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正常受试者对吸入沙丁胺醇的β-肾上腺素能受体反应。

Beta-adrenoceptor responses to inhaled salbutamol in normal subjects.

作者信息

Lipworth B J, McDevitt D G

机构信息

Department of Clinical Pharmacology, Ninewells Hospital and Medical School, Dundee, UK.

出版信息

Eur J Clin Pharmacol. 1989;36(3):239-45. doi: 10.1007/BF00558154.

Abstract

The aim of the present study was to quantify and compare the airways and systemic beta-adrenoceptor responses to inhaled salbutamol in normal subjects. Seven non-atopic, normal subjects were given cumulative doubling doses of inhaled salbutamol (100 micrograms to 4000 micrograms) or placebo in a single-blind cross-over design. Airways (sGaw, FEF 50%, FEF 25%), tremor, haemodynamic and metabolic responses were measured at each dose increment. There were dose-related changes in sGaw, FEF 50% and FEF 25% up to a plateau at 1.0 mg. Analysis of individual responses showed that most subjects required either 1.0 or 2.0 mg for maximum bronchodilatation, independent of the parameter of airflow. There was no correlation between maximum bronchodilatation, independent of the parameter of airflow. There was no correlation between maximum response and baseline airway calibre. In contrast to airways effects, systemic beta-adrenoceptor responses did not occur until 500 micrograms, and a ceiling in the dose-response curve was not reached. There were significant correlations between airways, tremor and haemodynamic responses, and between different metabolic variables. The intraindividual variability was greatest for tremor and sGaw, although this was small in comparison to the size of maximum change with salbutamol. The converse applied to the hypomagnesaemic response.

摘要

本研究的目的是对正常受试者气道和全身β-肾上腺素能受体对吸入沙丁胺醇的反应进行量化和比较。采用单盲交叉设计,对7名非特应性正常受试者给予累积加倍剂量的吸入沙丁胺醇(100微克至4000微克)或安慰剂。在每次剂量增加时测量气道(比气道传导率、50%用力呼气流量、25%用力呼气流量)、震颤、血流动力学和代谢反应。比气道传导率、50%用力呼气流量和25%用力呼气流量在剂量增加至1.0毫克时达到平台期,呈剂量相关变化。个体反应分析表明,大多数受试者无论气流参数如何,达到最大支气管扩张所需剂量为1.0毫克或2.0毫克。最大支气管扩张与气流参数无关;最大反应与基线气道口径之间无相关性。与气道效应相反,全身β-肾上腺素能受体反应直到500微克时才出现,且未达到剂量反应曲线的平台期。气道、震颤和血流动力学反应之间,以及不同代谢变量之间存在显著相关性。震颤和比气道传导率的个体内变异性最大,不过与沙丁胺醇引起的最大变化幅度相比,这种变异性较小。低镁血症反应情况相反。

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