American heart journal
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American heart journal · Oct 1999
Review Comparative StudyPharmacokinetics and pharmacodynamics of glycoprotein IIb-IIIa inhibitors.
Antagonists of the platelet receptor glycoprotein (GP) IIb-IIIa are a novel class of antithrombotic agents that provide more comprehensive platelet blockade than the combination of aspirin and heparin. Studies in patients scheduled for percutaneous coronary intervention and those with unstable angina or non-Q-wave myocardial infarction have shown that a combination of intravenous GP IIb-IIIa inhibitors with aspirin and heparin is associated with a reduction in death or myocardial infarction compared with therapy with aspirin and heparin alone. As with other antithrombotic agents, the principal safety issue with GP IIb-IIIa inhibitors is bleeding, because the potent antiplatelet effect of these drugs may adversely affect hemostasis. ⋯ Additionally, antagonists of GP IIb-IIIa may increase the risk of thrombocytopenia. The safety profiles of various GP IIb-IIIa inhibitors are largely a function of their pharmacokinetic and pharmacodynamic properties, most notably the reversibility of platelet inhibition and the rate of plasma clearance. Knowledge of the pharmacokinetic and pharmacodynamic properties of the GP IIb-IIIa inhibitors is critical for the appropriate utilization of this new class of drugs.
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American heart journal · Oct 1999
Review Comparative StudySafety of glycoprotein IIb-IIIa inhibitors: A heart surgeon's perspective.
Platelet-mediated coronary thrombosis is the primary pathophysiologic mechanism of acute coronary syndromes (ACS) and acute ischemic complications of percutaneous coronary intervention (PCI). The final common pathway of platelet aggregation that leads to thrombotic occlusion of coronary arteries involves cross-linking of receptor glycoprotein (GP) IIb-IIIa on adjacent platelets by adhesive plasma proteins, primarily fibrinogen. Clinical trials of several GP IIb-IIIa inhibitors have demonstrated an unequivocal clinical benefit of this potent antithrombotic therapy in patients with ACS as well as in those undergoing PCI. ⋯ Therefore, among patients requiring CABG after treatment with GP IIb-IIIa inhibitors, eptifibatide and tirofiban may be associated with fewer bleeding episodes than is abciximab. With recent approval of eptifibatide for patients with ACS and those scheduled for PCI and of tirofiban for patients with ACS, the number of patients receiving GP IIb-IIIa inhibitor therapy who subsequently undergo CABG is expected to increase significantly. Strategies for improved management of bleeding complications in these patients, including the choice of a GP IIb-IIIa inhibitor, are clearly needed and are discussed in detail.