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溶栓药物的发展历程

曹苑 崔丽英

曹苑, 崔丽英. 溶栓药物的发展历程[J]. 协和医学杂志, 2020, 11(2): 121-126. doi: 10.3969/j.issn.1674-9081.20190278
引用本文: 曹苑, 崔丽英. 溶栓药物的发展历程[J]. 协和医学杂志, 2020, 11(2): 121-126. doi: 10.3969/j.issn.1674-9081.20190278
Yuan CAO, Li-ying CUI. The Development of Thrombolytic Agents[J]. Medical Journal of Peking Union Medical College Hospital, 2020, 11(2): 121-126. doi: 10.3969/j.issn.1674-9081.20190278
Citation: Yuan CAO, Li-ying CUI. The Development of Thrombolytic Agents[J]. Medical Journal of Peking Union Medical College Hospital, 2020, 11(2): 121-126. doi: 10.3969/j.issn.1674-9081.20190278

溶栓药物的发展历程

doi: 10.3969/j.issn.1674-9081.20190278
详细信息
    通讯作者:

    崔丽英 电话:010-69155682, E-mail:pumchcuily@sina.com

  • 中图分类号: R45;R-1

The Development of Thrombolytic Agents

More Information
  • 摘要: 血栓性疾病是临床上常见的一类疾病, 溶栓药物对于其急性期治疗起到了关键作用。自1933年链激酶被发现以来, 溶栓药物发展迅速。从早期不具有纤维蛋白特异性的第一代溶栓药物, 发展为目前临床上广泛应用的新一代基因重组药物, 溶栓的有效性和安全性得到了巨大提升。临床的不断探索, 使得溶栓药物在急性血栓性疾病治疗中得到越来越广泛的应用, 在降低疾病致残率、病死率中起到了决定性作用。但已有的溶栓药物仍然存在可导致严重出血、再通率有限、半衰期短、有免疫原性及价格昂贵等缺点, 未来仍需不断探索, 寻求新的突破。
    利益冲突  无
  • 图  1  溶栓药物发展历程

    t-PA:组织型纤溶酶原激活剂;rt-PA:重组组织型纤溶酶原激活剂;FDA:食品药品监督管理局;AMI:急性心肌梗死;AIS:急性缺血性卒中

    图  2  溶栓药物作用机制

    t-PA:同图 1;u-PA:尿激酶型纤溶酶原激活剂

    表  1  溶栓药物及其特点

    药物名称 适应证* 纤维蛋白选择性 PAI-1抑制性 血浆半衰期(min) 抗原性 血脑屏障破坏
    第一代            
       链激酶 AMI等血栓性疾病 6 阳性 未知
       尿激酶 AMI、急性广泛性肺栓塞、
    AIS、视网膜动脉栓塞等
    15 阴性 未知
    第二代            
       t-PA 未知 5 未知 未知
    第三代            
       rt-PA AMI、急性广泛性肺栓塞、AIS 高(++) 4~5 阴性
       替奈普酶 AMI 高(+++) 1~20 未知 未知
       瑞替普酶 AMI 高(+++) 未知 11~16 阴性 未知
    其他            
       去氨普酶 高(+++) 未知 138 阳性
       重组人尿激酶原 AMI 高(+++) 未知 114 阴性 未知
       重组葡激酶 AMI 高(+++) 未知 3 阳性 未知
    t-PA、rt-PA、AMI、AIS:同图 1;PAI-1:纤溶酶原激活剂抑制剂-1;*适应证均为国内批准
    下载: 导出CSV
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  • 收稿日期:  2019-12-12
  • 刊出日期:  2020-03-30

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