Image for Melatonin (N-acetyl-5-methoxytryptamine)
Melatonin (N-acetyl-5-methoxytryptamine)

Synonyms/Common Names/Related Substances:

  • 5-Methoxy-N-acetyltryptamine, 6-sulfatoxymelatonin, acetamide, agomelatine, aMT6s, beta-methyl-6-chloromelatonin, BMS-214778, CAS 73-31-4, hypnotic, indole, luzindol, luzindole, mel, MEL, melatonia, melatonine, Melaxen®, melaxene, MLT, MT, N-2-(5-methoxyindol-3-ethyl)-acetamide, N-acetil-5-metoxitriptamina, N-acetyl-5-methoxytryptamine, neurohormone, ramelteon (CAS 196597-26-9, TAK-375), tryptophan.
  • Brand names: Accurate Release®; Appleheart Melatonin®; Circadin®; Inspired by Nature®; Mel®; Melatonin Controlled Release®; Melatonin Olympian Labs®; Melatonin Tablets®; Melatonin Time Release®; Melatonin-BioDynamax®; Melatonin-Metabolic Response Modifier®; Melatonin-New Hope Health Products®; Melatonin-Optimum Nutrition®; Melaxen®; Nature's Bounty®; Puritan's Pride®; Rozerem®; Twinlab® Melatonin; Valdoxan®.
  • Combination product examples: Melatonex® (vitamin B6); Melatonin Forte® (Piper methysticum, kavalactones, valeriana); Melatonin PM Complex® (vitamin B6, vitamin B2, vitamin B3); Melatonin spray® (gamma-aminobutyric acid, pyridoxal-5-phosphate); Super Snooze with Melatonin® (valerian root, hop, skullcap, chamomile, passion flower).

Clinical Bottom Line/Effectiveness

Brief Background

  • Endogenous melatonin is an indole neurohormone produced in the brain by the pineal gland, from the amino acid tryptophan (1), with regulation of day-night changes in synthesis regulated by changes in the activity of serotonin N-acetyltransferase (2). The synthesis and release of melatonin are stimulated by darkness and suppressed by light, suggesting the involvement of melatonin in circadian rhythm and regulation of diverse body functions. Levels of melatonin in the blood are highest prior to bedtime. Melatonin acts on MT(1) and MT(2) melatonin receptors located in the hypothalamic suprachiasmatic nuclei, the site of the body's master circadian clock.
  • Due to increases in melatonin levels at night, the most common use of melatonin is to aid in sleep. The uses of melatonin which have the strongest supporting evidence are delayed sleep phase syndrome, insomnia in children and the elderly, jet lag, and sleep disorders in individuals with behavioral, developmental, or intellectual disorders. The weakest evidence in support of melatonin is in relation to work shift sleep disorder. While this is promising and the subject of future clinical research, good evidence in support of melatonin for other uses is lacking.
  • New drugs that block the effects of melatonin are in development, such as BMS-214778 or luzindole, and they may have uses in various disorders (3;4;5). Ramelteon (Rozerem®) and agomelatine (Valdoxan®) (the latter not yet U.S. Food and Drug Administration (FDA) approved) are drugs that have a high affinity for the melatonin receptors MT1 and MT2, present in the suprachiasmatic nucleus, the circadian pacemaker (6). Melatonin agonists, such as beta-methyl-6-chloromelatonin, have also been studied (7). Details and clinical trials of these drugs are not included in this monograph.

Dosing/Toxicology

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Precautions/Contraindications

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Interactions

Most herbs and supplements have not been thoroughly tested for interactions with other herbs, supplements, drugs, or foods. The interactions listed below are based on reports in scientific publications, laboratory experiments, or traditional use. You should always read product labels. If you have a medical condition, or are taking other drugs, herbs, or supplements, you should speak with a qualified healthcare provider before starting a new therapy.

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Mechanism of Action

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History

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Evidence Table

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Evidence Discussion

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Products Studied

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Author Information

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References

Natural Standard developed the above evidence-based information based on a thorough systematic review of the available scientific articles. For comprehensive information about alternative and complementary therapies on the professional level, go to www.naturalstandard.com. Selected references are listed below.

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The information in this monograph is intended for informational purposes only, and is meant to help users better understand health concerns. Information is based on review of scientific research data, historical practice patterns, and clinical experience. This information should not be interpreted as specific medical advice. Users should consult with a qualified healthcare provider for specific questions regarding therapies, diagnosis and/or health conditions, prior to making therapeutic decisions.