Health Benefits of Melatonin

Melatonin does far more than just help you sleep, it’s a potent antioxidant that protects the brain from free radical damage known to be involved in brain ageing and mental health problems.
Melatonin also protects the blood-brain barrier and can be used as a remedy for healing a leaky blood-brain barrier.
Melatonin is anti-inflammatory another factor also involved in mental health problems and brain degeneration.

Melatonin also protect us from cardiovascular disease, osteoporosis, cancer, it improves the outcomes of cancer treatments and heals the intestines.
 
Melatonin protects and heals the brain in several ways, by acting as an antioxidant that protects the brain from free radical damage, melatonin protects the blood-brain barrier from damage and helps us to heal it when it has become damaged, melatonin is also anti-inflammatory and inflammation is now known to breakdown the function of key structures in the brain involved in mental health problems.
 
You can add melatonin to your wellness regime to overcome mental health problems, obviously don’t expect melatonin on its own to be the whole cure. Furthermore you have to get the dosage right because if you get the dosage wrong some people experience an increase in depression.
 

Does melatonin help or worsen depression?

Melatonin is a sedating and in some people to higher dose can actually make them feel more depressed the next day however we now know that oxidation damage and particularly inflammation are fundamental causes of the changes the curve in the brain that drive depression and so the powerful anti-inflammatory and antioxidant properties of melatonin mean it can be very useful for treating depression, you just have to get the dosage right if you feel any lingering after-effects of drowsiness the following morning or increase depression you’ve taken too much, sometimes micro doses of say 300 µg for more therapeutic than high doses of say 3 mg, I’ll say more about this below.
 

Melatonin as an Anti-Oxidant

Melatonin is a powerful antioxidant naturally produced mainly by the pineal gland predominantly during the night when it helps to protect and regenerate our brain and body while we sleep.  A` good dose of melatonin throughout the night forms part of our body’s way of fighting diseases such as cancer, repairing the brain and slowing down the ageing process, you can think of melatonin as essential to the repair process that occurs in the body and brain when we sleep.
 
Since 1993 over 800 publications have directly or indirectly confirmed that melatonin is a powerful free radical scavenger (1).  Antioxidants are chemicals that protect the essential structures of our body from oxidising, damage and ageing effects. Melatonin has broad-spectrum antioxidant effects that protect both protein and oil molecules within the body from free radical damage, including the damaging effects of singlet oxygen, nitric oxide, peroxynitrite anion hydroxyl radicals and hydrogen peroxide.  The antioxidant effects of melatonin are several times more potent than vitamins C and vitamin E when compared in equivalent amounts (1). Unlike many other antioxidants melatonin easily defuses into all cells of the body and can easily cross the blood-brain barrier to enter and protect the brain (2).  
 

Anti-Ageing & Brain Protective Effects of Melatonin

As we age our body produces less melatonin leaving older adults with diminishing antioxidant protection, particularly from brain degeneration and ageing. Maximising melatonin production by preventing blue light pollution in the evening and supplementing melatonin with advancing years may slow the ageing process.
 
Melatonin has been shown to decrease cognitive deterioration in individuals with Alzheimer’s disease possibly by protecting the brain from a toxic protein called beta-amyloid (3) (4).  A study in 2007 assessed the benefit of melatonin in 50 sufferers of mild cognitive impairment, a collection of conditions that precedes dementia and Alzheimer’s disease 3 to 9 mg of melatonin nightly for 9-18 months to half of the study group. Researchers found that the supplemental patients had significantly better performance on a host of neurological and psychological tests while experiencing improvements in sleep quality and wakefulness during the day. (Furio AM at al. Possible therapeutic value of melatonin in mild cognitive impairment: a retrospective study. J Pineal Res. 2007 November; 43 (4): 404-9.)

