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Semin Vasc Med 2003; 03(4): 385-390
DOI: 10.1055/s-2004-817687
THERAPEUTICS

Copyright © 2003 by Thieme Medical Publishers, Inc., 333 Seventh Avenue, New York, NY 10001, USA. Tel.: +1(212) 584-4662

Glycoprotein IIb/IIIa Antagonists in Acute Coronary Syndromes: Where Are We Now?

Andrew Maree, Desmond J. Fitzgerald
  • Department of Clinical Pharmacology, Royal College of Surgeons in Ireland, Dublin, Ireland
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Publication History

Publication Date:
03 February 2004 (online)

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ABSTRACT

Vascular inflammation, coronary constriction, and thrombus formation are central to all acute coronary syndromes (ACSs). Adhesion and aggregation of activated platelets, initially described during thrombosis, now appear pivotal to all three processes. Several platelet adhesion receptors participate but the integrin glycoprotein (GP) IIb/IIIa occupies a critical role. GPIIb/IIIa antagonists used as an adjunct to percutaneous coronary intervention show clear benefit. However in the setting of ACS results have been disappointing. Indeed, trials of oral GPIIb/IIIa antagonists in patients with ACS were associated with increased mortality. Difficulties with drug dosing and variable pharmacodynamics may contribute to suboptimal receptor occupancy, incomplete inhibition of platelet aggregation, paradoxical partial agonist activity, and proinflammatory effects. Moreover, variable responses of patients to GPIIb/IIIa antagonists may reflect population heterogeneity.

KEYWORDS

Glycoprotein IIb/IIIa antagonist - thrombosis - inflammation - partial agonist

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