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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。Abstract: Thrombotic diseases are common in clinical practice, and thrombolytic agents play a key role in the treatment during the acute period. Thrombolytic agents have developed rapidly since the discovery of streptokinase in 1933. The efficacy and safety of thrombolysis have been improved significantly as the agents progressed from the early generation without fibrin specificity to the current generation of gene recombinant drugs. With continuous exploration in clinical practice, thrombolytic agents that are used widely in the treatment during the acute period of thrombotic diseases are the key to reduce disability and mortality. However, current existing thrombolytic agents still have disadvantages such as severe bleeding, limited recanalization, short half-life, immunogenicity, high price, and so on. It still needs to explore new breakthroughs in the future.
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Key words:
- thrombotic diseases /
- fibrinolysis system /
- thrombolytic agents /
- plasminogen activator
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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 低 低 6 阳性 未知 尿激酶 AMI、急性广泛性肺栓塞、
AIS、视网膜动脉栓塞等低 低 15 阴性 未知 第二代 t-PA 无 中 未知 5 未知 未知 第三代 rt-PA AMI、急性广泛性肺栓塞、AIS 高(++) 低 4~5 阴性 中 替奈普酶 AMI 高(+++) 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 无 高(+++) 未知 138 阳性 低 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 
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