Product Information

Melatonin regulates the sleep-wake cycle, allowing the body to benefit from a good night’s sleep

Melatonin is secreted by the pineal gland, a pea-size structure at the center of the brain, as our eyes register the fall of darkness. At night, Melatonin is produced to help our bodies regulate our sleep-wake cycles. The amount of Melatonin produced by our body seems to lessen as we get older. Scientists believe this may be why young people have less problem sleeping than older people.

Melatonin's main use has been to regulate sleep and circadian rhythms and allow the individual to feel more refreshed and alert the following day. As Melatonin is directly involved with sleep regulation, the supplement's use in the treatment of age-related sleep disorders, jet lag or shift work is impressive. Furthermore, Melatonin has also been shown to improve the condition of Seasonal Affected Disorder (SAD).

Antioxidant effects

As an antioxidant, Melatonin has been shown in vitro to be a highly efficient scavenger of the very reactive and toxic hydroxyl radical. Indeed, on an equimolar basis, Melatonin proved significantly more efficient in neutralizing the hydroxyl radical than the two well-known scavengers, glutathione and mannitol. Likewise, Melatonin was found to also scavenge the peroxyl radical which is generated during lipid peroxidation; in this regard it was roughly twice as effective as vitamin E (alpha-tocopherol).

Melatonin’s antioxidant activities have been well documented. When rats are treated with the chemical carcinogen safrole, this agent induces the generation of free radicals which in turn extensively damage nuclear DNA; this damage is almost totally eliminated if the animals are cotreated with Melatonin. Also, damage to DNA in human lymphocytes due to ionizing radiation, another treatment which is known to induce free radical formation, is greatly reduced if the cells are treated with Melatonin prior to radiation. Cytosolic protein seems also to be protected from free radical damage when melatonin is present. When newborn rats are treated with a glutathione-depleting drug at birth, by 2 weeks of age the animals have cataracts. Cataracts form because oxidants damage protein in the presence of low intracellular levels of glutathione. Cataracts induced by this means are essentially prevented if the glutathione-depleted rats are supplemented with Melatonin.

Finally, membrane lipid peroxidation, induced either in vivo or in vitro by any of several means, all of which involve free radicals, is drastically attenuated in the presence of Melatonin. Considering Melatonin’s ability to cross all morphophysiological barriers and to enter every cell, and all subcellular compartments, the implication is that this indole may play a very important role in the antioxidative defense system of the organism. These findings potentially have important implications for a wide variety of age-related diseases and to aging itself.

Anti-aging effects

Tests on both rats and mice Melatonin caused a significant 20% increase in their lifespan. If Melatonin does allow you to live longer and healthier it could be because Melatonin reduces free radical damage; stimulates an aging immune system; protects the cardiovascular system; preserves a youthful circadian rhythm; and stimulates the production of growth hormone. For these reasons, Melatonin is considered to be a vital anti-aging substance.

Whilst some Melatonin supplements have become widely available, IAS offes a specific type, that has been formatted by Dr. Pierpaoli called TI-MElatonin®. It is a pharmaceutical grade Melatonin that is bonded with selenium and zinc. These substances work synergistically with Melatonin and produce a much greater affect (even by themselves, zinc and selenium are important anti-aging supplements).

If you've tried other Melatonins and didn’t notice a significant effect, try TI-MElatonin®, and you’ll soon feel the difference.

Dosage:
Take half to one (maximum two) 3mg tablets at bedtime only. Only use Melatonin ® when you are prepared to sleep and have the light switched off, this is because light entering the eye destroys Melatonin.

Side effects:
A small number of users experience varying degrees of nightmares, headaches, morning groginess, mild depression and low sex drive.

Caution:
Should not be used by women who are pregnant or nursing (since no one knows how excessive exposure to the hormone might affect a fetus or infant); people with severe allergies or autoimmune diseases (Melatonin could exacerbate such conditions by stimulating the immune system); people with immune-system cancers such as lymphoma or leukemia (for the same reason), and healthy children (who already produce it in abundance). Women trying to conceive should also think twice about taking the hormone, since high doses can act as a contraceptive.

