Agomelatine is an agonist at melatonergic MT1 and MT2receptors, and an antagonist at 5-HT2C receptors. Agomelatine resynchronizes circadian rhythms in animal models of circadian rhythm disruption. Agomelatine increases noradrenaline and dopamine release specifically in the frontal cortex and has no influence on the extracellular levels of serotonin.

Rapidly and well absorbed (≧80%) after oral administration; but a low absolute bioavailability of less than 5% with substantial inter-individual variability. Duration: 24hr; Protein binding: 95 %; Metabolism: mainly via liver: 90%( CYP1A2), 10% (CYP2C9 & 2C19); Elimination half-life: 1~2 hr.

Hypersensitivity to the active substance or to any of the excipients; hepatic impairment. (i.e. cirrhosis or active liver disease) or transaminase levels greater than 3 times ULN; concomitant use of potent CYP1A2 inhibitors (eg, fluvoxamine, ciprofloxacin).

B1

Avoided.

Most common: nausea and dizziness. Common: other gastrointestinal disturbances, headache, somnolence, insomnia, migraine, hyperhidrosis, back pain, and fatigue. Less common: paraesthesia, blurred vision, eczema, nightmares, insomnia, anxiety, agitation, increase ALT or AST.

25 mg ORALLY at bedtime; if no response after 2 weeks, may increase to 50 mg ORALLY at bedtime for at least 6 months duration (European Medicines Agency-approved dosing).
Unlike many other antidepressants, there is no need to taper the dose of agomelatine when treatment is stopped.
Pediatric dose: safety and efficacy in pediatric patients younger than 18 years not established.
Geriatric dose: No adjustment required in patients 74 years or younger. Use is not recommended in patients 75 years or older