Melatonin is a hormone whose function is to regulate the body's biological clock. Simply put, normal long-term sleep, the ability to quickly fall asleep, and feel cheerful in the morning depend on it. The deficiency of this hormone can be compensated for.

With a lack of melatonin, a person begins to have problems sleeping. Most often, it is simple insomnia, which negatively affects your entire life and daily routine.

Melatonin tablets help eliminate problems with falling asleep and also normalize sleep phases. In addition, this remedy is recommended for those who travel frequently, since time zone changes may also cause sleep problems.

You need to take Melatonin before bed. You should not take the medicine if you wake up at night and cannot sleep, as this will only worsen the disruption of your biological clock.

After taking melatonin, be sure to turn off the lights. The trick is that this hormone is produced only in complete darkness.

Therefore, to enhance the effect of the drug, this condition should not be neglected. 70% of melatonin is produced at night.

Melatonin is an antioxidant, and therefore it is used for various diseases. It helps to activate the work of immune cells, thus strengthening the immune system. In cardiology, it is used to prevent hypertension and other diseases. In particular, melatonin helps prevent the formation of atherosclerotic plaques in blood vessels.


Normal melatonin levels have a positive effect on the nervous system, including helping to prevent neuron death. This hormone helps improve memory and activates mental abilities. In addition, the product is used to prevent cancer.

Melatonin is recommended to be consumed 1-2 hours before bedtime, since it is during this period after administration that its active effect begins. However, depending on the picture of the disease, the time of administration and dosage may vary.

For insomnia, as well as problems falling asleep, Melatonin should be taken 3-4 hours before going to bed. In case of frequent night awakenings, the drug is taken 15 minutes before bedtime.

The duration of such therapy, as a rule, continues until problems with falling asleep completely disappear.


When changing time zones, the product should be taken for 3-4 days, before bedtime. This will help the body quickly adjust to the new time.

The dosage of "Melatonin" for sleep disorders is also determined individually and is 1-2 tablets, which contain 1.5-3 mg of the active substance. For other diseases, the dosage is determined by the doctor.

Melatonin is available in 2 forms:

Tablets for oral use

In the first case, the medicine is washed down with water.

For sublingual use

Sublingual tablets should be placed under the tongue and held until dissolved. In this form, the drug acts faster because it immediately enters the bloodstream.

Questions and answers:

What are the dangers of an overdose of melatonin?

Responsibility for melatonin overdose usually lies with the patient. The doctor prescribes a certain dose, which should be taken once a day in a certain amount. Melatonin is often prescribed 20-30 minutes before bedtime. In cases where a person personally decides to increase the dose of the drug, he may experience diarrhea or vomiting. Therefore, overdose is unacceptable. The same applies to pregnant women, drivers, people who suffer from nervous or central nervous system disorders. Even one tablet can react with medications you are already taking, such as ibuprofen, and cause harm to the body. Therefore, if a person is experiencing insomnia, he should consult a doctor to see if he can take any sleeping pills.

Is melatonin addictive?

The uniqueness of melatonin is that it is not addictive, unlike other sleeping pills. It should be taken for a while (how long is decided by the attending physician), and then the body’s ability to enter the sleep stage and wake up in the morning full of energy will return again. Whatever form you take the medicine - liquid, tablets, capsules - after the treatment period ends, the body will return to normal. There is no habituation.

How long can I take it?

The length of time you take melatonin depends on the problem itself and how long the person has been complaining about problems falling asleep. His age, weight, working conditions (night/day shifts), stress level, family situation, age, emotional state, and the presence of other diseases are taken into account. Taking melatonin is highly individual.

Frequently asked questions and answers

Is melatonin addictive?

Compared to other sleeping pills, melatonin is not addictive. It relieves stress, relieves the effects of negative or positive emotions, helps you fall asleep and relax while you sleep. The body prepares itself for the process of falling asleep. Later, as soon as the course of treatment is over, the person will be able to fall asleep again on his own, as before. Therefore, there will be no addiction or dependence.

Why doesn't melatonin help you fall asleep?

Melatonin is prescribed to combat insomnia. It helps you sleep. But, if insomnia still remains after taking the medicine, there may be several reasons. For example, a person himself changed the dose, increased or decreased. Sometimes melatonin does not work because the patient is taking other strong medications. A negative reaction to the drug may also occur. Some component causes nausea, diarrhea or headache. You should consult a doctor immediately.

Is melatonin harmful?

Unlike other drugs, melatonin is harmless. It is able to correct the causes of sleep disturbances by plunging a person into normal normal sleep. Waking up in the morning, a person will feel active and cheerful. Melatonin calms the body. It even allows you to protect yourself from aging. While other sleeping pills are addictive, melatonin is not. It is enough to complete the entire course of treatment. Then the ability to fall asleep on your own, get rid of stress and relax will return again. So it can be considered harmless.

