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用于治疗失眠和心境障碍睡眠障碍的褪黑素能药物。

Melatonergic drugs for therapeutic use in insomnia and sleep disturbances of mood disorders.

机构信息

Sri Sathya Sai Medical Educational and Research Foundation, Prasanthi Nilayam, 40-Kovai Thirunagar, Coimbatore-641014, Tamilnadu, India.

出版信息

CNS Neurol Disord Drug Targets. 2012 Mar;11(2):180-9. doi: 10.2174/187152712800269740.

Abstract

Insomnia is common among elderly people and nearly 30 to 40% of the adult population also suffer from insomnia. Pharmacological treatment of insomnia include the use of benzodiazepine and non-benzodiazepine drugs like zolpidem, zaleplon, Zopiclone. Although these drugs improve sleep, their usage is also associated with number of adverse effects, Melatonin, the hormone secreted by the pineal gland of all animals and human beings has been used for treatment of insomnias, since the timing of its secretion in humans as well as in most of the animals coincides with the increase of nocturnal sleep propensity. Because of its short half life, melatonin slow release preparations were introduced for treatment of insomnia. Recently ramelteon, a selective MT1, MT2 receptor agonist with greater efficacy of action in treating insomnia has been used clinically and has been found effective in improving sleep quality, sleep efficacy and also in reducing the sleep onset time when compared to melatonin or slow melatonin preparations. The mechanism of action of ramelteon in improving sleep is discussed in the paper. Another melatonergic drug agomelatine besides acting on MT1/MT2 receptors also displays 5-HT2c antagonism and this drug has been found effective as a novel antidepressant for treating major depressive disorders. Agomelatine besides causing remission of depressive symptoms also improves sleep quality and efficiency. Other antidepressants depressants that are in clinical use today do not improve sleep. There are other melatonergic drugs like tasimelteon, 6-chloromelatonin. But ramelteon and agomelatine deserve special attention for treatment of insomnia and sleep disturbances associated with depressive disorders and have promising role for treatment of sleep disorders.

摘要

失眠在老年人中很常见,成年人中也有近 30%到 40%患有失眠症。失眠的药物治疗包括使用苯二氮䓬类和非苯二氮䓬类药物,如唑吡坦、扎来普隆、佐匹克隆。虽然这些药物可以改善睡眠,但它们的使用也与许多不良反应有关。褪黑素是所有动物和人类的松果腺分泌的激素,已被用于治疗失眠症,因为褪黑素在人类和大多数动物中的分泌时间与夜间睡眠倾向的增加相吻合。由于其半衰期短,褪黑素的缓释制剂被引入用于治疗失眠症。最近,雷美尔酮,一种选择性 MT1、MT2 受体激动剂,在治疗失眠症方面具有更大的疗效,已在临床上使用,并已被发现可有效改善睡眠质量、睡眠效果,并减少入睡时间,与褪黑素或慢释放褪黑素制剂相比。本文讨论了雷美尔酮改善睡眠的作用机制。另一种褪黑素能药物阿戈美拉汀,除了作用于 MT1/MT2 受体外,还显示出 5-HT2c 拮抗作用,这种药物已被发现是一种治疗重性抑郁症的新型抗抑郁药,有效。阿戈美拉汀除了引起抑郁症状的缓解外,还能改善睡眠质量和效率。目前临床使用的其他抗抑郁药都不能改善睡眠。还有其他褪黑素能药物,如他司美琼、6-氯褪黑素。但是雷美尔酮和阿戈美拉汀在治疗失眠和与抑郁障碍相关的睡眠障碍方面值得特别关注,并且在治疗睡眠障碍方面具有有前途的作用。

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