Posted on December 07 2019
Human life is subject to a certain biological rhythm, through which precise regulation of the work of different organs and systems is carried out. In the complex system of regulating this rhythm, the melatonin secretes into the brain and influences sleep.
Melatonin is a hormone that is strongly influenced by "dark" and "light" therapies and can be used as a means to improve sleep. It is preferable to some medication because it does not lead to addiction.
Like all protein articles, it is recognized that the most important is the high protein diet, not the intake of powders in particular, and in melatonin articles, it must be recognized that the body needs a proper rhythm of sleep. Some of the long-term benefits of melatonin may be due to
normalizing sleep and resulting from this fact, not direct melatonin induction.
What is melatonin?
Melatonin (5-methoxy-N-acetyltryptamine) is a peptide hormone and a nitrotransmitter present in the organisms of all living beings (from algae to humans) at levels that change in a daily cycle. In higher animals, it is produced by pinealocytes (cell types) in the pineal gland (located in the brain) as well as by the retina and the gastrointestinal tract. It is synthesized by the amino acid tryptophan by synthesis of serotonin by the enzyme 5-hydroxyindole-O-methyltransferase.
Melatonin is produced in the pineal gland (small gland in the brain) under the serotonin conductor (one of the most important neurotransmitters). Like a vampire, melatonin appears in the blood only at night and disappears in the day. At twilight, the pineal gland gradually begins to increase melatonin secretion, which reaches its maximum in full darkness.
In the morning, the light activates the optic nerve, as the generated impulse passes through the spine and the upper conduction paths to reach the pineal gland that blocks the synthesis and secretion of melatonin. In practice, a metronome that regulates the activity of the central nervous system works.
By receiving continuous pulses through the optic nerve, the pineal gland is likely to be able to regulate the activity of different organs and systems, and to stimulate a switch to a "sleep mode" when it is dark, thus greatly reducing the body's energy costs. A key element of this regulatory mechanism is also melatonin.
Melatonin is found naturally in a number of plants in sufficiently bioactive doses. Among the best sources of melatonin are tomatoes, walnuts, barley, rye, strawberries, olive oil, raw cow's milk, wine, beer and cherries.
How does melatonin work?
It has been found that the synthesis of melatonin in the human body plays an extremely important role in the control of the 24-hour rhythm of alertness and the associated changes in the secretion of various hormones (cortisol, testosterone, growth hormone) associated with these conditions.
Melatonin is a fundamental regulator of the cyclical rhythms of the human body. It shows a 24-hour synthesis and release pattern. Its natural bioavailability over an extended period of time (5-6 hours) during the night also determines the effect on the cyclic system of biological rhythms.
As has already been said, melatonin regulates the wakefulness-sleep cycle and synchronizes the biorhythms. This precise rhythm, individual to each person, can come out of the rails if there is a melatonin secretion disorder. When in sufficient quantity, melatonin slightly decreases the body temperature of the person - this reduces energy consumption and accelerates the regeneration of cells that are not active during the sleep phase.
It is believed that melatonin is also one of the most powerful antioxidants known to date that act both at the cell membrane level and inside the cell itself. In the course of evolution, one has lost his ability to produce some powerful antioxidants such as beta-carotene and vitamin C in his body but has retained other antioxidants (such as melatonin) that deactivate free radicals (a major threat to the body) and thus form a powerful defense system against them.
For example, the brain, made up of 50% fat, 1/3 of which is unsaturated fatty acids, is very sensitive to free radicals. The pineal gland, which is at the base of the brain, synthesizes melatonin, which is the "last rung" against free radicals attacking the brain.
Melatonin also lowers the level of "bad" LDL-cholesterol, protects against some cancers and stimulates the immune system.
Serum levels and metabolism
In studies on a number of models related to insomnia or difficulty falling asleep, it was found that small doses of 0.3 or 0.5 mg were effective as ten-fold higher doses. It has also been found that a "super" dose of 20 mg has a lesser effect than the conventional dosage.
The detection of serum melatonin peaks is extremely difficult, varying in each study. There is little difference in the different dosages, but in all cases serum melatonin concentrations are increased several times compared to any physiological concentration. Doses of 3 to 5 mg increase concentration and slow down half-life.
