Melatonin: From Pharmacokinetics to Clinical Use in Autism Spectrum Disorder
Open accessAbstract
The role of melatonin has been extensively investigated in pathophysiological conditions, including autism spectrum disorder (ASD). Reduced melatonin secretion has been reported in ASD and led to many clinical trials using immediate-release and prolonged-release oral formulations of melatonin. However, melatonin's effects in ASD and the choice of formulation type require further study. Therapeutic benefits of melatonin on sleep disorders in ASD were observed, notably on sleep latency and sleep quality. Importantly, melatonin may also have a role in improving autistic behavioral impairments. The objective of this article is to review factors influencing treatment response and possible side effects following melatonin administration. It appears that the effects of exposure to exogenous melatonin are dependent on age, sex, route and time of administration, formulation type, dose, and association with several substances (such as tobacco or contraceptive pills). In addition, no major melatonin-related adverse effect was described in typical development and ASD. In conclusion, melatonin represents currently a well-validated and tolerated treatment for sleep disorders in children and adolescents with ASD. A more thorough consideration of factors influencing melatonin pharmacokinetics could illuminate the best use of melatonin in this population. Future studies are required in ASD to explore further dose-effect relationships of melatonin on sleep problems and autistic behavioral impairments.
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Long-acting melatonin has been shown to increase total sleep time in individuals with ASD across multiple studies.
“Long-acting melatonin has been shown to increase total sleep time in individuals with ASD across multiple studies [62]”
From Pharmacological treatment in autism: a proposal for guidelines on common co-occurring psychiatric symptoms (2025) · cites this paper as [62]
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Self-citationAgomelatine: A Potential Multitarget Compound for Neurodevelopmental Disorders
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Non-Excitatory Amino Acids, Melatonin, and Free Radicals: Examining the Role in Stroke and Aging
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Melatonin Attenuates Dextran Sodium Sulfate Induced Colitis in Obese Mice
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ACOLHIMENTO DE REFUGIADOS: UM RELATO DE EXPERIÊNCIA
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MELATONIN AND NEURODEGENERATION (ANALYTICAL LITERATURE REVIEW)
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Tratamento farmacológico atual do transtorno do espectro autista
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- Authors
- Lalanne, S., Fougerou-Leurent, C., Anderson, G. M., Schroder, C. M., Nir, T., Chokron, S., Delorme, R., Claustrat, B., Bellissant, E., Kermarrec, S., Franco, P., Denis, L., & Tordjman, S.
- Affiliations
- Inserm (FR)
- Experimental and Clinical Pharmacology Department, CHU Rennes, 35033 Rennes, France
- Yale University (US)
- Centre National de la Recherche Scientifique (FR)
- Neurim Pharmaceuticals (Israel) (IL)
- Integrative Neuroscience and Cognition Center (INCC), CNRS UMR 8002 and University of Paris, 75006 Paris, France
- Université Paris Cité (FR)
- Centre Hospitalier Guillaume Régnier (FR)
- Lyon 1 Université (FR)
- Corresponding author
- Lalanne, Sébastien
- Tordjman, Sylvie
- ORCID
- Venue
- International Journal of Molecular Sciences
- Publisher
- MDPI AG
- Published
- 2021-02-02
- Volume
- 22
- Issue
- 3
- Pages
- 1490
- ISSN
- 1422-0067 (ISSN-L)
- PMC
- PMC7867370
- OpenAlex
- W3127752314
- Cited by
- 90
- References
- 111
- Citations by year
- 2026: 11 · 2025: 17 · 2024: 19 · 2023: 19 · 2022: 17 · 2021: 7
- FWCI
- 1.98
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- International Journal of Molecular Sciences (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, other-oa)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- HAL (submittedVersion, cc-by)
- HAL (submittedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Topics
- Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Circadian rhythm and melatonin
- Life Sciences › Neuroscience › Cognitive Neuroscience › Autism Spectrum Disorder Research
- Social Sciences › Psychology › Experimental and Cognitive Psychology › Sleep and related disorders
- Keywords
- melatonin, autism spectrum disorder, sleep disorders, sleep latency, sleep quality, treatment response, adverse effects, dose-response relationship, children and adolescents
- MeSH terms
- Autism Spectrum Disorder, Sleep Latency, Administration, Oral, Adult, Biological Availability, Child, Child, Preschool, Circadian Rhythm, Delayed-Action Preparations, Female, Humans, Injections, Intravenous, Male, Melatonin, Saliva, Seasons, Serotonin, Social Behavior Disorders, Tryptophan, Dietary Supplements, Sleep Disorders, Intrinsic, Receptors, Melatonin
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