Indication
PO: 25-50 mg at bedtime.
Recommended Dose: 25 mg once daily taken orally at bedtime.
Decision of dose increase has to be balanced with a higher risk of transaminases elevation. Any dose increase to 50 mg should be made on an individual patient benefit/risk basis and with strict respect of liver function test (LFT) monitoring.
After 2 weeks of treatment, if there is no improvement of symptoms, the dose may be increased to 50 mg once daily ie, two 25-mg tab, taken together at bedtime.
Hepatic Impairment: Contraindicated in patients with hepatic impairment.
Administration
Increased or decreased bioavailabity w/ CYP1A2 (eg, fluvoxamine, ciprofloxacin), oestrogens. CYP1A2 inhibitors (eg propanolol, enoxacin). Decreased bioavailabilty w/ rifampicin, smoking. Alcohol.
Adult Dose
Suicidal thoughts & worsening of depression. Mania, dementia, lactose intolerance. May affect ability to drive or operate machinery. Pregnancy & lactation. Childn & adolescent <18 yr.
lactation: It is not known whether agomelatine is excreted into human milk.
Renal Dose
Agomelatine possesses both melatonin receptor (MT1 and MT2) agonist and 5-hydroxytryptamine receptor (5-HT2C) antagonist properties. These properties act in a complementary and perhaps synergistic manner to improve depressed states by resynchronization of circadian rhythms, enhancement of dopaminergic and adrenergic input to the frontal cortex, induction of neurogenesis, as well as through other mechanisms. Furthermore, melatonergic agonism and 5-HT2C receptor antagonism also act in harmony to favourably influence anxious symptoms, sleep and sexual function.
Mode of Action
May be taken with or without food.
Precaution
Major depressive disorder
Side Effect
Renal Impairment: No relevant modification in agomelatine pharmacokinetic parameters in patients with severe renal impairment has been observed.
Pregnancy Category Note
Dizziness, somnolence, insomnia, migraine, headache, nausea, diarrhoea, constipation, upper abdominal pain, hyperhidrosis, back pain, tiredness, anxiety, elevated liver enzymes.
Interaction
Co-administration of potent CYP1A2 inhibitors (eg fluvoxamine or ciprofloxacin). Hepatic impairment.