Melatonin
Endogenous pineal hormone and circadian regulator, an MT1/MT2 agonist sleep aid.
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Pharmacology
Contents
WHAT IS MELATONIN?
Detailed overview
Melatonin (N-acetyl-5-methoxytryptamine) is a hormone secreted by the pineal gland in darkness that signals biological night and regulates the sleep-wake rhythm. Acting on MT1 and MT2 receptors in the brain's master clock (the suprachiasmatic nucleus), it works as a chronobiotic rather than a classic hypnotic: it primarily tunes the timing of sleep onset instead of suppressing consciousness like a sedative. Meta-analyses of randomized trials show a modest but consistent reduction in sleep-onset latency and improved sleep quality, and it is particularly effective for jet lag and circadian misalignment. It is also a direct free-radical-scavenging antioxidant. Smaller doses often work as well as large ones, and excess mainly causes next-day grogginess.
Mechanism
MT1/MT2 receptor agonist (chronobiotic)
Half-life
About 20-50 min (standard form)
Legal status
OTC supplement; Rx in EU (Circadin)
Receptor profile
- MT1 and MT2 melatonin receptorsStrong
- Suprachiasmatic nucleus (master clock)Moderate
- Free radicals / oxidative stress (direct antioxidant)Moderate
Safety
Side effects, stop signs, contraindications
Side effects · 5
- Morning grogginess or drowsiness if taken too late or in excessive doses
- Vivid or unusual dreams reported by some users
- Occasional headache or dizziness
- Mistiming can shift the circadian clock in an unhelpful direction
- Transient mood changes or irritability in some sensitive individuals
Contraindications · 4
- Pregnancy and breastfeeding: routine use not advised, medical consultation needed
- Autoimmune conditions: caution advised due to melatonin's immunomodulatory activity
- Avoid activities requiring alertness (driving, operating machinery) shortly after dosing
- Increased caution with anticoagulants (e.g. warfarin) and some antiepileptic drugs
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Meta-analysis: melatonin for the treatment of primary sleep disorders
Ferracioli-Oda E, Qawasmi A, Bloch MH
Effects of exogenous melatonin on sleep: a meta-analysis
Brzezinski A, Vangel MG, Wurtman RJ, et al.
Melatonin for the prevention and treatment of jet lag
Herxheimer A, Petrie KJ
The efficacy and safety of exogenous melatonin for primary sleep disorders. A meta-analysis
Buscemi N, Vandermeer B, Hooton N, et al.
FAQ
FAQ
Endogenous pineal hormone and circadian regulator, an MT1/MT2 agonist sleep aid.
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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.
