Melatonin (N-acetyl-5-methoxytryptamine) is a naturally occurring hormone produced by the pineal gland in our brains. Melatonin helps regulate our circadian rhythm (body clock) which dictates our sleep/wake cycles. It plays a critical role in helping us fall asleep and stay asleep throughout the night. It also regulates the release of hormones that control body temperature, hunger, energy and even mood. It may also have a roll in the biological regulation tumour growth, aging and perhaps reproduction.
In the biosynthesis of melatonin, tryptophan is converted to 5-hydroxytryptophan, which is then decarboxylated to serotonin (an important neurotransmitter). Serotonin is then catalysed by two enzymes to form melatonin. In humans, melatonin secretion increases soon after the onset of darkness, peaks in the middle of the night (between 2 and 4 am), and gradually falls during the second half of the night. Serum levels of melatonin are known to decrease with age which may contribute to the increased frequency of sleep disorders in the elderly and the aging process itself.
There are many benefits of supplementing declining levels of melatonin which include:
Research has shown that many patients with insomnia have decreased nocturnal melatonin secretion. This is especially the case in the elderly which have only half the amount of melatonin released compared to that of young adults. Several studies have shown that insomnia may be effectively treated by supplementing melatonin. Melatonin has been found to decrease the time needed to fall asleep and increase the total sleep time. It also profoundly effects the quality of sleep we experience. Melatonin has been shown to promote dreaming REM (rapid eye movement) sleep which is of paramount importance for quality sleep. Increases in daytime alertness and decreased midafternoon tiredness were also reported. Melatonin has also been reported to be effective in treating chronic insomniacs, frequent night awakenings, delayed sleep phase insomnia and waking too early.
Melatonin is not addictive, does not produce tolerance, is not abused, and does not possess the side effects commonly observed with other synthetic sleeping pills (Benzodiazepines). Melatonin produces a very natural desire for sleep rather than a heavy “drugged” sedation caused by synthetic sleeping pills. It does not interfere with normal sleep cycles and thereby disrupt the pattern of REM and NREM sleep unlike all other sleeping pills which are known to disrupt normal sleeping patterns. Melatonin actually treats the cause of insomnia by correcting any circadian rhythm imbalance that prevent a good night’s sleep rather than sleeping pills which only treat the symptoms.
Conditions related to circadian rhythms such as jet lag, night-shift work, seasonal effective disorder (winter depression) and delayed-sleep-phase syndrome respond well to melatonin supplementation.
Melatonin has been shown to be a powerful protector against cancer and also a effective treatment against certain cancers (breast, prostate and skin cancers). It strengthens your immune system’s ability to spot and destroy abnormal cells that may turn cancerous, and it prevents the age related decline in immunity that leaves you vulnerable to cancer. When combined with traditional chemotherapy it has shown to improve the performance of anticancer drugs, but can also lessen the severity of side effects. Melatonin may enhance the action of chemicals called endorphin’s produced by the body as a natural pain killers making the patient feel better. Melatonin has also been shown to protect bone marrow from the devastating effects of chemotherapy.
Melatonin has been shown to be more effective than any other known antioxidant in protecting against oxidative damage. Free radicals cause accumulated damage to our cells resulting with the aging process, heart disease, cancer, cataracts and immune impairment to mention a few. By supplementing with a potent antioxidant such as melatonin many of these diseases may be avoided.
Melatonin supplementation may slow the aging process due to its potent antioxidant effects preventing further cellular damage. It may also help by preventing the disruption of the pineal glands regulatory function, which occurs with age, that weakens the immune system contributing towards degenerative disease and eventually death.
Melatonin has been shown to normalize elevated serum cholesterol levels which can prevent the formation of plaque deposits that can clog arteries and block the flow of blood. It does this by encouraging the breakdown of the thyroid hormone T 4 to T 3 which is able to breakdown and utilize cholesterol more effectively. Melatonin has also been shown to protect against high blood pressure. It does this by normalizing the level of kidney hormones, aldosterone and renin, which control sodium retention and blood volume and other factors that control blood pressure. Melatonin can also protect the heart from the devastating effects of stress by decreasing the production corticosteroids and thus help dampen their effects on the heart. And finally its potent antioxidant effects helps protect the heart from oxidative damage.
Melatonin helps prevent the decline in thyroid function that occurs later in life by keeping the thyroid gland active and functioning normally.
Melatonin inhibits 5-alpha -reductase, an enzyme responsible for converting testosterone into dihydrotestosterone (DHT). DHT is believed to enlarge the prostate so by reducing its level the prostate is protected. Melatonin also protects against atherosclerosis which is the leading cause of impotency.
Melatonin is currently being investigated as a treatment for many different disease states such as asthma (melatonin as a bronchodilator), diabetes (melatonin prevents insulin resistance) and Down Syndrome (melatonin improves immune function).
