» Articles » PMID: 27652589

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

Overview
Publisher Wiley
Specialty Pharmacology
Date 2016 Sep 23
PMID 27652589
Citations 1
Authors
Affiliations
Soon will be listed here.
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.

Citing Articles

Evaluation of Tolerability, Pharmacokinetics and Pharmacodynamics of Vicagrel, a Novel P2Y12 Antagonist, in Healthy Chinese Volunteers.

Li X, Liu C, Zhu X, Wei H, Zhang H, Chen H Front Pharmacol. 2018; 9:643.

PMID: 29973877 PMC: 6019484. DOI: 10.3389/fphar.2018.00643.

References
1.
Riesmeyer J, Salazar D, Weerakkody G, Ni L, Wrishko R, Ernest 2nd C . Relationship between exposure to prasugrel active metabolite and clinical outcomes in the TRITON-TIMI 38 substudy. J Clin Pharmacol. 2011; 52(6):789-97. DOI: 10.1177/0091270011406280. View

2.
Small D, Kothare P, Yuen E, Lachno D, Li Y, Winters K . The pharmacokinetics and pharmacodynamics of prasugrel in healthy Chinese, Japanese, and Korean subjects compared with healthy Caucasian subjects. Eur J Clin Pharmacol. 2009; 66(2):127-35. DOI: 10.1007/s00228-009-0737-1. View

3.
Jakubowski J, Payne C, Li Y, Farid N, Brandt J, Small D . A comparison of the antiplatelet effects of prasugrel and high-dose clopidogrel as assessed by VASP-phosphorylation and light transmission aggregometry. Thromb Haemost. 2008; 99(1):215-22. DOI: 10.1160/TH07-09-0555. View

4.
Small D, Li Y, Ernest 2nd C, April J, Farid N, Payne C . Integrated analysis of pharmacokinetic data across multiple clinical pharmacology studies of prasugrel, a new thienopyridine antiplatelet agent. J Clin Pharmacol. 2010; 51(3):321-32. DOI: 10.1177/0091270010367429. View

5.
Brandt J, Payne C, Wiviott S, Weerakkody G, Farid N, Small D . A comparison of prasugrel and clopidogrel loading doses on platelet function: magnitude of platelet inhibition is related to active metabolite formation. Am Heart J. 2006; 153(1):66.e9-16. DOI: 10.1016/j.ahj.2006.10.010. View