Which melatonin is best?

Melatonin comes in various forms. You can buy it in the form of tablets, capsules, drops, ointment, gel and even chewing gum. Whatever is more convenient for you, accept it. For example, instant action tablets are very popular. You just need to put them under your tongue and wait a few minutes. Melatonin is then absorbed into the body and begins to act. The medicine in the form of drops is also loved by patients. It works quickly. Melatonin is a remedy that will allow you to sleep well and improve the process of falling asleep. Melaxen can be called a good remedy. It is harmless and relatively inexpensive.

What are the side effects of melatonin?

If a person suffers from diabetes, ischemia, gastritis, or an ulcer, and decides to prescribe melatonin to himself as a treatment for insomnia, his body may protest. Headaches, increased blood pressure, and arrhythmia may begin. The same applies to pregnant women. Only a doctor, after a qualitative examination and tests taken, can decide whether melatonin is suitable in such situations. An incorrectly calculated dose can also cause arrhythmia and discomfort. Side effects of melatonin include allergies, rashes on the face, neck, arms, diarrhea, dizziness, vomiting. Therefore, before taking the drug, you need to consult a doctor.

What is the lethal dose of Melaxen?

A huge advantage of melatonin is that it is practically harmless. Side effects may occur (if a person takes more or less than prescribed), or a reaction may occur due to taking other medications that should not be taken together. But it is impossible to die from an overdose of Melaxen. According to animal testing, it has been proven that the absence of toxins in this drug does not cause death in animals. Unlike other sleeping pills, Melaxen is safe.

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Adaptogenic drug

Active substance

Melatonin

Release form, composition and packaging

◊ Film-coated tablets white or almost white, round, biconvex, with a notch on one side; On a cross section, the core of the tablet is white or almost white.

Excipients: microcrystalline cellulose - 48.5 mg, sodium carboxymethyl starch - 6.5 mg, calcium dihydrogen phosphate dihydrate - 41 mg, magnesium stearate - 1 mg.

Shell composition: hypromellose - 1.53 mg, polysorbate 80 (Tween 80) - 0.64 mg, talc - 0.51 mg, titanium dioxide (E171) - 0.32 mg.

10 pieces. - contour cellular packaging (1) - cardboard packs.
10 pieces. - contour cell packaging (2) - cardboard packs.
10 pieces. - contour cell packaging (3) - cardboard packs.
30 pcs. - contour cellular packaging (1) - cardboard packs.
30 pcs. - contour cell packaging (2) - cardboard packs.
30 pcs. - polymer jars (1) - cardboard packs.
30 pcs. - polymer bottles (1) - cardboard packs.

pharmachologic effect

A synthetic analogue of the pineal gland hormone (epiphysis); has an adaptogenic, sedative, hypnotic effect. Normalizes circadian rhythms. Increases the concentration of gamma-aminobutyric acid (GABA) in the midbrain and hypothalamus, changes the activity of pyridoxal kinase, which is involved in the synthesis of GABA, dopamine and serotonin. Regulates the sleep-wake cycle, daily changes in locomotor activity and body temperature, has a positive effect on the intellectual and mnestic functions of the brain, on the emotional and personal sphere. Helps organize biological rhythm and normalize night sleep. Improves sleep quality, speeds up falling asleep, regulates neuroendocrine functions. Adapts the body of weather-sensitive people to changes in weather conditions.

Pharmacokinetics

Suction

Melatonin after oral administration is quickly absorbed from the gastrointestinal tract. In elderly people, the rate of absorption may be reduced by 50%. The kinetics of melatonin in the range of 2-8 mg is linear. When administered orally at a dose of 3 mg, Cmax in the blood and saliva is achieved after 20 minutes and 60 minutes, respectively. The time to reach the maximum concentration of Tmax in the blood serum is 60 minutes (normal range 20-90 minutes). After taking 3-6 mg melatonin, the serum Cmax is typically 10 times the endogenous serum melatonin at night. Concomitant meals delay the absorption of melatonin.

Bioavailability. The oral bioavailability of melatonin ranges from 9 to 33% (approximately 15%).

Distribution

In in vitro studies, the binding of melatonin to plasma proteins is 60%. Melatonin mainly binds to α1-acid glycoprotein and LDL. V d about 35 l. It is quickly distributed into saliva, penetrates the BBB, and is detected in the placenta. The concentration in cerebrospinal fluid is 2.5 times lower than in plasma.

