Shammas Nicolas W
Midwest Cardiovascular Research Foundation, Cardiovascular Medicine, PC, 1236 E. Rusholme, Suite 300, Davenport, IA 52803, USA.
Cardiovasc Drug Rev. 2005 Winter;23(4):345-60. doi: 10.1111/j.1527-3466.2005.tb00177.x.
Bivalirudin (Hirulog, Angiomax) is a specific, reversible and direct thrombin inhibitor with a predictable anticoagulant effect. It is cleared by both proteolytic cleavage and renal mechanisms, predominantly glomerular filtration. Bivalirudin inhibits both circulating thrombin and fibrin bound thrombin directly by binding to thrombin catalytic site and anion-binding exosite I in a concentration-dependent manner. Bivalirudin prolongs activated partial thromboplastin time, prothrombin time, thrombin time and activated clotting time (ACT). ACT levels with bivalirudin do not correlate with its clinical efficacy. Bivalirudin with a provisional GpIIb/IIIa inhibitor is indicated in elective contemporary percutaneous coronary intervention (PCI). In respect to combined ischemic and hemorrhagic endpoints of death, myocardial infarction, unplanned urgent revascularization and major bleeding during PCI (including subgroups of patients with renal impairment and diabetes) bivalirudin is not inferior to unfractioned heparin and planned GpIIb/IIIa inhibitors. In addition, bivalirudin has been consistently shown to have significantly less in-hospital major bleeding than heparin alone or heparin in combination with a GpIIb/IIIa inhibitor. Bivalirudin appears to be also safe and effective during PCI in patients with heparin-induced thrombocytopenia. Finally, data from PCI studies support the safety and efficacy of bivalirudin, although its direct randomized comparison with unfractionated heparin is lacking.
比伐卢定（希美加群，Angiomax）是一种具有可预测抗凝作用的特异性、可逆性直接凝血酶抑制剂。它通过蛋白水解裂解和肾脏机制清除，主要是肾小球滤过。比伐卢定通过以浓度依赖的方式与凝血酶催化位点和阴离子结合外位点I结合，直接抑制循环凝血酶和纤维蛋白结合的凝血酶。比伐卢定可延长活化部分凝血活酶时间、凝血酶原时间、凝血酶时间和活化凝血时间（ACT）。使用比伐卢定时的ACT水平与其临床疗效无关。比伐卢定与临时的糖蛋白IIb/IIIa抑制剂联合用于选择性现代经皮冠状动脉介入治疗（PCI）。在PCI期间的死亡、心肌梗死、计划外紧急血运重建和大出血等缺血和出血联合终点方面（包括肾功能不全和糖尿病患者亚组），比伐卢定不劣于普通肝素和计划使用的糖蛋白IIb/IIIa抑制剂。此外，与单独使用肝素或肝素与糖蛋白IIb/IIIa抑制剂联合使用相比，比伐卢定一直显示出住院期间大出血明显减少。在肝素诱导的血小板减少症患者的PCI过程中，比伐卢定似乎也是安全有效的。最后，PCI研究的数据支持比伐卢定的安全性和有效性，尽管缺乏其与普通肝素的直接随机对照比较。
