The harm and benefits of melatonin: instructions for use for sleep. Melatonin: instructions for use and what it is for, price, reviews, analogues Use during pregnancy and lactation
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. It has a positive effect 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.
The pharmacokinetics of the active substance is influenced by caffeine, smoking, oral contraceptives, and the age of the patient. 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.
The maximum daily dose of Melatonin-SZ is 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, care should be taken 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.
The description is up to date 11.11.2014- Latin name: Melatonin
- ATX code: H06A
- Active substance: Melatonin
- Manufacturer: Healthway Production Inc., USA
Compound
The composition of the drug includes the active ingredient, as well as a number of auxiliary components: microcrystalline cellulose, disubstituted calcium phosphate anhydrous, magnesium stearate, colloidal silicon dioxide, croscarmellose sodium, stearic acid.
Release form
Melatonin is available in film-coated tablets. The blister contains 12 tablets.
pharmachologic effect
The sleep hormone melatonin is produced in the human body by the pineal gland, which is located at the base of the brain. This substance contains animal food, in food of plant origin there is a smaller amount of this hormone. The secretion of melatonin also depends on the degree of illumination. With poor lighting, its production increases, with good lighting, it slows down.
In the human body, approximately 70% of the daily amount of this hormone is produced at night. Under the influence of melatonin, the amount of gamma-aminobutyric acid and serotonin in the hypothalamus and midbrain increases.
Melatonin is a solid substance, it can absorb or dissolve fat. It is very strong natural origin. In the process of synthesis of this hormone, the body provides protection from the influence of free radicals, which provoke the acceleration of the aging process and the development of malignant diseases. This substance can penetrate into all cells of the body and provide specific protection to the nucleus. As a result, damaged cells are restored.
Hormone melatonin also exists in a synthetic form, used as an additive, which provides a sedative effect , and also acts as antioxidant . This hormone is a natural regulator of the circadian rhythm, ensuring healthy sleep, fast falling asleep and waking up.
If a person exposes the body to violations of temporal adaptation, the hormone ensures the correction of the daily rhythms of the body, as well as the regulation of the cycle of wakefulness and sleep. Melatonin tablets facilitate the process of falling asleep at an atypical time for this, reduce the frequency of awakenings at night and normalize sleep in general.
The drug has a sedative, adaptogenic and hypnotic effect, if taken in high doses, it also has an antioxidant and immunostimulating effect. Also, under its influence, the frequency of seizures decreases, the intensity of stress reactions decreases, and neuroendocrine functions are regulated.
Pharmacokinetics and pharmacodynamics
Wikipedia indicates that the drug begins to act 1-2 hours after oral administration. Once inside, melatonin is converted during the initial passage through the liver. The level of bioavailability is 30-50%. The substance is able to penetrate the blood-brain barrier. The average elimination half-life is 45 minutes. It is excreted from the body through the kidneys.
Indications for use
It should be understood when taking Melatonin that this is a drug that promotes sleep.
Therefore, melatonin preparations are prescribed for the following diseases and conditions:
- body conditions in which sleep disorders are noted;
- the need to regulate the biological cycle of awakening and sleep;
- the need to act as an antioxidant in order to protect against the influence of free radicals;
- to stimulate the immune system;
- in order to stabilize blood pressure and regulate the content of cholesterol in the blood;
- in order to prevent tumor diseases;
- disorders of mental adaptation;
- anxiety-depressive conditions;
- to improve sleep in the elderly.
Contraindications
The following contraindications are defined:
- to the components;
- autoimmune diseases;
- lymphoma;
- lymphogranulomatosis;
- myeloma;
- pregnancy and lactation;
- childhood.
Carefully you need to take the drug to those people who, by the nature of their activities, need to concentrate. It is also prescribed with caution for hormonal disorders, during hormone replacement treatment, for people suffering.
Side effects
When taking, it should be remembered that such treatment can provoke the manifestation of side effects. In particular, the following side effects may occur: heaviness and discomfort in the stomach, headaches, heaviness in the head,. If these or other side effects appear during treatment, you should tell your doctor about it.
