Cardiovascular Institute, Loyola University Medical Center, 2160 S. First Avenue, Maywood, IL 60153, USA.
Expert Rev Hematol. 2010 Oct;3(5):527-39. doi: 10.1586/ehm.10.53.
Argatroban is a synthetic, small-molecule direct thrombin inhibitor that is approved in the USA, the EU and Japan for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT), and for anticoagulation of HIT patients undergoing PCI. Argatroban binds reversibly to, and inhibits both soluble and clot-bound thrombin. Argatroban does not generate antibodies, is not susceptible to degradation by proteases and is cleared hepatically. It has a predictable anticoagulant effect and there is a good correlation between dose, plasma concentration and pharmacodynamic effect. Initial clinical studies suggest that further investigations to establish the use of argatroban in ischemic stroke, acute coronary syndrome, hemodialysis, blood oxygenation, off-pump cardiac surgery and other clinical indications are warranted.
阿加曲班是一种合成的小分子直接凝血酶抑制剂，已在美国、欧盟和日本获批，用于预防或治疗肝素诱导的血小板减少症（HIT）患者的血栓形成，以及用于接受经皮冠状动脉介入治疗（PCI）的 HIT 患者的抗凝治疗。阿加曲班可逆地结合并抑制可溶性和纤维蛋白结合的凝血酶。阿加曲班不会产生抗体，不易被蛋白酶降解，而是经肝脏清除。它具有可预测的抗凝作用，并且剂量、血浆浓度和药效之间具有良好的相关性。初步临床研究表明，有必要进一步研究以确定阿加曲班在缺血性脑卒中、急性冠状动脉综合征、血液透析、血氧、非体外循环心脏手术和其他临床适应证中的应用。
