Monitoring Platelet GP IIb/IIIa Antagonist Therapy

Coller, Barry S.

doi:10.1161/01.cir.97.1.5

Cited by 75 publications

(49 citation statements)

References 43 publications

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“…Experimental and clinical studies have suggested that occupancy of at least 80% of the receptor population and inhibition of platelet aggregation to ADP (5 to 20 micromoles per liter) by at least 80% results in potent antithrombotic effects. 497 The various GP IIb/IIIa antagonists, however, possess significantly different pharmacokinetic and pharmacodynamic properties. 498 Abciximab is a Fab fragment of a humanized murine antibody that has a short plasma half-life but strong affinity for the receptor, which results in some receptor occupancy that persists in part for weeks.…”

Section: Platelet Gp Iib/iiia Receptor Antagonistsmentioning

confidence: 99%

2011 ACCF/AHA Focused Update Incorporated Into the ACC/AHA 2007 Guidelines for the Management of Patients With Unstable Angina/Non–ST-Elevation Myocardial Infarction

Anderson¹,

Adams²,

Antman³

et al. 2011

Circulation

681

367

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Section: Platelet Gp Iib/iiia Receptor Antagonistsmentioning

confidence: 99%

2011 ACCF/AHA Focused Update Incorporated Into the ACC/AHA 2007 Guidelines for the Management of Patients With Unstable Angina/Non–ST-Elevation Myocardial Infarction

Anderson¹,

Adams²,

Antman³

et al. 2011

Circulation

681

367

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“…58 Therefore, the discussion of the pharmacodynamic assessment of blood samples from patients undergoing GP IIb/IIIa antagonist therapy will focus on several key issues. The pharmacological effects of GP IIb/IIIa antagonists can be assessed in a number of different ways.…”

Section: Platelet Monitoring: Pharmacodynamic Surrogatesmentioning

confidence: 99%

“…27,36,59,60 Although the relative ease of measuring ex vivo platelet aggregation might suggest that this measurement would be appropriate for these purposes, platelet aggregation is highly variable within patient populations, is highly dependent on the skill and experience of the investigators performing the measurements, and may be affected by preparation and handling of blood samples. 58 Although most laboratories assess the extent of platelet aggregation by the maximal change in percentage of light transmission, it is also possible, and perhaps equally valid, to measure the initial slope of the aggregation response.…”

Section: Platelet Monitoring: Pharmacodynamic Surrogatesmentioning

confidence: 99%

Platelet Glycoprotein IIb-IIIa Antagonists as Prototypical Integrin Blockers: Novel Parenteral and Potential Oral Antithrombotic Agents

2000

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Abstract-During the last decade, intensive efforts have been made to evaluate the role of the platelet glycoprotein (GP) IIb/IIIa complex in platelet-mediated thrombus formation. Significant efforts have also been made to design potent antagonists of this "final common pathway" of platelet aggregation to be used as novel therapeutic strategies to treat acute coronary syndromes. Although several different GP IIb/IIIa antagonists have convincingly demonstrated the usefulness of this platelet-directed therapeutic strategy, a number of lingering unsolved and sometimes misunderstood issues concerning the pharmacology and optimal clinical usefulness of these agents remain to be explored. This article reviews these issues, which include antagonist affinity, reversibility, and receptor specificity. Other issues are related to the effects of GP IIb/IIIa receptor availability, neoepitopes induced by antagonist binding with the potential to mediate thrombocytopenia, optimal methods of platelet monitoring and, perhaps ultimately, the potential therapeutic index of the oral class of GP IIb/IIIa antagonists. All of these specific issues are likely to be illuminated in the next several years, which will greatly determine the breadth of this therapeutic class. (Circulation. 1999;100:437-444.)Key Words: platelet aggregation inhibitors Ⅲ pharmacology Ⅲ angioplasty Ⅲ angina Ⅲ thrombosis E vidence that platelets play a central role in acute coronary syndromes has accumulated over the last several decades and verifies the need for more effective, yet safe, antiplatelet agents. 1 Aspirin continues to be used routinely in coronary angioplasty and to treat patients with myocardial infarction or unstable angina. Mechanistic considerations argue that a more vigorous approach to the inhibition of platelet aggregation should afford greater antithrombotic protection. Glycoprotein (GP) IIb/IIIa (␣ IIb ␤ 3 ) serves as the receptor on platelets that binds plasma-borne adhesive proteins, such as fibrinogen and von Willebrand factor (vWF), to permit platelet aggregation. 2 Aggregation is mediated by this pathway, irrespective of the agonist that stimulates platelets and irrespective of the stimulus-response-coupling pathway that is used to activate GP IIb/IIIa to aggregate platelets. Agents that block this final common pathway by blocking the binding of adhesive proteins to GP IIb-IIIa, termed GP IIb/IIIa antagonists, are currently considered the most powerful specific inhibitors of platelet participation in acute thrombosis. 3 However, the hemostatic function of platelets is also dependent on this pathway. Thus, this novel form of antiplatelet therapy comes with potential safety risks, yet the first fruits of the benefits of this therapeutic approach have begun to emerge.Various antagonists of GP IIb/IIIa are currently receiving considerable attention from the pharmaceutical industry and clinical cardiologists, and they are being studied in a variety of clinical settings. 4 -7 The first of these agents, the monoclonal antibody abciximab, has...

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“…The platelet GP IIb/IIIa receptor antagonists act by occupying the receptors, preventing fibrinogen from binding and thereby preventing platelet aggregation. Experimental and clinical studies have suggested that occupancy of 80% or more of the receptor population and inhibition of platelet aggregation to adenosine diphosphate (5 to 20 micromoles per liter) by 80% or more results in potent anticoagulant effects (169).…”

Section: Platelet Gp Iib/iiia Receptor Antagonistsmentioning

confidence: 99%

ACC/AHA 2007 Guidelines for the Management of Patients With Unstable Angina/Non–ST-Elevation Myocardial Infarction: Executive Summary

Anderson¹,

Adams²,

Antman³

et al. 2007

Circulation

188

View full text Add to dashboard Cite

Monitoring Platelet GP IIb/IIIa Antagonist Therapy

Cited by 75 publications

References 43 publications

2011 ACCF/AHA Focused Update Incorporated Into the ACC/AHA 2007 Guidelines for the Management of Patients With Unstable Angina/Non–ST-Elevation Myocardial Infarction

2011 ACCF/AHA Focused Update Incorporated Into the ACC/AHA 2007 Guidelines for the Management of Patients With Unstable Angina/Non–ST-Elevation Myocardial Infarction

Platelet Glycoprotein IIb-IIIa Antagonists as Prototypical Integrin Blockers: Novel Parenteral and Potential Oral Antithrombotic Agents

ACC/AHA 2007 Guidelines for the Management of Patients With Unstable Angina/Non–ST-Elevation Myocardial Infarction: Executive Summary

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