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溶栓药物的药理学

Pharmacology of thrombolytic drugs.

作者信息

Verstraete M, Collen D

出版信息

J Am Coll Cardiol. 1986 Dec;8(6 Suppl B):33B-40B. doi: 10.1016/s0735-1097(86)80005-5.

Abstract

Streptokinase and urokinase have proved to be useful in a limited number of clinical conditions. Mainly because of the risk and unpredictability of bleeding with this first generation of thrombolytic agents, thrombolysis has not been ingrained in medical practice. In the interim, more fibrin-specific thrombolytic agents have been developed such as acylated streptokinase-human plasminogen complex, tissue-type plasminogen activator (t-PA) and single chain urokinase-type plasminogen activator (scu-PA or pro-urokinase). Only the latter two drugs do not induce major systemic fibrinogenolysis at thrombolytic effective doses. These two agents, obtained by recombinant techniques, as well as acylated streptokinase-plasminogen complex are available for clinical investigations. The first results of systemic administration of recombinant tissue-type plasminogen activation (t-PA) in patients with acute myocardial infarction were published and are promising. Continued experimentation with t-PA and pro-urokinase in evolving myocardial infarction and other thrombotic disorders is essential to better delineate their therapeutic index.

摘要

链激酶和尿激酶已被证明在有限的临床情况下有用。主要由于第一代溶栓剂存在出血风险且不可预测,溶栓疗法尚未在医学实践中根深蒂固。在此期间,已开发出更多纤维蛋白特异性溶栓剂,如酰化链激酶 - 人纤溶酶原复合物、组织型纤溶酶原激活剂(t-PA)和单链尿激酶型纤溶酶原激活剂(scu-PA或尿激酶原)。只有后两种药物在溶栓有效剂量下不会引起主要的全身性纤维蛋白原溶解。这两种通过重组技术获得的药物以及酰化链激酶 - 纤溶酶原复合物可用于临床研究。重组组织型纤溶酶原激活剂(t-PA)在急性心肌梗死患者中全身给药的首批结果已发表,且前景乐观。在进展性心肌梗死和其他血栓性疾病中继续对t-PA和尿激酶原进行实验对于更好地确定其治疗指数至关重要。

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