Melatonin is produced by the pineal gland, a small endocrine gland a located near the center of the brain.
Philosophers and mystics throughout time have referred to the pineal gland as the “third eye.” The French philosopher Descartes even declared that the pineal gland is the seat of the human soul. Because of its special location near the center of the brain, between the two hemispheres, some people still attribute a special power to the pineal gland and associate it with the sixth chakra (also called Ajna or the third eye chakra in yoga).
Some also believe that it is a dormant organ that can be awakened to enable telepathic communication.
As it turns out, scientists now know that the pineal gland is a small endocrine gland about the size of a pea that, in addition to producing the hormone melatonin—which regulates our internal body clock and sleep cycle, is stimulated by darkness and inhibited by light.1
How does melatonin work?
Melatonin levels peak at about 2 a.m. in normal, healthy young people and about 3 a.m. in elderly people. The maximum amount of melatonin released in the bloodstream of the elderly is only half of that in young adults, which is why many scientists and health professionals believe that melatonin levels are a good marker of aging and longevity.
Melatonin levels are low during the day. At sunset, the cessation of light triggers neural signals which stimulate the pineal gland to begin releasing melatonin. This rise continues for hours, eventually peaking around 2 a.m. (3 a.m. for the elderly), after which it steadily declines to minimal levels by morning. The delay in timing and decrease in intensity of the melatonin pulse is a result of the aging process. 2
Why does jet lag make you feel so lousy?
The melatonin pulse regulates many neuroendocrine functions. When the timing or intensity of the melatonin peak is disrupted—as in aging, stress, jet lag, working the night shift, or staying up all night—mental and physiological functions are adversely affected. And if you’ve ever been on a trans-continental flight, pulled an all-nighter, or worked the night shift, you know exactly what we’re talking about. Your mind doesn’t work as clearly as usual, you forget details and facts, you may feel irritable and have trouble making decisions—all because your biological clock isn’t ticking the way it normally does.
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Work and other activities that disrupt the normal circadian cycle in a way similar to jet lag are said to cause “artificial jet lag.” But if you take melatonin in the evening (in the new time zone that you’ve traveled to, for instance) it will rapidly reset your biological clock and almost totally alleviate—or prevent—the symptoms of jet lag. The ability of melatonin to alleviate jet lag was demonstrated in a study of 17 people flying from San Francisco to London, eight time zones away. Eight of the subjects took 5 mg of melatonin, while nine subjects took a placebo. Those who took melatonin had almost no symptoms of jet lag. Six out of nine placebo subjects scored above 50 on the jet lag scale, and all of the melatonin subjects scored below.3 Most people sleep well with melatonin, and wake up the next day refreshed with no symptoms of jet lag 4 —although they may still have some fatigue from the wear and tear of traveling.
Whether you experience jet lag or artificial jet lag, studies show that if you take melatonin in a low dose before sleep, it increases your circulating melatonin levels to those normally observed at night, so that you can fall asleep, stay asleep, and wake up feeling refreshed instead of groggy.5
Melatonin is a powerful antioxidant
Melatonin supports a lot more than normal sleep patterns, and the ability to function and think clearly. Scientists have discovered that it’s a powerful antioxidant that helps protect us from infection, inflammation, and autoimmunity.6,7 Additionally, many believe that suppression of melatonin by light at night (experienced by night-shift workers) is a possible risk factor for developing a serious illness.8
In fact, a paper recently published in Neuroendocrinology Letters says that disruption of the circadian rhythms caused by over-exposure to light at night—because of both night work and as a personal choice and life style—has been associated with cancer in humans. And there’s evidence of increased breast and colon cancer risk in shift workers. Interestingly, the author of this paper, as well as other studies, found that cancer growth was inhibited in laboratory animals that were treated with melatonin.8,9,10
Melatonin extends longevity
Although the studies have only been done on animals, melatonin has been shown to improve immunity and extend lifespan.10,11 In one study, middle-aged animals were given melatonin each evening. The treated animals became healthier, and exhibited better posture, increased activity levels, more lustrous fur, and lived an average of 20% longer than the control animals.12
In a recent study, animals with leukemia that were treated with melatonin had a survival rate of 30-40% versus animals that were untreated and had a 0% survival rate.13
Melatonin and the elderly
The animal longevity study makes perfect sense and would seem to correlate to humans as well, since melatonin is a potent free radical scavenger, and disease is caused by free radical damage. Also, as we age our melatonin levels decrease—which may be one of the contributing factors to age-related disease and poor sleeping patterns. Although melatonin hasn’t been called a rejuvenating supplement—yet—it appears that it can be significantly beneficial to the elderly and to the aging process for these reasons:
- The amount of melatonin that is secreted by the pineal gland falls gradually over one’s lifetime.
- Melatonin was recently discovered to be a potent antioxidant and oxidative stress is believed to be a contributor to aging, as well as to age-related diseases such as Alzheimer’s and Parkinson diseases.
- Melatonin is naturally produced by the body as a sleep-inducing agent, and its reduced concentrations may result in insomnia and/or sleep disturbances, which are very often associated with advancing age.
