
Melatonin is a very popular over-the-counter or over-the-counter remedy supplement for insomnia and traveller’s jet lag.
I am often asked what do I recommend for insomnia and poor sleep? Invariably, the conversation often includes talk about melatonin, a hormone produced in the pineal gland of the brain. It is produced in small amounts when photoreceptors in the eyes detect darkness or lack of light. Melatonin causes drowsiness and helps to induce the sleep cycle.
It is also found in small amounts in many animals and plants, dairy products, nuts and seeds and fruit like bananas and cherries.
Melatonin is like another brain hormone called serotonin and both are made from the essential amino acid L-tryptophan. When lack of light is detected, the pineal gland releases less than 0.1 milligram of melatonin. Some of the melatonin goes to part of the brain called the hypothalamus which helps to regulate the biological clock or circadian rhythm. Melatonin also travels to and affects other parts of the body including the heart, kidneys and the immune system.
Interestingly, while melatonin is an over-the-counter supplement in both the USA and Canada, it is a prescription in many countries including the United Kingdom, Germany and Japan.
It has other biological effects in the human body. It is a strong antioxidant that prevents oxidative damage to many tissues of the body. It has been shown to prevent damage to cell membranes, DNA and mitochondria. In this way, melatonin has been postulated to be an anti-cancer compound and has been utilized by many patients who are fighting cancer. It can help the immune system by stimulating production of cellular messengers and certain white blood cells.
Melatonin has been shown to promote bone growth and inhibit bone resorption and it can suppress ovulation and promote infertility.
Melatonin is a relatively short-lived molecule with a half-life between 30 and 60 minutes. Most experts advise taking melatonin between 30 and 60 minutes before the anticipated time to fall asleep. For those individuals who have no trouble falling asleep but experience frequent nighttime awakenings, melatonin can be taken at that time when awakened. It can be consumed if you wake up at say 1 a.m. or 2 a.m. It is best consumed in the smallest dose that gives the individual the best sleep results.
That sweet spot is unique to every individual. Melatonin has an absorption rate between 10% to 50% of what is consumed orally. That means, at an average 30% absorption rate, taking a three-milligram tablet would lead to about one milligram being absorbed.
If you want to mimic a physiologic dose of what the pineal gland would normally produce, you don’t need a lot of melatonin. Generally, that would mean 0.5 mg to 1.5 mg would be sufficient to mimic normal human physiology at bedtime.
Melatonin still appears to be a very safe supplement with very few side effects. Most side effects reported include drowsiness, daytime fatigue, dizziness, irritability, headache, dry mouth, nausea, unusual dreams and other relatively benign symptoms. Many patients who come to see me report taking melatonin in doses of 5 mg, 10 mg, 20 mg and even up to 30 mg.
Most experts consider it not to be addictive. However, like anything, a certain degree of dependence and habituation can occur. It appears to be a lot safer to take than most prescription and other over-the-counter sleeping medications. Some patients say it controls their anxiety and helps moods. Some cancer patients take it at large doses without side effects.
In clinical practice, I estimate it helps half the patients to some degree with sleep issues. For about the other 50%, it really doesn’t seem to do anything at all. It appears much safer to take than prescription sleep medicine and that is why it is regulated as an over-the-counter product. Again, take the lowest specific dose for you that gives you the best results.
Caution should be taken when given to children and pregnant women. I have seen many parents who give it to their children for sleep, anxiety or even attention deficit issues. It is probably safe in small amounts for shorter periods of time for children but it would be wise to consult a medical professional if there are any questions or concerns.
The information provided in this article does not, and is not intended to, constitute medical advice. All information and content are for general information purposes only.
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