Recovery of platelet function after discontinuation of clopidogrel treatment in healthy volunteers

Br J Clin Pharmacol. 2001 Sep;52(3):333-6. doi: 10.1046/j.0306-5251.2001.01453.x.

Abstract

Aims: To study the recovery of platelet function after discontinuation of clopidogrel treatment in healthy volunteers.

Methods: Ten healthy volunteers were treated with clopidogrel (75 mg day(-1)) for 7 days. CD62P expression and PAC-1 binding were measured by flow cytometry.

Results: Adenosine diphosphate (ADP, 30 microM)-induced platelet responses were almost completely inhibited by clopidogrel. After discontinuation of the drug, platelet function gradually increased and complete recovery was seen 7 days after the last clopidogrel dose. The mean difference (95% CI) for ADP-induced PAC-1 binding (fluorescence intensity) between baseline and 7 days after the last dose was 0.01 (0.61, -0.59). Single cell analysis provides direct evidence for an irreversible mode of action of clopidogrel.

Conclusions: This is the first report to directly demonstrate irreversibility of clopidogrel action in humans.

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Diphosphate / pharmacology
  • Adult
  • Binding, Competitive / drug effects
  • Blood Platelets / drug effects*
  • Blood Platelets / metabolism
  • Blood Platelets / physiology
  • Clopidogrel
  • Flow Cytometry
  • Humans
  • Male
  • P-Selectin / drug effects
  • P-Selectin / metabolism
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / pharmacology*
  • Ticlopidine / analogs & derivatives
  • Ticlopidine / pharmacology*
  • Time Factors

Substances

  • P-Selectin
  • Platelet Aggregation Inhibitors
  • Adenosine Diphosphate
  • Clopidogrel
  • Ticlopidine