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Agomelatine

Agomelatine (Valdoxan) melatonergic antidepressant

Agomelatine (Valdoxan) is an EU-authorised prescription antidepressant for major depressive episodes in adults, not a dietary supplement or established nootropic. It acts as an MT1/MT2 agonist and 5-HT2C antagonist; sleep-pattern effects are part of depression treatment, while healthy-user memory and focus claims are unsupported. Its risk profile is high because the current EU label requires baseline and repeated liver tests, contraindicates hepatic impairment and potent CYP1A2 inhibitors such as fluvoxamine and ciprofloxacin, and reports rare serious liver injury. U.S. status differs: current Drugs@FDA and FDA-label searches returned no agomelatine result, and NDC entries were bulk ingredients rather than approved finished-drug evidence.

Sleep SupportMood SupportDopaminergicSerotonergicSyntheticClinical ResearchHigh Risk Profile
Updated July 2026/7 min read/10 citations
Prepared by the NootropicsIndex editorial team.Method: prioritize cited human research and official safety or regulatory sources; compare retailer-listed prices without endorsing products.Affiliate disclosure
01

What is it?

What Agomelatine is

2

Agomelatine is a synthetic prescription antidepressant and melatonin analogue, not a nutrient or botanical supplement. EMA lists Valdoxan for major depressive episodes in adults and as prescription-only in the European Union.

02

Names, aliases and forms

Common NameAgomelatine
Brand NamesValdoxan; Thymanax; Agoprex
Research CodeS-20098
Iupac NameN-[2-(7-methoxynaphthalen-1-yl)ethyl]acetamide
Cas Number138112-76-2
Pubchem Cid82148
Molecular FormulaC15H17NO2
Regulatory NameN06AX22
03

Mechanisms of action

Melatonin receptors plus 5-HT2C blockade

2

Agomelatine stimulates MT1 and MT2 receptors and blocks 5-HT2C receptors. EMA says this may increase dopamine and noradrenaline signalling and help normalise sleep patterns in depression; this is psychiatric-drug pharmacology, not a supplement mechanism.

04

Potential effects and evidence map

Agomelatine has regulatory and clinical evidence for major depressive episodes in adults, but the effect is condition-specific and the trial record is not uniformly positive. EMA notes mixed placebo-controlled results and says benefits may be lower than with some other antidepressants; a large 2018 network meta-analysis nevertheless found agomelatine and the other included antidepressants more efficacious than placebo, with certainty ranging from moderate to very low across comparisons. No comparable evidence establishes memory, focus, productivity, or acute mood enhancement in healthy users. Liver monitoring and prescription oversight are inseparable from the evidence-based use case.

Effect domainMagnitudeGrade
Mood / wellbeing5
CumulativeConfidence: High

Supports treatment of major depressive episodes in adults under prescription supervision; this is not evidence for casual mood enhancement.

Note Regulatory approval and meta-analysis support an antidepressant effect, while EMA describes mixed individual trials and potentially lower benefit than some alternatives.

3/5
B
Sleep quality2
CumulativeConfidence: Medium

May help normalise sleep patterns within depression treatment, but is not established as a standalone sleep supplement or insomnia self-treatment.

Note Keep the effect within the authorised depression context.

2/5
B
Focus / attention5
UnknownConfidence: Medium

No reliable human evidence establishes a focus, concentration, or productivity benefit in healthy users.

Note This explicitly corrects the unsupported claims on the legacy page.

0/5
D
05

Typical dosages and timing

Prescriber-managed tablets325 mg; possible 50 mg

The current EU label recommends 25 mg once daily at bedtime for major depressive episodes in adults. A prescriber may increase this to 50 mg after two weeks without improvement, but only after individual benefit-risk review and with the full liver-test schedule. No consumer ?typical dose? is shown on this page.

06

Timing & effect horizon

Effect horizonAcute + cumulative
AcuteCumulative
Peak3Acute
1-2 hours
Half-life3Acute
1-2 hours
Study window2Cumulative
6 weeks
Follow-up2Cumulative
24-26 weeks
Plasma timing is not effect duration3

Peak plasma concentration and mean plasma The time for blood levels to fall by half during the final elimination phase.Source are each about 1-2 hours. Those pharmacokinetic figures do not establish an acute nootropic effect, a same-night clinical onset, or a therapeutic-effect duration; depression outcomes were assessed over weeks.

07

Safety, side effects and risk profile

Liver / kidney caution3
Confidence: High

Baseline and repeated liver-function testing are required; hepatic impairment and baseline transaminases above three times normal are contraindications, and rare serious hepatic outcomes are reported.

Note The label reports ALT/AST elevations above three times normal in 1.2% at 25 mg and 2.6% at 50 mg versus 0.5% with placebo.

4/5
A
Interaction risk3
Confidence: High

Potent CYP1A2 inhibitors such as fluvoxamine and ciprofloxacin are contraindicated; moderate inhibitors, smoking, rifampicin, alcohol, and hepatotoxic medicines require clinician review.

Note Fluvoxamine increased agomelatine exposure about 60-fold in the EU label.

4/5
A
Legal / regulatory risk2
Confidence: High

Agomelatine is a prescription medicine where authorised, not a dietary supplement; approved uses, import rules, and lawful dispensing vary by jurisdiction.

Note Valdoxan is EU-authorised for adult major depression. Current U.S. approval-database searches returned no agomelatine result.

4/5
B
Headache / dizziness3
Confidence: High

Headache is very common and dizziness and nausea are common in the EU label; early adverse effects can affect tolerability and safety-sensitive activity.

