Agomelatine, a melatonin agonist with antidepressant properties.
Agomelatine (beta-methyl-6-chloromelatonin), which is structurally homologous to melatonin, is a potent agonist of melatonin MT1 and MT2 receptors as well as an antagonist of serotonin 5-HT(2C) receptors. Agomelatine appears to improve sleep without causing daytime sedation. It has not been found to be associated with sexual side effects and discontinuation symptoms. Three placebo-controlled trials, one of them a dose finding study and two of them pivotal trials, suggest that agomelatine is an antidepressant at doses of 25 - 50 mg/day. Agomelatine appears to be well tolerated, without sexual or cardiac adverse effects, weight gain or discontinuation syndromes. Animal studies suggest a possible neuroprotective action of agomelatine, although there are more data in favor of an anxiolytic effect. Substantially more research is needed to establish its role in the treatment of mood and circadian rhythm disorders.
Dubovsky
Steven L
SL
University at Buffalo, Department of Psychiatry, 462 Grider St, Buffalo NY 14215, USA. dubovsky@buffalo.edu
Warren
Calvert
C
D000081:Acetamides / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D000928:Antidepressive Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D003865:Major Depressive Disorder / Q000188:drug therapy / Q000503:physiopathology*; D006801:Humans; D044122:Receptor, Melatonin, MT1 / Q000819:agonists; D044123:Receptor, Melatonin, MT2 / Q000819:agonists; D058830:Serotonin 5-HT2 Receptor Antagonists; D012890:Sleep / Q000187:drug effects; D009281:Naphthalenes
D000081:Acetamides; D000928:Antidepressive Agents; D044122:Receptor, Melatonin, MT1; D044123:Receptor, Melatonin, MT2; D058830:Serotonin 5-HT2 Receptor Antagonists; C084711:agomelatine; D009281:Naphthalenes