Another study in 2006 found that nightly supplementation of melatonin significantly improved memory in ageing animals tested in the maze, but had no effect on learning in younger adults, suggesting that melatonin has a protective effect against age related cognitive decline. (Vinogradova IA. A comprehensive study of the effects of melatonin and epitalon on the protracted memory under the shuttle labyrinth test conditions in rats in the course of ageing. Eksp Klin Farmakol. 2006 November; 69 (6): 13-6.) 
Melatonin may also be protective against the progression of Parkinson’s disease (5).
 

Melatonin Protects and Heals the Blood-Brain Barrier

Melatonin inhibits an enzyme called MMP9 that makes the blood-brain barrier more permeable, it has also been shown to protect the blood-brain barrier from inflammatory molecules. [Ref]
 

Cancer Fighting Effects of Melatonin

The antioxidant, anti-inflammatory and immune system supportive properties of melatonin give it application in both cancer prevention and as a supportive treatment for cancer therapy ([No authors listed] Melatonin. Monograph. Altern Med Rev. 2005 Dec;10(4):326-36)
 
Multiple scientific trials (meta-analysis of 10 randomised controlled trials) demonstrated the usefulness of melatonin either alone or as an adjunctive treatment for patients with various types of cancer. The inclusion of melatonin supplementation reduces the relative risk of death at one year by an impressive 34% regardless of the type of cancer of the melatonin dosage and without an adverse side-effects. (Mills E, Wu P, Seely D, Guyatt G. Melatonin in the treatment of cancer: a systematic review of randomized controlled trials and meta-analysis. J Pineal Res. 2005 Nov;39(4):360-6.) This is an impressive and encouraging finding promoting the inclusion of melatonin to any cancer treatment program.
 
In one study women with breast cancer that had failed to respond to tamoxifen alone received a combination of tamoxifen and 20 mg of evening melatonin, more than a quarter of the subjects then began to respond to the combination treatment. (Lissoni P, Barni S, Meregalli S, et al. Modulation of cancer endocrine therapy by melatonin: a phase II study of tamoxifen plus melatonin in metastatic breast cancer patients progressing under tamoxifen alone. Br J Cancer.1995 Apr;71(4):854-6.).  20 mg is a very high dose but has no toxic effects and could be considered by anyone as a supportive adjunctive therapy to chemotherapy drug treatments.
 
Melatonin is also beginning to show promise as a protective and supportive adjunctive therapy for prostate cancer.
Sainz RM, Mayo JC, Tan DX, Leon J, Manchester L, Reiter RJ. Melatonin reduces prostate cancer cell growth leading to neuroendocrine differentiation via a receptor and PKA independent mechanism. Prostate. 2005 Apr 1;63(1):29-43.
Sainz RM, Mayo JC, Tan DX et al. Melatonin reduces prostate cancer cell growth leading to neuroendocrine differentiation via
a receptor and PKA independent mechanism. Prostate. 2005 Apr 1;63(1):29-43.
 

Cardiovascular Protection

Following a heart attack melatonin is a potentially a useful antioxidant and anti-inflammatory substance that may prevent further damage and limit the size of an infarction (area of heart cell death) (Tengattini S at al. Cardiovascular disease: protective effects of melatonin. J Pineal Res. 2008 January; 44 (1): 16-25.) (Chen Z at al. Protective effects of melatonin on myocardial infarction. Am J Physiol Heart Cir Physiol. 2003 May; 284 (5):H 1618-24 )
Melatonin has also been shown to improve the strength of the heart’s pumping action following an infarction in laboratory animals (Sallinen P 2008). 
 
The conclusion of this is that if you’ve had a heart attack immediately start supplementing melatonin as part of your recuperation and recovery. 
 
As far as preventing cardiovascular disease goes there is no direct evidence that melatonin is helpful; however melatonin has been shown to regulate one specific risk factor for cardiovascular disease and that is night-time hypertension. During the night owl blood pressure is supposed to naturally dip and it is known that in people who do not properly lower their blood pressure during the night there is a greater risk of cardiovascular events including/and heart attacks (Grossman E, et al. Melatonin reduces night blood pressure in patients with nocturnal hypertension. Am J Med 2006 October; 119 (10): 898-902). 
 
