Melatonin daily intake. What is melatonin for, side effects, how to take

Modern world is experiencing a real boom in melatonin. This hormone - a natural sleeping pill, antioxidant and immunomodulator - is called the elixir of youth, beauty and health, which can significantly improve the quality of human life. Clinical researches melatonin has also been shown to be effective in treating a range of conditions, from coronary heart disease to stomach ulcers. What is this mysterious melatonin? What is the reason for such a wide range of its action? What is the mechanism of action of melatonin? Should it be taken and by whom? Is it safe? We will try to answer all these questions.

Discovery of melatonin

In 1917, the English scientists C. McFord and F. Allen fed the epiphyses of animals to tadpoles, after which they discovered that the skin of the tadpoles was discolored. This scientific fact was recorded, but did not attract attention until 1953, when it caught the eye of Aaron Lerner, a dermatologist at Yale University, who was trying to solve the problem of vitiligo (spots on the skin) and, during a literary search, somehow discovered an article written by those same experimenters from 1917.

The article reported that the crushed epiphyses of cows, placed in a jar of tadpoles, within 30 minutes cause a complete discoloration of the skin, which loses pigment and becomes so transparent that one can easily observe the work of their heart and intestines through it. There have been no other publications about this phenomenon since then.

Lerner began to study this issue and as a result discovered a hormone produced by the pineal gland (pineal gland), which he called melatonin and for the first time described its calming effect on humans.

After that, the hormone became interested in the scientific community, and in the course of a number of studies its truly unique effect on the human body was discovered, which made it possible to use melatonin in the treatment of a wide range of diseases and seriously improve the quality of life of patients. Melatonin quickly became legendary, research continues, and to this day, scientists are discovering new, amazing and sometimes unexpected properties.

What is melatonin?

Melatonin is produced by the pineal gland and controls the course of our biological clock, and therefore all life. We only have 3 milligrams of this miraculous substance in our body, and its blood levels fluctuate—low during the day and high at night.

Melatonin lives in the dark. Melatonin production begins to rise at dusk, peaks from midnight to 4:00 am, and falls off at dawn. When we fall asleep, melatonin gets to work - it restores, repairs and strengthens all our systems and organs, is the most powerful natural immunomodulator and absorbs free radicals - unstable molecules that destroy our DNA, cells, tissues and contribute to the development of oncological and heart diseases.

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Melatonin protects us from stress and premature aging, promotes sleep and is responsible for our deep, restful and even sleep, bringing natural rest and recovery. With age, the production of melatonin in the body decreases, and this is the signal for all body systems that it is time to grow old.

Almost every second inhabitant of the metropolis today has problems with sleep. A broken day and night regimen is a problem for all modern citizens. People tend to artificially lengthen their day, going to bed long after midnight, sitting up - some at the TV, some at the laptop, some at the bar with friends, and some at work. There is a huge group of people who consider it normal to call themselves owls and think that this way of life is in accordance with their constitution and does no harm.

However, the nocturnal lifestyle plays a cruel joke with us! The thing is that spending hours of melatonin production in wakefulness, we do not allow it to be produced and do its job - as a result, no matter how much we sleep later in the late morning or afternoon, such a dream will not bring proper rest and recovery. Even if it seems to us that we have had enough sleep, our organs and systems need help - they need melatonin, which we did not allow to develop at night.

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Numerous studies carried out in different countries world have shown that the disturbed rhythm of melatonin formation significantly affects the quality of life, reduces its duration and eventually causes serious diseases. People who stay awake at night (whether they work the night shift or spend time watching TV) are guaranteed to be chronically deficient in melatonin. All groups of studies have shown that those who are nocturnal are 40-60% more prone to the risk of diabetes, hypertension, obesity, atherosclerosis and cancer. Artificial lengthening of daylight hours, unfortunately, leads to the disruption of the work of all body systems, with all the ensuing deplorable consequences.