Manufacturer's Insert

MELATONIN ®

Melatonin: Biological effects and scientific information:
Melatonin expresses the best imaginable melatonin preparation available on the world-market and is now available as a food additive and dietary supplement to anybody wanting to take advantage of the extraordinary scientific observations of Dr. Walter Pierpaoli and his co-workers. The basic experimental findings of 35 years of research, resulted in the discovery of the undeniable existence of a programmed “Aging Clock” in the pineal gland complex of the brain. We have investigated the possible mechanisms and also the molecules which presumably cooperate and synergize with melatonin in the regulation and re-synchronization of the fundamental immunological and hormonal functions, (which are normally lost or deranged in the course of aging). In recent studies and long-term experiments with old rodents it has been observed that zinc can completely correct aging-dependent immuno-depression and several other hormonal and metabolic alterations typical of aging. It has been found that the low zinc levels in aging animals can be restored to normal values with nocturnal administration of melatonin or transplantation of the pineal gland from young animals into older animals6-9. Zinc is an essential component of more than 200 enzymes and one of the most relevant trace elements in the body8,9. It is therefore clear that additional zinc must be supplemented daily to the body of an aging organism with a low zinc balance, in-order that melatonin can better exert its anti-aging activities on the entire neuroendocrine and immune systems! This important and novel scientific observation of the powerful anti-aging and immuno-enhancing activity of the combination of zinc and melatonin has now resulted into the development of Melatonin. Furthermore, selenium is a fundamental trace element of the body and possesses powerful anti-cancer effects. But modern agriculture and alimentary habits have dramatically decreased the daily input of selenium from the diet. Selenium is essential for the enzymatic reaction responsible for the synthesis of glutathione, a powerful physiological molecule which constantly protects the body from oxidative damage. A lack of selenium will thus result in a loss of the detoxification capacity of the body, immuno-depression and onset of degenerative diseases and cancer10. This is the reason why Melatonin combines, (in a unique synergistic combination), the three fundamental anti-aging molecules of melatonin, zinc and selenium. Whilst melatonin plays the master role for reactivation and restoration of its natural night peak to juvenile levels, (this resulting into normalization of all measurable immunological and endocrine functions in the course of aging), the positive age-postponing, metabolic and immunological effects of Melatonin can be measured easily by anybody with a normal periodic check-up! These restoring metabolic changes will become progressively more visible and remarkable over the course of years, after initiation of the treatment with Melatonin. Further studies are now in progress and they will allow us to progressively add more elements suitable to further improve and accelerate the rejuvenizing effects of nocturnal melatonin. But the “programme of aging” can be slowed down now to a more acceptable rate with regular nocturnal use of Melatonin.

Melatonin: Composition of active components in each tablet:
Melatonin (N-acetyl-5-methoxytryptamine), 3mg, synthetic, certified purity: (99.9 % (HPLC), Zinc-orotate x 2H2O, 50mg corresponding to 8.7mg zinc. Selenium, 50mcg, from sodium selenite pentahydrate. Melatonin is produced in Switzerland in compliance with the severe international rules of Good Manufacturing Practise (GMP) and under licence of Swiss Health Authorities.

