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酰化纤溶酶原-链激酶激活剂复合物:溶栓治疗的新方法。

Acylated plasminogen-streptokinase activator complex: a new approach to thrombolytic therapy.

作者信息

Crabbe S J, Grimm A M, Hopkins L E

机构信息

Department of Pharmacy, Thomas Jefferson University Hospital, Philadelphia, Pennsylvania 19107.

出版信息

Pharmacotherapy. 1990;10(2):115-26.

PMID:2140889
Abstract

Acylated plasminogen-streptokinase activator complex (APSAC; antistreplase) is an inactive complex of human plasminogen and streptokinase. When it is injected, a controlled deacylation of the catalytic center occurs, activating the complex so that thrombolysis may begin. This process extends the half-life of streptokinase, allowing for 4-6 hours of fibrinolytic activity. Anistreplase has demonstrated equivalent efficacy to intracoronary streptokinase with regard to reperfusion rates in acute myocardial infarction. In addition, patients have shown a 56% reduction in mortality at 28 days with anistreplase compared to heparin. The adverse effect profile of anistreplase includes minor bleeding and hematoma formation at the site of venipuncture, hypotensive and bradycardic episodes, arrhythmias, facial flushing, fever, and rarely, allergic reactions. Serious bleeding reactions are uncommon, with the frequency of cerebrovascular accident reported at 0.4-0.6%. The special advantage of anistreplase is its administration as a 30-U intravenous bolus injected over 5 minutes, eliminating the need for long infusions and increasing the ease of administration. Based on its efficacy and ease of administration, anistreplase may become the drug of choice in the emergency treatment of acute myocardial infarction.

摘要

酰化纤溶酶原-链激酶激活剂复合物(APSAC;抗链激酶)是一种人纤溶酶原与链激酶的无活性复合物。注射后,催化中心会发生可控的脱酰基作用,激活该复合物,从而启动溶栓过程。这一过程延长了链激酶的半衰期,使其具有4至6小时的纤溶活性。在急性心肌梗死的再灌注率方面,抗链激酶已证明与冠状动脉内注射链激酶具有等效疗效。此外,与肝素相比,使用抗链激酶的患者在28天时死亡率降低了56%。抗链激酶的不良反应包括穿刺部位轻微出血和血肿形成、低血压和心动过缓发作、心律失常、面部潮红、发热,以及罕见的过敏反应。严重出血反应并不常见,脑血管意外的发生率报告为0.4%至0.6%。抗链激酶的特殊优势在于它可以在5分钟内静脉推注30单位,无需长时间输注,给药更方便。基于其疗效和给药便利性,抗链激酶可能会成为急性心肌梗死急诊治疗的首选药物。

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