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The thienopyridine derivatives (platelet adenosine diphosphate receptor antagonists), pharmacology and clinical developments
Author(s) -
Kam P. C. A.,
Nethery C. M.
Publication year - 2003
Publication title -
anaesthesia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.839
H-Index - 117
eISSN - 1365-2044
pISSN - 0003-2409
DOI - 10.1046/j.1365-2044.2003.02960.x
Subject(s) - ticlopidine , medicine , thienopyridine , clopidogrel , pharmacology , platelet , p2y12 , antiplatelet drug , prodrug , aspirin , thrombotic thrombocytopenic purpura , anesthesia
Summary The thienopyridines, ticlopidine and clopidogrel, are antiplatelet drugs. They are prodrugs and are metabolised in the liver to active metabolites that are non‐competitive antagonists of the platelet adenosine diphosphate receptor, P2Y 12 . Inhibition of platelet aggregation by these drugs is delayed until 24–48 h after administration, with maximal inhibition achieved after 3–5 days. Recovery of platelet function after drug withdrawal is slow (7–14 days). Ticlopidine and clopidogrel are effective in preventing atherothrombotic events in cardiovascular, cerebrovascular and peripheral vascular disease. Gastrointestinal side effects and skin rashes are common. However, neutropenia and thrombotic thrombocytopenic purpura are significant and sometimes fatal adverse effects of ticlopidine. Clopidogrel appears to offer several advantages over ticlopidine: a more rapid onset of action and a lower incidence of neutropenia and thrombotic thrombocytopenic purpura.A combination of clopidogrel and aspirin has become standard for antithrombotic therapy in cardiovascular disease. The anaesthetic considerations of patients taking the thienopyridine compounds are discussed.