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艾司洛尔:一种用于急性重症监护环境的可滴定短效静脉注射β受体阻滞剂。

Esmolol: a titratable short-acting intravenous beta blocker for acute critical care settings.

作者信息

Turlapaty P, Laddu A, Murthy V S, Singh B, Lee R

机构信息

Department of Clinical Research, Du Pont Critical Care, Waukegan, IL 60085.

出版信息

Am Heart J. 1987 Oct;114(4 Pt 1):866-85. doi: 10.1016/0002-8703(87)90797-6.

Abstract

Esmolol (Brevibloc) is an intravenous, short-acting, titratable, cardioselective beta blocker with a very rapid onset and offset of action (t1/2 = 9.2 minutes). Esmolol-induced beta blockade can be maintained as long as infusion is continued. It exhibits neither intrinsic sympathomimetic activity nor significant membrane-stabilizing activity. It is rapidly metabolized by an esterase in the erythrocyte cytosol to an inactive acid metabolite. Its hemodynamic and electrophysiologic effects are similar to those of other beta blockers. Unlike the effects of other beta blockers, however, the effects of esmolol dissipate rapidly to baseline within 30 minutes after its discontinuation. Evidence obtained from clinical studies indicates that esmolol is effective and safe in reducing the ventricular rate in patients with supraventricular tachyarrhythmias, and in reducing the heart rate in patients with acute myocardial infarction and/or unstable angina. Esmolol has also been shown to be effective and safe in attenuating the tachycardia and hypertension seen during the intraoperative period. Data from postoperative patients indicate that esmolol is ideal as sole-agent therapy for the treatment of moderate postoperative hypertension associated with a hyperdynamic state. The short duration of action and titratability of esmolol make it an ideal drug for use in patients in whom the clinical need for beta blockade is limited in duration, and it offers additional safety in patients in whom beta blockade is beneficial; however, it might be precluded because of coexisting contraindications. To date, experience with esmolol in over 1200 patients has been gathered, and the adverse effect profile is basically similar to that reported here.

摘要

艾司洛尔(Brevibloc)是一种静脉注射用的短效、可滴定的心脏选择性β受体阻滞剂,起效和失效都非常迅速(半衰期 = 9.2分钟)。只要持续输注,艾司洛尔诱导的β受体阻滞作用就能维持。它既没有内在拟交感活性,也没有显著的膜稳定活性。它在红细胞胞质溶胶中被酯酶迅速代谢为无活性的酸性代谢产物。其血流动力学和电生理效应与其他β受体阻滞剂相似。然而,与其他β受体阻滞剂的作用不同,艾司洛尔的作用在停药后30分钟内迅速消散至基线水平。临床研究获得的证据表明,艾司洛尔在降低室上性快速心律失常患者的心室率以及降低急性心肌梗死和/或不稳定型心绞痛患者的心率方面是有效且安全的。艾司洛尔在减轻术中出现的心动过速和高血压方面也已被证明是有效且安全的。术后患者的数据表明,艾司洛尔是治疗与高动力状态相关的中度术后高血压的理想单一药物疗法。艾司洛尔作用持续时间短且可滴定,使其成为临床对β受体阻滞需求持续时间有限的患者的理想用药,并且在β受体阻滞有益的患者中提供了额外的安全性;然而,由于存在共存的禁忌证可能无法使用。迄今为止,已收集了超过1200例患者使用艾司洛尔的经验,其不良反应情况与本文报道的基本相似。

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