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Esmolol 是第一个超短期作用、静脉注射的β-受体阻滞剂。动物实验证明本药有效作用大约9min;且具有高度选择性,对右心房β-受体(β_1)比支气管受体(β_2)的作用大13倍;无拟交感胺和膜抑制作用;但具有抑制左室功能的作用。临床研究证明此药半衰期为9.2min。注射后5分钟起效,停药后2min 作用明显减弱,18min 消失。Esmolol 具有典型β-受体阻滞作用,可降低窦房结和房室传导功能。血液酯酶使esmolol 迅速水解为甲醇和大部分(80~85%)无活
Esmolol is the first ultra-short-term, intravenous beta-blocker. Animal experiments show that the drug has an effective effect of about 9min; and has a high degree of selectivity, right atrial β-receptor (β_1) than the role of bronchial receptor (β_2) 13 times larger; no sympathetic amines and membrane inhibition; but with Inhibition of left ventricular function. Clinical studies have shown that the half-life of this drug 9.2min. 5 minutes after injection, 2 minutes after stopping the role of significantly weakened, 18min disappeared. Esmolol has a typical β-receptor blockade, can reduce the sinus node and atrioventricular conduction. Blood esterases rapidly hydrolyze esmolol to methanol and most of them (80-85%) have no activity