Savino Rosa, Polito Anna Nunzia, Marsala Gabriella, Ventriglio Antonio, Di Salvatore Melanie, De Stefano Maria Ida, Valenzano Anna, Marinaccio Luigi, Bellomo Antonello, Cibelli Giuseppe, Monda Marcellino, Monda Vincenzo, Messina Antonietta, Polito Rita, Carotenuto Marco, Messina Giovanni
Department of Woman and Child, Neuropsychiatry for Child and Adolescent Unit, General Hospital "Riuniti" of Foggia, 71122 Foggia, Italy.
Drug's Department ASP Catania, 95100 Catania, Italy.
Brain Sci. 2023 Apr 27;13(5):734. doi: 10.3390/brainsci13050734.
Agomelatine (AGM) is one of the latest atypical antidepressants, prescribed exclusively for the treatment of depression in adults. AGM belongs to the pharmaceutical class of melatonin agonist and selective serotonin antagonist ("MASS"), as it acts both as a selective agonist of melatonin receptors MT1 and MT2, and as a selective antagonist of 5-HT2C/5-HT2B receptors. AGM is involved in the resynchronization of interrupted circadian rhythms, with beneficial effects on sleep patterns, while antagonism on serotonin receptors increases the availability of norepinephrine and dopamine in the prefrontal cortex, with an antidepressant and nootropic effect. The use of AGM in the pediatric population is limited by the scarcity of data. In addition, few studies and case reports have been published on the use of AGM in patients with attention deficit and hyperactivity disorder (ADHD) and autism spectrum disorder (ASD). Considering this evidence, the purpose of this review is to report the potential role of AGM in neurological developmental disorders. AGM would increase the expression of the cytoskeleton-associated protein (ARC) in the prefrontal cortex, with optimization of learning, long-term memory consolidation, and improved survival of neurons. Another important feature of AGM is the ability to modulate glutamatergic neurotransmission in regions associated with mood and cognition. With its synergistic activity a melatoninergic agonist and an antagonist of 5-HT2C, AGM acts as an antidepressant, psychostimulant, and promoter of neuronal plasticity, regulating cognitive symptoms, resynchronizing circadian rhythms in patients with autism, ADHD, anxiety, and depression. Given its good tolerability and good compliance, it could potentially be administered to adolescents and children.
阿戈美拉汀（AGM）是最新的非典型抗抑郁药之一，仅用于治疗成人抑郁症。AGM属于褪黑素激动剂和选择性5-羟色胺拮抗剂（“MASS”）这一药物类别，因为它既作为褪黑素受体MT1和MT2的选择性激动剂，又作为5-HT2C/5-HT2B受体的选择性拮抗剂。AGM参与中断的昼夜节律的重新同步，对睡眠模式有有益影响，而对血清素受体的拮抗作用增加了前额叶皮质中去甲肾上腺素和多巴胺的可用性，具有抗抑郁和益智作用。AGM在儿科人群中的使用受到数据稀缺的限制。此外，关于AGM在注意力缺陷多动障碍（ADHD）和自闭症谱系障碍（ASD）患者中的使用，很少有研究和病例报告发表。考虑到这些证据，本综述的目的是报告AGM在神经发育障碍中的潜在作用。AGM会增加前额叶皮质中细胞骨架相关蛋白（ARC）的表达，优化学习、长期记忆巩固，并改善神经元的存活。AGM的另一个重要特征是能够调节与情绪和认知相关区域的谷氨酸能神经传递。凭借其作为褪黑素能激动剂和5-HT2C拮抗剂的协同活性，AGM可作为抗抑郁药、精神兴奋剂和神经元可塑性的促进剂，调节认知症状，使自闭症、ADHD、焦虑症和抑郁症患者的昼夜节律重新同步。鉴于其良好的耐受性和良好的依从性，它可能潜在地用于青少年和儿童。
