title: Platelet Aggregation Inhibitory Effects and Pharmacokinetics of Prasugrel Used in Combination With Aspirin in Healthy Japanese Subjects.
abstract: We evaluated the pharmacokinetics and pharmacodynamics of prasugrel used in combination with aspirin in healthy Japanese subjects. All subjects received aspirin 100 mg/day. Subsequently, in the single-administration study, 23 subjects also received prasugrel 20 or 30 mg, and in the multiple-administration study, 20 subjects received a loading dose of prasugrel 20 or 30 mg on day 1, followed by a maintenance dose of prasugrel 5 or 7.5 mg/day, respectively, on days 2-5. In both studies, the plasma concentration of the active metabolite of prasugrel, R-138727, reached a maximum 0.5 hours after administration and rapidly decreased within 4 hours. In the single-administration study, the inhibitory effect on adenosine diphosphate-induced platelet aggregation was significantly higher in the prasugrel 20- and 30-mg groups than in the placebo group at all times (1-144 hours) after administration. In the multiple-administration study, a similar antiplatelet effect was found after both the loading dose and the maintenance dose and was maintained for 3-6 days after the last administration. There were study drug-related adverse events; however, all were mild, and none was clinically significant.
authors.affiliation: Department of Pharmacology, Hamamatsu University School of Medicine, Hamamatsu-shi, Shizuoka, Japan.
authors.forename: Kazuo
authors.initials: K
authors.lastname: Umemura
authors.affiliation: Department of Pharmacology, Hamamatsu University School of Medicine, Hamamatsu-shi, Shizuoka, Japan.|Shin-nakagawa Hospital, Yokohama-shi, Kanagawa, Japan.
authors.forename: Yasuhiko
authors.initials: Y
authors.lastname: Ikeda
authors.affiliation: Translational Medicine and Clinical Pharmacology Department, Daiichi Sankyo Co., Ltd, Shinagawa-ku, Tokyo, Japan.|Clinical Pharmacology Department, Janssen Pharmaceutical K.K. , Chiyoda-ku, Tokyo, Japan.
authors.forename: Nobuko
authors.initials: N
authors.lastname: Matsushima
authors.affiliation: Department of Pharmacology, Fujita Health University School of Medicine, Toyoake-shi, Aichi, Japan.
authors.forename: Kazunao
authors.initials: K
authors.lastname: Kondo
mesh_terms: D000328:Adult; D019540:Area Under Curve; D001241:Aspirin / Q000008:administration & dosage / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D004311:Double-Blind Method; D004334:Drug Administration Schedule; D004359:Drug Therapy, Combination; D064368:Healthy Volunteers; D006801:Humans; D007564:Japan; D010879:Piperazines / Q000097:blood; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics*; D010979:Platelet Function Tests; D000068799:Prasugrel Hydrochloride / Q000008:administration & dosage / Q000493:pharmacokinetics*; D055815:Young Adult
chemical_list: D010879:Piperazines; D010975:Platelet Aggregation Inhibitors; C510685:R-138727; D000068799:Prasugrel Hydrochloride; D001241:Aspirin
keywords: aspirin; healthy Japanese subjects; inhibition of platelet aggregation; pharmacokinetics; prasugrel