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三环类抗抑郁药的外周抗胆碱能活性:阿米替林与地昔帕明在人类志愿者中的比较。

The peripheral anticholinergic activity of tricyclic antidepressants: comparison of amitriptyline and desipramine in human volunteers.

作者信息

Szabadi E, Gaszner P, Bradshaw C M

出版信息

Br J Psychiatry. 1980 Nov;137:433-9. doi: 10.1192/bjp.137.5.433.

Abstract

The effects of three single oral doses (25 mg, 50 mg and 100 mg) of amitriptyline and desipramine, and of placebo, were compared on a range of cholinergic functions (resting pupil diameter, pilocarpine-evoked miosis, baseline-sweating, carbachol-evoked sweating, salivation, heart rate) in eight healthy volunteers. Three measures (pilocarpine-evoked miosis, carbachol-evoked sweating and salivation) reflected the antimuscarinic property of the antidepressants; in two tests (pilocarpine-evoked miosis and salivation) amitriptyline appeared to be more potent than desipramine. Resting pupil diameter was not affected by amitriptyline, whereas desipramine caused mydriasis, indicating that pupil size is not a reliable measure of anticholinergic activity in the case of drugs which also affect adrenergic mechanisms. Baseline-sweating and heart rate were not affected by the antidepressants.

摘要

在八名健康志愿者中,比较了三种单次口服剂量(25毫克、50毫克和100毫克)的阿米替林和地昔帕明以及安慰剂对一系列胆碱能功能(静息瞳孔直径、毛果芸香碱诱发的瞳孔缩小、基础出汗、卡巴胆碱诱发的出汗、唾液分泌、心率)的影响。三项指标(毛果芸香碱诱发的瞳孔缩小、卡巴胆碱诱发的出汗和唾液分泌)反映了抗抑郁药的抗毒蕈碱特性;在两项测试(毛果芸香碱诱发的瞳孔缩小和唾液分泌)中,阿米替林似乎比地昔帕明更有效。静息瞳孔直径不受阿米替林影响,而地昔帕明引起瞳孔散大,这表明对于同时影响肾上腺素能机制的药物,瞳孔大小不是抗胆碱能活性的可靠指标。基础出汗和心率不受抗抑郁药影响。

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