Cheng Judy W M
Long Island University, Mount Sinai Medical Center, Box 1211, One Gustave L. Levy Place, New York, NY 10029-6574, USA.
Am J Health Syst Pharm. 2002 Nov 1;59(21 Suppl 7):S5-14. doi: 10.1093/ajhp/59.suppl_7.S5.
The clinical efficacy of glycoprotein (GP) IIb/IIIa-receptor inhibitors is discussed. Over the past 10 years, GP IIb/IIIa-receptor inhibitors have become the standard of care for patients undergoing percutaneous coronary intervention (PCI). Abciximab, a monoclonal antibody fragment inhibitor of GP IIb/IIIa receptors, has been found to significantly reduce the frequency of death or myocardial infarction in patients undergoing PCI in several large trials. Board use of abciximab for this indication was precluded by the high cost of this agent. Significant benefits of the small-molecule GP IIb/IIIa-receptor inhibitor epitifibatide in patients undergoing PCI led to substantially greater use of GP IIb/IIIa-receptor inhibitors in these patients because of the considerably lower cost of this agent. Positive results of trials of abciximab and eptifibatide in patients receiving PCI can be attributed to the fact that the dosage regimens of these agents in large trials consistently inhibited > 80% of platelet aggregation, particularly during the critical periprocedural period. In contrast, the nonpeptide GP IIb/IIIa-receptor inhibitor tirofiban yielded negative results in two large trials, probably because of < 80% inhibition of platelet aggregation with the dosage regimen used, especially during the first hour of therapy when PCI is performed. Large clinical trials strongly support the use of abciximab or eptifibatide, but not tirofiban, in patients undergoing PCI.
本文讨论了糖蛋白(GP)IIb/IIIa受体抑制剂的临床疗效。在过去10年中,GP IIb/IIIa受体抑制剂已成为接受经皮冠状动脉介入治疗(PCI)患者的治疗标准。阿昔单抗是一种GP IIb/IIIa受体的单克隆抗体片段抑制剂,在多项大型试验中已发现其能显著降低接受PCI患者的死亡或心肌梗死发生率。但由于该药物成本高昂,限制了其在该适应症上的广泛应用。小分子GP IIb/IIIa受体抑制剂依替巴肽在接受PCI的患者中显示出显著益处,因其成本低得多,使得GP IIb/IIIa受体抑制剂在这些患者中的使用大幅增加。阿昔单抗和依替巴肽在接受PCI患者中的试验阳性结果可归因于在大型试验中这些药物的给药方案始终能抑制>80%的血小板聚集,尤其是在关键的围手术期。相比之下,非肽类GP IIb/IIIa受体抑制剂替罗非班在两项大型试验中得出阴性结果,可能是因为所用给药方案对血小板聚集的抑制<80%,尤其是在进行PCI治疗的第一个小时内。大型临床试验强烈支持在接受PCI的患者中使用阿昔单抗或依替巴肽,而非替罗非班。