Katayose Yasuko, Aritake Sayaka, Kitamura Shingo, Enomoto Minori, Hida Akiko, Takahashi Kiyohisa, Mishima Kazuo
Department of Psychophysiology, National Institute of Mental Health, National Center of Neurology and Psychiatry, Tokyo, Japan.
Hum Psychopharmacol. 2012 Jul;27(4):428-36. doi: 10.1002/hup.2244.
Antihistamines with strong sedative-hypnotic properties are frequently prescribed for insomnia secondary to allergy, but the potential risks of such administration have not been fully elucidated.
This randomized, double-blind, placebo-controlled crossover study was conducted to evaluate next-day sleepiness and psychomotor performance following the administration of antihistamines. Twenty-two healthy male participants participated in four drug administration sessions with more than a 1-week interval between the sessions. Either zolpidem 10 mg, or diphenhydramine 50 mg, or ketotifen 1 mg, or a placebo was administered before sleep, and polysomnography was conducted to evaluate sleep. In the morning and afternoon of the day after administration, the participants were evaluated for subjective sleepiness, objective sleepiness, and psychomotor performance.
The antihistamines with high blood-brain barrier-crossing efficiency were significantly associated with sleepiness and psychomotor performance decline the next day. Ketotifen showed the strongest carryover effect, followed by diphenhydramine. Compared with the placebo, no significant carryover effect was observed with zolpidem.
The results suggest that the risk-benefit balance should be considered in the ready use of antihistamines that easily cross the blood-brain barrier for alleviating secondary insomnia associated with allergies.
具有较强镇静催眠特性的抗组胺药常用于治疗继发于过敏的失眠，但此类用药的潜在风险尚未完全阐明。
本随机、双盲、安慰剂对照交叉研究旨在评估抗组胺药给药后的次日嗜睡情况及精神运动表现。22名健康男性参与者参加了4次给药环节，各环节之间间隔超过1周。睡前分别给予唑吡坦10毫克、苯海拉明50毫克、酮替芬1毫克或安慰剂，并进行多导睡眠图检查以评估睡眠情况。在给药后次日的上午和下午，对参与者的主观嗜睡、客观嗜睡及精神运动表现进行评估。
血脑屏障穿透效率高的抗组胺药与次日嗜睡及精神运动表现下降显著相关。酮替芬的残留效应最强，其次是苯海拉明。与安慰剂相比，唑吡坦未观察到显著的残留效应。
结果表明，在使用易于透过血脑屏障的抗组胺药缓解与过敏相关的继发性失眠时，应考虑风险效益平衡。
