Melatonin

July 2019

sleeping woman
the Bottom LineMelatonin is an important hormone produced by the body in the evening and helps with rest and restoration. Supplementing melatonin may help with falling and staying asleep, especially for people who are older. However, overuse could lead to dependency. Start with a low dose of 300 mcg as it tends to work best for most people.

Which is the Best Melatonin Supplement?

Check out our unbiased recommendation of the best products on the market using our rigorous methodology. We screen products for the right formulation, bioavailability, safety, and efficacy to bring you only the best supplements available in 2019.

What You Should Know About Melatonin

If you’re suffering from insomnia, a sleep disorder, fatigue, jet lag, or need help resetting your sleep patterns due to night shift, then you should consider taking a low-dose of melatonin. By promoting drowsiness, melatonin can help individuals fall asleep and stay asleep longer. We all know that sleep is important and melatonin, “the sleep” hormone, plays a huge role in the immune system. Melatonin production has also been linked to chronic pain, depression, insomnia, schizophrenia, oxidative damage, inflammation, cardiac disease, weight maintenance, and various cancers. Supplemental melatonin is much safer than other types of over the counter sleep-aids.

Anything that disrupts your sleep cycle and schedule like nights shifts, insomnia, chronic stress, jet lag, and alcohol or caffeine can disrupt your natural production of melatonin. Artificial light, especially blue light, which is produced by all screens (computers, TVs, and cell phones) will lower your body’s natural melatonin levels at night. Age too affects melatonin levels with production of melatonin steadily declining as we age. Reducing your exposure to artificial light, getting 8 hours of sleep, avoiding caffeine, and eating high-protein foods that contain tryptophan, are ways to promote your melatonin levels naturally.

If you decide to take melatonin, be sure to take the synthetic kind, engineered plant matter that mirrors the naturally produced hormone, rather than the “natural” kind, which is taken from the pineal gland of animals and could potentially carry diseases. Also, be sure to take a low dose at about .3 mg as higher doses can desensitize melatonin receptors, causing the supplements to lose their effects after a few days, and end up exacerbating insomnia. Unfortunately, many melatonin supplements contain 10-20 times more than that amount. Also, many experts recommend taking melatonin in the short-term. Over a long period of time of taking supplemental melatonin, the body could potentially get desensitized and stop responding to both the supplemental and naturally producing melatonin, amplifying the effects of insomnia in the long-term.

A Closer Look at Melatonin

Melatonin, known as the “sleep” hormone, helps with regulating the immune system, healing damaged tissue, resolving sleep disorders, helping to treat mood disorders, and may play a role in preventing various cancers. The brain and the gut naturally produce and release melatonin, producing more in the evening and less in the morning. Artificial light at night blocks melatonin production, potentially leading to various sleep disorders and health ailments. An estimated 3 million adults in the U.S. report using supplemental melatonin to help combat sleep disorders. As we age, our bodies naturally produce less of this vital hormone.

Supplemental melatonin has been shown to help people fall and stay asleep faster, which can prevent fatigue during the day. Supplemental melatonin seems to work best for individuals who suffer from Delayed Sleep Phase Syndrome (DSPS), a sleep disorder where a person’s natural sleep and wake cycle is delayed, causing them to deviate from normal sleep patterns by going to bed later and waking up later. Supplemental melatonin can promote drowsiness, providing short-term relief for those who suffer from jet lag, insomnia, or those who need help resetting sleep patterns.

Why Melatonin is Crucial for Health

While best known for its role in sleep pattern maintenance, melatonin has also been shown to have a range of other beneficial properties. It’s been shown to resolve sleep disorders, decrease chronic pain, help treat depression, insomnia, and schizophrenia, reduce oxidative damage, exhibit anti-inflammatory properties, and even help heal damaged tissues.[1] Melatonin has also been been shown to play a role in the skeleton, helping to improve bone mineral density in postmenopausal women.[2] Melatonin is also believed to play a role in the immune system and, in one study involving rats, a melatonin deficiency caused the thymus gland, a key part of the immune system, to atrophy.[3]

