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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.

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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