Application instruction of Melatonin (Way and dosage)
The instruction for Melatonin provides that the tablets are taken orally, while they do not need to be cracked. The remedy should be taken with water. Adult patients should take 1-2 tablets at bedtime. Adolescents who are already 12 years old are prescribed 1 tablet at bedtime. Instructions for the use of Melatonin provide that the tablets are taken 30-40 minutes before bedtime. You can take no more than 6 mg of the substance per day.
How to take the pills, in each case, explains the attending physician.
Sports nutrition, including Melatonin, should be carried out strictly under the supervision of specialists.
Overdose
There is no sufficient data on drug overdose. When taking more than 24 mg of the drug, patients experienced prolonged sleep, memory problems, and disorientation. For the purpose of treatment, it is necessary to perform a gastric lavage, take. Symptomatic therapy is also practiced.
Interaction
With simultaneous treatment, it is possible to increase the dopaminergic and serotonergic effects of methamphetamines.
During treatment Melatonin potentiated antibacterial effect .
Terms of sale
In pharmacies, the drug is sold without a prescription.
Storage conditions
It is necessary to keep the product at room temperature, you need to protect the tablets from the access of children. After the expiration date, you can not use the medicine.
Shelf life
You can store the drug for 3 years.
special instructions
It should be borne in mind that when taking pills, there may be an adverse effect on concentration, on the speed of physical and mental reactions. It is not recommended to drive vehicles and perform potentially dangerous activities requiring special attention during the period of therapy.
When treating with Melatonin, you should not smoke or drink alcohol.
Women who are trying to get pregnant should be aware that Melatonin can act as a weak drug.
During the period of taking the medicine, too bright lighting should be avoided.
Analogues
Analogues of the drug Melatonin - drugs Melapur , Yukalin , Melaton . Despite the fact that these drugs have a similar effect, analogues should not be used without prior concentration with a doctor.
children
Children under 12 years of age are not prescribed this medicine. To normalize sleep, you can use products containing this substance. First of all, it is food of animal origin. What products contain melatonin, the doctor can tell in detail.
With alcohol
It is undesirable to drink alcohol during treatment with Melatonin.
Melatonin is a synthetic analogue of the hormone of the brain structure of the pineal gland (pineal gland) melatonin.
In the mechanism of action, the main ability to provide a biological change of wakefulness and sleep, circadian rhythms through the neurohumoral mechanisms of the central nervous system.
Increases mental and physical performance, reduces the manifestation of stress reactions. It has an antioxidant and immunomodulatory effect; stabilizes cell membranes, normalizes the permeability of the vascular wall and increases its resistance, improves microcirculation.
Pharmacokinetics.
After ingestion, intravenous melatonin undergoes significant metabolism during the primary passage through the liver. Bioavailability of melatonin - 30 - 50%. When taken orally at a dose of 3 mg, the maximum concentration in blood serum and saliva is reached, respectively, up to 20 and 60 minutes. Melatonin crosses the blood-brain barrier and is determined in the placenta. The half-life is 45 minutes. It is excreted from the body with urine.
Indications for use:
Melatonin is intended for the prevention and treatment of sleep disorders, insomnia, the negative effects of stress reactions (especially in elderly patients), seasonal affective disorders (winter depression); to facilitate adaptation when changing time zones.
Mode of application:
The dosing regimen is set individually.
For insomnia, adults - inside from ½ to 2 tablets 30 to 40 minutes before bedtime with water. The duration of the course is determined by the doctor.
To adapt when changing time zones - 1 - 2 tablets once a day, at 18 o'clock, for one week, starting 3 days before the flight.
Melatonin should not be used in the morning in bright daylight.
Side effects:
When using the drug Melatonin possible morning drowsiness, moderate swelling (in the first week of treatment).
With the phenomena of allergic reactions (skin rash), digestive disorders (nausea), dysphoria (in patients with depression), dizziness, the drug should be discontinued. May have a slight contraceptive effect, impaired sexual function.