Useful darkness

The production of melatonin is hindered not only by late falling asleep, but also by an excess of light while we sleep. So much so that scientists believe that it is excessive illumination that shortens the life of residents of large cities - and even introduced a special term "light pollution".

For the full production of melatonin, you need to sleep with curtains tightly drawn, excluding the penetration of lanterns into the window, do not use nightlights and try not to turn on bright lights at night if you suddenly wake up and you need to get up for a while. If you are working at night and this cannot be avoided, keep lighting to a minimum.

Melatonin treatment

Of course, the described mechanism of action and the problem of the widespread failure of the biological clock led scientists to the idea that melatonin can and should be taken additionally. At the same time, melatonin is not considered a medical drug, it is a dietary supplement and in small doses today it is recommended to be taken for any violations of the mode of life, sleep and many other deviations.

At the same time, it is wrong to consider melatonin as just sleeping pills. "The natural structure of sleep depends on melatonin," says Walter Pierpaoli, an immunologist and bestselling author of "The Melatonin Miracle." "adults have erotic dreams. It would be wrong to identify melatonin with sleeping pills: it has a completely different mechanism of action."

Melatonin preparations can not only regulate the quality of sleep, but also make up for the chronic lack of healthy sleep results - and all the accompanying effects in the form of good health, restoration of organs and systems, and prevention of many diseases. It can be said that melatonin treatment is when you take sleep pills.

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But scientists today are interested not only in the preventive effect of the sleep hormone. "Today, there is already convincing evidence to recommend melatonin for the treatment of coronary heart disease, hypertension, peptic ulcer. We introduced melatonin into the regimens for the treatment of hypertension and heart disease, and this made it possible to reduce the usual dose of drugs, - says Semyon Rapoport, MD, professor of MMA named after. I. M. Sechenova, Chairman of the Commission "Chronobiology and Chronomedicine" of the Russian Academy of Medical Sciences. “I really hope that this will soon enter into widespread clinical practice.”

Who Should Take Melatonin?

In general, melatonin is beneficial for all people over the age of 35. It is usually taken in courses of about 1-3 mg at night. The frequency of admission per week varies individually. For example, those suffering from insomnia are advised to take melatonin more often 2-3 times a week.

It also makes sense to keep melatonin capsules on hand if you have a rush job and are forced to work late at night. So you get the right amount of the hormone, even if you didn’t sleep and make it easier to fall asleep later - after all, overwork causes, among other things, insomnia.

Melatonin is often also referred to as a travel medicine. With a sharp change in time zones, when it’s morning on the internal biological clock, and in the city where we arrived, it’s already late at night and it’s time to sleep, this hormone will gently transfer our arrows to a new time.

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The lack of melatonin also explains the age-related insomnia of the elderly, because over the years the activity of the pineal gland decreases. Therefore, it can be recommended to people of age as a dietary supplement that will make sleep better and improve overall well-being.

"There are no side effects from seasonal intake in such small doses. No addiction develops, and the production of one's own hormone does not decrease," says Semyon Rapoport.

However, a small number of people have experienced side effects such as headache, depression and stomach discomfort.

Who should not take melatonin?

The drug is contraindicated in diabetics, because it does not combine well with antidiabetic drugs, pregnant and lactating women, children under 16 years of age, is used with caution in severe depression. Several cases of allergy to melatonin have been recorded.

In addition, the drug is contraindicated in epilepsy, children under 12 years of age, patients with autoimmune diseases and leukemia.

The role of melatonin in the fight against oncological diseases while being studied. There are some results, but the effectiveness of the method has not yet been clinically proven, so the properties of the hormone should not be exaggerated and unreasonable hopes for a new "cure for cancer" should not be, scientists say.

Gross formula

C 13 H 16 N 2 O 2

Pharmacological group of the substance Melatonin

Nosological classification (ICD-10)

CAS code

75-31-4

Characteristics of the substance Melatonin

Synthetic analogue of the hormone of the pineal gland (pineal gland).

