Diaz Jose F, Cardenal Rosa, Gomez-Manchero Antonio, Sanchez-Gonzalez Carlos
Interventional Cardiology Unit, Juan Ramon Jimenez University Hospital, Huelva, Spain.
Cardiovasc Hematol Agents Med Chem. 2011 Jul 1;9(3):147-53. doi: 10.2174/187152511797037475.
Tirofiban is a nonpeptide tyrosine derivative that together with eptifibatide (both small molecules) and abciximam belongs to the group of glycoprotein IIb/IIIa inhibitors. Though similar to abciximab in that it has a high affinity for the GP IIbIIIa inhibitor receptor, tirofiban dissociates from it much faster tan abciximab, what makes its action reversible in a few hours. Initially used upstream for treatment of patients with non ST-elevation acute coronary síndromes, recent evidence has shown its role as adjuntive therapy in patients with ST-elevation acute myocardial infarction treated with primary angioplasty when used at a higher dose. In this article, we performed a thorough and systematic review of randomized trials comparing tirofiban versus pacebo and tirofiban versus abciximab when used in this subset of patients. All these studies showed tirofiban to be a well tolerated and effective IIbIIIa inhibitor. When compared with placebo, tirofiban was associated with a significant reduction in mortality and myocardial infarction at one month, with a higher risk of minor bleeding in the follow-up. When compared with abciximab, tirofiban showed no difference in mortality and a tendency to higher rate of the composite of death and myocardial infarction in the short term follow-up that disappeared when only studies with high-dose tirofiban were considered. On the basis of the high-dose regimen, tirofiban may be considered useful in the management of patients with ST-elevation myocardial infarction who undergo primary angioplasty.
替罗非班是一种非肽类酪氨酸衍生物,与依替巴肽(均为小分子)和阿昔单抗同属糖蛋白IIb/IIIa抑制剂类。尽管替罗非班与阿昔单抗类似,对GP IIbIIIa抑制剂受体具有高亲和力,但它从该受体上解离的速度比阿昔单抗快得多,这使得其作用在数小时内即可逆转。替罗非班最初用于非ST段抬高急性冠脉综合征患者的上游治疗,最近有证据表明,在接受直接经皮冠状动脉腔内血管成形术(primary angioplasty)治疗的ST段抬高急性心肌梗死患者中,高剂量使用时它可作为辅助治疗。在本文中,我们对在这部分患者中使用替罗非班与安慰剂以及替罗非班与阿昔单抗进行比较的随机试验进行了全面而系统的综述。所有这些研究均表明替罗非班是一种耐受性良好且有效的IIbIIIa抑制剂。与安慰剂相比,替罗非班在1个月时可显著降低死亡率和心肌梗死发生率,但随访时轻微出血风险较高。与阿昔单抗相比,替罗非班在短期随访中的死亡率无差异,且死亡和心肌梗死综合发生率有升高趋势,但仅考虑高剂量替罗非班的研究时,该趋势消失。基于高剂量方案,替罗非班可被认为对接受直接经皮冠状动脉腔内血管成形术的ST段抬高心肌梗死患者的治疗有益。