Contraindications:
Contraindications to the use of the drug Melatonin are: individual drug, autoimmune diseases, lymphogranulomatosis, leukemia, lymphoma, myeloma, epilepsy, diabetes mellitus, pregnancy, lactation, simultaneous treatment with monoamine oxidase inhibitors, corticosteroids, cyclosporine; childhood and adolescence.
Interaction with other drugs:
β-adrenergic blockers, clonidine, dexamethasone, fluvoxamine, and some other drugs can alter the secretion of endogenous melatonin.
Melatonin may affect the effectiveness of hormonal drugs (estrogens, androgens, etc.), increase the binding of benzodiazepines to specific receptors, so their simultaneous use requires medical supervision.
Melatonin may enhance the antitumor effect of tamoxifen.
The dopaminergic and serotonergic effects of methamphetamine may be enhanced by its simultaneous use with melatonin.
Melatonin may enhance the antibacterial action of isoniazid.
Overdose:
Cases of overdose of melatonin (24 - 30 mg) are described.
Overdose Melatonin the most likely are disorientation, prolonged sleep, vtratapamyati on previous events. In these conditions, it is necessary to wash the stomach. Therapy is symptomatic.
Storage conditions:
Keep out of the reach of children, dry, dark place at a temperature not exceeding 25 ° C. Shelf life - 5 years.
Release form:
Coated tablets.
Compound:
1 coated tablet, Melatonin contains melatonin 3 mg;
excipients: anhydrous dibasic calcium phosphate, microcrystalline cellulose, croscarmellose sodium, silicon dioxide, magnesium, stearic acid.
Additionally:
It is prescribed with caution to patients whose activities are associated with the need for increased concentration of attention and a high concentration of psychomotor reactions.
After taking the drug, it is not recommended to drive a car or any other complex machinery.
It is prescribed with caution for hormonal disorders and / or hormone therapy, as well as for patients with allergic diseases.
In patients with liver cirrhosis, the level of endogenous melatonin secretion is reduced.
When taking melatonin, bright lights should be avoided.
If you are often forced to move from one time zone to another, if you have sleep disturbances, and your immune system is noticeably weakened, then Melatonin will come to your aid. It will help you adjust to the new time zone and avoid the side effects that conventional sleeping pills usually produce, such as lethargy and daytime sleepiness.
We will talk in this article about how to take the named remedy correctly, how to set its dosage correctly and in what cases it is worth resorting to such treatment. It will also be possible to get acquainted with melatonin-containing drugs produced in Russia, Ukraine and abroad: Melatonin Plus, Melaksen, Vita-Melatonin. Reviews of patients and specialists about them will help you in choosing.
What is melatonin?
First of all, let's figure out what substance we are talking about and why our body needs it.
Melatonin is the so-called one that produces the size of a pea, located at the base of the brain. Since ancient times, by the way, it was considered the organ of clairvoyance - the "third eye" of man. This is probably why a lot of mysterious and not fully understood is still associated with this hormone.
You can read about preparations containing it here) in modern medicine they are considered the regulator of the body's circadian rhythm. So, its especially high level is observed at night - the peak of production falls on the period from 12 o'clock at night to 4 o'clock in the morning. That is, melatonin is a kind of natural sleeping pill.
But, in addition, this hormone is also a powerful antioxidant, with the help of which the body is saved from cancer and premature aging. Melatonin is able to penetrate into any cell and exert its protective effect on its nucleus, which contains DNA, and this allows the damaged cell to recover.
Studies on laboratory animals have shown that the lack of melatonin in the body of highly organized mammals leads to rapid aging, early menopause, reduced insulin sensitivity, and the development of obesity and cancer.
The drug "Melatonin": application
But the amount of this hormone produced by the pineal gland (pineal gland) is not always enough to provide the full variety of biological effects. For this, a preparation containing synthetic melatonin is used.
Preparations with melatonin contribute well to the onset of sleep, since the hormone is able to regulate the sleep-wake cycle (which is especially necessary when forced to change time zones), the functioning of the gastrointestinal tract, the endocrine system and brain cells. This hormone also stabilizes blood pressure and cholesterol levels.