Melatonin use has been proven to be very safe exhibiting very few side effects. Less than 5% of people experience vivid dreams and morning grogginess which can be eliminated with a reduction in the dose. Even at very high doses of 6.6g (2000 times the normal dose) taken daily for over a month reported no short or long term toxicity. Melatonin has been successfully used over the past two decades or so by hundreds of thousands of people throughout America and Europe, and more recently in Australia, with a very impressive track record.
Unfortunately very few doctors are aware of melatonin because it is not listed in their desk top medical reference books. This is because being a natural hormone it cannot be patented so there are no financial incentives for pharmaceutical companies to do the very expensive research and development to register it as commercial product. As most medical reference books only list registered products providing medical practitioners with information supplied by pharmaceutical companies melatonin is omitted from these texts. The development of dosage protocols has therefore been left up to pioneering medical doctors in America and Europe.
Melatonin has a short serum half-life of only 40 to 50 minutes; serum concentrations peak within 20 minutes and then fall rapidly. In order to maintain effective serum concentrations throughout the night slow release capsules are essential. They avoid large fluctuations in serum levels and prevent waking in the middle of the night due to lingering melatonin levels. Research has shown that normal fast release melatonin only improves sleep initiation but does not increase sleep maintenance, unlike slow release melatonin. To maintain effective concentrations of the normal fast release melatonin throughout the night high doses or repeated low-dose administration is required.
In Australia therapeutic doses of Melatonin are only available with a doctors prescription although is available over the counter in many other countries. A homeopathic version of melatonin is available in health food stores and is often mistaken for the real therapeutic dose. In this case the tablets are labelled 3mg 6X which means it contains one millionth of a 3mg dose obtained through six serial dilutions. For those body types not sensitive enough for homeopathics to be effective this dose is far to small to have any real benefit.
Melatonin should only be taken at night
Melatonin should only be taken at night about half an hour before bed and taken no later than 3 am. It must not be taken throughout the day as it will alter your natural sleep/wake body cycle. The appropriate dose can vary from person to person. It is recommended to start taking 3 mg at night and then adjusted the dose from there. If morning drowsiness occurs reduce the dose by half. If the dose had little or no sleep-inducing effect then increase the dose by 3 mg each night until the desired effect is achieved. Most people get good results with doses between 3 and 10 mg. Some sensitive individuals find that they respond better by reducing the dose and often get better results on 0.5mg to 1mg at night.
Insomnia or Restless Sleep
3 – 10 mg (usually 2- 3mg) given half an hour before bed for two to four weeks to reset the body clock. Elderly patients may require ongoing treatment to compensate for naturally declining levels.
If you take a trip that involves travel across time zones take 3 to 5 mg prior to bedtime once you reach your new destination. Continue to take it at bedtime for 4 nights until your body clock is completely reset.
10 – 20 mg every night.
Drug Induced Insomnia
Certain drugs can disrupt melatonin production and thus cause sleep disorders. Benzodiazepines (Serepax, Valium, Normison, Mogadon), b -Blockers (Betaloc, Tenormin), nonsteroidal anti-inflammatory drugs (aspirin, neurofen) and recreational drugs (amphetamines, alcohol) inhibit melatonin production or disrupt normal night time melatonin cycles which may exacerbate or cause sleeping disorders. Do not stop taking these drugs but talk to your doctor about other treatment options to avoid these side effects.
Supplementation with tryptophan may cause an increase in melatonin production so should be used with care if taking melatonin. A synergistic effect may be observed between melatonin and narcotics and tranquillisers so dose adjustments may be necessary.
The timing of melatonin doses are crucial for effective use. As previously mentioned it must only be taken at night no later than 3am. Because melatonin may increase the immune system it may have adverse effects in people with conditions involving an overactive immune system such as lupus, rheumatoid arthritis, multiple sclerosis, etc. It should not be used before puberty as declining levels of melatonin are believed to trigger the onset of puberty. Its use should also be avoided during pregnancy and lactation. If you are under the age of 40 the use of melatonin on a regular basis is not recommended as younger people generally have sufficient levels.
Side effects are uncommon with doses below 3 mg however the most common side effects include:
- Daytime sleepiness
A reduction in dose often overcomes these side effects.
Other, less common side effects might include abdominal discomfort, mild anxiety, irritability, confusion and short-lasting feelings of depression.
Insomnia in many cases can simply be caused by stress or an overactive mind. Simple meditation techniques before bed can help reduce stress and help calm a busy mind and thus place it in a more receptive state to sleep. This technique addresses the cause of insomnia rather than treating the symptoms.
Other Causes of Insomnia
Insomnia can also be caused by a variety of other factors which will require investigation in order to treat the cause. Commonly we see many women in their late 30’s and into their 50’s entering perimenopause or in menopausewith ongoing sleeping problems. These are usually hormone related and by balancing their hormones we are able to effectively treat the insomnia.
5-HYDROXYTRYPTOPHAN for Melatonin Production – Non Prescription
The amino acid metabolite of tryptophan called 5-hydroxytryptophan (5-HT) may also be used before bed to help increase the bodies own production of melatonin. Doses of 100 – 300mg before bed can help treat insomnia.