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艾司洛尔(一种短效β受体阻滞剂)的电生理特性。

The electrophysiologic properties of esmolol, a short acting beta-blocker.

作者信息

Greenspan A M, Spielman S R, Horowitz L N, Laddu A, Senior S

机构信息

Likoff Cardiovascular Institute of Hahnemann University, Philadelphia, Pennsylvania 19102.

出版信息

Int J Clin Pharmacol Ther Toxicol. 1988 Apr;26(4):209-16.

PMID:2900217
Abstract

Although beta-blockers have established efficacy in treating ventricular ectopy and PSVT, their applicability for acute antiarrhythmic interventions in patients with organic heart disease or COPD, is frequently limited by negative inotropic or bronchospastic side effects. The development of an ultrashort acting beta-blocker with rapid reversibility of its side effects would widen their applicability. Therefore, we tested the electrophysiologic properties of such a new short acting beta-blocker, esmolol, in 14 patients (10 with organic heart disease) with a mean EF of 47.6 +/- 17%, undergoing standard clinical electrophysiologic studies for various indications. Like most other beta-blockers, esmolol's major direct effects were on sinus node function and AV nodal conduction characteristics; significantly prolonging sinus cycle length, cycle length to Wenckebach and AH interval in sinus rhythm and at a paced cycle length of 600 ms. In contrast to most other beta-blockers, following termination of its infusion, esmolol shortened parameters of sinus node function and AV nodal refractoriness, with respect to the control values, suggesting a possible rebound phenomena. These effects occurred within 5 min of terminating the intravenous drug infusion. Esmolol had no significant effect on systolic blood pressure, electrocardiographic intervals and had rare adverse reactions. We conclude that esmolol is an ultra-short acting beta-blocker, with typical direct electrophysiologic effects on sinus node and AV nodal function, and a possible rebound phenomena following its discontinuation that may make it particularly suited to acute antiarrhythmic interventions in patients susceptible to adverse beta-blocker side effects.

摘要

虽然β受体阻滞剂在治疗室性早搏和阵发性室上性心动过速方面已证实有效,但其在患有器质性心脏病或慢性阻塞性肺疾病(COPD)患者的急性抗心律失常干预中的适用性,常常受到负性肌力或支气管痉挛副作用的限制。开发一种副作用能快速逆转的超短效β受体阻滞剂将扩大其适用性。因此,我们在14例患者(10例患有器质性心脏病)中测试了这种新型短效β受体阻滞剂艾司洛尔的电生理特性,这些患者平均左室射血分数(EF)为47.6±17%,因各种适应症正在接受标准临床电生理研究。与大多数其他β受体阻滞剂一样,艾司洛尔的主要直接作用是对窦房结功能和房室结传导特性;显著延长窦性心律以及起搏周期长度为600毫秒时的窦性周期长度、文氏周期长度和AH间期。与大多数其他β受体阻滞剂不同的是,在停止输注后,相对于对照值,艾司洛尔缩短了窦房结功能参数和房室结不应期,提示可能存在反跳现象。这些效应在静脉药物输注停止后5分钟内出现。艾司洛尔对收缩压、心电图间期无显著影响,不良反应罕见。我们得出结论,艾司洛尔是一种超短效β受体阻滞剂,对窦房结和房室结功能具有典型的直接电生理作用,停药后可能出现反跳现象,这可能使其特别适用于易发生β受体阻滞剂副作用的患者的急性抗心律失常干预。

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