Pharmacology

pharmachologic effect- antioxidant, adaptogenic, hypnotic.

It inhibits the secretion of gonadotropins, to a lesser extent - other hormones of the adenohypophysis - corticotropin, thyrotropin, somatotropin. Normalizes circadian rhythms. Increases the concentration of GABA in the central nervous system and serotonin in the midbrain and hypothalamus, changes the activity of pyridoxalkinase involved in the synthesis of GABA, dopamine and serotonin. Regulates the sleep-wake cycle, daily changes in locomotor activity and body temperature, positively affects the intellectual and mnestic functions of the brain, the emotional and personal sphere. Contributes to the organization of the biological rhythm and the normalization of night sleep. Improves the quality of sleep, reduces the frequency of attacks of headaches, dizziness, improves mood. Accelerates falling asleep, reduces the number of nocturnal awakenings, improves well-being after morning awakening, does not cause a feeling of lethargy, weakness and fatigue upon awakening. Makes dreams more vivid and emotionally rich. It adapts the body to the rapid change of time zones, reduces stress reactions, regulates neuroendocrine functions. It has immunostimulating and antioxidant properties, prevents the development of atherosclerosis and neoplasms. It has the most pronounced effect with prolonged pronounced sleep disorders.

When taken orally, it is quickly and completely absorbed, easily passes histohematic barriers, including the BBB. Has a short T 1/2, quickly excreted from the body.

Application of the substance Melatonin

Sleep disorders, fatigue, depressive syndrome, desynchronosis.

Contraindications

Hypersensitivity, chronic kidney failure, allergic, autoimmune diseases, lymphogranulomatosis, leukemia, lymphoma, myeloma, epilepsy, diabetes, pregnancy, breastfeeding.

Use during pregnancy and lactation

Contraindicated in pregnancy. should be discontinued for the duration of treatment. breast-feeding.

Side effects of Melatonin

Headache, nausea, vomiting, diarrhea, allergic reactions.

Interaction

Enhances the effect (mutually) of drugs that depress the central nervous system and beta-blockers. Incompatible with MAO inhibitors, glucocorticoids, cyclosporine.

Routes of administration

inside.

Precautions Substance Melatonin

Simultaneous administration with NSAIDs (acetylsalicylic acid, ibuprofen), with agents that depress the central nervous system and beta-blockers is not recommended. It should not be used during work by drivers of vehicles and people whose profession is associated with increased concentration of attention. It is necessary to inform women who wish to become pregnant that the drug has a weak contraceptive effect.

special instructions

Avoid bright lighting during treatment.

Interactions with other active substances

Trade names

Name The value of the Wyshkovsky Index ®
0.0865
0.0287

The site provides background information for informational purposes only. Diagnosis and treatment of diseases should be carried out under the supervision of a specialist. All drugs have contraindications. Expert advice is required!

General information

Melatonin is natural hormone organism responsible for the regulation of sleep and wakefulness. It is thanks to the pineal gland - a tiny pea-sized formation located in the center of the brain - that we want to fall asleep from time to time. Melatonin is released cyclically to help the body regulate the sleep-wake cycle. Its amount decreases with age, and it is suspected that this is the reason why young people are less likely to suffer from sleep problems than the elderly.

What is the benefit of melatonin?

Studies show that low doses of melatonin help improve sleep, and it is easy to survive long plane flights, jet lag, and without the side effects that are common with sleeping pills. It also helps improve general state health, strengthen immune system and quickly reduces the number free radicals in body tissues.

There are many scientific studies on melatonin currently underway. They are associated with its antioxidant properties, effects on immunity. However, the exact mechanism of action of melatonin in the human body is not yet known in detail, and requires a number of further studies.

Who benefits the most?

