纤溶药物出血机制的进展及分析  

Progresses and analysis in fibrinolytic drugs induced hemorrhage

作　　者：唐明青[1] 胡承佳 许瑞安[1] TANG Ming-qing;HU Cheng-jia;XU Rui-an(Engineering Research Center of Molecular Medicine,Ministry of Education,Xiamen 361021,China)

机构地区：[1]分子药物教育部工程研究中心,福建厦门361021

出　　处：《药学学报》2023年第6期1521-1527,共7页Acta Pharmaceutica Sinica

基　　金：福建省自然科学基金资助项目(2019J01070);厦门市自然科学基金资助项目(350Z20227197)。

摘　　要：传统的溶栓药多为纤溶酶原激活剂类药物,严重依赖于患者本身的纤溶酶原水平,溶栓效果受到限制。与之不同的是,纤溶药物具有直接纤维蛋白水解活性,能够直接溶解血栓,是一种新型的具有“直接疗效”的溶栓药物,具有更高的溶栓效率和安全性,是目前的研究热点之一。虽然能作为纤溶药物的纤溶物质不断被发现研究,但真正开发成新药、成功运用于临床的却很少,主要是其出血风险限制了发展。本文综合国内外有关纤溶药物的最新研究进展,就其出血机制及应对策略进行系统综述,总结了纤溶药物的5类出血机制,提出了3类应对策略,为研发更安全、高效的纤溶药物提供理论依据。At present,most clinical thrombolytic drugs are plasminogen activators,which are highly dependent on the plasminogen level of the patient.Therefore,the efficacy of those drugs is restricted.Unlike the conventional thrombolytic plasminogen activator drugs,fibrinolytic drugs have direct fibrinolytic activity.Thus,fibrinolytic drugs can directly dissolve the thrombus,and its thromlysis efficacy is not restricted by the patients'plasminogen.This is a new type of thrombolytic drug with higher thrombolytic efficiency and safety,and has become one of the research hotspots at present.Although more and more agents that can be used as fibrinolytic drugs have been discovered,only a few of them can successfully be applied in clinical practice.The mainly underlying reason is the risk of bleeding.In this paper,based on the latest research progress of fibrinolytic drugs,the bleeding mechanisms and coping strategies of fibrinolytic drugs were systematically reviewed,five types of bleeding mechanisms of fibrinolytic drugs were summarized,and three types of coping strategies were proposed.We hope our work can provide theoretical basis for the development of safer and more efficient fibrinolytic drugs.

关 键 词：血栓 纤溶 出血 金属蛋白酶 丝氨酸蛋白酶 

分 类 号：R966[医药卫生—药理学]