From the Guidelines
Melatonin is primarily used to help with sleep issues, including insomnia, jet lag, and sleep schedule disruptions, as well as REM sleep behavior disorder (RBD), with a recommended starting dose of 3 mg taken at bedtime, which can be titrated up to 15 mg as needed. According to the most recent and highest quality study, melatonin binds to the M1 and M2 receptors, suppressing REM sleep motor tone and renormalizing other circadian features of REM sleep 1. This is particularly relevant for patients with isolated RBD, where melatonin has been shown to improve symptoms of dream enactment and REM sleep motor tone.
Key Points
- Melatonin is a hormone naturally produced by the pineal gland in the brain that regulates sleep-wake cycles
- It is typically taken in doses of 0.5-5mg about 30-60 minutes before bedtime
- For jet lag, it's often recommended to take it closer to the target bedtime at your destination
- For shift workers, taking melatonin after work can help establish a new sleep pattern
- Melatonin works by signaling to your body that it's time to sleep, helping to reset your internal clock
- Most people tolerate melatonin well, though some may experience mild side effects like headaches, dizziness, or daytime drowsiness
Clinical Considerations
- Melatonin is considered a dietary supplement and is available over the counter in the United States and Canada, but its bioavailability and content may be less consistent across formulations 1
- Combination therapy using clonazepam and melatonin is common in clinical practice if response to monotherapy is inadequate, although there is a paucity of data examining combination therapies 1
- Clinicians should consider the patient’s underlying disease and attendant symptoms when choosing a medication, as patients with neurodegenerative disorders frequently experience other symptoms affecting motor function, cognitive domains, and the autonomic system 1
From the FDA Drug Label
Helps establish normal sleep patterns nighttime sleep aid for occassional sleeplessness
- Melatonin helps with:
- Establishing normal sleep patterns
- Occasional sleeplessness 2
From the Research
Melatonin's Effects on Sleep
- Melatonin can influence sleep-promoting and sleep/wake rhythm-regulating actions through the specific activation of MT(1) and MT(2) receptors, which are highly concentrated in the suprachiasmatic nucleus (SCN) 3.
- Exogenous melatonin induces sleep in diurnal animals and healthy humans, with its maximum hypnotic effectiveness influenced by the circadian phase 3.
- Melatonin therapy may be beneficial for ameliorating insomnia symptoms in individuals with primary insomnia, as nocturnal plasma melatonin levels tend to be lower than those in healthy controls 3.
Melatonin's Therapeutic Uses
- Melatonin has been successfully used to treat insomnia in children with attention-deficit hyperactivity disorder or autism, as well as in other neurodevelopmental disorders with sleep disturbances 3.
- Melatonin can significantly advance the phase of the sleep/wake rhythm in circadian rhythm sleep disorders, such as delayed sleep-phase syndrome 3.
- Melatonin is beneficial for promoting adjustment to work schedules and improving sleep quality among shift workers or individuals experiencing jet lag 3, 4, 5.
- Melatonin may be effective in treating sleep disorders, including jet lag, shift work disorder, insomnia, and sleep cycle disorders in neurologically impaired patients 4.
Melatonin's Mechanism of Action
- 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 5.
- Melatonin resets disturbed circadian rhythms and promotes sleep in jet lag and other circadian rhythm sleep disorders 5.
- Melatonin has anti-oxidation, circadian rhythmicity maintenance, sleep regulation, and neuronal survival properties, making it a potential alternative treatment for sleep disorders with fewer side effects 6.