These are, first of all, travelers who are struggling with the consequences of jet lag, as well as people suffering from insomnia.
The optimal dose varies individually. According to various studies, good results have been achieved with melatonin in amounts ranging from 0.1 to 200 mg! Controlled medical studies have concluded that even a tenth of a milligram (0.1 mg or 100 mcg) helps you fall asleep easily at any time of the day. Thus, start with a very low dose of melatonin taken at night before bed (eg 0.1 mg) and increase this dose every night until the desired effect is achieved.

What are mg (milligram) and mcg (microgram), and what is the difference between these units?

Micrograms and milligrams are units of weight representing a specific fraction of a gram:
  • 1 microgram = 1 microgram = one millionth of a gram (1/1000000);
  • 1 mg = 1 milligram = one thousandth of a gram (1/1000);
  • 1 mg = 1000 mcg.
The 1.5mg tablet contains five times the dose of melatonin compared to the 300mcg (0.3mg) tablet.

Side effects

According to studies, 10% of people who take melatonin do not get any effect from it. Another 10% reported side effects such as nightmares, headaches, increased morning fatigue, mild depression, and decreased sex drive. In other studies, in which doses of melatonin 600 to 3000 times higher than normal were used, no signs of intoxication were found.

Additional effects

In animal studies, melatonin has been shown to have a cytoprotective effect, strengthen the immune system, and slow down the growth of certain tumors. Experiments on mice have shown that melatonin can slow down the aging process. However, to what extent these results can be extrapolated to humans is still unclear. Some experts are concerned that so many people are experimenting with such a powerful substance, as the long-term effects of taking high doses of melatonin are still undetermined. Even a dose of less than one milligram, which is presented by many manufacturers as the lowest possible dose, is still three times more than the total amount of melatonin produced in the body in a day.

Contraindications

Due to the fact that the effect of high doses of melatonin on unborn children and infants has not yet been clearly established, it should not be taken by pregnant and lactating women. Since this hormone stimulates the immune system, it is not recommended for people prone to allergies and suffering from autoimmune diseases. Children should also avoid high doses of melatonin because their bodies already produce this hormone in high doses on their own. High doses may have a contraceptive effect, so women who want to have children should not take melatonin preparations.

Life Extension

Currently, there are no studies proving a direct relationship between melatonin intake and human life expectancy. However, in rats and mice, the lifespan can be increased by 20%. If the use of this hormone does lead to a longer and healthier life, then this is most likely due to:
1. Reducing the amount of free radicals in the body, which stimulate the aging of the immune system;
2. Protective effect on the cardiovascular system
3. Increased secretion of growth hormone.

Melatonin deficiency as a cause of early aging - video

Melatonin improves sex life?

This hypothesis has not yet been confirmed in humans. A rodent study from as early as 1995, however, suggests that frequent small amounts of melatonin can prevent age-related decline in testosterone production in men, and thus help maintain an active sex life well into old age.

Can melatonin poison you?

Melatonin is one of the least toxic substances. In carefully controlled medical studies, melatonin doses as high as 6 grams (600 to 3000 times the usual dose) have not resulted in any symptoms of poisoning. Overall, there are only four known cases of significant side effects of melatonin in the world. Minor, but more common side effects are drowsiness and a decrease in reaction rate. The largest study to identify side effects was held in the Netherlands. It involved 1400 women who received 75 mg of the drug per day. None developed any serious side effects. Now in this country, melatonin is available in pharmacies without a prescription and, despite this, there have been no reports of its abnormal action.

What time to take?

Melatonin should only be taken in the evening, about 30 minutes before bed. To avoid the consequences of changing time zones, it is taken right before the plane takes off. The drug should not be taken during the day - otherwise, you can simply bring down your "internal clock".

Does melatonin cause lethargy and drowsiness in the morning?

No, you will wake up in the morning after taking melatonin refreshed and full of energy. But if there is still a feeling of fatigue in the morning, the evening dose of melatonin should be adjusted downward.

Hormone production methods

Natural, animal or bovine melatonin is produced by extracting extracts from animal pineal glands. Since these extracts are extracted from tissues that are foreign to the body, it can trigger an immune response in humans. In this regard, such drugs are recommended to be used very carefully.