Metabolism

Melatonin is metabolized primarily in the liver. After oral administration, melatonin undergoes significant transformation during the “first pass” through the liver, where it is hydroxylated and conjugated with sulfate and glucuronide to form 6-sulfatoxymelatonin; the level of first-pass metabolism can reach 85%. Experimental studies suggest that isoenzymes CYP1A1, CYP1A2 and, possibly, CYP2C19 of the cytochrome P450 system are involved in the metabolism of melatonin. The main metabolite of melatonin, 6-sulfatoxymelatonin, is inactive.

Removal

Melatonin is excreted from the body by the kidneys. The average half-life of melatonin is 45 minutes. Excretion is carried out in the urine, about 90% in the form of sulfate and glucuronic conjugates of 6-hydroxymelatonin, and about 2-10% are excreted unchanged.

Pharmacokinetics in special groups of patients

Pharmacokinetic parameters are affected by age, caffeine intake, smoking, and oral contraceptives.

In critically ill patients, accelerated absorption and impaired elimination are observed.

Elderly patients. Melatonin metabolism is known to slow down with age. At different doses of melatonin, higher values ​​of AUC and Cmax were obtained in the elderly, which reflects a reduced metabolism of melatonin in this group of patients.

Patients with impaired renal function. With long-term treatment, no accumulation of melatonin was observed. These data are consistent with the short half-life of melatonin in humans.

Patients with impaired liver function. The liver is the main organ involved in melatonin metabolism, so liver diseases lead to increased concentrations of endogenous melatonin. In patients with liver cirrhosis, plasma melatonin concentrations increased significantly during the daytime.

Indications

- for sleep disorders, incl. caused by a disturbance in the sleep-wake rhythm, such as desynchronosis (sudden change of time zones).

Contraindications

- hypersensitivity to the components of the drug;

— autoimmune diseases;

- liver failure;

- severe renal failure;

- pregnancy;

- period of breastfeeding;

- children under 18 years of age.

Carefully use Melatonin-SZ in patients with varying degrees of renal failure.

Dosage

At sleep disorder- 3 mg 1 time/day 30-40 minutes before bedtime.

At desynchronosis as an adaptogen when changing time zones - 1 day before the flight and in the next 2-5 days - 3 mg 30-40 minutes before bedtime.

The maximum daily dose is 6 mg.

Elderly patients: With age, melatonin metabolism decreases, which must be taken into account when choosing a dosage regimen for elderly patients. Taking this into account, in elderly patients, it is possible to take the drug 60-90 minutes before bedtime.

Kidney failure: The effect of varying degrees of renal impairment on the pharmacokinetics of melatonin has not been studied, so melatonin should be used with caution in such patients. The use of the drug is contraindicated in patients with severe renal failure.

Side effects

Classification of the frequency of side effects according to WHO recommendations: very often (≥1/10), often (from ≥1/100 to<1/10), нечасто (от ≥1/1000 до <1/100), редко (от ≥1/10 000 до <1/1000), очень редко (<1/10 000), включая отдельные сообщения; частота неизвестна (по имеющимся данным установить частоту возникновения не представляется возможным).

From the hematopoietic and lymphatic systems: rarely - leukopenia, thrombocytopenia.

From the immune system: frequency unknown - hypersensitivity reactions.

Metabolism and nutrition: rarely - hypertriglyceridemia, hypokalemia, hyponatremia.

Mental disorders: infrequently - irritability, nervousness, anxiety, insomnia, unusual dreams, nightmares, anxiety; rarely - mood swings, aggression, agitation, tearfulness, symptoms of stress, disorientation, early morning awakening, increased libido, decreased mood, depression.

From the nervous system: uncommon - migraine, headache, lethargy, psychomotor hyperactivity, dizziness, drowsiness; rarely - fainting, memory impairment, impaired concentration, delirium, restless legs syndrome, poor quality of sleep, paresthesia.

From the side of the organ of vision: rarely - decreased visual acuity, blurred vision, increased lacrimation.

Hearing and labyrinth disorders: rarely - vertigo, positional vertigo.

From the cardiovascular system: infrequently - arterial hypertension; rarely - angina pectoris, palpitations, hot flashes.

From the gastrointestinal tract: uncommon - abdominal pain, abdominal pain in the upper abdomen, dyspepsia, ulcerative stomatitis, dry mouth, nausea; rarely - gastroesophageal disease, gastrointestinal disorder or disorder, bullous stomatitis, ulcerative glossitis, vomiting, increased peristalsis, bloating, hypersecretion of saliva, bad breath, abdominal discomfort, gastric dyskinesia, gastritis.

From the liver and biliary tract: infrequently - hyperbilirubinemia.

For the skin and subcutaneous tissues: uncommon - dermatitis, night sweats, itching and generalized itching, rash, dry skin; rarely - eczema, erythema, hand dermatitis, psoriasis, generalized rash, itchy rash, nail damage; frequency unknown - Quincke's edema, swelling of the oral mucosa, swelling of the tongue.

