A Comprehensive Monograph on Clopidogrel (DB00758)

Introduction and Drug Profile

Overview and Therapeutic Significance

Clopidogrel is a cornerstone antiplatelet agent belonging to the thienopyridine class of medications. For over two decades, it has been a principal therapy for the secondary prevention of atherothrombotic events in a broad spectrum of patients with cardiovascular disease.[1] Its fundamental therapeutic action stems from its role as a prodrug that, following metabolic activation, functions as an irreversible inhibitor of the P2Y12 adenosine diphosphate (ADP) receptor located on the surface of platelets.[1] By blocking this key receptor, clopidogrel effectively prevents platelet activation and aggregation, the critical initial steps in the formation of pathological thrombi that can lead to myocardial infarction (MI) and ischemic stroke.[3]

The profound clinical impact and widespread use of clopidogrel are underscored by its inclusion on the World Health Organization's List of Essential Medicines and its consistent ranking as one of the most commonly prescribed medications globally. In 2022, it was the 47th most prescribed medication in the United States, with over 13 million prescriptions filled, attesting to its enduring role in cardiovascular medicine despite the advent of newer agents.[1]

Chemical Identity and Structural Elucidation

Systematic Identification