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单次口服给药后去甲丙咪嗪、氟伏沙明和吗氯贝胺的中枢镇痛作用:一项在健康志愿者中的研究。

Central analgesic effects of desipramine, fluvoxamine, and moclobemide after single oral dosing: a study in healthy volunteers.

作者信息

Coquoz D, Porchet H C, Dayer P

机构信息

Division of Clinical Pharmacology, University Hospital, Geneva, Switzerland.

出版信息

Clin Pharmacol Ther. 1993 Sep;54(3):339-44. doi: 10.1038/clpt.1993.156.

DOI:10.1038/clpt.1993.156
PMID:8375130
Abstract

The antinociceptive effect of three antidepressants with different postulated modes of action, 75 mg desipramine, 225 mg fluvoxamine, and 450 mg moclobemide, was evaluated after single oral dosing in a randomized, double-blind, placebo-controlled crossover study in 10 healthy volunteers. Experimental pain thresholds (polysynaptic R-III reflex and subjective pain rating) were monitored over 23 hours. Compared with placebo, all drugs induced significant subjective pain threshold increases (maximal increase: desipramine, +20%; fluvoxamine, +17%; moclobemide, +13%). However, only desipramine (maximal increase, +25%) and moclobemide (maximal increase, +14%) displayed a significative effect on R-III threshold. Antidepressants thus exert an antinociceptive effect after a single oral dose. The level of their action apparently relies on the postulated mode of action.

摘要

在一项针对10名健康志愿者的随机、双盲、安慰剂对照交叉研究中,单次口服给药后,评估了三种作用机制假定不同的抗抑郁药(75毫克地昔帕明、225毫克氟伏沙明和450毫克吗氯贝胺)的抗伤害感受作用。在23小时内监测实验性疼痛阈值(多突触R-III反射和主观疼痛评分)。与安慰剂相比,所有药物均使主观疼痛阈值显著升高(最大升高幅度:地昔帕明,+20%;氟伏沙明,+17%;吗氯贝胺,+13%)。然而,只有地昔帕明(最大升高幅度,+25%)和吗氯贝胺(最大升高幅度,+14%)对R-III阈值有显著影响。因此,抗抑郁药单次口服给药后具有抗伤害感受作用。其作用水平显然取决于假定的作用机制。

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