Individuals who suffer from dementia, some mood disorders, such as depression, and anxiety severe pain, cancer, and diabetes type 2 have shown to have reduced melatonin levels.[4] Lower levels of melatonin, which leads to an increase in sympathetic nervous system activity, may increase the risk for hypertension, coronary heart disease, and diabetes mellitus.[5] Melatonin has been shown to modulate pain mechanisms, body temperature, stress hormones, and neurotransmitters, which is partly why sleep is so vital for emotional and physical health.[6] Melatonin is also believed to play a role in weight maintenance with one study showing that melatonin supplementation improved sleep quality and led to weight reductions in postmenopausal women.[7]

Additionally, melatonin has been shown to play a major part in the growth rate and preventions of various cancers. In clinical trials, melatonin treatment was shown to reduce the risk of death from cancer and slow the growth of prostate and breast cancer.[8, 9, 10] In one study, women with ovarian cancer were shown to have much lower levels of melatonin, suggesting that melatonin plays a role in the pathogenesis of ovarian cancer.[11]

Internal Processing of Melatonin

The pineal gland in the brain naturally produces melatonin daily with peak levels occurring at night around 2 AM. Melatonin then circulates to all areas of the body, where there are protein receptors that detect the circulating melatonin and signal to the body that it is night time, time to power down, and fall asleep. Melatonin membrane receptors, MT1, MT2 and MT3, can be found in almost every cell and tissue in the body, which is why melatonin may have an apoptotic effect on cancer cells and play such a pivotal role in the immune system and overall health. During the period when melatonin is secreted (at night), we sleep more soundly, and when there are lower levels of melatonin (in the morning) we are more awake.

The suprachiasmatic nuclei is the region of the brain responsible for executing the daily rhythm of melatonin production, also known as the circadian rhythm. The suprachiasmatic nuclei is synchronized with daylight input from the eyes. During the day, the nuclei inhibits melatonin production by the pineal gland, and then at night, reduces this inhibition.This is why artificial light at night can greatly interfere with the body’s ability to produce melatonin and maintain its natural circadian rhythm.

Tryptophan is an amino acid that is a precursor for serotonin, which is in turn a precursor for the production of melatonin. The body converts tryptophan into a substance called 5-HTP, or 5-hydroxytryptophan. 5-HTP is then turned into serotonin, which is converted into melatonin. Therefore, maintaining adequate tryptophan levels is vital to ensure that the body can produce adequate amounts of melatonin. Tryptophan can be found in high-protein foods like chicken, fish, nuts and spinach. In fact, the myth of the post-Thanksgiving turkey drowsiness initially began because of the links between turkey, tryptophan, and melatonin—although now we know that has post meal fatigue has more to do with overconsumption of carbohydrates than from the tryptophan found in the turkey. 5-HTP supplements are also available.

We also need proper stomach acid levels and proper pancreatic function as well as the vitamins and minerals niacin, iron, folate, zinc, B6, magnesium, and vitamin C in order to break down proteins into tryptophan, which is why a vitamin deficiency or lower production of stomach acid could lead to a lower production of melatonin. As they age, adults produce less stomach acid and less melatonin and are more likely to experience disturbances in their sleep cycle.

Melatonin Deficiency and Insufficiency

In healthy young adults, the body produces on average about 10 pg per milliliter of melatonin during the day and peaks at about 60 pg per milliliter at night, or 40 and 260 pmol per liter, respectively. The main causes of melatonin deficiency are a lack of sleep or anything that disrupts the sleep cycles and schedules. Individuals who work nights, suffer from insomnia, chronic stress, jet lag, consume alcohol and caffeine, or have blood sugar imbalances can be at risk for melatonin deficiency.

Age greatly affects melatonin production levels with adults steadily producing less melatonin as they age. One study found that examined changes in melatonin production found that 20 to 39 year-olds naturally produce on average around 12 micrograms of melatonin per night while those over 80 produce on average about 6 micrograms per night.[12]

Overexposure to artificial light, especially blue light, the light produced by computers, TVs, and cell phones, as well as electromagnetic waves, can disrupt melatonin production and lead to melatonin deficiency. There are “blue light filters” that can be used for most electronic devices as well as physical “blue light glasses” that can prevent some of the harmful effects of blue light. Older adults are also more likely to be a risk for melatonin deficiency with some adults producing no melatonin at all. One study gave one group of night shift workers glasses that filtered short-wavelength light and found that those with the glasses produced about 30 percent more melatonin and reported better night sleeps. On average melatonin levels peaked at about 30 pg/ml with the glasses and about 20 pg/ml without them, signifying a significant difference.[13]