- Melatonin is a natural immune enhancer, and as we age the immune system seems to work less efficiently.14,15
Alleviates SAD and depression
Two particularly notable features of depression and seasonal affective disorder (SAD) are diminished nighttime release of melatonin and abnormal sensitivity to melatonin suppression by light. This has led researchers and health practitioners to try melatonin as an experimental treatment for depression, with good results.2,16,17
Relieves migraine headaches
The pineal gland and melatonin have even been implicated in how a migraine is triggered. Many people who suffer from migraines are susceptible to various environmental triggers that influence the secretion of melatonin from the pineal gland. Studies have also shown abnormalities in melatonin secretion in patients who experience migraines and that they show an improvement after taking melatonin.18
A recent study at a neurological center in Naples, Italy, interestingly found that melatonin alleviates what’s known as a hypnic headache. This is a rare sleep-associated headache disorder, usually affecting elderly people. The headaches can appear single or multiple in one night, occur exclusively during sleep, and tend to occur at a consistent time each night, sometimes during a dream.19
The list of possible benefits of melatonin supplementation continues to grow
Melatonin has also been shown to be beneficial for these conditions:
- Alzheimer’s disease, especially for sleep disorders and during the period called “sundowning,” when patients become agitated during late afternoon and early evening20
- Gastric ulcers21
- Hot flashes in menopausal women because melatonin suppresses luteinizing hormone (LH) in postmenopausal women22
- Cardiovascular disease, since melatonin helps regulate nitric oxide production, which plays a vital role in ensuring proper cardiovascular function23
- ADD and insomnia in children24
The Importance of Sleep
Scientists know that sleep is as important as food and air, and the quantity and quality an individual gets is also extremely important. Six and one-half to seven hours of uninterrupted sleep seem to be the magic number for a lot of people. Interestingly, research shows that sleeping more than eight hours may have deleterious effects, although the reasons for this are less clear. According to data from the Cancer Prevention Study II, individuals who average seven hours of sleep each night have a lower mortality rate than do those who sleep eight hours or more.1
“The lowest [mortality] group actually slept between six and one-half to seven and one-half hours.”
Daniel F. Kripke, MD, a Professor of Psychiatry at the University of California, San Diego
“The major mortality risk associated with habitual sleep duration is among long sleepers, by which I mean those sleeping eight hours or more. Incidentally, calling them long sleepers is accurate, because from the new data we know that the average American on weekdays sleeps about six and one-half hours.”
Specifically, he said, individuals who slept eight hours per night were 12% more likely to die within six years than were those who slept seven hours. The highest mortality rates occurred among men and women who slept more than eight and one-half hours. This group had at least a 15% increased risk of death, said Dr. Kripke. As for short sleep, men who slept less than four and one-half hours and women who slept less than three and one-half hours also had at least a 15% increased risk of death. Dr. Kripke presented his findings at the 16th Annual Meeting of the Associated Professional Sleep Societies.2
How much should you take?
The appropriate dose can vary enormously from person to person. Some users will feel great with a few hundred micrograms, and others will need a few thousand micrograms, others take 1.5 to 3 milligrams. Several intelligent melatonin users we know started by taking 3 mg at 11 p.m., and then adjusted the dose from there. If they found that they slept well but were drowsy in the morning, they cut the dose in half. If they found the dose had little or no sleep-inducing effect, they increased the dose by 3 mg each night until they got the desired effect. We have received reports from people who gets good results with less than 1 mg, and others use it in the vicinity of 3 mg.2
Timing may be crucial for the most effective use of melatonin. Individual differences in the absorption and metabolism of melatonin may account for the differences in effectiveness. When you take melatonin seems to be much more critical than when you take other supplements. One melatonin user reported that he gave himself terrible jet lag by absent-mindedly taking melatonin at 3 a.m. after staying up late. He recovered from his error, resetting his circadian rhythm back to normal with melatonin at 10 p.m. the following evening, but not before he had to spend an entire day experiencing the lousy, dull “jet lag hangover.” 2
Additionally, some people take melatonin and fall asleep for a few hours and wake, unable to fall back asleep. Using time-released melatonin may help by mimicking the natural release during sleep.
But again, if you take too much time-released melatonin, or time-released melatonin with an inconsistent release pattern, this can actually cause jet lag type symptoms by providing a melatonin peak at the wrong time. So you’ll need to experiment a bit to see what best suits your needs. Your best bet is to follow the directions on the label and go from there.
There’s a lot we know about melatonin supplementation and there’s a lot more for scientists to discover. We know that it can help with sleep and jet lag problems, and that it’s a potent antioxidant that is proving to be beneficial for numerous health problems including depression and cancer. It also shows great potential as an anti-aging supplement.
Although you may find that you need to experiment with dosage, start out by taking the recommended dosage on the label before sleep. And if you’re curious to know how much melatonin you are producing, you can order a saliva test that you can do right in the privacy of your home.