Contraindications and general suggestions:
Melatonin should not be given to healthy children, pregnant women and lactating mothers unless specifically prescribed by a physician. There is no evidence that Melatonin could adversely influence the effects and activity of estrogens. On the contrary, melatonin increases the density of estrogen receptors in sensitive target tissues (mammary gland, womb, ovaries, etc.) and greatly improves their actions. There are no contraindications for dietary supplements containing melatonin, zinc and selenium. No ascertained, life-threatening, acute or moderate, short- or long-term side-effects have been scientifically demonstrated or reported. Melatonin must be taken late in the evening at bedtime in order to mimic and restore the physiological night peak, which normally declines progressively during the course of aging. As mentioned in the literature reported above, the progressive abrogation of melatonin night-cyclicity during aging is considered to be a basic signal expressing the extinction of the most fundamental regulatory system in the body. This brain “clock” is genetically and evolutionary linked to the sun, the planetary system and the obvious dependence of our health from daily and nocturnal, rhythmic cyclicity. Every person expresses their own genetically inherited nocturnal peak of melatonin, with very large individual variability. However, in the majority of the population, the night elevation of melatonin declines and most of us become “flat” after 80 years of age. This is a basic aging message from the “clock”11. The dosage of melatonin is still rather empirical and based on animal and human studies. The blood night level generated by 3mg by far exceeds the normal night levels of healthy young persons. However, melatonin is rapidly metabolized and excreted by the kidneys with no consequences. Use of beta-blockers in the evening may abrogate the night peak of melatonin. If they must be taken, it may be necessary to take them in the morning or to increase the dosage of melatonin. Circadian, night melatonin seems to produce a resynchronization of the entire neuroendocrine system and will certainly improve metabolic and hormonal functions, including blood pressure, cholesterol levels, thyroid, gonadal and adrenal functions. These effects can be easily evaluated with a routine check-up. Melatonin will counteract the negative side-effects of cortico-steroids and of di-stressful agents, thus protecting the immune system. Melatonin does not induce sleep but facilitates its onset and produces a sleep pattern which is typical of children or young persons. It greatly improves the quality of sleep and its restoring physical and psychological effects, with a clear improvement of morning mood and body muscle strength. Melatonin is not a drug and it is not itself a cure for any disease! Melatonin is ubiquitous in nature, cells, plants, animals, tissues and any living organism. Milk, vegetables, cereals, rice, meat, etc., contain variable amounts of melatonin. Synthetic melatonin could be theoretically replaced by alimentary melatonin in the daily food, but its replacement would be problematic and difficult to achieve for everybody. Melatonin produced by the pineal gland seems to be responsible for the night peak, while melatonin produced by the gut and the retina does not seem to affect the nocturnal levels. It is thus evident that the night peak of melatonin initiates a sequence of positive effects with a cascade of events which maintain the body systems synchronized with the physiological cyclicity of hormones and cells. This night “signal” is essential for the maintenance of immunity and the “surveillance” against the onset of tumors. Therefore melatonin is a fundamental element for prevention of aging-related diseases, including cancer, autoimmune and cardiovascular diseases. Melatonin cannot be considered a classical “hormone,” although it is so-named. It does not possess any of the qualities of the classical hormones like growth hormone, cortisol, estrogens, thyroid hormones etc. It is rather a chemical mediator whose mechanism is still unknown. It modulates and controls the synthesis and secretion of all hormones within a circadian and seasonal periodicity and variability. It has been given at a huge dosage of grams daily for prolonged periods, and to 1500 women at the daily dosage of 300mg for years with no observed late side-effects and consequences. The administration of melatonin to restore the physiological adaptation of the body to circadian and seasonal periodicity is only the beginning of a new medicine based on the concept that nobody can escape the established laws of Nature within the solar-planetary system, in which man developed as a mammalian species. We must be able to restore and correct the derangements of this adaptation system and maintain it in its original juvenile conditions. These metabolic conditions can be perfectly measured and maintained under balance, not with a cumbersome and complex hormonal supplementation (e.g. testosterone, growth hormone, pregnenolone, etc.), but with a correction of the central regulatory system located in the “pineal complex” (pineal gland and the many anatomical and functional connections in the brain and the neuroendocrine-immune systems). Melatonin is perfectly suitable to re-synchronize all neuroendocrine functions. Melatonin contains basic elements which will synergize in order to obtain more rapid effects and to compensate the loss of fundamental minerals, due to a wrong diet or to aging. The beneficial effects of melatonin in the normalization of zinc levels have been scientifically proven and constitute a basic tool for maintenance of hormonal and immune functions and to restore these functions during aging.

Common agents which antagonize synthesis and secretion of melatonin:
Alcohol, cortico-steroids, beta-blockers (especially in the evening), caffeine, nicotine and many chemical substances with pharmacological activity can antagonize the synthesis and secretion of Melatonin. But melatonin does not itself antagonize the activity of any drug and can be used in combination with any medical drug and pharmaceutical specialty. Nocturnal melatonin will in-fact improve the effectiveness and activity of drugs as a consequence of its synchronizing properties on the entire neuroendocrine and immune systems.

Melatonin: Suggested daily dosages as a dietary supplement:
Between 40 and 50 years of age: 1.5mg to 3mg at bedtime (peremptorily at the same hour, with half an hour tolerance). After 50 years until 75 years of age: 3mg at bedtime- as above. From 75 years of age: 3-6mg at bedtime- as above. Although not mandatory, it is indicated to take Melatonin for 5 months in summer (May-June-July-August-September) and for 5 months in winter (November-December-January-February-March). Melatonin can be safely taken without intervals after 50 years of age, in the presence of chronic, degenerative diseases and cancer, or as a protective agent under stressful conditions (night-work, exposition to poisons and noxious agents, time-zone travel etc.). It is strongly recommended to take Melatonin for periods of weeks before and after surgical interventions to ameliorate general conditions (mood, immunity, etc.) and to accelerate immunological reconstitution, wound healing, tissue regeneration and recovery from anesthesia toxicity after the operation. For jet-lag we suggest taking 3mg of Melatonin for four to five days at 10-11 PM, local time, on arrival at the place of destination and to repeat the same procedure after returning to the original place of departure.