阿加曲班的研究进展阿加曲班的研究进展.pdf

• 12 • 现代药物与临床 Drugs Clinic 第 28 卷 增刊 2013 年 4 月 阿加曲班的研究进展 1 2 1 1 1 1 肖桂芝 ，胡雅萍 ，邰 文 ，田 红 ，赵丽嘉 ，陈常青 1. 天津药物研究院 医药信息中心，天津 300193 2. 天津药物研究院药业有限责任公司，天津 300193 摘 要：凝血酶是一种关键酶，在正常血液凝固和病理血液凝块过程中发挥重要作用，因此凝血酶成为一个重要的靶点。阿 加曲班是一种有效的、可逆的直接凝血酶抑制剂（DTI ）。在日本作为抗凝血剂应用于临床已有20 多年，包括急性脑血栓， 抗凝血酶缺乏者的血液透析和肝素诱导的血小板减少症（HIT ）等。此外，阿加曲班已获得美国，加拿大和一些欧洲国家的 批准上市，用于成年人 II 型肝素诱导的血小板减少症（HIT II 型）的抗血栓治疗。在欧盟，阿加曲班也被批准用于 HIT 患 者经皮冠状动脉介入治疗。介绍阿加曲班的详细信息，包括作用机制、合成路线、药效学、药代学、药物相互作用和临床研 究等。 关键词：阿加曲班；急性缺血性脑卒中；血液净化；肝素诱导的血小板减少症；凝血酶抑制剂 Progress of argatroban 1 2 1 1 1 1 XIAO Gui-zhi , HU Ya-ping , TAI Wen , TIAN Hong , ZHAO Li-jia , CHEN Chang-qing 1. Center of Information, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China 2. TIPR Pharmacutical Responsible Co., Ltd., Tianjin 300193, China Abstract ：Thrombin is a key enzyme in the generation of a hypercoagulable state and pathologic blood clot formation. The regulation of thrombin activity is, therefore, an important therapeutic target. Argatroban is a potent, reversible direct thrombin inhibitor (DTI) that has been used clinically as an anticoagulant for over 20 years in various thrombotic conditions in Japan, including acute cerebral thrombosis, hemodialysis in antithrombin (AT) deficiency and heparin-induced thrombocytopenia (HIT). Additionally ，it has been approved and launched in the US, Canada and certain European countries as an anticoagulant for use in adult patients with heparin-induced thrombocytopenia type II (HIT type II) who require parenteral anti-thrombotic therapy. It is also approved in the EU for the treatment of HIT in patients undergoing percutaneous coronary intervention. This paper reviews detailed information of argatroban, which includes the m