Therapeutics of platelet glycoprotein IIb/IIIa receptor antagonism.

摘要

The integrin glycoprotein IIb/IIIa receptor is the final common pathway to platelet aggregation. Administration of glycoprotein IIb/IIIa receptor antagonists reduces acute ischemic complications following plaque fissuring or rupture. Research on this subject was initially limited to patients undergoing percutaneous coronary intervention. Further studies evaluating the role of glycoprotein IIb/IIIa receptor antagonists in patients with non-ST segment elevation acute coronary syndrome have shown benefit of these drugs in reducing adverse cardiac events and death. Intravenous glycoprotein IIb/IIIa receptor inhibitors (abciximab, tirofiban, and eptifibatide) given in combination with traditional regimens are superior to placebo in management of non-ST elevation acute myocardial infarction. Oral glycoprotein IIb/IIIa receptor inhibitors (orbofiban, sibrafiban, and xemilofiban) are not effective in reducing ischemic events when used on a long-term basis after acute coronary syndrome. Pharmacokinetics, efficacy, and safety of glycoprotein IIb/IIIa receptor antagonists are elaborated.