Melatonin is a naturally occurring neurohormone that plays plays an essential role is sleep. It is produced
and secreted by the pineal gland. Melatonin is secreted as the visual system senses sundown and is at its
peak level approximately two hours after sundown to aid the brain into a sleep state.
What is melatonin used for?
Shift work sleep disorder
Melatonin is not contained in any food sources. Melatonin is also found in small amounts in the plants that
used in Feverfew (Tanacetum parthenium), and St John's wort (Hypericum perforatum). 1
occurs in the body and is synthetically made for supplements.
How does beta melatonin work?
The day/night cycle of melatonin secretion is controlled by the vision-processing center in the brain and is
strongly influenced by light. The main effect of light is to regulate melatonin secretion in synchrony with
the days light-dark cycles. As bedtime approaches, melatonin release continues to increase and reaches a
peak level between 2 and 4 am. The release of the melatonin gradually falls during the latter part of the
night and is present at very low levels during the day.2
When people travel outside of their time zone and
the light pattern changes significantly the day/night phases are out of synchrony with their environment.
Melatonin was first used with great success treating jet lag sleep disorders and for treatment of shift work
Shift work sleep disorders occur in people that rotate shifts on a weekly or monthly basis. For example,
nurses, police officers and fire fighters. They may work 4ppm until midnight for a week, the change to
midnight to 8am. Melatonin helps “reset” there 8 hour sleep pattern since their brain cannot go by the
natural light-dark day cycle.
Melatonin is a natural hypnotic and has been determined to be a safe and effective sleep aid for long-term
use in the elderly. Melatonin has minimal signs of toxicity and a limited side effect profile. Melatonin
replacement therapy has been found beneficial in treating many with sleep disturbances. Melatonin has an
active period once it is absorbed through the stomach. It lasts for about 4 hours. It is therefore helpful for
those who have difficulty falling asleep, but is less effective for those who experience frequent nighttime
awakenings or early morning waking and cannot fall back asleep. Several slow-absorption and sustained
released formulations are available to allow elevated melatonin levels throughout the night.
Orally administered melatonin is rapidly absorbed, with peak plasma concentrations occurring between 20
and 120 minutes. This is effective for those who have trouble falling asleep. However, this is inadequate for
those with frequent nighttime or early morning awakening. Therefore, in order to maintain continued
elevated concentrations of melatonin throughout the night, repeated administration of low doses are
required or a sustained released formulation with a higher dose is required. A formulation of a prolonged-
release melatonin (PR-melatonin), is available to provide a sustained elevation of melatonin throughout the
night and more closely mimics to the normal physiological release pattern of endogenous melatonin.3
The sleep-promoting effects become most prominent about 2 hours after intake, similar to the physiological
sequence at night. Melatonin was found to be effective in adjusting the sleep–wake cycle in the blind
individuals, where the light–dark cycles do not exist.4
DOES MELATONIN SUPPLEMENT WORK – THE
SLEEP ENHANCEMENT/INSOMNIA AND JET LAG
Melatonin reduces sleep latency and therefore shortens the time it takes to fall asleep.
Several studies have shown this reduction in time to fall asleep in both healthy subjects and those with
insomnia. In one study, patients with insomnia that were treated with PR-melatonin 2 mg at bedtime for 3
weeks, benefits were compared to a control group treated with placebo. In the PR-melatonin group there
were improvements in sleep latency and in subjective quality of sleep as well as improved daytime
functioning. The subjects taking the melatonin formulation were found to have no impairment of vigilance
the following day and even some improvements in performance in the morning were recorded. The
reported quality of sleep, number of nighttime awakenings, morning alertness and quality of life were
significantly improved with PR-melatonin compared to placebo.5
The sleep-promoting effects of PR-
melatonin are similar in magnitude to those of other drugs used to help sleep onset. At the same time, PR-
melatonin does not impair psychomotor performance, driving performance, and memory.5
Sleep enhancement/ Insomnia
Van Geijlswijk and co-workers, 2010. The Use of Exogenous Melatonin in Delayed Sleep Phase Disorder:
A meta-analysis of data of randomized controlled trials involving individuals with delayed sleep phase
disorder that were published .The 5 trials including 91 adults and 4 trials including 226 children showed
that melatonin treatment cause the start of peak levels of the body’s internal melatonin1 hour sooner and
helped the patients fall asleep about 1 hour sooner as well.6
Herxheimer and co-workers, 2008. Melatonin for the prevention and treatment of jet lag.
Eight of the ten trials found that melatonin, taken close to the target bedtime at the destination (10pm to
midnight), decreased jet-lag from flights crossing five or more time zones. Daily doses of melatonin
between 0.5 and 5mg are similarly effective, except that people fall asleep faster and sleep better after 5mg
than 0.5mg. Doses above 5mg appear to be no more effective. 7
There are few side effects reported for melatonin. However, low blood pressure, rise in blood sugar, nausea
and stomach discomfort have been reported
ALWAYS FOLLOW INSTRUCTIONS ON THE LABEL! NO DOT EXCEED THE
RECOMMENDED DAILY DOSE!
Melatonin has been used in doses up to 4 milligrams a day. It is recommended to start with 2 mg, about 45
minutes before bedtime
1. Melatonin helps most people fall asleep faster.
2. Melatonin supplement improves the symptoms of jet lag
3. Beta alanine supplement improves sleep pattern in those with work-shift disorder.
1. Paredes SD, Korkmaz A, Manchester LC, Tan DX, Reiter RJ. Phytomelatonin: a review.
Journal of experimental botany. 2009;60(1):57-69.
2. Shochat T, Haimov I, Lavie P. Melatonin--the key to the gate of sleep. Annals of
medicine. Feb 1998;30(1):109-114.
3. Wade A, Downie S. Prolonged-release melatonin for the treatment of insomnia in
patients over 55 years. Expert opinion on investigational drugs. Oct 2008;17(10):1567-
4. Arendt J, Skene DJ, Middleton B, Lockley SW, Deacon S. Efficacy of melatonin
treatment in jet lag, shift work, and blindness. Journal of biological rhythms. Dec
5. Wade AG, Crawford G, Ford I, et al. Prolonged release melatonin in the treatment of
primary insomnia: evaluation of the age cut-off for short- and long-term response.
Current medical research and opinion. Jan 2011;27(1):87-98.
6. Andrew Herxheimer, Petrie KJ. Melatonin for the prevention and treatment of jet lag. The
Cochrane Library. 2009.
7. van Geijlswijk IM, Korzilius HP, Smits MG. The use of exogenous melatonin in delayed
sleep phase disorder: a meta-analysis. Sleep. Dec 2010;33(12):1605-1614.