Symptoms of melatonin deficiency are fatigue, introversion, waking up frequently at night, irritability, and insomnia. Melatonin levels can be tested with a blood test, urine test or saliva test. The best way to improve a melatonin deficiency is by restoring sleep patterns and getting enough sleep. Blackout curtains, reducing exposure to artificial light, avoiding caffeine, are all ways to promote melatonin production naturally. Some foods naturally contain small amounts of melatonin, such as bananas, cherries, and red wine, but likely not enough to make an impact. Foods that contain tryptophan, however, such as sea foods, meat, whole grains, seeds, nuts and rice could help with melatonin production. Vegans and vegetarians who are deficient in B12 are also more likely to be deficient in melatonin.

Supplementation with Melatonin

Melatonin supplements can also be taken to help aid with melatonin production. A supplement will be made with either “natural” melatonin, derived from the pineal glands of cows, or synthetic melatonin. This may be the one case where natural is not better as natural supplements have the slight risk of being contaminated from various viruses such as mad cow disease.

Supplemental melatonin can be used to reset natural circadian rhythms. One study found that melatonin supplements help patients fall asleep faster and help with the effects of jet lag by decreasing fatigue and helping to reset sleep patterns.[14] One review that analyzed 35 different studies on melatonin found that taking melatonin led to very few side-effects and improved jet lag, insomnia, sleep quality, and helped individuals fall asleep faster.[15]

Another review that analyzed melatonin studies found that while safe, supplemental melatonin did not help with treating primary sleep disorders, but did help with treating Delayed Sleep-Phase Syndrome with short term use (DSPS).[16] Those who suffer from DSPS have a naturally delayed circadian rhythm sleep cycle, causing them to go to bed later and wake up later. Therefore, supplemental melatonin can help them reset their sleep schedule to a more regular time table.

Many times a good night of sleep can reset the body in many ways, including reducing stress and anxiety, and promoting general well-being. Melatonin is an excellent short-term tool that could be effective in resetting sleep patterns and helping someone build good sleep habits.

Proper Dosage and Contraindications

As melatonin is a dietary supplement, rather than a drug, there aren’t clear guidelines when it comes to dosage. Some studies have found that lower doses of melatonin at .3 mg (300 mcg) are more effective for treating insomnia. Many melatonin supplements are dosed at 10x to 30x this amount, commonly found as 3 mg, 5 mg, and even 10 mg. It is theorized that higher doses used over a longer period of time can desensitize melatonin receptors, causing them to lose their effects after a few days, and end up exacerbating insomnia.[17, 18] Also, according to a few studies, by taking too high of a dose, individuals may miss the actual benefits of taking supplemental melatonin by not being able to fall asleep as easily. Anecdotally, many people who take melatonin have also reported that smaller doses (0.3 to 1 mg) were more effective for them. Many clinical trials that studied whether melatonin supplements could help sleep disorders, jet lag, and/or fatigue, did use much higher doses at about 3 – 5 mg. However, that doesn’t mean that lower doses wouldn’t have been as effective or more effective. One study that compared 5 mg and 10 mg doses found no difference between the two doses.[19]

It’s important to be cautious of when you take melatonin as it can affect your natural biological clock and cause drowsiness, which is why it is recommended you take it at night, one hour before sleep. Most dietary supplements, including melatonin, haven’t been tested in pregnant women, nursing mothers, or children, but are likely safe and proper doses. Some common side effects of melatonin are daytime sleepiness, headaches, and dizziness, but overall melatonin has less side effects than other common pharmaceutical sleep aids.

Individuals who take blood-thinning medications (anticoagulants), medications that suppress the immune system (immunosuppressants), diabetes medications, as well as antidepressants and ADHD medications should consult with their doctors before taking melatonin as melatonin can have negative interactions with these medications. Additionally, smokers tend to be less responsive to melatonin supplementation than other demographics.

