Platelet P2Y12 receptor antagonist pharmacokinetics and pharmaco -dynamics: A foundation for distinguishing mechanisms of bleeding and anticipated risk for platelet-directed therapies

Richard C. Becker; Paul A. Gurbel

doi:10.1160/TH09-07-0491

Thrombosis and Haemostasis, Table of Contents

Thromb Haemost 2010; 103(03): 535-544
DOI: 10.1160/TH09-07-0491

Theme Issue Article

Schattauer GmbH

Platelet P2Y₁₂ receptor antagonist pharmacokinetics and pharmaco -dynamics: A foundation for distinguishing mechanisms of bleeding and anticipated risk for platelet-directed therapies

Authors

Richard C. Becker

¹Duke University School of Medicine, Durham, North Carolina, United States
Paul A. Gurbel

²Sinai Center for Thrombosis Research, Baltimore, Maryland, United States

Abstract

Summary

The platelet P2Y₁₂ receptor is involved in all aspects of arterial thrombosis, including adhesion, activation, aggregation, secretion and development of a stable aggregate on which coagulation proteins can assemble and fibrin strands can mesh. Inhibition of the P2Y₁₂ receptor has been shown convincingly to reduce cardiovascular events among patients with acute coronary syndromes (ACS) and in patients undergoing percutaneous intervention (PCI). Current studies are exploring whether there is a threshold of platelet aggregation below which only more bleeding occurs, without a concomitant reduction in clinical events. The following review considers the potential relevance of reversible and irreversible mechanisms of P2Y₁₂ inhibition to bleeding risk, posing the question, “Is it not only how much but how a platelet P2Y₁₂ receptor is inhibited that determines the attributable safety profile?”

Keywords

Platelet P2Y₁₂ receptor - clopidogrel - prasugrel - ticagrelor - cangrelor

Full Text

References

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