The best is considered to be a drug made in a factory from pharmaceutically pure ingredients. The molecular structure of such melatonin is identical to that of a hormone produced by the body itself. In addition, it is absolutely free from any contamination.

Melatonin-SZ: instructions for use and reviews

Melatonin-SZ is an adaptogenic drug that normalizes physiological sleep and biological rhythms.

Release form and composition

The drug is produced in the form of film-coated tablets: round, biconvex, on one side there is a separating risk, the shell and core are almost white or white (in blister packs of 10 tablets, in a carton pack 1, 2 or 3 packs; in blister packs of 30 tablets, in a carton pack 1 or 2 packs; in polymer jars / bottles of 30 tablets, in a carton pack 1 jar / bottle and instructions for use of Melatonin-SZ).

1 tablet contains:

  • active ingredient: melatonin - 3 mg;
  • auxiliary components: sodium carboxymethyl starch, MCC (microcrystalline cellulose), calcium hydrogen phosphate dihydrate, magnesium stearate;
  • composition of the film shell: polysorbate 80 (tween 80), hypromellose, titanium dioxide (E171), talc.

Pharmacological properties

Pharmacodynamics

Melatonin-SZ is an adaptogenic drug, its active substance, melatonin, is a synthetic analog of the pineal gland hormone (pineal gland) and, along with adaptogenic, sedative and hypnotic effects.

The therapeutic effect of the drug is realized by normalizing circadian rhythms, increasing the concentration of serotonin and GABA (gamma-aminobutyric acid) in the midbrain and hypothalamus. Melatonin affects changes in the activity of pyridoxal kinase involved in the synthesis of dopamine, serotonin and GABA, regulates the sleep-wake cycle, changes in locomotor activity and body temperature that occur during the day. Renders positive impact on the intellectual-mnestic functions of the brain and the emotional-personal sphere.

Melatonin is involved in the organization of the biological rhythm and the regulation of neuroendocrine functions. Promotes the normalization of night sleep, accelerating falling asleep and improving the quality of sleep. In weather-sensitive people, it helps the body adapt to changes in weather conditions.

Pharmacokinetics

After oral administration, melatonin is rapidly absorbed from the gastrointestinal tract (GIT). When used at a dose of 3 mg, its maximum concentration (Cmax) in blood plasma is reached after 20 minutes, in blood serum and saliva - 60 minutes. C max in blood serum when taking melatonin in the dose range from 3 to 6 mg is 10 times higher than the level of endogenous melatonin in blood serum at night. With the simultaneous intake of food, absorption slows down. Against the background of therapeutic doses (2–8 mg), the pharmacokinetics of melatonin remains linear. Bioavailability averages 15%.

Binding of melatonin (in vitro) to plasma proteins (mainly albumin, alpha 1-acid glycoprotein, high density lipoproteins) - 60%. The volume of distribution (V d) is approximately 35 liters.

The substance overcomes the blood-brain barrier, penetrates the placenta. The concentration of melatonin in the cerebrospinal fluid is 2.5 times lower than its level in plasma.

Melatonin is metabolized mainly in the liver with the participation of isoenzymes of the cytochrome P450 system (CYP1A1, CYP1A2 and, presumably, CYP2C19). It undergoes significant (up to 85% of the accepted dose) biotransformation during the primary passage through the liver, by hydroxylation and conjugation with sulfate and glucuronides, with the formation of the main inactive metabolite - 6-sulfatoxymelatonin.

The average half-life (T 1/2) is 45 minutes. Excreted from the body through the kidneys - approximately 90% in the form of glucuronic and sulfate conjugate of 6-hydroxymelatonin, the rest - unchanged.

For pharmacokinetics active substance caffeine, smoking, oral contraceptives, age of the patient influence. In critically ill patients, absorption is accelerated and elimination is impaired.