The described remedy is produced in tablets. It begins its action within an hour or two after ingestion.
The drug "Melatonin": analogues
According to numerous reviews, synthetic melatonin is considered the least toxic among known substances. For him, the so-called LD-50 was never found (we are talking about the dose of the drug at which half of the experimental animals die).
In the United States, where it was discovered in the 1950s, the synthetic hormone is generally classified as a food supplement. In Russia, this is a drug, which, by the way, is also available in sports nutrition stores under the name Melatonin (“Melatonin”).
Analogues of this drug, sold in pharmacies, are called: "Vita-Melatonin", "Melaxen", "Melaton", "Melapur", "Circadin", "Yukalin". They are well-deservedly popular in cases where it is necessary to increase physical and mental performance, reduce the impact of stressful situations and improve the quality of sleep.
When are melatonin tablets used?
Accompanying almost every remedy containing indicates that it is prescribed for sleep disorders, problems with the human immune system, and also to alleviate premenstrual conditions in women. By the way, the described hormone is 9 times more effective than the familiar vitamin C, strengthening the immune system and saving our body in autumn and winter from colds and infections.
In addition, melatonin markedly improves memory, learning, and the ability to focus. It can be used as part of complex therapy in neurotic patients, as well as in depressive states. Melatonin also significantly reduces the energy costs of the myocardium, transferring it to a more economical mode.
The drug showed excellent results in the treatment of patients with eczema.
Melatonin and longevity
It is impossible not to draw the reader's attention to the amazing feature of the hormone to influence the aging process in the body.
As it turned out during research, the level of melatonin in the blood of a person by the age of forty-five is only half the amount produced in adolescence. This is due to the fact that in the epiphysis, where the hormone is produced, by adulthood, as a rule, morphological changes are already detected with the degeneration of cell elements and their death.
Interestingly, in rats that were transplanted with epiphyses from young donors, life expectancy increased significantly. And this allows us to conclude that the amount of melatonin in the body directly affects how many years youth will remain.
How does melatonin prolong life?
And although serious studies on this subject have not yet been conducted, experts already confirm that if melatonin helps to live healthier and longer, then this is due to:
- reduce cell damage by free radicals;
- slowing down the aging of the immune system;
- high security of the cardiovascular system;
- and also due to the maintenance of a normal daily rhythm and stimulation of the production of growth hormone.
What other possibilities are hidden in the hormone
According to scientists who conducted research on volunteers for five years in Norway, seasonal melatonin intake does not have any side effect. Moreover, the body practically does not develop addiction to it, and the production of its own hormone does not decrease.
Recent studies allow us to state that melatonin is very useful for patients with ischemia of the heart, hypertension and gastric or duodenal ulcers. But the mentioned hormone gives the most promising effect in the fight against breast cancer associated with an increase in the level of female estrogen hormones.
Does melatonin cause drowsiness like sleeping pills?
The undoubted advantages of the synthetic hormone include the reviews available about all preparations containing melatonin, which emphasize that neither in the morning nor during the day, these drugs do not give the effect of drowsiness and stupor characteristic of hypnotics and sedatives. If such a reaction to it is still present, it is enough to reduce the dosage to the one that will not cause it.
All patients taking hormone pills noted a feeling of cheerfulness and energy after a sound sleep, if the dosage was chosen correctly.
Features of taking melatonin
Despite the reviews already available about preparations containing melatonin, consumers should not forget that this hormone is still fraught with many secrets and mysteries. It continues to be actively studied all over the world.
As already mentioned, the level of production of the “sleep hormone” in the body changes markedly with age. It is produced best and in the largest quantity in children, so there is no need for them to take melatonin.
There are other situations in which you need to refrain from taking melatonin:
- due to the still unknown effect of the drug on the fetus, it should be abandoned by pregnant and lactating women;
- Melatonin should not be taken by patients with epilepsy, autoimmune and allergic diseases, as well as by women seeking to conceive a child (since the drug has some contraceptive effect);
- in addition, it was found that the drug interacts negatively with substances containing, for example, acetylsalicylic acid and ibuprofen.
