Agomelatine
Melatonergic antidepressant (MT1/MT2 agonist, 5-HT2C antagonist) with a sleep-improving profile.
The links above are labelled third-party affiliate links. MolekulaX does not sell and does not verify product quality.
Pharmacology
Contents
WHAT IS AGOMELATINE?
Detailed overview
Agomelatine (Valdoxan) is a prescription antidepressant that works through a dual mechanism: it agonizes the melatonin MT1 and MT2 receptors and antagonizes serotonin 5-HT2C receptors. The melatonergic action resynchronizes the circadian rhythm disrupted in depression and improves sleep quality, while 5-HT2C blockade increases dopamine and noradrenaline in the frontal cortex, lifting mood. Compared with SSRIs it causes less sexual dysfunction and weight gain. Its main safety concern is elevation of liver enzymes, so periodic liver-function monitoring is mandatory. It was approved by the EMA in the EU in 2009; it was never approved by the FDA.
Mechanism
MT1/MT2 agonist + 5-HT2C antagonist
Half-life
~1-2 hours (dosed at bedtime)
Legal status
Prescription antidepressant (EMA 2009)
Receptor profile
- Melatonin MT1/MT2 receptors (agonist)Strong
- Serotonin 5-HT2C receptors (antagonist)Moderate
- Frontal cortex dopamine and noradrenaline (indirect increase)Moderate
Safety
Side effects, stop signs, contraindications
Side effects · 5
- Nausea, dizziness and headache, typically in the first weeks of treatment
- Elevated liver enzymes (transaminases): periodic liver function monitoring is mandatory
- Rare but serious liver injury (hepatitis, hepatic failure) warranting discontinuation
- Somnolence or fatigue, or in some people disturbed sleep and vivid dreams
- Anxiety, restlessness, digestive complaints (diarrhea, abdominal pain)
Contraindications · 4
- Active liver disease or transaminases above three times the upper normal limit: contraindicated
- Concomitant strong CYP1A2 inhibitors (fluvoxamine, ciprofloxacin): contraindicated due to greatly increased exposure
- Elderly patients with dementia: efficacy and safety not established
- Pregnancy and breastfeeding: insufficient human data, medical judgment required
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Efficacy and safety of agomelatine in the treatment of patients with depressive disorder: A meta-analysis
Guo YH, Zhou L, Cui ZA, Wang J
Safety and efficacy of agomelatine in children and adolescents with major depressive disorder receiving psychosocial counselling: a double-blind randomised controlled trial
Arango C, Buitelaar JK, Fegert JM, Olivier V
Efficacy and safety of agomelatine (10 or 25 mg/day) in non-depressed out-patients with generalized anxiety disorder: A 12-week, double-blind, placebo-controlled study
Stein DJ, Ahokas A, Jarema M, Avedisova AS
Agomelatine in generalized anxiety disorder: an active comparator and placebo-controlled study
Stein DJ, Ahokas A, Marquez MS, Hoschl C
The efficacy and safety of agomelatine, sertraline, and escitalopram for senile post-stroke depression
Yao XW, Li YL, Yu ZJ, Mo CY
FAQ
FAQ
Melatonergic antidepressant (MT1/MT2 agonist, 5-HT2C antagonist) with a sleep-improving profile.
Telegram
Have a question about Agomelatine?
Reach out to us on Telegram for a personalized stack. We'll be happy to help.
Personalized consultation
Want a detailed conversation tailored to your data?
Fill out the prep intake form (your goals, training and health data), and the advisor prepares from it to give genuinely personalized guidance.
Fill out the form~5–7 min · prep questionnaire · confidential · GDPR-compliant
Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.