Half-life of melatonin is only 24 minutes and blood levels remain stable until 150 minutes after dosing. Half-life does not differ in small and large doses. The same applies to the onset of serum peaks that occur after 45-75 minutes of taking.
There is a study according to which melatonin injection into the nose may be far more effective than standard oral intake.
Melatonin is metabolised and expelled quickly from the body. Its metabolism accelerates from flavoring, and some habits, such as smoking, intensify its elimination from the body.
Melatonin and age
The levels of melatonin in peripheral blood are different in young and adult individuals. It has been shown that with age the circadian systems in the human organism "spoil". As with most hormones, when aging, the melatonin level drops dramatically - for example, for an 80-year-old man, its serum values are only 10% of the 20-year-olds.
A consequence of this is the significant change in a number of vital parameters. Particularly, it affects negatively the cycle of sleep - cheerfulness, at night the temperature of the adults does not fall, which means that reconstructive processes of the tissues and organs can not take place.
Proven and potential human benefits
Sleep and reassurance
Melatonin is best known for improving sleep and treating insomnia. It is for this reason that it is used as a reference substance for the testing of others. The most commonly used dose is 3 mg with gradual release.
The main mechanism of action is associated with a reduction in sleep time, with melatonin also benefiting in healthy individuals. In some studies, melatonin is reported to even improve sleep quality, but this is not proven in healthy individuals. However, the same does not apply to elderly people and children suffering from insomnia, where melatonin also has a positive effect on the quality of sleep. This also applies to people who suffer from migraine or subjective ringing in the absence of an external source as well as in schizophrenic patients.
The effect of melatonin on lowering body temperature has been proven, which also has its benefits for easier sleep.
Melatonin has the strongest effect in people over 55 years of age or suffering from insomnia.
Melatonin also improves sleep when there are external or internal factors for its poor quality. External factors are daytime and nighttime cycles, and internal factor is the inner clock of each individual. When internal or external factors are not "tuned", melatonin helps to balance.
One of the most valuable benefits of melatonin is for traveling people and is expressed in the ability to regulate circadian rhythm on long journeys in different time zones. This is evidenced by a huge meta-analysis of ten different studies. Taken prior to travel or hourly dosages, melatonin regulates circadian rhythm and avoids the specific fatigue state and difficulty falling asleep when passing through several time zones. An even more impressive fact is that this phenomenon also applies to night work shifts.
The effect of melatonin on sleep is often associated with exposure to light. Melatonin works best with exposure to bright light in the first part of the day but does not combine well with exposure to bright light before falling asleep.
One of the most impressive effects of melatonin is associated with stomach function.
Melatonin successfully increases serum gastrin levels, which are low in gastric ulcers, which is associated with the healing properties of melatonin in this regard.
All studies so far have shown that melatonin has strong protective properties against ulcers, and the effect is self-evident, with results demonstrating complete recovery. Melatonin has a protective effect against the harmful effects of certain bacteria and aspirin.
Taking melatonin before sleep reduces the symptoms of gastroesophageal reflux disease (GERD), as well as heart failure in the course of reflux.
Melatonin affects some neurotransmitters in the body. For example, it keeps increasing the levels of adrenaline and noradrenaline in stressful situations, but does not completely eliminate them. In non-stress situations, melatonin also reduces adrenaline levels.
Melatonin reduces blood flow to the brain and is thought to be beneficial for migraines, although this effect is controversial and not fully proven. It is assumed that melatonin may have its benefits, especially for improving the quality of sleep in people with migraines.
There is a theory that melatonin can help in some depressive states, especially those associated with changes in daylight in the winter. Melatonin, along with light therapy, helps normalize circadian rhythm in the winter and improve the depressive state.
The neurological benefits of melatonin are also associated with improved memory. Melatonin may help to improve memory markers in older people, but data are currently based only on combinations with other substances. However, melatonin alone improves the memory of young individuals in stressful situations.