By reducing night-time high blood pressure nightly melatonin supplementation may also reduce one of the leading risk factors for stroke (7) and would therefore be a good idea for anybody suffering from high blood pressure or following a previous stroke.
You can find it suggested that supplemental melatonin may reduce damage to the brain following a stroke, however the dosages used were extremely high and by injection. (6) (7).
 

Migraine Preventing Effect of Melatonin

A study in 2004 study 3 mg of melatonin 30 mins before bed for 3 months achieved a 50% reduction in the number of migraines along with a reduction in the severity and duration of the headraces.  For a single remedy 50% is not bad, in my practice I combine several remedies, specific dietary changes, screen people for allergies and teach a relaxation technique that changes the level of stress hormones which can contribute switching on migraines. Each remedy/technique contributes something and combined together maximises the chances of success. 
Peres MF, Zukerman E, da Cunha TF, Moreira FR, Cipolla-Neto J. Melatonin, 3 mg, is effective for migraine prevention. Neurology. 2004 Aug 24;63(4):757
 

Melatonin in the Gastrointestinal Tract

It may surprise you to know but melatonin is not only produced in the perennial gland at night and perhaps more than 500 times as much melatonin is produced in our intestines. The stomach in particular needs a lot of protection from free radicals because of its constant exposure to strong stomach acid which generates storms of free radicals.
 
Melatonin can reduce the injury caused to the stomach by non-steroidal anti-inflammatory drugs, NSAIDs, such as aspirin by as much as 90% compared with controls and so is recommended for anyone taking these drugs long-term (Bandyopadhyay D at al. Melatonin protects against piroxicam-induced gastric ulceration. J Pineal Res. 2004 April; 36 (3): 195-203. And Reactive oxygen species-induced gastric ulceration: protection by melatonin. Curr Med Chem 2006; 13 (10): 1187-202.)
 
Research has shown that melatonin accelerates the healing of chronic ulcers by stimulating blood flow (Jaworek J at al 2005 at al. Melatonin as an organ protector in the stomach and pancreas. J Pineal Res. 2005 March; 38 (2): 73-83).
 
Supplemental melatonin has been shown to be a useful treatment for dyspepsia stop dyspepsia is stomach ache and indigestion characterised by recurrent pain in the upper abdomen, upper abdominal fullness, and feeling full earlier than expected when eating; it is often accompanied by the sensation of bloating, belching, nausea and heartburn. Gastro-oesophageal reflux where food or the stomach contents comes up ones throat. Antacid medications have been found to be no better than a placebo (Talley NJ at al 2005. Guidelines for the management of dyspepsia. Am.J Gastroenterology. 100 (10): 2324-37).
 
In a placebo-controlled trial 60 patients with dyspepsia were treated with either 5 mg of melatonin or a placebo, for 12 weeks in the evening. Of the melatonin treated group 57% showed complete resolution of symptoms and a further 30% had partial improvements; in the placebo group 93% of participants reported no change at all.  Besides melatonin studies in 2002 of herbal medicines such as peppermint, caraway and ginger, and a 2004 meta analysis (from three double-blind placebo-controlled studies) of a herbal formula called Iberogast to be significantly more effective than placebo in the treatment of dyspepsia. (Thompson Coon J, October 2002. Systemic review: herbal medicinal products for non-ulcer dyspepsia. Aliment. Pharmacol. Ther. 16 (10): 1689-99). (Melzer J at al December 2004. Meta analysis: Phytotherapy of functional dyspepsia with the herbal drug preparation STW 5 (Iberogast) Aliment. Pharmacol. Ther. 20 (11-12): 1279-87.
 
So in conclusion if you have dyspepsia (and you’ll need to get a proper diagnosis that differentiates your symptoms from other similar looking problems) you may obtain the best treatment by combining the herbal formula Iberogast with melatonin supplementation, a low inflammatory and high in antioxidant diet.   I have an information sheet treatment program for this.
 
