Agomelatine for depression: expanding the horizons?

Introduction: Agomelatine is an antidepressant with unique pharmacological actions; it is both a melatonin agonist and selective serotonin antagonist. Both actions combined are necessary for antidepressant efficacy. Effects on melatonin receptors enable resynchronisation of disrupted circadian rhythms with beneficial effects on sleep patterns.

Areas covered: The issue of use of an antidepressant for depression co-morbid with somatic disorders is covered by the authors. A review of the literature from 2000 to August 2018 was undertaken using Scopus and Web of Science with the key words: agomelatine, depression, medical illness. Depression in Parkinson’s disease, cardiovascular illness and type II diabetes is reviewed with evidence of efficacy. Bipolar depression and seasonal affective disorder may also react favourably. Agomelatine may have specific efficacy on symptoms of anhedonia.

Expert opinion: Despite approval in some major jurisdictions, the drug has failed to gain registration in the United States. A defining issue may be questions about longer term efficacy: unequivocal effectiveness in placebo-controlled relapse prevention studies has not always been demonstrated. Continuation studies suggest maintenance of clinical responsiveness. A major disadvantage of the drug is its’ potential hepatotoxicity and the need for repeated clinical laboratory tests.     

Agomelatine,a novel intriguing antidepressant option enhancing neuroplasticity: A critical review

Abstract

Objectives. The treatment of major affective disorders, commonly associated with high disability and elevated social costs may be still considered unsatisfactory. Among all antidepressant drugs, predominantly acting through monoaminergic mechanisms, agomelatine is of particular interest due to another alternative mechanism of action. Targeting melatonergic receptors, agomelatine play a crucial role in synchronizing circadian rhythms, known to be altered in depressed subjects. Methods. A critical review of the literature focusing on efficacy, safety and tolerability of agomelatine in major affective disorders was performed. Additionally, we focused on the potential of agomelatine in enhancing neuroplasticity mechanisms and promote neurogenesis. A total of 136 articles from peer-reviewed journals were identified, of which 50 were assessed for eligibility and 21 were included. Results. Agomelatine, a melatonergic analogue drug acting as MT₁/MT₂ agonist and 5-HT_2C antagonist, has been reported to be effective as antidepressant drug. Studies confirmed not only clinical efficacy but also safety and tolerability of agomelatine. Also, it enhances neuroplasticity mechanisms and adult neurogenesis in brain areas such as hippocampus and prefrontal cortex. Conclusions. Agomelatine actually represents an intriguing option in the treatment of affective disorders.     

褪黑素与抑郁症关系的研究进展

褪黑素是人脑松果体分泌的一种吲哚类激素.研究显示褪黑素对昼夜节律、睡眠、社会行为等方面有影响.抑郁症患者大多存在睡眠障碍和昼夜节律紊乱,有研究证实褪黑素可改善抑郁症患者的这些症状,提示褪黑素对抑郁症有潜在的治疗作用.现对近年来褪黑素与抑郁症和昼夜节律之间关系的研究新进展进行综述.     

阿戈美拉汀治疗重度抑郁症的临床疗效

目的 探讨新型抗抑郁药物阿戈美拉汀在治疗重度抑郁患者方面的临床疗效和安全性.方法 选取我院2013年2月～2014年2月收住院的重度抑郁症患者58例随机分为两组,研究组应用阿戈美拉汀25～50mg/d,平均剂量（46.36±4.48）mg/d,对照组选用艾司西酞普兰10～20mg/d,平均剂量（16.83±2.94）mg/d,均治疗8周.治疗前及治疗后第2,4,8周分别采用汉密尔顿抑郁量表（HAMD-17）对两组进行评估,在治疗过程中应用治疗不良反应量表（TESS）进行测量.结果 治疗2周后研究组HAMD减分为（8.36±4.07）分,对照组为（6.19±3.68）分,两组减分情况比较差异有统计学意义（q=3.38,P＜0.05）.治疗8周后阿戈美拉汀组HAMD减分为（18.15±4.29）分,艾司西酞普兰组HAMD减分为（16.26±3.83）分,两组减分情况比较差异有统计学意义（q=4.12,P＜ 0.05）.药物安全性方面,研究组主要不良反应依次是头痛（5例）、便秘（4例）和肝功能异常（3例）;对照组主要不良反应依次是头痛（9例）、恶心呕吐（6例）和血压升高（5例）.TESS总分比较,研究组（3.42±1.24）分低于对照组（4.08±1.69）分,差异有统计学意义（t=7.45,P＜0.01）.结论 阿戈美拉汀在治疗重度抑郁症方面,较艾司西酞普兰起效快,疗效明显,不良反应少.     

阿戈美拉汀的临床应用研究进展

阿戈美拉汀是一种新型的抗抑郁剂,它是神经褪黑色素受体激动剂和5-羟色胺2C受体拮抗剂,目前已经应用于临床实践,尤其适用于伴有睡眠障碍的抑郁症患者.现重点总结该药物的药理机制、临床治疗特点以及治疗的不良反应等方面,希望有利于临床医生更好地了解该药物,并且合理使用该药物.     

抗抑郁药阿戈美拉汀合成综述

抑郁症的发病率逐年增高,抗抑郁药物的开发和利用也越来越受到国外跨国企业的关注。阿戈美拉汀是2009年刚在欧盟上市的第一个褪黑激素类抗抑郁药,能有效治疗抑郁症,改善睡眠参数和保持性功能。本文介绍了抗抑郁药的种类,总结了阿戈美拉汀合成路线并简要介绍了其应用前景。     

火焰原子吸收法测定阿戈美拉汀原料中镍残留量

目的：建立阿戈美拉汀原料中镍残留量的检测方法。方法：采用火焰原子吸收分光光度法,以吡咯烷二硫代氨基甲酸铵-甲基异丁基酮体系萃取富集制备样品,在232.0 nm波长处测定吸光度,按外标法计算镍含量。结果：镍在0.05～4.00μg·ml-1浓度范围内有良好的线性关系（r=0.999 0）,平均回收率为93.3%。结论：该法简便快捷,重复性好,能准确测定阿戈美拉汀原料中镍残留量。     

阿戈美拉汀治疗首发抑郁症的临床效果

目的观察阿戈美拉汀治疗首发抑郁症的有效性及安全性。方法将76例首发抑郁症患者按照随机数字表法分为阿戈美拉汀组和氟西汀组各38例,分别以阿戈美拉汀25~50 mg/d和氟西汀20~40 mg/d治疗,两组均治疗6周。分别于治疗前及治疗第1、2、4、6周末采用汉密尔顿抑郁量表17项版(HAMD-17)评定临床疗效,于治疗6周末采用副反应量表(TESS)评定药物的安全性。结果阿戈美拉汀组有效率为86.84%,氟西汀组有效率为84.21%,两组差异无统计学意义(P0.05);在治疗第1、2周末,阿戈美拉汀组HAMD-17总评分及焦虑/躯体化、睡眠障碍因子评分均低于氟西汀组,差异均有统计学意义(P均0.05)。治疗6周末,两组TESS评分比较差异无统计学意义[(2.92±2.11)分vs.(3.42±2.13)分,P0.05]。结论阿戈美拉汀对首发抑郁症的疗效较好、安全性较高,尤其适用于伴有焦虑、失眠的抑郁症患者。