Platelet glycoprotein IIb/IIIa inhibitors

Platelet glycoprotein IIb/IIIa inhibitors

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Platelet glycoprotein IIb/IIIa inhibitors (abciximab, eptifibatide, tirofiban) bind to the glycoprotein IIb/IIIa receptor on the surface of platelets and prevent binding of fibrinogen, von Willebrand factor, and other adhesive molecules to the receptor sites, thereby blocking platelet aggregation. They are used as an adjunct to heparin and aspirin therapy in patients undergoing percutaneous transluminal coronary procedures, including angioplasty and stenting (abciximab and eptifibatide). Eptifibatide and tirofiban are used in unstable angina and non–Q wave myocardial infarction in high-risk patients. Abciximab is used in unstable angina where percutaneous coronary intervention is planned.

Adverse effects and precautions: Bleeding and thrombocytopenia are common adverse effects. Platelet count should be monitored. These drugs should not be given to anyone who is actively bleeding, or to patients at increased risk of bleeding, including those with bleeding disorders, cerebrovascular disorders, uncontrolled hypertension or those who have recently undergone major surgery. Human antichimeric antibodies can develop to abciximab 2 to 4 weeks after administration, and hypersensitivity can develop with readministration; therefore repeat administration is not recommended. Abciximab is not recommended in people with severe renal or hepatic impairment. Eptifibatide is contraindicated in severe renal impairment, and dose reduction may be required in patients with mild to moderate renal impairment. Tirofiban also requires dose modification in renal impairment, and the dose should be halved when creatinine clearance is less than 30 mL/minute.