Zeymer Uwe
Herzzentrum Ludwigshafen, Department of Cardiology, Medizinische Klinik B, Bremserstrasse 79, D-67063 Ludwigshafen, Germany.
Expert Opin Pharmacother. 2007 Jun;8(8):1147-54. doi: 10.1517/14656566.8.8.1147.
Glycoprotein (GP) IIb/IIIa receptor antagonists inhibit the binding of ligands to activated platelet GP IIb/IIIa receptors and, therefore, prevent the formation of platelet thrombi. They have been extensively studied in patients undergoing percutaneous coronary intervention (PCI). Eptifibatide, one of the approved GP IIb/IIIa inhibitors, is a small heptapeptide that is highly selective and rapidly dissociates from its receptor after cessation of therapy. In clinical studies, concomitant administration of eptifibatide in patients undergoing elective PCI reduced thrombotic complications in the IMPACT-II (Integrilin to Minimize Platelet Aggregation and Prevent Coronary Thrombosis II) and ESPRIT (Enhanced Suppression of the Platelet IIb/IIIa Receptor with Integrilin Therapy) trials. In the PURSUIT (Platelet Glycoprotein IIb/IIIa in Unstable Angina: Receptor Suppression Using Integrilin Therapy) trial, which included 10,948 patients with non-ST-elevation acute coronary syndromes, eptifibatide significantly reduced the primary end point of death and non-fatal myocardial infarction at 30 days compared with placebo. In patients with ST-segment elevation myocardial infarction (STEMI), eptifibatide has been studied as adjunct to primary PCI and improved epicardial flow and tissue reperfusion. Studies are now evaluating eptifibatide in high-risk patients with non-ST elevation acute coronary syndromes (NSTE-ACS) and a planned early invasive strategy in the EARLY-ACS (Eptifibatide Administration prior to Diagnostic Catherization and Revascularization to Limit Myocardial Necrosis in Acute Coronary Syndrome) trial and in patients with primary PCI for STEMI in comparison to abciximab in the EVA-AMI (Eptifibatide versus Abciximab in Primary PCI for Acute Myocardial Infarction) trial. After the completion of these trials, the value of etifibatide in patients undergoing PCI in different indications can be determined.
糖蛋白(GP)IIb/IIIa受体拮抗剂可抑制配体与活化血小板GP IIb/IIIa受体的结合,从而防止血小板血栓形成。它们已在接受经皮冠状动脉介入治疗(PCI)的患者中得到广泛研究。依替巴肽是一种已获批准的GP IIb/IIIa抑制剂,它是一种小的七肽,具有高度选择性,在治疗停止后能迅速从其受体上解离。在临床研究中,接受择期PCI的患者同时使用依替巴肽,在IMPACT-II(依替巴肽减少血小板聚集和预防冠状动脉血栓形成II)和ESPRIT(依替巴肽增强抑制血小板IIb/IIIa受体治疗)试验中降低了血栓并发症。在PURSUIT(不稳定型心绞痛中血小板糖蛋白IIb/IIIa:依替巴肽受体抑制治疗)试验中,该试验纳入了10948例非ST段抬高急性冠状动脉综合征患者,与安慰剂相比,依替巴肽在30天时显著降低了死亡和非致命性心肌梗死的主要终点。在ST段抬高型心肌梗死(STEMI)患者中,依替巴肽已作为直接PCI的辅助药物进行研究,并改善了心外膜血流和组织再灌注。目前正在EARLY-ACS(急性冠状动脉综合征诊断性导管插入术和血运重建术前给予依替巴肽以限制心肌坏死)试验中评估依替巴肽在非ST段抬高急性冠状动脉综合征(NSTE-ACS)高危患者和计划早期侵入性策略中的作用,以及在EVA-AMI(急性心肌梗死直接PCI中依替巴肽与阿昔单抗对比)试验中与阿昔单抗相比在STEMI直接PCI患者中的作用。这些试验完成后,可确定依替巴肽在不同适应症的PCI患者中的价值。