[關(guān)鍵詞]
[摘要]
阿加曲班為一種直接凝血酶抑制劑,通過(guò)抑制纖維蛋白形成,血小板聚集,凝血因子Ⅴ、Ⅷ和Ⅻ和蛋白C的活性,發(fā)揮其抗凝血作用,不但滅活液相凝血酶,還能夠滅活與纖維蛋白血栓結(jié)合的凝血酶。阿加曲班對(duì)凝血酶具有高度親和性,具有無(wú)抗原性、構(gòu)效關(guān)系明確、半衰期短、臨床使用安全等特點(diǎn)??捎糜诩毙匀毖阅X卒中、經(jīng)皮冠狀動(dòng)脈介入術(shù)、慢性動(dòng)脈閉塞癥和肝素誘導(dǎo)血小板減少癥等的治療。阿加曲班還通過(guò)對(duì)凝血酶的抑制,發(fā)揮抗炎、抑制血栓形成和抑制腫瘤轉(zhuǎn)移等的作用。此外,阿加曲班還有非凝血酶抑制作用,如擴(kuò)張血管和改善微循環(huán)等,以及潛在的抗病毒活性。對(duì)阿加曲班的藥理作用、臨床應(yīng)用研究進(jìn)展以及臨床應(yīng)用需要注意的問題等方面進(jìn)行綜述,為阿加曲班臨床更高效合理使用提供參考。
[Key word]
[Abstract]
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.
[中圖分類號(hào)]
R971
[基金項(xiàng)目]