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索他洛尔:从“只是另一种β受体阻滞剂”到“Ⅲ类抗心律失常化合物的原型”

Sotalol: from "just another beta blocker" to "the prototype of class III antidysrhythmic compound".

作者信息

Claudel J P, Touboul P

机构信息

Service de Soins Intensifs Cardiologiques (U-51), Hôpital Cardiovasculaire Louis Pradel, Lyon, France.

出版信息

Pacing Clin Electrophysiol. 1995 Mar;18(3 Pt 1):451-67. doi: 10.1111/j.1540-8159.1995.tb02545.x.

DOI:10.1111/j.1540-8159.1995.tb02545.x
PMID:7770366
Abstract

Sotalol is a beta-blocking drug devoid of membrane stabilizing properties, as well as intrinsic sympathomimetic actions, or cardioselectivity. In addition, sotalol prolongs atrial and ventricular repolarization (Class III antiarrhythmic activity). It appears to have less myocardial depressant effect than other beta-blocking agents. Given orally, bioavailability of the drug reaches 100%. Sotalol's plasma half-life is 15 hours (range 7-18) and is dependent only on renal function. In clinical practice, it has been found effective in the suppression of nearly all supraventricular and ventricular dysrhythmias except those related to prolonged ventricular repolarization. Most common adverse effects are dyspnea, bradycardia, and fatigue, which results in drug termination in 16% of the cases. Torsades de pointes usually associated with bradycardia and drug induced QTc prolongation has been reported in 1.9%-3.5% of the patients receiving sotalol. This complication may be reduced by limiting the dose (< 640 mg/day) especially in patients with impaired renal function. In addition hypokalemia must be avoided. To sum up, the combination of Class II and Class III effects may carry additional benefits. However, further studies are required to test such hypotheses.

摘要

索他洛尔是一种β受体阻滞剂,不具有膜稳定特性、内在拟交感神经活性或心脏选择性。此外,索他洛尔可延长心房和心室复极(III类抗心律失常活性)。它的心肌抑制作用似乎比其他β受体阻滞剂小。口服给药时,该药物的生物利用度可达100%。索他洛尔的血浆半衰期为15小时(范围7 - 18小时),且仅取决于肾功能。在临床实践中,已发现它对几乎所有室上性和室性心律失常均有效,但与心室复极延长相关的心律失常除外。最常见的不良反应是呼吸困难、心动过缓和疲劳,16%的病例因这些不良反应而停药。在接受索他洛尔治疗的患者中,有1.9% - 3.5%的患者报告发生了通常与心动过缓和药物诱导的QTc延长相关的尖端扭转型室性心动过速。通过限制剂量(< 640毫克/天),尤其是在肾功能受损的患者中,这种并发症可能会减少。此外,必须避免低钾血症。综上所述,II类和III类效应的联合可能具有额外的益处。然而,需要进一步的研究来验证这些假设。

相似文献

1
Sotalol: from "just another beta blocker" to "the prototype of class III antidysrhythmic compound".索他洛尔:从“只是另一种β受体阻滞剂”到“Ⅲ类抗心律失常化合物的原型”
Pacing Clin Electrophysiol. 1995 Mar;18(3 Pt 1):451-67. doi: 10.1111/j.1540-8159.1995.tb02545.x.
2
Antiarrhythmic actions of DL-sotalol in ventricular and supraventricular arrhythmias.DL-索他洛尔对室性和室上性心律失常的抗心律失常作用。
J Cardiovasc Pharmacol. 1992;20 Suppl 2:S75-90.
3
Sotalol. An updated review of its pharmacological properties and therapeutic use in cardiac arrhythmias.索他洛尔。其药理特性及在心律失常治疗应用中的最新综述。
Drugs. 1993 Oct;46(4):678-719. doi: 10.2165/00003495-199346040-00007.
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Clinical experience with sotalol in the treatment of cardiac arrhythmias.索他洛尔治疗心律失常的临床经验。
Clin Ther. 1994 May-Jun;16(3):346-64.
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Sotalol: An important new antiarrhythmic.索他洛尔:一种重要的新型抗心律失常药物。
Am Heart J. 1999 Mar;137(3):388-409. doi: 10.1016/s0002-8703(99)70484-9.
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Sotalol: a new agent for the treatment of ventricular arrhythmias.
Am J Med Sci. 1994 Jan;307(1):49-53. doi: 10.1097/00000441-199401000-00010.
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Sotalol: a breakthrough antiarrhythmic?索他洛尔:一种突破性的抗心律失常药物?
Ann Pharmacother. 1993 Nov;27(11):1359-68. doi: 10.1177/106002809302701110.
8
Sotalol.
J Cardiovasc Electrophysiol. 1993 Feb;4(1):81-98. doi: 10.1111/j.1540-8167.1993.tb01215.x.
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Concentration/response relations for the multiple antiarrhythmic actions of sotalol.索他洛尔多种抗心律失常作用的浓度/反应关系。
Am J Cardiol. 1990 Jan 2;65(2):22A-27A; discussion 35A-36A. doi: 10.1016/0002-9149(90)90197-9.
10
Pharmacodynamic, pharmacokinetic and antiarrhythmic properties of d-sotalol, the dextro-isomer of sotalol.索他洛尔的右旋异构体d-索他洛尔的药效学、药代动力学及抗心律失常特性。
Drugs. 1995 May;49(5):664-79. doi: 10.2165/00003495-199549050-00003.

引用本文的文献

1
[Bioavailability of sotalol in short bowel syndrome].[索他洛尔在短肠综合征中的生物利用度]
Med Klin (Munich). 1999 Nov 15;94(11):638-41. doi: 10.1007/BF03045005.
2
Sotalol facilitates spontaneous ventricular defibrillation by enhancing intercellular coupling. An entirely new mechanism for its antiarrhythmic action.索他洛尔通过增强细胞间偶联促进自发性心室除颤。这是其抗心律失常作用的一种全新机制。
Heart Vessels. 1995;10(4):185-9. doi: 10.1007/BF01744984.