Glycoprotein IIb/IIIa Antagonists
Mortality from ischemic cardiac disease in adults has been dramatically reduced by the development of novel therapies for inhibiting platelet function. Circulating platelets are maintained in a resting state and are activated at sites of vascular injury b
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Contents 1 Introduction . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 2 GPIIb/IIIa Structure . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 3 Ligand Binding to GPIIb/IIIa . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 4 Development of Glycoprotein IIb/IIIa Inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 5 Abciximab . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 6 Small Molecule GP IIb/IIIa Antagonists . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 7 Eptifibatide . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 8 Tirofiban . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 9 Oral GP IIb/IIIa Inhibitors . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 10 Observations from Clinical Trials . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 11 Risk of Bleeding with GP IIb/IIIa Antagonists . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 12 Procedural Factors Affecting Bleeding Risk . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 13 Use of GP IIb/IIIa Antagonists with Newer Agents . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 14 Guidelines for the Use of GP IIb/IIIa Antagonists . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 15 Future Indications for GP IIb/IIIa Antagonists . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . References . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .
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Abstract Mortality from ischemic cardiac disease in adults has been dramatically reduced by the development of novel therapies for inhibiting platelet function. Circulating platelets are maintained in a resting state and are activated at sites of vascular injury by exquisitely controlled mechanisms, thereby maintaining vascular integrity without causing intravascular thrombosis. As it became clear that platelets
K.M. Hook The Carole and Ray Neag Comprehensive Cancer Center, University of Connecticut Health Center, 263 Farmi
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