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单剂量(+)-索他洛尔对轻度稳定型哮喘患者的不良反应。

Adverse effects of a single dose of (+)-sotalol in patients with mild stable asthma.

作者信息

Devereux G, Fishwick K, Aiken T C, Bourke S J, Hendrick D J

机构信息

Department of Respiratory Medicine, Royal Victoria Infirmary, University of Newcastle upon Tyne.

出版信息

Br J Clin Pharmacol. 1998 Jul;46(1):79-82. doi: 10.1046/j.1365-2125.1998.00039.x.

DOI:10.1046/j.1365-2125.1998.00039.x
PMID:9690953
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1873981/
Abstract

AIMS

To investigate the effect of (+)-sotalol, which is not thought to possess clinically significant beta-adrenoceptor blocking activity, on airway responsiveness in subjects with mild asthma.

METHODS

A placebo controlled, double-blind, single dose, cross over study, evaluating the effects of oral (+)-sotalol 300 mg and oral (+/-)-sotalol 240 mg, on airway responsiveness, FEV1, and heart rate in 18 asthmatic volunteers with quantifiable levels of airway responsiveness.

RESULTS

Compared with placebo, (+)-sotalol induced a significant increase in airway responsiveness, and a significant decrease in FEV1, but there was no significant change in heart rate. Following (+/-)-sotalol there was no significant effect on airway responsiveness, but there were significant decreases in FEV1 and heart rate. In one subject both (+)-sotalol and (+/-)-sotalol provoked a 49% decrement in FEV1, and in another there were decrements of 20% and 18%, respectively.

CONCLUSIONS

Despite theoretical considerations, it cannot be assumed that (+)-sotalol is safe in patients with asthma.

摘要

目的

研究(+)-索他洛尔(一种被认为不具有临床显著β-肾上腺素能受体阻断活性的药物)对轻度哮喘患者气道反应性的影响。

方法

一项安慰剂对照、双盲、单剂量、交叉研究,评估口服300毫克(+)-索他洛尔和口服240毫克(±)-索他洛尔对18名具有可量化气道反应性水平的哮喘志愿者的气道反应性、第一秒用力呼气容积(FEV1)和心率的影响。

结果

与安慰剂相比,(+)-索他洛尔可导致气道反应性显著增加,FEV1显著降低,但心率无显著变化。服用(±)-索他洛尔后,对气道反应性无显著影响,但FEV1和心率显著降低。在一名受试者中,(+)-索他洛尔和(±)-索他洛尔均使FEV1下降49%,在另一名受试者中,分别下降20%和18%。

结论

尽管从理论上考虑,但不能认为(+)-索他洛尔对哮喘患者是安全的。

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本文引用的文献

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Pharmacokinetics and pharmacodynamics of (+/-)-sotalol in healthy male volunteers.(±)-索他洛尔在健康男性志愿者体内的药代动力学和药效学
Br J Clin Pharmacol. 1996 Nov;42(5):583-8. doi: 10.1111/j.1365-2125.1996.tb00113.x.
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Measurement of airway responsiveness to methacholine: relative importance of the precision of drug delivery and the method of assessing response.气道对乙酰甲胆碱反应性的测量:药物递送精度和反应评估方法的相对重要性。
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d-sotalol reduces heart rate in vivo through a beta-adrenergic receptor-independent mechanism.d-索他洛尔通过一种不依赖β-肾上腺素能受体的机制在体内降低心率。
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Pharmacologic basis of the antiarrhythmic and hemodynamic effects of sotalol.索他洛尔抗心律失常及血流动力学效应的药理学基础。
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Airway responsiveness to histamine and methacholine: relationship to minimum treatment to control symptoms of asthma.气道对组胺和乙酰甲胆碱的反应性:与控制哮喘症状的最低治疗的关系。
Thorax. 1981 Aug;36(8):575-9. doi: 10.1136/thx.36.8.575.
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Bronchial response to beta-adrenergic blockade.支气管对β-肾上腺素能阻滞剂的反应。
N Engl J Med. 1966 Sep 15;275(11):580-4. doi: 10.1056/NEJM196609152751103.
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Inotropic and chronotropic effects of a series of beta-adrenergic blocking drugs: some structure-activity relationships.一系列β-肾上腺素能阻断药物的变力性和变时性效应:一些构效关系
Proc Soc Exp Biol Med. 1966 Jun;122(2):373-9. doi: 10.3181/00379727-122-31138.
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Electrophysiologic effects of the levo- and dextrorotatory isomers of sotalol in isolated cardiac muscle and their in vivo pharmacokinetics.索他洛尔左旋和右旋异构体对离体心肌的电生理效应及其体内药代动力学
J Am Coll Cardiol. 1986 Jan;7(1):116-25. doi: 10.1016/s0735-1097(86)80268-6.
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The relationship between bronchial responsiveness to methacholine and bronchial responsiveness to histamine in asthmatic subjects.哮喘患者中支气管对乙酰甲胆碱的反应性与支气管对组胺的反应性之间的关系。
Pulm Pharmacol. 1988;1(1):53-8. doi: 10.1016/0952-0600(88)90011-7.
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Comparative beta-blocking activities and electrophysiologic actions of racemic sotalol and its optical isomers in anesthetized dogs.消旋索他洛尔及其光学异构体在麻醉犬体内的比较β受体阻滞活性和电生理作用。
Eur J Pharmacol. 1986 Dec 16;132(2-3):123-35. doi: 10.1016/0014-2999(86)90597-2.