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普罗帕酮与其他Ⅰc类药物的区别,重点在于其β受体阻滞作用对心室反应率的影响。

The differentiation of propafenone from other class Ic agents, focusing on the effect on ventricular response rate attributable to its beta-blocking action.

作者信息

Faber T S, Camm A J

机构信息

Department of Cardiological Sciences, St. George's Hospital Medical School, London, UK.

出版信息

Eur J Clin Pharmacol. 1996;51(3-4):199-208. doi: 10.1007/s002280050184.

Abstract

Propafenone, encainide and flecainide have been categorized as class Ic antiarrhythmic drugs, since they produce similar clinical electrophysiological effects. However, propafenone has also modes of action that differ substantially from pure class Ic activity. The most distinctive electrophysiological difference from other class Ic antiarrhythmic drugs stems from its structural similarity with other beta-adrenoceptor antagonists. The potency of the beta-adrenoceptor blocking property of propafenone has been estimated to range from 1/20 to 1/50 that of propranolol on a molar basis. Because the plasma concentrations of propafenone during long-term treatment may be up to 50 or more times that of propranolol, the beta-adrenoceptor blocking effect may be clinically relevant. However, although the beta-adrenoceptor blocking effects are readily demonstrable in vitro, clinical data are more inconsistent, because the beta-adrenoceptor blocking action has been reported as being undetectable to significant. During atrial fibrillation, with or without accessory pathways, propafenone exerts effective and prompt control of the ventricular rate in patients who fail to convert to sinus rhythm. However, compared with other class Ic antiarrhythmic drugs, propafenone has not been proved generally better in controlling the ventricular rate.

摘要

普罗帕酮、恩卡尼和氟卡尼被归类为Ic类抗心律失常药物,因为它们产生相似的临床电生理效应。然而,普罗帕酮还具有与纯Ic类活性有显著差异的作用模式。与其他Ic类抗心律失常药物最显著的电生理差异源于其与其他β-肾上腺素能受体拮抗剂的结构相似性。据估计,普罗帕酮的β-肾上腺素能受体阻断特性的效力在摩尔基础上为普萘洛尔的1/20至1/50。由于长期治疗期间普罗帕酮的血浆浓度可能高达普萘洛尔的50倍或更多,因此β-肾上腺素能受体阻断作用在临床上可能具有相关性。然而,尽管β-肾上腺素能受体阻断作用在体外很容易得到证实,但临床数据却更不一致,因为据报道β-肾上腺素能受体阻断作用从无法检测到显著存在。在房颤患者中,无论有无旁路,普罗帕酮对未能转为窦性心律的患者能有效且迅速地控制心室率。然而,与其他Ic类抗心律失常药物相比,普罗帕酮在控制心室率方面尚未被普遍证明更具优势。

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