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Melatonin USP

Also known as: N-acetyl-5-methoxytryptamine, Melatonin

Overview

Melatonin is a neurohormone primarily produced by the pineal gland in the brain, regulating sleep-wake cycles. It is also available as a dietary supplement and is found in some foods like cherries and walnuts. As a supplement, it is commonly used to improve sleep quality, treat insomnia, and manage various sleep disorders. Melatonin's primary function is to regulate circadian rhythms by interacting with melatonin receptors in the brain. It is well-studied, with high-quality evidence supporting its efficacy in improving sleep parameters such as sleep onset latency and total sleep time. Melatonin is rapidly absorbed after oral administration and has a short half-life, making it suitable for promoting sleep initiation. It is available in immediate-release and sustained-release forms.

Benefits

Melatonin significantly improves sleep quality, reduces sleep onset latency, and increases total sleep time. A meta-analysis showed that melatonin decreases sleep onset latency by approximately 7.06 minutes and increases total sleep time by about 8.25 minutes compared to placebo, with a standardized mean difference of 0.22 for overall sleep quality improvement. It is particularly beneficial for adults and children with sleep disorders, including those with cerebral palsy, where it has been shown to improve sleep latency and total sleep time. Some research suggests it may also have antioxidant properties and potential benefits in assisted reproduction, though these effects are considered secondary. Effects on sleep are generally observed within a few days to weeks of supplementation.

How it works

Melatonin primarily works by interacting with melatonin receptors, specifically MT1 and MT2, in the brain to regulate the sleep-wake cycle. This interaction influences the hypothalamic-pituitary-adrenal axis and other neurotransmitter systems involved in sleep regulation. Upon oral administration, melatonin is rapidly absorbed and enters the bloodstream, where it binds to these receptors, promoting feelings of drowsiness and facilitating the onset of sleep. Its short half-life means it primarily aids in initiating sleep rather than maintaining it throughout the night, although sustained-release formulations can address this.

Side effects

Melatonin is generally considered safe, with a low risk of serious side effects. Common side effects, occurring in more than 5% of users, include dizziness, headache, and nausea. Uncommon side effects, affecting 1-5% of users, may include vivid dreams and morning grogginess. Rare side effects, occurring in less than 1% of users, include allergic reactions. Melatonin may interact with blood thinners, diabetes medications, and sedatives, potentially altering their effects. It is contraindicated in pregnancy and breastfeeding due to insufficient safety data. Caution is advised when using melatonin in children and individuals with autoimmune disorders. It's important to consult a healthcare provider before use, especially when taking other medications.

Dosage

The minimum effective dose of melatonin typically starts at 0.5 mg for sleep disorders. Optimal dosage ranges are between 0.5 mg to 5 mg, taken 30-60 minutes before bedtime. It is generally not recommended to exceed 10 mg. Timing is crucial; melatonin should be taken in the evening to align with natural melatonin production. Immediate-release forms are common, while sustained-release forms may be beneficial for maintaining sleep throughout the night. Food intake may affect absorption, so it is best taken on an empty stomach. No specific cofactors are required for melatonin to be effective.

FAQs

When is the best time to take melatonin?

Take melatonin 30-60 minutes before your desired bedtime to help regulate your sleep-wake cycle. Consistency in timing is key for optimal results.

How long does it take for melatonin to work?

Melatonin typically starts working within 30-60 minutes of ingestion. You should notice improved sleep quality within a few days to weeks of consistent use.

Is melatonin safe to take with other medications?

Melatonin may interact with blood thinners, diabetes medications, and sedatives. Consult a healthcare provider before use, especially if you are taking other medications.

Is melatonin a sedative?

No, melatonin is not a sedative. It regulates sleep-wake cycles by interacting with melatonin receptors in the brain, promoting feelings of drowsiness.

Research Sources

  • https://pubmed.ncbi.nlm.nih.gov/33417003/ – This systematic review examined the effects of melatonin supplementation on sleep quality in adults, as measured by the Pittsburgh Sleep Quality Index. The findings suggest that melatonin has a positive impact on sleep quality, making it a potentially useful supplement for individuals experiencing sleep disturbances. The study highlights the importance of considering melatonin as a non-pharmacological approach to improving sleep.
  • https://pubmed.ncbi.nlm.nih.gov/38971124/ – This meta-analysis demonstrated that melatonin decreases sleep onset latency by approximately 7.06 minutes and increases total sleep time by about 8.25 minutes compared to placebo. The results indicate a modest but significant effect on sleep parameters, supporting the use of melatonin for improving sleep quality. The study provides quantitative evidence for the efficacy of melatonin in addressing sleep-related issues.
  • https://observatorio.fm.usp.br/entities/publication/0d16853e-470a-4411-9624-65a2b51fcafa – This study investigates the effects of melatonin on sleep in children with cerebral palsy. The research found that melatonin significantly improved sleep latency and total sleep time, with a notable 31-minute difference in total sleep time compared to placebo. These findings suggest that melatonin can be a beneficial intervention for improving sleep in children with cerebral palsy.
  • https://www.scielo.br/j/clin/a/sFK689NyjR7BwvjsFCjQ6Hc/ – This article discusses the role of melatonin in clinical practice, focusing on its applications in sleep disorders and other conditions. It provides an overview of melatonin's mechanisms of action and its potential benefits, as well as considerations for its use in different populations. The article serves as a comprehensive resource for healthcare professionals seeking to understand and utilize melatonin effectively.
  • https://pm.amegroups.org/article/view/5803/html – This article reviews the use of melatonin in pediatric sleep disorders. It discusses the efficacy and safety of melatonin in treating insomnia and other sleep-related issues in children. The review highlights the importance of considering melatonin as a therapeutic option for pediatric sleep disorders, while also emphasizing the need for careful monitoring and individualized treatment plans.

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