For gastro-oesophageal reflux where the stomach contents leaks out of the stomach up into your throat or more properly the oesophagus, melatonin supplementation may also be useful.  When the acidic contents of the stomach leaks into the oesophagus the acid can burn the delicate walls of the oesophagus which are not designed to cope with stomach acid this can actually be a potentially dangerous condition that can lead to oesophageal cancer.  In a 2006 study (Periera et al) the effectiveness of alternative remedies were tested against standard drug therapy for the treatment of gastro-oesophageal reflux disease. 175 patients were given the standard drug treatment Omeprazole and the 176 received a combination of melatonin, L-tryptophan and B vitamins over a 40 day treatment period. All the patients in the melatonin supplement group reported complete regression of symptoms by the end of the study compared with only 66% in the drug treated group. (Pereira RS. Regression of gastroesophageal reflux disease symptoms using dietary supplementation with melatonin,
vitamins and aminoacids: comparison with omeprazole. J Pineal Res. 2006 Oct;41(3):195-200.

It is thought that melatonin has an anti-inflammatory and blood flow enhancing effect in the gastro-oesophageal (throat and stomach) walls.  ( Konturek SJ, Zayachkivska O, Havryluk XO, et al. Protective influence of melatonin against acute esophageal lesions involves prostaglandins, nitric oxide and sensory nerves. J Physiol Pharmacol. 2007 Jun;58(2):361-77.)
 

Osteoporosis

Data derived from animal research suggests that melatonin has beneficial effects on bone repair and remodeling, and bone mineral density, which would make it an ideal candidate for the prevention of osteoporosis or as adjuvant after bone fractures.
A very small, yet compelling recently published double-blind, placebo-controlled pilot study investigated the effects of melatonin on bone health and quality of life in 18 peri-menopausal women (ages 45-54) for 6 months. It found that melatonin improved physical symptom scores (e.g., feeling and sleeping better), increased osteocalcin (a marker for bone formation), and decreased levels of Type-I collagen cross-linked N-telopeptide (a marker for bone resorption), indicating that melatonin may restore imbalances in bone remodeling and prevent bone loss.  However, while the results from this small study appear clinically relevant, further investigation is warranted.
Kotlarczyk MP, Lassila HC, O'Neil CK, et al. Melatonin osteoporosis prevention study (MOPS): a randomized, double-blind, placebo-controlled study examining the effects of melatonin on bone health and quality of life in perimenopausal women. J Pineal Res. 2012 May;52(4):414-26.
Sleep and Jetlag Effect of Melatonin
 

Is Melatonin Safe?

Melatonin is very safe, toxicity has not been seen in doses as high as 200 mg/kg bodyweight in mice.
 

Dosageing and Format

If you have good sleep and when you take melatonin it doesn’t affect your sleep then you could just use the standard 1-3 mg Time release tablet to help your brain regeneration treatment, however if you have poor sleep or you find melatonin affect your sleep you can consider the below.
 
In humans, 90% of melatonin is cleared in a single pass through the liver. This is why those who use melatonin supplements to improve the length and depth of sleep may not find success, as over-the-counter melatonin supplements create a rapid blood spike that is rapidly washed out. Seabra MLV, Bignotto M, Pinto LR Jr, Tufik S. Randomized, double-blind clinical trial, controlled with placebo, of the toxicology of chronic melatonin treatment. J Pineal Res. 2000;29:193–200.
 
You should first experiment with dosages, try 0.3 mg (300 mcg), 1 mg, 3 mg, 5 mg and rarely up to 10 mg; you’re looking for the dosage that gives you the optimal effect on your sleep without any lingering drowsiness after-effects in the morning and also without producing nightmares which is a common indicator that you have taken either to higher dose for you need to switch to an alternative manufacturer. Once you have homed in on the right dosage experiment with different ways of delivering the melatonin to your system, if you have difficulty falling asleep you may do better with sublingual or instant release preparations, or liquids held under the tongue for sublingual delivery; alternatively if you have difficulty staying asleep you may do better with time-release products, if you have difficulty falling asleep and staying asleep you can take a mixed product or a mixture of instant release and time release.
 
