Platelet Aggregation Inhibitory Effects and Pharmacokinetics of Prasugrel Used in Combination With Aspirin in Healthy Japanese Subjects

Kazuo Umemura, Yasuhiko Ikeda, Nobuko Matsushima, Kazunao Kondo

Research output: Contribution to journalArticle

1 Citation (Scopus)

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.

Original languageEnglish
Pages (from-to)398-407
Number of pages10
JournalClinical Pharmacology in Drug Development
Volume6
Issue number4
DOIs
Publication statusPublished - 01-07-2017

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science
  • Pharmacology (medical)

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