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Clopidogrel, owing to its excellent inhibitory property of platelet aggregation, is used to reduce the cardiovascular risks in patients with multiple co‐morbid conditions such as stroke, myocardial infarction and atherosclerosis. The current review focuses distinctly on three aspects: (a) an in‐depth coverage on the bioanalytical methods for the quantification of clopidogrel and its inactive carboxylic acid metabolite as well as the active metabolite in pre‐clinical and clinical samples; (b) an overview of the pharmacokinetic/pharmacodynamic aspects of clopidogrel; and (c) enumerating the key findings from drug–drug interaction studies of clopidogrel with various co‐substrates such as lanzoprazole, fluvastatin, atorvastatin, pravastatin, digoxin, ketoconazole, donezepil and theophylline. Copyright © 2008 John Wiley & Sons, Ltd.