In elderly patients, the absorption rate can be reduced by 50% and the metabolism of melatonin is slowed down.

In case of impaired renal function, long-term use of Melatonin-SZ does not cause cumulation of the drug.

In violation of liver function, the level of endogenous melatonin increases. In patients with cirrhosis of the liver during the daytime, the plasma concentration of the drug increases significantly.

Indications for use

The use of Melatonin-SZ is indicated for sleep disorders, including those caused by a violation of the rhythm of sleep and wakefulness with a sharp change in time zones (desynchronization).

Contraindications

Absolute:

  • liver failure;
  • autoimmune pathologies;
  • severe renal failure;
  • period of pregnancy;
  • breast-feeding;
  • age up to 18 years;
  • hypersensitivity to the components of the drug.

Melatonin-SZ, instructions for use: method and dosage

Melatonin-SZ tablets are taken orally.

  • sleep disturbance: 3 mg 1 time per day 0.5 hours before going to bed;
  • desynchrosis (when changing time zones as an adaptogen): 3 mg 1 time per day. The first dose should be taken 1 day before the intended flight, then continue for 2-5 days in the new time zone.

Maximum daily dose Melatonin-SZ - 6 mg.

Elderly patients should take tablets 1-1.5 hours before bedtime.

Side effects

The incidence of side effects according to the recommendations of the WHO (World Health Organization) [very often (> 0.1); often (>0.01 to<0,1); нечасто (от >0.001 to<0,01); редко (от >0.0001 to<0,001), очень редко (<0,0001, в т. ч. отдельные сообщения); частота неизвестна (установить частоту возникновения по имеющимся данным невозможно)]:

  • from the lymphatic system and blood: rarely - leukopenia, thrombocytopenia;
  • invasions and infections: rarely - herpes zoster;
  • mental disorders: infrequently - anxiety, irritability, nervousness, unusual and / or nightmares, anxiety, insomnia; rarely - tearfulness, mood changes, aggression, stress symptoms, disorientation, agitation, early awakening in the morning, increased libido, low mood, depression;
  • on the part of the organ of vision: rarely - blurred vision, decreased visual acuity, increased lacrimation;
  • from the nervous system: infrequently - lethargy, headache, migraine, dizziness, drowsiness, psychomotor hyperactivity; rarely - poor quality sleep, fainting, impaired memory and / or concentration, restless legs syndrome, delirium, paresthesia;
  • on the part of the organ of hearing, labyrinth disorders: rarely - dizziness, benign paroxysmal positional vertigo (BPPV);
  • from the side of the cardiovascular system: infrequently - arterial hypertension; rarely - hot flashes, palpitations, angina pectoris;
  • on the part of metabolism and nutrition: rarely - hypokalemia, hyponatremia, hypertriglyceridemia;
  • from the digestive system: infrequently - dry mouth, ulcerative stomatitis, nausea, abdominal pain (including the upper abdomen), dyspepsia, hyperbilirubinemia; rarely - bad breath, saliva hypersecretion, ulcerative glossitis, vomiting, bullous stomatitis, increased peristalsis, gastrointestinal upset, bloating, abdominal discomfort, gastroesophageal reflux disease, gastric dyskinesia, gastritis;
  • on the part of the immune system: the frequency is not established - hypersensitivity reactions;
  • dermatological reactions: infrequently - dry skin, itching (including generalized itching), night sweats, rash, dermatitis; rarely - erythema, hand dermatitis, itchy rash, generalized rash, nail damage, eczema, psoriasis; frequency not established - Quincke's edema, swelling of the tongue and / or oral mucosa;
  • from the urinary system: infrequently - proteinuria, glucosuria; rarely - nocturia, polyuria, hematuria;
  • from the musculoskeletal system and connective tissue: infrequently - pain in the extremities; rarely - neck pain, muscle spasm, night cramps, arthritis;
  • on the part of the genital organs and the breast: infrequently - symptoms of menopause; rarely - prostatitis, priapism; frequency not established - galactorrhea;
  • laboratory changes: infrequently - a deviation from the norm of liver function tests, increased body weight; rarely - a deviation from the norm of the results of laboratory tests, an increase in the activity of hepatic transaminases, a change in the content of electrolytes in the blood;
  • general disorders: infrequently - chest pain, asthenia; rarely - thirst, fatigue, pain.

