[Clopidogrel and its salts: any clnical implication?].
Clopidogrel hydrogen sulfate is an antiplatelet agent administered, alone or in combination with acetyl salicylic acid, approved in the prevention of cardiovascular events based on large-scale clinical trials. The new salt formulations clopidogrel where approved based on pharmacokinetic measurements of the inactive prodrug on few healthy volunteers, without any other medication. Clopidogrel hydrogen sulfate has a wide variability in platelet response and the pharmacokinetic of the active metabolite is not dose-linear. Ideally, new clopidogrel salts should be tested for therapeutic equivalence in the target patient population. Should this not be feasible, consistent bioequivalence data should be obtained for the active metabolite, using a properly validated and standardized test method.
Kummer
Oliver
O
Division de pharmacologie et toxicologie cliniques, Hôpital régional de Thoune, 3600 Thoune. oliver.kummer@spitalstsag.ch
Roffi
Marco
M
Marti
Grischa
G
Mach
François
F
D001279:Atracurium / Q000493:pharmacokinetics / Q000627:therapeutic use; D002318:Cardiovascular Diseases / Q000097:blood / Q000188:drug therapy*; D002697:Chloral Hydrate / Q000493:pharmacokinetics / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D000077144:Clopidogrel; D006801:Humans; D006993:Hypnotics and Sedatives / Q000627:therapeutic use; D018722:Nicotinic Agonists / Q000627:therapeutic use; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000493:pharmacokinetics / Q000627:therapeutic use*; D013810:Therapeutic Equivalency; D013988:Ticlopidine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000627:therapeutic use
D006993:Hypnotics and Sedatives; D018722:Nicotinic Agonists; D010975:Platelet Aggregation Inhibitors; D001279:Atracurium; D002697:Chloral Hydrate; D000077144:Clopidogrel; D013988:Ticlopidine