Clopidogrel generic formulations in the era of new antiplatelets: a systematic review

Curr Vasc Pharmacol. 2014;12(5):766-77. doi: 10.2174/15701611113119990135.

Abstract

Clopidogrel is a thienopyridine that selectively and irreversibly inhibits the ADP purinergic receptor P2Y12 and the subsequent ADP-mediated platelet activation. Clopidogrel has been approved for clinical use as clopidogrel hydrogen sulfate (bisulfate) salt. The clinical usefulness of clopidogrel bisulfate salt has been proved in a wide variety of large scale clinical trials, thus clopidogrel bisulfate has been extensively used in a large spectrum of patients been under thrombotic risk. Recently, several generic clopidogrel formulations have been approved for clinical use. Consequently, clopidogrel is currently a cost-effective antiplatelet agent. Only small studies have compared the pharmacokinetic and pharmacodynamic properties of various clopidogrel generic salt formulations with the innovator bisulfate salt. In addition few data are available concerning the clinical efficacy and safety of these generic clopidogrel formulations in order to guide clinicians in deciding when generic substitution is appropriate. The aim of this review is to summarize the physicochemical properties as well as the pharmacokinetic and pharmacodynamic characteristics of the generic clopidogrel salts. We also critically present existing data on the clinical efficacy and safety of the generic clopidogrel formulations compared with the innovator clopidogrel bisulfate salt in patients with cardiovascular disease.

Publication types

  • Review
  • Systematic Review

MeSH terms

  • Animals
  • Cardiovascular Diseases / drug therapy
  • Cardiovascular Diseases / metabolism
  • Chemistry, Pharmaceutical
  • Clinical Trials as Topic / methods
  • Clopidogrel
  • Drugs, Generic / chemistry
  • Drugs, Generic / pharmacokinetics
  • Drugs, Generic / therapeutic use
  • Humans
  • Platelet Aggregation Inhibitors / chemistry*
  • Platelet Aggregation Inhibitors / pharmacokinetics
  • Platelet Aggregation Inhibitors / therapeutic use*
  • Ticlopidine / analogs & derivatives*
  • Ticlopidine / chemistry
  • Ticlopidine / pharmacokinetics
  • Ticlopidine / therapeutic use

Substances

  • Drugs, Generic
  • Platelet Aggregation Inhibitors
  • Clopidogrel
  • Ticlopidine