Overdose

  • symptoms: involuntary loss of consciousness during the use of melatonin at a dose of 1000 mg. When taking Melatonin-SZ in doses exceeding 3000 mg for several weeks, abdominal cramps, diarrhea, the development of drowsiness, flushing, headache and scotoma may occur;
  • treatment: immediate gastric lavage, activated charcoal. Appointment of symptomatic therapy. After oral administration, the active substance is spontaneously excreted from the body within about 12 hours.

special instructions

During the treatment period, exposure to bright light should be avoided.

The simultaneous use of alcoholic beverages is contraindicated.

Influence on the ability to drive vehicles and complex mechanisms

Since the action of the drug causes drowsiness, reduces the speed of psychomotor reactions and concentration of attention, during the period of use of Melatonin-SZ, one should refrain from driving vehicles and performing other potentially hazardous activities.

Use during pregnancy and lactation

The use of Melatonin-SZ is contraindicated during pregnancy and lactation.

Women planning pregnancy should be aware that the drug has a weak contraceptive effect.

Application in childhood

Melatonin-SZ tablets should not be taken by persons under the age of 18 years.

For impaired renal function

The use of Melatonin-SZ is contraindicated in severe renal failure.

Caution should be exercised in patients with renal insufficiency of varying severity.

For impaired liver function

The use of Melatonin-SZ is contraindicated in liver failure.

Use in the elderly

Elderly patients should take the tablets 60-90 minutes before bedtime.

drug interaction

When used simultaneously with Melatonin-SZ:

  • fluvoxamine: inhibits the metabolism of melatonin, which leads to a significant increase in the concentration of the latter in the blood; it is recommended to avoid this combination;
  • 5- and 8-methoxypsoralen: when combined with these agents, caution should be exercised due to an increase in the concentration of melatonin;
  • cimetidine (an inhibitor of CYP2D isoenzymes): increases the content of melatonin in plasma;
  • estrogen-containing agents (including oral contraceptives): against the background of concomitant hormone replacement therapy, the concentration of melatonin increases;
  • quinolones and other inhibitors of CYPA2 isoenzymes: an increase in melatonin exposure is possible;
  • carbamazepine, rifampicin (inducers of the CYP1A2 isoenzyme): contribute to a decrease in the plasma concentration of melatonin;
  • nicotine: in smokers, a decrease in the concentration of melatonin is possible;
  • hypnotics of the benzodiazepine and non-benzodiazepine series: melatonin potentiates the sedative effect of zaleplon, zolpidem, zopiclone. A combination with these agents may result in a progressive disorder of coordination, attention and memory;
  • thioridazine, imipramine: co-administration of drugs that affect the central nervous system does not cause a clinically significant pharmacokinetic interaction with melatonin. Perhaps an increase in the feeling of calmness, difficulty in performing certain actions, an increase in the feeling of clouding in the head;
  • Ethanol: Alcohol consumption and ingestion of ethanol-containing drugs reduce the effectiveness of Melatonin-SZ.

Analogues

Analogues of Melatonin-SZ are Kakspal Neo, Melarena, Melaksen, Melaksen Balance, Melarithm, Sonnovan, Circadin, etc.

Terms and conditions of storage

Keep away from children.

Store at temperatures up to 25 ° C in a place protected from light.

Shelf life - 3 years.

Poor quality sleep, morning weakness, headache and dizziness, memory loss - all this can be not only a sign of stress or banal fatigue. Exactly the same symptoms accompany the internal disturbance of circadian rhythms, which occurs due to a lack of the hormone melatonin.

natural logistics

In our brain there is a very small gland - the pineal gland, or the pineal gland. The functions of the pineal gland are not fully understood, but it is reliably known that it is its cells that secrete an amazing hormone called melatonin into the blood. It performs many tasks - from slowing down the aging process to regulating the frequency of sleep.

