阿加曲班药理作用和临床应用研究进展

阿加曲班为一种直接凝血酶抑制剂，通过抑制纤维蛋白形成，血小板聚集，凝血因子Ⅴ、Ⅷ和Ⅻ和蛋白C的活性，发挥其抗凝血作用，不但灭活液相凝血酶，还能够灭活与纤维蛋白血栓结合的凝血酶。阿加曲班对凝血酶具有高度亲和性，具有无抗原性、构效关系明确、半衰期短、临床使用安全等特点。可用于急性缺血性脑卒中、经皮冠状动脉介入术、慢性动脉闭塞症和肝素诱导血小板减少症等的治疗。阿加曲班还通过对凝血酶的抑制，发挥抗炎、抑制血栓形成和抑制肿瘤转移等的作用。此外，阿加曲班还有非凝血酶抑制作用，如扩张血管和改善微循环等，以及潜在的抗病毒活性。对阿加曲班的药理作用、临床应用研究进展以及临床应用需要注意的问题等方面进行综述，为阿加曲班临床更高效合理使用提供参考。

Advances in pharmacology and clinical application of argatroban

Argatroban is a direct thrombin inhibitor. It plays its anticoagulant role by inhibiting fibrin formation, platelet aggregation, the activities of coagulation factors V, VIII and XII and protein C. It can not only inactivate liquid thrombin, but also inactivate thrombin bound to fibrin thrombus. Argatroban has high affinity for thrombin, no antigenicity, clear structure-activity relationship, short half-life and safe clinical use. It can be used in the treatment of acute ischemic cerebral infarction, percutaneous coronary intervention, chronic arterial occlusion and heparin induced thrombocytopenia. Agatroban also plays the role of anti-inflammation, inhibition of thrombosis and inhibition of tumor metastasis through the inhibition of thrombin. In addition, argatroban has non thrombin inhibitory effects, such as expanding blood vessels and improving microcirculation, as well as potential antiviral activity. This paper introduces the above pharmacological effects, clinical application research progress and problems needing attention in clinical application of argatroban, so as to provide reference for more efficient and rational clinical use of argatroban.