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吸入异丙肾上腺素与非诺特罗对正常受试者血浆环磷腺苷及心率影响的比较。

Comparison between the effects of inhaled isoprenaline and fenoterol on plasma cyclic AMP and heart rate in normal subjects.

作者信息

Fairfax A J, Rehahn M, Jones D, O'Malley B

出版信息

Br J Clin Pharmacol. 1984 Feb;17(2):165-70. doi: 10.1111/j.1365-2125.1984.tb02332.x.

Abstract

The time course of changes in plasma cyclic AMP, heart rate and bronchial tone after inhalation of fenoterol or isoprenaline from a dose-metered aerosol are reported in a group of normal subjects. After isoprenaline, plasma cyclic AMP increased rapidly reaching a peak by 10 min and returned to basal levels within 60 min. A rapid, transient rise in heart rate occurred that was maximal by 5 min and returned to a basal level by 45 min. After fenoterol, the changes in cyclic AMP and heart rate were of much longer duration. The rise in plasma cyclic AMP was slower in onset and of greater magnitude than for isoprenaline, reaching a peak by 20 min and remaining above basal level for more than 6 h. The maximum increase in heart rate after fenoterol was less than that observed with isoprenaline but an elevated rate persisted for 4 h after inhalation of fenoterol. Fenoterol is known to have a longer duration of action as a bronchodilator in comparison with isoprenaline. The prolonged rise in plasma cyclic AMP in normal subjects given inhaled fenoterol may reflect this long duration of action. The concomitant rise in heart rate, however, suggests that the duration of plasma cyclic AMP response may in part be due to the systemic effect of the fraction of inhaled fenoterol known to be absorbed via the buccal and intestinal routes.

摘要

一组正常受试者吸入定量气雾剂中的非诺特罗或异丙肾上腺素后,血浆环磷腺苷、心率和支气管张力的变化时间进程被报道。吸入异丙肾上腺素后,血浆环磷腺苷迅速升高,10分钟时达到峰值,并在60分钟内恢复到基础水平。心率迅速出现短暂上升,5分钟时达到最大值,45分钟时恢复到基础水平。吸入非诺特罗后,环磷腺苷和心率的变化持续时间长得多。血浆环磷腺苷的升高起效较慢,幅度大于异丙肾上腺素,20分钟时达到峰值,并在基础水平以上持续超过6小时。非诺特罗后心率的最大增幅小于异丙肾上腺素,但吸入非诺特罗后心率升高持续4小时。已知与异丙肾上腺素相比,非诺特罗作为支气管扩张剂的作用持续时间更长。吸入非诺特罗的正常受试者血浆环磷腺苷的持续升高可能反映了这种长作用持续时间。然而,伴随的心率上升表明,血浆环磷腺苷反应的持续时间可能部分归因于已知通过颊部和肠道途径吸收的吸入非诺特罗部分的全身效应。

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