The Pharmacokinetics, Dosage, Preparation Forms, and Efficacy of Orally Administered Melatonin for Non-Organic Sleep Disorders in Autism Spectrum Disorder During Childhood and Adolescence: A Systematic Review

<b>Background:</b> To date, it remains unclear which oral doses and preparation forms of melatonin should be recommended for children and adolescents with non-organic sleep disorders and autism spectrum disorder (ASD). We reviewed the current state of knowledge on this topic based on ran...

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Main Authors: Ekkehart Paditz, Bertold Renner, Rainer Koch, Barbara M. Schneider, Angelika A. Schlarb, Osman S. Ipsiroglu
Format: Article
Language:English
Published: MDPI AG 2025-05-01
Series:Children
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Online Access:https://www.mdpi.com/2227-9067/12/5/648
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author Ekkehart Paditz
Bertold Renner
Rainer Koch
Barbara M. Schneider
Angelika A. Schlarb
Osman S. Ipsiroglu
author_facet Ekkehart Paditz
Bertold Renner
Rainer Koch
Barbara M. Schneider
Angelika A. Schlarb
Osman S. Ipsiroglu
author_sort Ekkehart Paditz
collection DOAJ
description <b>Background:</b> To date, it remains unclear which oral doses and preparation forms of melatonin should be recommended for children and adolescents with non-organic sleep disorders and autism spectrum disorder (ASD). We reviewed the current state of knowledge on this topic based on randomised placebo-controlled trials (RCTs) and diagnosis-related blood melatonin concentrations available in this age group. <b>Method:</b> Two investigators independently searched PubMed, PsycINFO, MEDLINE, and Cochrane CENTRAL on 1 March 2025 for the keywords “melatonin”, “autism”, and “randomised” in titles and abstracts in all languages, including an evaluation of the references of the reviews, systematic reviews, and meta-analyses published up to that date, some of which were based on searches in numerous databases. Based on this, additional in-depth searches were carried out in PubMed for pharmacokinetic, physiological, and pathophysiological data on melatonin in children and adolescents, with a special focus on ASD. <b>Results</b>: To date, five RCTs on non-organic sleep disorders in children and adolescents with the sole diagnosis of ASD or with subgroup analyses in the presence of several initial diagnoses such as ADHD, epilepsy, Smith–Magenis, or Fragile X syndrome are available. In these studies, rapid-release, non-delayed preparations were administered orally. In one of these studies, the clinical efficacy of a combination preparation with a sustained-release and a non-released active substance component was tested. Pharmacokinetic data with multiple determinations of melatonin concentrations in the blood are only available for children with ASD in the form of a case series (N = 9). <b>Discussion</b>: RCTs comparing the efficacy of delayed melatonin preparations with non-delayed rapid-release oral preparations are not yet available. Physiological data and clinical effects documented in five RCTs indicate that non-delayed melatonin preparations with an initial rapid onset of action are effective for non-organic sleep disorders in children and adolescents with ASD. <b>Conclusions</b>: From a clinical, pharmacokinetic, and physiological point of view, the RCTs available to date and the data on melatonin concentrations in the blood of children with ASD, measured several times over 24 h, suggest that a low oral melatonin dose and a non-delayed preparation with rapid onset should be started in children and adolescents with non-organic sleep disorders in ASD, if sleep hygiene advice and psychotherapeutic interventions have not demonstrated sufficient effects.