From the musculoskeletal system and connective tissue: infrequently - pain in the limbs; rarely - arthritis, muscle spasms, neck pain, night cramps.

From the urinary system: uncommon - glucosuria, proteinuria; rarely - polyuria, hematuria, nocturia.

From the genital organs and breast: infrequently - menopausal symptoms; rarely - priapism, prostatitis; frequency unknown: galactorrhea.

General reactions: infrequently - asthenia, chest pain; rarely: fatigue, pain, thirst.

Laboratory and instrumental data: infrequently - deviation from the norm in laboratory parameters of liver function, weight gain; rarely - increased activity of liver transaminases, deviation from the norm in the content of electrolytes in the blood, deviation from the norm in the results of laboratory tests.

Overdose

Symptoms: According to available literature data, the use of melatonin in a daily dose of up to 300 mg did not cause clinically significant adverse reactions. Flushing, abdominal cramps, diarrhea, headache and scotoma have been observed when melatonin was used in doses of 3000-6600 mg for several weeks. When very high doses of melatonin (up to 1 g) were used, involuntary loss of consciousness was observed.

In case of overdose, drowsiness may develop.

Treatment: gastric lavage and use of activated carbon, symptomatic therapy.

The active substance is expected to be eliminated within 12 hours after oral administration.

Drug interactions

Pharmacokinetic interaction

It is known that at concentrations significantly higher than therapeutic levels, melatonin induces the CYP3A isoenzyme in vitro. The clinical significance of this phenomenon is not fully understood. If signs of induction develop, consider reducing the dose of concomitantly used drugs.

At concentrations significantly higher than therapeutic levels, melatonin does not induce CYP1A isoenzymes in vitro. Therefore, the interaction of melatonin with other drugs due to the effect of melatonin on CYP1A isoenzymes is apparently insignificant.

Melatonin metabolism is mainly mediated by CYP1A isoenzymes. Therefore, it is possible that melatonin may interact with other drugs due to the effect of melatonin on isoenzymes of the CYP1A group.

Caution should be exercised in patients taking fluvoxamine, which increases the concentration of melatonin (increase in AUC by 17 times and C max by 12 times) due to inhibition of its metabolism by cytochrome P450 isoenzymes: CYP1A2 and CYP2C19. This combination should be avoided.

Caution should be exercised in patients taking 5- and 8-methoxypsoralen, which increases melatonin concentrations due to inhibition of its metabolism.

Caution should be exercised in patients taking (CYP2D isoenzyme inhibitor) as it increases plasma melatonin levels by inhibiting the latter.

Smoking can reduce melatonin concentrations due to the induction of the CYP1A2 isoenzyme.

Caution should be exercised in patients taking estrogens (e.g., contraceptives or hormone replacement therapy), which increase melatonin concentrations by inhibiting their metabolism by CYP1A1 and CYP1A2.

Inducers of the CYP1A2 isoenzyme, such as rifampicin, can reduce the plasma concentration of melatonin.

In modern literature there is a lot of data regarding the effect of agonists/antagonists of adrenergic and opioid receptors, antidepressants, prostaglandin inhibitors, benzodiazepines, tryptophan and alcohol on the secretion of endogenous melatonin. There have been no studies of the mutual influence of these drugs on the dynamics or kinetics of melatonin.

Pharmacodynamic interaction

You should not drink alcohol while taking melatonin, because... it reduces the effectiveness of the drug.

Melatonin potentiates the sedative effect of benzodiazepine and non-benzodiazepine hypnotics such as zaleplon, zolpidem and. In a clinical study, clear evidence of a transient pharmacodynamic interaction between melatonin and zolpidem was observed one hour after administration. Combined use may lead to progressive impairment of attention, memory and coordination compared to zolpidem monotherapy.

In studies, melatonin was administered in conjunction with thioridazine and imipramine, drugs that affect the central nervous system. In none of the cases was there a clinically significant pharmacokinetic interaction. However, concomitant use with melatonin resulted in increased feelings of calmness and difficulty performing certain tasks compared with imipramine monotherapy, as well as increased feelings of brain fog compared with thioridazine monotherapy.

special instructions

During the period of use of the drug Melatonin-SZ, it is recommended to avoid exposure to bright light.

It is necessary to inform women who want to become pregnant that the drug has a weak contraceptive effect.

There are no clinical data on the use of melatonin in patients with autoimmune diseases, and therefore, use in this category of patients is contraindicated.

Impact on the ability to drive vehicles and machinery

The drug Melatonin-SZ causes drowsiness; therefore, during the treatment period, you should refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.