We recommend ordering from:
Direct Laboratory Services
300 Mariners Plaza
Mandeville, LA 70448
Whether you need help sleeping through the night, feeling good while traveling across time zones, or just want to boost your immunity and possibly add some years to your life, you can’t go wrong with melatonin.
- Axelrod J. The pineal gland. Endeavour. 1970 Sep;29(108):144-8.
- Dean, W., Morgenthaler, J. Fowkes, SW. Smart Drugs II: The Next Generation. Smart Publications, Petaluma, CA, 1993.
- Leger D, Laudon M, Zisapel N. Nocturnal 6-sulfatoxymelatonin excretion in insomnia and its relation to the response to melatonin replacement therapy. Am J Med. 2004 Jan 15;116(2):91-5.
- Arendt J, Aldhous M and Marks V. Alleviation of jet-lag by melatonin: Preliminary results of controlled double-blind trial. Brit Med J. 1986: 292: 1170.
- Zhdanova IV, Tucci V. Melatonin, Circadian Rhythms, and Sleep. Curr Treat Options Neurol. 2003 May;5(3):225-229.
- Arendt J. Melatonin and human rhythms. Chronobiol Int. 2006;23(1-2):21-37.
- Carillo-Vico A, Reiter RJ, Lardone PJ, Herrera JL, Fernandez-Montesinos R, Guerrero JM, Pozo D.The modulatory role of melatonin on immune responsiveness. Curr Opin Investig Drugs. 2006 May;7(5):423-31.
- Anisimov VN. Light pollution, reproductive function and cancer risk. Neuro Endocrinol Lett. 2006 Apr 25;27(1-2):35-52; [Epub ahead of print].
- Anisimov VN, Popovich IG, Zabezhinski MA, Anisimov SV, Vesnushkin GM, Vinogradova IA. Melatonin as antioxidant, geroprotector and anticarcinogen. Biochim Biophys Acta. 2006 Apr 17; [Epub ahead of print].
- Regelson W., Pierpaoli W. Melatonin: a rediscovered antitumor hormone? Cancer Investig 5:379-385, 1987.
- Pierpaoli W, Changxian VI and Dall’aza A. Aging: Postponing effect of circadian melatonin: Experimental evidence, significance and possible mechanism. InternJ Neuroscience 51:334-342, 1990.
- Maestroni GJ, Conti A, Pierpaoli W. Pineal melatonin, its fundamental immuno-regulatory role in aging and cancer. Ann NY Acad Sci 521: 140-8, 1988.
- Miller SC, Pandi PS, Esquifino AI, Cardinali DP, Maestroni GJ. The role of melatonin in immuno-enhancement: potential application in cancer. Int J Exp Pathol. 2006 Apr;87(2):81-7.
- Poeggeler B. Melatonin, aging, and age-related diseases: perspectives for prevention, intervention, and therapy. Endocrine. 2005 Jul;27(2):201-12.
- M. Karasek, R.J. Reiter: Melatonin and aging 2002; 23 (suppl 1):14-16 pii:NEL230702R03 PMID: Neuroendocrinology Letters (NEL).
- Lewy AJ, Lefler BJ, Emens JS, Bauer VK. The circadian basis of winter depression. Proc Natl Acad Sci U S A. 2006 May 9;103(19):7414-9. Epub 2006 Apr 28.
- Brown GM. Psychoneuroendocrinology of depression. Psychiatr J Univ Ott 14(2): 344-8; Jun 1989.
- De Simone R, Marano E, Ranieri A, Bonavita V. Hypnic headache: an update. Neurol Sci. 2006 May;27 Suppl 2:S144-8.
- Vogler B, Rapoport AM, Tepper SJ, Sheftell F, Bigal ME.Role of melatonin in the pathophysiology of migraine : implications for treatment. CNS Drugs. 2006;20(5):343-50.
- D.P. Cardinali, L.I. Brusco, C. Liberczuk & A.M. Furio: The use of melatonin in Alzheimer’s disease 2002; 23 (suppl 1):20-23 pii:NEL230702R04 PMID: Neuroendocrinology Letters.
- Bandyopadhyay D, Chattopadhyay A. Reactive oxygen species-induced gastric ulceration: protection by melatonin. Curr Med Chem. 2006;13(10):1187-202.
- Kripke DF M D, Kline LE D O, Shadan FF M D Ph D, Dawson A M D, Poceta JS M D, Elliott JA Ph D. Melatonin effects on luteinizing hormone in postmenopausal women: A pilot clinical trial NCT00288262. BMC Womens Health. 2006 May 16;6(1):8. [Epub ahead of print).
- Aydogan S, Yerer MB, Goktas A.Melatonin and nitric oxide. J Endocrinol Invest. 2006 Mar;29(3):281-7.
- Weiss MD, Wasdell MB, Bomben MM, Rea KJ, Freeman RD. Sleep hygiene and melatonin treatment for children and adolescents with ADHD and initial insomnia. J Am Acad Child Adolesc Psychiatry. 2006 May;45(5):512-9.
- Kripke DF, Garfinkel L, Wingard DL, et al. Mortality associated with sleep duration and insomnia. Arch Gen Psychiatry. 2002;59:131-136.