National Health Service, Department of Mental Health, Psychiatric Service of Diagnosis and Treatment, "G. Mazzini" Hospital, Piazza Italia 1, 64100 Teramo, Italy.
CNS Neurol Disord Drug Targets. 2011 Feb;10(1):119-32. doi: 10.2174/187152711794488674.
Major Depressive Disorder (MDD) is an extremely disabling, chronic and recurrent disease. Moreover, subthreshold depressive symptoms often persist during periods of apparent remission. Such symptoms include sleep disturbances, sexual dysfunction, weight gain, fatigue, disinterest, anxiety, and/or emotional blunting, which do not often respond to available antidepressant treatments. Agomelatine is a melatonergic agonist (at both MT1 and MT2 receptors) and serotonin 2C (5-HT2C) receptor antagonist. Agomelatine should be particularly useful in the treatment of MDD because of its unique pharmacological profile, accounting for its effective antidepressant action with a relative lack of serious adverse effects. Several clinical trials confirmed the antidepressant efficacy of agomelatine in patients with MDD, with significant efficacy even in severe manifestations of disease and on residual subtreshold symptoms. This compound showed a relative early onset of action as well as an excellent safety and tolerability profile linked to a low discontinuation rate in MDD patients. Moreover, some data suggest that agomelatine has not only antidepressant effects but also anxiolytic effects, with a potential benefit both on anxiety symptoms associated with MDD and in the treatment of generalised anxiety disorder. This review will summarise the role of the melatonergic system in MDD and will describe the characteristics of agomelatine, focusing on its efficacy and safety in the treatment of MDD.
重性抑郁障碍（MDD）是一种极其致残、慢性和复发性疾病。此外，阈下抑郁症状在明显缓解期间经常持续存在。这些症状包括睡眠障碍、性功能障碍、体重增加、疲劳、兴趣减退、焦虑和/或情绪迟钝，这些症状通常不会对现有的抗抑郁治疗产生反应。阿戈美拉汀是一种褪黑素能激动剂（在 MT1 和 MT2 受体上）和 5-羟色胺 2C（5-HT2C）受体拮抗剂。阿戈美拉汀在治疗 MDD 方面应该特别有用，因为它具有独特的药理学特性，这解释了其有效的抗抑郁作用，同时相对较少出现严重的不良反应。几项临床试验证实了阿戈美拉汀在 MDD 患者中的抗抑郁疗效，即使在疾病的严重表现和残留阈下症状方面也具有显著疗效。这种化合物表现出相对较早的作用起效时间，以及出色的安全性和耐受性特征，与 MDD 患者的低停药率相关。此外，一些数据表明，阿戈美拉汀不仅具有抗抑郁作用，而且具有抗焦虑作用，对与 MDD 相关的焦虑症状和广泛性焦虑症的治疗都有潜在益处。这篇综述将总结褪黑素系统在 MDD 中的作用，并描述阿戈美拉汀的特征，重点介绍其在治疗 MDD 中的疗效和安全性。
