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溶栓药物药理学特征在临床实践中的重要性。

Importance of the pharmacological profile of thrombolytic agents in clinical practice.

作者信息

Alpert J S

机构信息

Division of Cardiovascular Medicine, University of Massachusetts Medical School and Center, Worcester 01655.

出版信息

Am J Cardiol. 1991 Dec 5;68(16):3E-7E. doi: 10.1016/0002-9149(91)90298-y.

Abstract

Three thrombolytic agents are frequently used in the United States for treating patients with acute myocardial infarction: streptokinase, alteplase (tissue plasminogen activator [t-PA]), and anistreplase (anisoylated plasminogen-streptokinase activator complex [APSAC]). A fourth agent, urokinase, is occasionally used but clinical experience is considerably more limited with this agent. Streptokinase, alteplase, and anistreplase differ in a number of pharmacologic properties, which include half-life, enzymatic efficiency, and induction of platelet aggregation; these differences may be clinically important. For example, anistreplase and alteplase have high affinity for fibrin and bind to intravascular thrombi after intravenous administration, which may result in higher clot specificity. Anistreplase has the longest half-life of the 3 agents and, therefore, can be administered conveniently and quickly. Alteplase has a shorter half-life and heparin is generally a necessary adjunctive agent. These differences can be clinically significant in various settings and application of such theoretical advantages is just beginning.

摘要

在美国,有三种溶栓药物常用于治疗急性心肌梗死患者:链激酶、阿替普酶(组织型纤溶酶原激活剂[t-PA])和茴香酰纤溶酶原-链激酶激活剂复合物(APSAC,即茴酰化纤溶酶原-链激酶激活剂复合物)。第四种药物尿激酶偶尔使用,但关于这种药物的临床经验要有限得多。链激酶、阿替普酶和茴香酰化纤溶酶原-链激酶激活剂复合物在许多药理学特性方面存在差异,这些特性包括半衰期、酶促效率和诱导血小板聚集;这些差异可能具有临床重要性。例如,茴香酰化纤溶酶原-链激酶激活剂复合物和阿替普酶对纤维蛋白具有高亲和力,静脉给药后可与血管内血栓结合,这可能导致更高的凝块特异性。茴香酰化纤溶酶原-链激酶激活剂复合物是这三种药物中半衰期最长的,因此可以方便快捷地给药。阿替普酶半衰期较短,肝素通常是必要的辅助药物。这些差异在各种情况下可能具有临床意义,而这种理论优势的应用才刚刚开始。

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