The pineal gland produces melatonin spasmodically: its synthesis is most active at night, closer to two o'clock, and with increasing illumination it decreases to a minimum. The hormone, entering the blood, contributes to a change in the concentration of other biologically active substances, including serotonin and hormones of the anterior pituitary gland, and forms circadian rhythms.

Melatonin sets the pace, telling the body when to be active and when to rest. However, sometimes the level of the hormone decreases, and then failures occur in the mechanism of the natural biological clock.

There are several reasons why the level of melatonin in the blood drops:

  • lack of sunlight;
  • unfavorable work schedule;
  • fast change of time zones;
  • periodic sharp change in sleep and rest;
  • age.

It is appropriate to talk about the shortage of sunlight in the conditions of the Far North. Short daylight hours and long nights "confuse the cards", as a result of which the biological clock "breaks".

But even in more favorable climates, problems with circadian rhythms can arise. In particular, specialists who, due to the peculiarities of the profession, are forced to stay awake at night, compensating for the lack of sleep during the daytime, know firsthand about them. And if your work schedule consists of oddly interspersed day and night shifts, the chances of a melatonin deficiency skyrocket.

Circadian rhythm disruption also occurs when crossing time zones quickly. This syndrome is called jet lag, which in English means "jet lag". The phenomenon of social jet lag, or Monday syndrome, is also known. It develops as a result of a sharp change in sleep and rest at the junction of working weeks.

On weekends, we often allow ourselves to rest longer and sleep better, while on weekdays our routine undergoes a serious transformation, moving into the category of very active. Such a “floating schedule” can bring discord to even the most perfectly tuned system!

There are also physiological causes of circadian rhythm disturbances. With age, the capacity of the pineal gland decreases, which leads to a decrease in the production of melatonin. Hormone deficiency occurs, in particular, in women who have entered the menopause.

Symptoms of melatonin deficiency are the same regardless of which factor triggered the disorder. Circadian rhythm disturbance is manifested by insomnia, fatigue, headache, irritability, and digestive disorders.

At the same time, sedatives do not bring relief: even falling into a dream, a person wakes up broken and tired. This is not surprising, because the problem is not associated with excessive fatigue or excitement, but with a failure of the circadian rhythm against the background of melatonin deficiency. And the only right decision in this case is to compensate for the deficiency of the hormone-regulator.

Biological clock in ... pills

Preparations that allow you to quickly restore the normal level of the natural regulator of circadian rhythms contain a synthetic analogue of the hormone melatonin (Melaxen, Circadin, Melarena).


Lab-produced melatonin exhibits all the effects of a natural substance. It regulates the sleep-wake cycle, relieves headaches, reduces the frequency of dizziness. In addition, melatonin preparations help improve morning well-being, mood, and reduce stress response. Their positive effect on intelligence and memory has also been recorded, which is why melatonin is prescribed for deterioration of cognitive function and is included in the list of nootropics.

With all the positive properties, circadian rhythm correctors containing melatonin have another important quality that further increases their value - a high safety profile. They are very well tolerated with very few side effects. This is eloquently evidenced by the fact that most melatonin preparations are sold in pharmacies without a doctor's prescription.

To compensate for the deficiency of the hormone, it is enough to take 1 tablet of melatonin at a dosage of 3 mg half an hour before bedtime until unpleasant symptoms persist. At the same time, there is no need to worry about addiction - resistance or dependence on melatonin does not occur, and the duration of its use is not at all limited.

If you have a jet lag flight, you should start taking melatonin at bedtime the day before your trip and continue for the next 3-5 days. And the syndrome with the sonorous name of jet lag will bypass you.

Marina Pozdeeva

Photo istockphoto.com