Interventional Cardiology, Morgagni-Pierantoni Hospital, Forli, Italy.
Curr Vasc Pharmacol. 2012 Jul;10(4):448-53. doi: 10.2174/157016112800812764.
The glycoprotein (GP) IIb/IIIa receptor is critical to the process of platelet aggregation and thrombus formation as it serves as the final common pathway for platelet aggregation. For this reason, the development of GP IIb/IIIa inhibitors that block fibrinogen binding to the receptor has become an attractive strategy for antiplatelet therapy with an expected strong and specific effect. Presently, there are three commercially available GP IIb/IIIa inhibitors: abciximab, eptifibatide and tirofiban. All three drugs are commonly administered intravenously, and large-scale clinical trials have demonstrated a clear clinical benefit and good safety profile in patients at high risk, especially those undergoing percutaneous coronary interventions (PCI). Recently, several studies tested the intracoronary (IC) route for GP IIb/IIIa inhibitors in order to verify its safety and its possible superiority as compared to the intravenous (IV) route. The majority of the studies testing the IC route were conducted using abciximab and in patients with STEMI with better results in terms of myocardial reperfusion and infarct size and also promising results in terms of clinical outcome. On the IC administration of eptifibatide and tirofiban only some, even if promising, data are available. Larger and randomized studies are warranted to confirm the superiority of the IC route of administration of the GP IIb/IIIa inhibitors to the IV one in patients with coronary artery disease undergoing PCI.
糖蛋白(GP)IIb/IIIa 受体在血小板聚集和血栓形成过程中至关重要,因为它是血小板聚集的最终共同途径。因此,开发能够阻断纤维蛋白原与受体结合的 GP IIb/IIIa 抑制剂已成为抗血小板治疗的一种有吸引力的策略,预计具有强大而特异的作用。目前,有三种市售的 GP IIb/IIIa 抑制剂:阿昔单抗、依替巴肽和替罗非班。这三种药物通常静脉给药,大规模临床试验表明,高危患者,特别是接受经皮冠状动脉介入治疗(PCI)的患者,具有明确的临床获益和良好的安全性。最近,一些研究测试了 GP IIb/IIIa 抑制剂的冠状动脉内(IC)途径,以验证其安全性及其与静脉内(IV)途径相比可能具有的优势。大多数测试 IC 途径的研究都使用阿昔单抗进行,在 STEMI 患者中,在心肌再灌注和梗死面积方面取得了更好的结果,在临床结局方面也取得了有希望的结果。关于依替巴肽和替罗非班的 IC 给药,只有一些数据,即使有希望,也是如此。需要更大规模的随机研究来证实在接受 PCI 的冠状动脉疾病患者中,GP IIb/IIIa 抑制剂的 IC 给药途径优于 IV 给药途径。