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索他洛尔对人心脏单相动作电位的延长作用。

Prolongation of the human cardiac monophasic action potential by sotalol.

作者信息

Echt D S, Berte L E, Clusin W T, Samuelsson R G, Harrison D C, Mason J W

出版信息

Am J Cardiol. 1982 Nov;50(5):1082-6. doi: 10.1016/0002-9149(82)90421-0.

Abstract

Sotalol and propranolol are nonselective beta-adrenergic blocking agents. Sotalol at low concentration, unlike propranolol, prolongs the duration of the transmembrane action potential. In a double-blind study, the electrophysiologic effects of intravenous sotalol (0.30 or 0.60 mg/kg; n = 9) were compared with intravenous propranolol (0.15 or 0.20 mg/kg; n = 8) in 17 patients with use of bipolar suction electrodes in the right atrium and right ventricle to determine whether sotalol prolongs the monophasic action potential duration in man. After administration of sotalol, there were significant increases (paired t test) in the Q-T interval (p less than 0.001), right atrial effective refractory period (p less than 0.05), right ventricular effective refractory period (p less than 0.005), right atrial monophasic action potential duration at 90% repolarization (p less than 0.01), and right ventricular monophasic action potential duration at 90% repolarization (p less than 0.005). Prolongation of the monophasic action potential duration was dependent on plasma sotalol concentration. There were no significant changes in these variables after propranolol. The spontaneous cycle length and Wenckebach cycle length increased significantly in both groups, and the mean blood pressure decreased in both, although not significantly after propranolol. In summary, sotalol but not propranolol prolonged atrial and ventricular effective refractory periods and lengthened the monophasic action potential and the Q-T interval of human myocardium after intravenous infusion. The ability to acutely prolong repolarization at therapeutic plasma concentration is unique among known competitive beta-adrenergic receptor antagonists.

摘要

索他洛尔和普萘洛尔是非选择性β肾上腺素能阻滞剂。与普萘洛尔不同,低浓度的索他洛尔可延长跨膜动作电位的持续时间。在一项双盲研究中,对17例患者静脉注射索他洛尔(0.30或0.60mg/kg;n = 9)和静脉注射普萘洛尔(0.15或0.20mg/kg;n = 8)的电生理效应进行了比较,使用双极吸引电极置于右心房和右心室,以确定索他洛尔是否能延长人体单相动作电位的持续时间。静脉注射索他洛尔后,Q-T间期(p<0.001)、右心房有效不应期(p<0.05)、右心室有效不应期(p<0.005)、90%复极化时右心房单相动作电位持续时间(p<0.01)以及90%复极化时右心室单相动作电位持续时间(p<0.005)均有显著增加(配对t检验)。单相动作电位持续时间的延长取决于血浆索他洛尔浓度。注射普萘洛尔后这些变量无显著变化。两组的自发周期长度和文氏周期长度均显著增加,两组的平均血压均下降,不过注射普萘洛尔后下降不显著。总之,静脉输注后,索他洛尔而非普萘洛尔可延长心房和心室有效不应期,延长人体心肌的单相动作电位和Q-T间期。在已知的竞争性β肾上腺素能受体拮抗剂中,索他洛尔在治疗血浆浓度下急性延长复极化的能力是独一无二的。

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