and T Ikeda}, journal={Xenobiotica; the fate of foreign compounds in biological systems}, year={2007}, volume={37 7}, pages={788-801} }