Note Adverse reactions were usually mild or moderate and often occurred in the first two treatment weeks, but individual response varies.

2/5
A
Sedation / impairment3
Confidence: High

Dizziness and somnolence are common, while insomnia can also occur; caution is needed for driving and operating machinery.

Note Do not assume bedtime administration guarantees sedation or improved sleep.

2/5
A
Pregnancy / lactation caution3
Confidence: High

Human pregnancy data are limited; the EU label prefers avoidance during pregnancy and requires a treatment-versus-breastfeeding decision during lactation.

Note This is a prescriber and obstetric risk-benefit decision, not a product-listing decision.

3/5
C
Evidence uncertainty5
Confidence: High

Depression evidence does not establish memory, focus, productivity, acute mood enhancement, or healthy-user safety.

Note Powder and cross-border listings add identity, dose, monitoring, and legal uncertainty.

3/5
C
Liver monitoring is a condition of use3

The EU label requires liver tests before treatment, around weeks 3, 6, 12 and 24, after dose increases, and later when clinically indicated. Treatment should not start, or should stop, when ALT or AST exceed three times the upper limit of normal.

Why the overall risk is high3

In trials, ALT/AST elevations above three times normal occurred in 1.2% at 25 mg and 2.6% at 50 mg versus 0.5% with placebo. The label also reports hepatitis, jaundice and rare hepatic failure, with exceptional fatal or transplant cases in people with hepatic risk factors. High risk reflects severity and mandatory monitoring, not a claim that serious injury is common.

Age, mania and suicidality cautions3

The EU label says agomelatine should not be used at age 75 or older and is not recommended under 18. Prescribing also requires caution with bipolar disorder or mania and close monitoring for worsening depression, suicidal thoughts, or behavioural changes, especially early and after dose changes.

Pregnancy and breastfeeding need specialist review3

Human pregnancy data are limited, and the EU label says it is preferable to avoid Valdoxan during pregnancy. During lactation, a clinician must weigh the benefit of treatment against breastfeeding because infant risk cannot be excluded.

08

Interactions and cautions

CYP1A2 interactions are central3

Agomelatine is metabolised mainly by CYP1A2. Fluvoxamine and ciprofloxacin are contraindicated; moderate CYP1A2 inhibitors such as propranolol or enoxacin require caution, and rifampicin or heavy smoking may reduce exposure. Medication and smoking changes belong with the prescriber.

Alcohol and liver-risk stacking3

The EU label says combining agomelatine with alcohol is not advisable. Alcohol use disorder, substantial alcohol intake, obesity or fatty-liver disease, diabetes, and other potentially hepatotoxic medicines raise the need for careful benefit-risk review and surveillance.

10

Practical buying and quality notes

  • For Agomelatine, Valdoxan, Thymanax, or Agoprex listings, verify tablet strength, pack size, manufacturer, pharmacy legitimacy, batch and expiry information, and whether a valid prescription is required in your jurisdiction. Product availability is not evidence of approval or safe self-treatment.10
  • Loose powder removes the standard tablet context and adds measurement, identity, contamination, storage, prescription, and monitoring risks. It should not be treated as a supplement substitute for a prescribed finished medicine.10
11

FAQ

Is Agomelatine a nootropic?

5

Not in the supplement sense. It is a prescription antidepressant where authorised, and its depression and sleep-pattern evidence does not establish memory, focus, or productivity benefits in healthy users.

What is the Agomelatine dose?

3

The EU prescription label describes 25 mg at bedtime and a possible prescriber-managed increase to 50 mg. Because this treatment requires liver testing and individual risk assessment, those figures are label context rather than self-dosing guidance.

Does Agomelatine have an acute effect?

3

It reaches peak plasma concentration in about 1-2 hours and has a mean plasma half-life of about 1-2 hours, but a reliable single-dose cognitive or antidepressant effect duration has not been established. Clinical depression outcomes are assessed over weeks.

Why is Agomelatine rated high risk?

7

The rating reflects required liver tests, contraindications in hepatic impairment, clinically important CYP1A2 interactions, and rare serious liver injury. It does not mean most users experience severe harm; it means unsupervised use has an unacceptable monitoring gap.

12

References

  1. PubChem. Agomelatine (CID 82148). Accessed 2026-07-14.
  2. European Medicines Agency. Valdoxan EPAR overview. Accessed 2026-07-14.
  3. European Medicines Agency. Valdoxan: EPAR product information, revision 27. Updated 2025-04-15; accessed 2026-07-14.
  4. Medicines and Healthcare products Regulatory Agency. Agomelatine (Valdoxan): risk of liver toxicity. GOV.UK Drug Safety Update. Published 2014-12-11.
  5. Cipriani A, et al. Comparative efficacy and acceptability of 21 antidepressant drugs for the acute treatment of adults with major depressive disorder. Lancet. 2018;391(10128):1357-1366.
  6. Hickie IB, Rogers NL. Agomelatine for the treatment of major depressive disorder. Expert Opin Pharmacother. 2011;12(13):2187-2196.
  7. Freiesleben SD, Furczyk K. A systematic review of agomelatine-induced liver injury. J Mol Psychiatry. 2015;3:4.
  8. FDA openFDA Drugs@FDA and prescription-label exact-name searches for agomelatine. Checked 2026-07-14.
  9. U.S. Food and Drug Administration. National Drug Code Database Background Information. Accessed 2026-07-14.
  10. NootropicsIndex indexed Agomelatine/Valdoxan listings. Accessed 2026-07-14.
Note

This page is informational and summarizes available evidence. It is not medical advice, a recommendation, or a substitute for guidance from a qualified clinician.