While supplemental melatonin can help with the effects of jet lag, insomnia, and other sleep disorders, it usually only recommended in the short term. Some experts suggest that over-consumption of melatonin from prolonged use can overwhelm protein receptors, changing how the body responds to the hormone. Over a long period of time of taking supplemental melatonin, it’s possible that the body will stop responding to both the supplemental melatonin and naturally produced melatonin, which can end up amplifying the effects of insomnia in the long-term. Anecdotally, there are many people who take it for years, both chronically and occasionally, to help with sleep and are happy with the effects.

Considerations in Choosing the Right Melatonin Supplement

Many melatonin supplement products contain much higher doses than the recommended amounts. One study found that that 71% of the melatonin supplements tested for the study did not meet the 10% margin of the concentration of melatonin that the label claimed. The actual amount ranged from 83% less to 478% more.[20] One reason for this variance and inaccuracy is that melatonin is considered dietary supplement and not a medication. The FDA does not verify the concentration amounts of supplements and other medications. Therefore, when choosing a supplement, be sure to find a supplement that is “UPS” verified and independently tested for purity and accurate dosage, as we ensure for all our recommended products.

Melatonin has a relatively long shelf-life of about 3 years, when it will start losing its potency. Light and heat can also affect its potency and effectiveness, which is why you should be sure to sure it in a cool, dark place.

Note that many melatonin supplements are meant be taken sublingually: you should place it under your tongue and let it dissolve there, rather than swallowing it like a normal pill. Read the product packaging to see if this is the case for the product you choose. Also note that sublingual melatonin may contain small amounts of some sugars to make it palatable.

Try starting with a low dose of 300 mcg (0.3 mg) and if that doesn’t work, trying 1 mg dosage. The right dosage for you could depend on a variety of factors including your height and weight, and other individual characteristics.

Which is the Best Melatonin Supplement?

Check out our unbiased recommendation of the best products on the market using our rigorous methodology. We screen products for the right formulation, bioavailability, safety, and efficacy to bring you only the best supplements available in 2019.

References:
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2 Shiu SY, Law IC, Lau KW, Tam PC, Yip AW, Ng WT. “Melatonin slowed the early biochemical progression of hormone-refractory prostate cancer in a patient whose prostate tumor tissue expressed MT1 receptor subtype.” J Pineal Res. 2003 Oct;35(3):177-82. PubMed PMID: 12932201. Accessed through: https://www.ncbi.nlm.nih.gov/pubmed/12932201
3 Oner H, Kus I, Oner J, Ogetürk M, Ozan E, Ayar A. “Possible effects of melatonin on thymus gland after pinealectomy in rats.” Neuro Endocrinol Lett. 2004 Feb-Apr;25(1-2):115-8. PubMed PMID: 15159694. Accessed through: https://www.ncbi.nlm.nih.gov/pubmed/15159694
4 Hardeland R. “Neurobiology, Pathophysiology, and Treatment of Melatonin Deficiency and Dysfunction.” Scientific World Journal. 2012; 2012: 640389. doi: 10.1100/2012/640389. Accessed through: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3354573/
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6 Nagai M, Hoshide S, Kario K. “Sleep Duration as a Risk Factor for Cardiovascular Disease- a Review of the Recent Literature.” Curr Cardiol Rev. 2010 Feb; 6(1) 54–61. doi: 10.2174/157340310790231635. Accessed through: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2845795/
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8 Shiu SY, Law IC, Lau KW, Tam PC, Yip AW, Ng WT. “Melatonin slowed the early biochemical progression of hormone-refractory prostate cancer in a patient whose prostate tumor tissue expressed MT1 receptor subtype.” J Pineal Res. 2003 Oct;35(3):177-82. PubMed PMID: 12932201. Accessed through: https://www.ncbi.nlm.nih.gov/pubmed/12932201
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11 Mostafavi SA, Akhondzadeh S, Mohammadi MR, Keshtkar AA, Hosseini S, Eshraghian MR, Ahmadi F, Alipour R, Keshavarz SA. “Role of melatonin in body weight: A systematic review and meta-analysis.” Curr Pharm Des. 2016 Nov 29. [Epub ahead of print] PubMed PMID: 27897121. Accessed through: https://www.ncbi.nlm.nih.gov/pubmed/27897121
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