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索他洛尔的D-和L-异构体对正常心肌的血流动力学影响。

Hemodynamic effects of the D- and L-isomers of sotalol on normal myocardium.

作者信息

Hoffmeister H M, Beyer M, Seipel L

机构信息

Medizinische Klinik, Abt. III, Universität Tübingen, Germany.

出版信息

Cardiovasc Drugs Ther. 1991 Dec;5(6):1027-33. doi: 10.1007/BF00143531.

Abstract

This study investigated the hemodynamic effects of the D-isomer of sotalol in open-chest rats and compared this to the action of the L-isomer and the racemic DL-sotalol. Hemodynamic and additional isovolumic maximum measurements were registered at the end and 5 minutes after an intravenous infusion period of 7 minutes. DL- (1 and 2 mg/kg) and L-sotalol (2 mg/kg) caused a significant reduction in the heart rate and in the indices of contractility during and after infusion. D-sotalol (2, 4, and 8 mg/kg), however, decreased the contractility only transiently after very high doses at high plasma concentrations. Thus, while the effects of the beta-blocking L-isomer were comparable to those of DL-sotalol, only a slight and transient hemodynamic action of comparable doses of D-sotalol was found. These findings may be of significance for the proposed use of the D-isomer as a class-III antiarrhythmic agent.

摘要

本研究调查了索他洛尔D-异构体对开胸大鼠的血流动力学影响,并将其与L-异构体和消旋DL-索他洛尔的作用进行比较。在7分钟静脉输注期结束时和结束后5分钟记录血流动力学及额外的等容最大值测量数据。DL-(1和2mg/kg)和L-索他洛尔(2mg/kg)在输注期间及之后导致心率和收缩性指标显著降低。然而,D-索他洛尔(2、4和8mg/kg)仅在高血浆浓度下的非常高剂量后使收缩性短暂降低。因此,虽然β受体阻滞L-异构体的作用与DL-索他洛尔相当,但发现相当剂量的D-索他洛尔仅有轻微且短暂的血流动力学作用。这些发现对于将D-异构体用作III类抗心律失常药物的提议用途可能具有重要意义。

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