Unfortunately to make matters even more complicated different brands may well affect you very differently, for example when I take Life Extension liquid melatonin I get great results however when I take Now Foods liquid melatonin it gives me a good sleep in the initial part of the night but then produces nightmares in the early morning, this is just how my brain responds to these products you may be different. Thankfully melatonin is cheap so I recommend buying a bunch of different melatonin preparations from different companies in different delivery systems so that you can work out how to use this very useful supplement, it’s worth putting in the effort.
 
I have worked out some ultra-low dose liquid melatonin I absorb through the skin to bypass the liver for a long sustained release which I use when I have time for a very long sleep, and others I use when I want a short but deep sleep.
 
If you have difficulty sleeping to book sleep called Sleep Better with Natural Therapies Available from Amazon which I discuss several techniques for improving sleep also available for private consultations.
I specialise in treating and coaching people with mental health problems how to obtain better mental health with natural remedies and self-help techniques. If you would like me to look into your individual case and develop a tailor-made programme of natural remedies, dietary advice and brain training exercises I’m available for private consultations at my London clinic and online for people that live too far away.
I also run regular meditation classes in London and online.
Click on the 
bookings tab to make an appointment.
I’m passionate about treating mental health and I’d be very happy to work with you.
 
References
  1. Tan, D-x.; Reiter, R.J.; Manchester, et al  Chemical and Physical Properties and Potential Mechanisms: Melatonin as a Broad Spectrum Antioxidant and Free Radical Scavenger
  2. : Current Topics in Medicinal Chemistry, Volume 2, Number 2, 1 February 2002 , pp. 181-197(17)
  3. Suzen S. Recent developments of melatonin related antioxidant compounds. Comb Chem High Throughput Screen. 2006 Jul;9(6):409-19
  4. Cardinali DP, Furio AM, Reyes MP. Clinical perspectives for the use of melatonin as a chronobiotic and cytoprotective agent. Ann NY Acad Sci. 2005 Dec;1057:327-36
  5. Miguel Pappolla at al Melatonin Prevents Death of Neuroblastoma Cells Exposed to the Alzheimer Amyloid Peptide . Journal of Neuroscience. 1 March 1997, 17 (5): 1683-1690.
  6. Isaac Antolin et al. Protective Effects of Melatonin in a Chronic Experimental Model of Parkinson’s Disease. Science direct, volume 943, issue 2, 12 July 2002.
  7. Reiter RJ, Tan DX, Leon J, Kilic U, Kilic E. When melatonin gets on your nerves: its beneficial actions in experimental models of stroke. Exp Biol Med (Maywood.). 2005 Feb;230(2):104-17.
  8. Scheer FA, Van Montfrans GA, van Someren EJ, Mairuhu G, Buijs RM. Daily nighttime melatonin reduces blood pressure in male patients with essential hypertension. Hypertension. 2004 Feb;43(2):192-7.
  9. Cagnacci A, Cannoletta M, Renzi A, et al. Prolonged melatonin administration decreases nocturnal blood pressure in women. Am J Hypertens. 2005 Dec;18(12 Pt 1):1614-8
  10. .
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Hi my name is Peter Smith I specialise in treating and coaching people how to live well with mental health problems, digestive health problems/IBS, sleep problems and type II diabetes using natural therapies.
I used these techniques to overcome and live well with my own bipolar disorder and IBS. I've been in practice as a natural medicine practitioner since 1988.
 

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If you’d like treatment for any of the issues discussed in this article I specialise in treating and coaching people how to obtain better mental health with natural remedies and self-help techniques. If you would like me to look into your individual case and develop a tailor-made programme of natural remedies, dietary advice and brain training exercises I’m available for private consultations and I’m available for private consultations at my London clinic and online for people that live too far away.
I also run regular meditation classes in London and online.
I’m passionate about treating mental health and I’d be very happy to work with you.
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