Review on Agomelatine: A Novel Melatonergic Antidepressant
Abstract
Agomelatine (AGM) is a novel, first melatonergic antidepressant agent. Agomelatine is a potential and well-tolerated medication for the treatment of major depressive disorder. It is also studied for its effects on sleep regulation. It is an acetamide naphthalene analogue of melatonin. It is soluble in organic solvents. AGM acts as a melatonergic receptor (MT1
/MT2) agonist and serotonergic receptor (5-HT2C) antagonist. AGM works by restoring the balance of the circadian rhythm. AGM shows a marked improvement on sleep. AGM has also proven to have anxiolytic properties and thus may prove to be very useful in the treatment of
anxiety disorders. Bioavailability is less than 5%. AGM is absorbed quickly in humans after oral administration. The mean half-life of AGM is 2.3 hours. AGM was bound to plasma proteins at 95% mainly to serum albumin (about 35%) and alpha1-acid glycoprotein (about 36%). The metabolism of AGM is almost completely hepatic. An extensive first pass hepatic effect is observed. The metabolites of AGM were excreted via urine and faeces. The recommended daily dose is one 25mg tablet taken orally at bedtime. AGM resynchronises circadian rhythms in animal models of delayed sleep phase syndrome and other circadian rhythm disruptions. It increases noradrenaline and dopamine release specifically in the frontal cortex and has no influence on the extracellular levels of serotonin. AGM is contraindicated in patients with a history of previous hypersensitivity to the active ingredient or any of the excipients; with hepatic impairment; or taking potent CYP1A2 inhibitors (e.g. fluvoxamine, ciprofloxacin). Common adverse effects include hyperhidrosis, abdominal pain, nausea, vomiting, diarrhoea, constipation, back pain, fatigue, headache, dizziness, somnolence, insomnia, migraine, anxiety.
How to cite this article: Firake BM, Siddaiah M, Pathak PV. Review on Agomelatine: A Novel Melatonergic Antidepressant. Int J Adv Res Pharm Edu 2019; 1(1): 1-8.
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