Small doses of 1-2 mg of melatonin lower blood pressure in men and women abruptly, which is associated with a decrease in adrenaline. The rate of blood pressure lowering is different in activity and passivity and it is assumed that such a decrease may not be relevant in any situation. In one of the studies on individuals with metabolic syndrome, melatonin successfully lowers diastolic and systolic blood pressure, and this decrease is not linked to body weight.
Melatonin further improves blood flow and has vasorelaxant properties. In this case it affects the blood flow to the limbs and kidneys, but not to the cerebral one.
In contrast to triglycerides and cholesterol in the blood, melatonin does not have a positive effect, but an interesting effect is found on melatonin administration before exercise, in which case peptide hormone enhances triglyceride lowering.
Peripheral organs (eyes and ears)
Melatonin has a positive effect on blood pressure in the eyes through the melatonin receptor. This effect is also associated with the decrease in adrenaline. There was a significant decrease to two hours after oral administration.
The benefits of melatonin for the eyes do not end there. Melatonin levels in glaucoma glaucoma have been found to be significantly lower in the evening, with melatonin in the case helping to improve the condition or at least halting its deterioration.
As already mentioned, melatonin also has benefits for the condition of subjective noise in the ears. Although it improves sleep and sleep quality in patients with this disease, it does not directly affect treatment.
Melatonin and pineal gland are associated with life expectancy. With age, melatonin levels in the body diminish, and additional supplementation is believed to help longevity.
The use of melatonin is associated with an effect on proinflammatory cytokines in cardiac tissues, which may increase life. A similar protective effect is also seen in pancreatic and hepatic tissues. Tests on animals also detect an anti-aging effect on the skin.
Dosage and route of use
Melatonin is not a sleeping remedy, it is not used to it - it simply synchronizes the biorhythms and ensures a calm and prolonged sleep.
It has been found that to improve the rhythm of sleep, doses between 0.5 mg and 5 mg work. Our recommendation is to start with the minimum dose and gradually increase if you do not have an effect. The benefits of melatonin are not dose-dependent, so a higher dose does not mean a stronger effect. Only the higher dose would benefit for slightly higher growth hormone peaks.
For better performance, it is recommended to administer one tablet per day, to be taken with a glass of water in the evening until 30 minutes before bedtime. The tablet should not be chewed. It is not recommended to exceed the daily dose.
Although melatonin is a nutritional supplement, self-medication is not recommended before a doctor is diagnosed!
Side Effects and Contraindications
Melatonin is one of the safest and non-toxic substances. Impaired doses up to 500 mg, whether administered orally or intravenously, do not have an intoxicating effect. It is not toxic in adults over 60 years of age. Doses up to 5 mg per day are also safe for children over 5 years of age and may be taken by younger children only after consultation with a pediatrician.
Melatonin does not lead to addiction. Several detailed, large-scale studies have found that even at steady intake of 6-12 months, it does not add up to the body.
There are hypotheses that it is possible to have an adverse effect on the suspension of melatonin supplementation. At this stage it has been shown that doses up to 2 mg should not have similar effects, but it is assumed that long-term higher doses may have side effects after stopping melatonin. The most well-established hypothesis so far is that a possible cause is not just stopping it, but the fact that the body is returning to its previous irregular sleeping regime.
With what to combine melatonin?
To improve sleep, melatonin can be used with other similar supplements such as gaba, 5-HTP, L-Teanin, zma and L-Tryptophan. Melatonin binds to enzymes that inhibit the transformation of L-tryptophan into 5-HTP, so their combination is recommended.
It also has an antioxidant effect. It is recommended to combine it with other antioxidants such as vitamin C, alpha lipoic acid and resveratrol. Combination with green tea is not recommended because the melatonin and antioxidant EGCG appear to be antagonists.
It is not clear at this stage whether alcohol prevents melatonin supplementation.
Where can we find melatonin?
Melatonin is one of the most affordable food supplements on the market and, as an economical one, almost every brand offers its version. You may find melatonin in food supplements or pharmacies.
Most commonly, melatonin is available on its own, and in most formulas on the market are capsule or tablet variants with doses of 3 to 5 mg. Higher dosages are rarely available. Primary release formulations are also advantageous.
Sometimes melatonin is also present in complex formulations to improve sleep. A similar formula is PN Z-Max, which combines classic ZMA with melatonin.
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