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spelling doaj-art-e9133d28a97a475591afe9727e8aecc82025-08-20T01:56:20ZengMDPI AGChildren2227-90672025-05-0112564810.3390/children12050648The Pharmacokinetics, Dosage, Preparation Forms, and Efficacy of Orally Administered Melatonin for Non-Organic Sleep Disorders in Autism Spectrum Disorder During Childhood and Adolescence: A Systematic ReviewEkkehart Paditz0Bertold Renner1Rainer Koch2Barbara M. Schneider3Angelika A. Schlarb4Osman S. Ipsiroglu5Centre for Applied Prevention/Zentrum für Angewandte Prävention, 01307 Dresden, GermanyInstitute of Clinical Pharmacology, Faculty of Medicine Carl Gustav Carus, Dresden University of Technology, 01069 Dresden, GermanyFormerly Institute for Medical Informatics and Biometry, Faculty of Medicine Carl Gustav Carus, Dresden University of Technology, 01069 Dresden, GermanyPaediatric Sleep Medicine Centre in Foundation, Vancouver, BC V5Z 4H4, CanadaFaculty of Psychology and Sports Science, Bielefeld University, 33615 Bielefeld, GermanyInterdisciplinary Sleep Program, Sleep/Wake-Behaviour Clinic, Departments of Pediatrics & Psychiatry, University of British Columbia, Vancouver, BC V6T 1Z4, Canada<b>Background:</b> To date, it remains unclear which oral doses and preparation forms of melatonin should be recommended for children and adolescents with non-organic sleep disorders and autism spectrum disorder (ASD). We reviewed the current state of knowledge on this topic based on randomised placebo-controlled trials (RCTs) and diagnosis-related blood melatonin concentrations available in this age group. <b>Method:</b> Two investigators independently searched PubMed, PsycINFO, MEDLINE, and Cochrane CENTRAL on 1 March 2025 for the keywords “melatonin”, “autism”, and “randomised” in titles and abstracts in all languages, including an evaluation of the references of the reviews, systematic reviews, and meta-analyses published up to that date, some of which were based on searches in numerous databases. Based on this, additional in-depth searches were carried out in PubMed for pharmacokinetic, physiological, and pathophysiological data on melatonin in children and adolescents, with a special focus on ASD. <b>Results</b>: To date, five RCTs on non-organic sleep disorders in children and adolescents with the sole diagnosis of ASD or with subgroup analyses in the presence of several initial diagnoses such as ADHD, epilepsy, Smith–Magenis, or Fragile X syndrome are available. In these studies, rapid-release, non-delayed preparations were administered orally. In one of these studies, the clinical efficacy of a combination preparation with a sustained-release and a non-released active substance component was tested. Pharmacokinetic data with multiple determinations of melatonin concentrations in the blood are only available for children with ASD in the form of a case series (N = 9). <b>Discussion</b>: RCTs comparing the efficacy of delayed melatonin preparations with non-delayed rapid-release oral preparations are not yet available. Physiological data and clinical effects documented in five RCTs indicate that non-delayed melatonin preparations with an initial rapid onset of action are effective for non-organic sleep disorders in children and adolescents with ASD. <b>Conclusions</b>: From a clinical, pharmacokinetic, and physiological point of view, the RCTs available to date and the data on melatonin concentrations in the blood of children with ASD, measured several times over 24 h, suggest that a low oral melatonin dose and a non-delayed preparation with rapid onset should be started in children and adolescents with non-organic sleep disorders in ASD, if sleep hygiene advice and psychotherapeutic interventions have not demonstrated sufficient effects.https://www.mdpi.com/2227-9067/12/5/648melatonin in children and adolescentsautism spectrum disordersleeppharmacokineticsRCTnon-delayed preparations
spellingShingle Ekkehart Paditz
Bertold Renner
Rainer Koch
Barbara M. Schneider
Angelika A. Schlarb
Osman S. Ipsiroglu
The Pharmacokinetics, Dosage, Preparation Forms, and Efficacy of Orally Administered Melatonin for Non-Organic Sleep Disorders in Autism Spectrum Disorder During Childhood and Adolescence: A Systematic Review
Children
melatonin in children and adolescents
autism spectrum disorder
sleep
pharmacokinetics
RCT
non-delayed preparations
title The Pharmacokinetics, Dosage, Preparation Forms, and Efficacy of Orally Administered Melatonin for Non-Organic Sleep Disorders in Autism Spectrum Disorder During Childhood and Adolescence: A Systematic Review
title_full The Pharmacokinetics, Dosage, Preparation Forms, and Efficacy of Orally Administered Melatonin for Non-Organic Sleep Disorders in Autism Spectrum Disorder During Childhood and Adolescence: A Systematic Review
title_fullStr The Pharmacokinetics, Dosage, Preparation Forms, and Efficacy of Orally Administered Melatonin for Non-Organic Sleep Disorders in Autism Spectrum Disorder During Childhood and Adolescence: A Systematic Review
title_full_unstemmed The Pharmacokinetics, Dosage, Preparation Forms, and Efficacy of Orally Administered Melatonin for Non-Organic Sleep Disorders in Autism Spectrum Disorder During Childhood and Adolescence: A Systematic Review
title_short The Pharmacokinetics, Dosage, Preparation Forms, and Efficacy of Orally Administered Melatonin for Non-Organic Sleep Disorders in Autism Spectrum Disorder During Childhood and Adolescence: A Systematic Review
title_sort pharmacokinetics dosage preparation forms and efficacy of orally administered melatonin for non organic sleep disorders in autism spectrum disorder during childhood and adolescence a systematic review
topic melatonin in children and adolescents
autism spectrum disorder
sleep
pharmacokinetics
RCT
non-delayed preparations
url https://www.mdpi.com/2227-9067/12/5/648
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