From which it follows that before taking any means with melatonin, it is necessary to consult a doctor!
In addition to the above, it should be remembered that taking Melatonin tablets, the instructions for which are now being considered, costs courses, giving the body a break.
When and how is it better to take drugs?
Experts advise taking these funds only immediately before bedtime, somewhere in half an hour. On long trips, it is better to take a tablet (1.5 mg) before going to bed. Often, the remedy is prescribed 3-4 days before the trip in order to synchronize the biological cycles and rhythms of our body. The tablet is not chewed and washed down with water.
Asking the question “How to take melatonin?”, Remember that you need to do this only in relation to the usual rhythm of sleep and wakefulness. So, if you sleep at night, then you should not take the remedy during the daytime, because it is this hormone that is responsible for the clarity of the biorhythms of our body. In addition, it has been proven that the hormone is destroyed in daylight, and this once again confirms the need to take it only in the evening.
Do melatonin medications have side effects?
Adverse reactions in the process of taking a synthetic hormone were extremely rare. As a rule, they were expressed by discomfort in the stomach, headache, drowsiness or "heavy head", depression.
Experts remind you that all cases of adverse reactions, even those that are not indicated by the instructions for use attached to any drug containing melatonin, must be reported to the doctor!
If melatonin was taken less than six hours before going to work, then the patient, by the way, may show a decrease in concentration and coordination of movements.
The state of drug overdose in patients was not noted. Only the reviews available for Vita-melatonin tablets noted the indicated condition after a single dose of 30 mg of the substance. This provoked disorientation, loss of memory for previous events and prolonged sleep.
Taking melatonin eliminates alcohol and smoking. Attention! Be sure to consult your doctor before using drugs!
Indications for the use of drugs containing melatonin
Once again, I would like to remind you in which cases you need to take drugs containing melatonin. Reviews about them certainly convinced the reader of the usefulness of this hormone. So, the described means are recommended first of all:
- persons suffering from sleep disorders,
- in frequent stressful situations,
- suffering from neurological disorders, depression and phobias;
- patients with endocrine disorders;
- with menopausal disorders;
- with some cardiovascular diseases and atherosclerosis;
- with immune disorders;
- older people (this hormone helps to resist polymorbidity - a condition in which a person has several diseases at the same time).
What are the signs that you may be suspected of having a lack of melatonin?
If you have swelling under your eyes, you look tired, look older than your age, your hair turns gray prematurely, and irritability and anxiety are increasingly noticed in your behavior, then your body may have reduced production of melatonin.
An equally bright signal of this is superficial sleep, without dreams, as well as gloomy thoughts that overcome you before falling asleep. If you feel like you never get enough sleep, are having a hard time with the transition to summer or winter time, and you are haunted by a state of tension and anxiety - it is obviously time to seek the advice of a doctor so that he selects the correct dose of a drug containing melatonin for you.
Few people know that sound and deep sleep is not possible without a sufficient amount of melatonin in the body. Melatoninum is an endocrine hormone synthesized by the pineal gland and regulates the body's circadian rhythms. The lack of this hormone manifests itself in the form of problems with falling asleep, a person loses the ability to adapt to different time zones, there are problems with pressure, in the endocrine system, immunity decreases, which causes other somatic problems. In case of a decrease in hormone synthesis, experts recommend starting medications or nutritional supplements containing melatonin, which, according to the instructions for use, can normalize sleep and increase stress resistance.
General information about the drug
Medicines containing melatonin have a hypnotic and sedative effect, help eliminate problems with falling asleep, restore circadian rhythms and increase efficiency, reducing the impact of stress on the body. The hormone is a natural antioxidant and prevents the synthesis of free radicals, substances that accelerate the aging process and provoke the appearance of cancers.
Melatonin in the composition of medicines is a synthetic analogue of the natural hormone of internal secretion. The release rate is without a prescription, since melatonin-containing drugs in Russia do not belong to medicines, but are sold as food supplements.
Drug group, INN, scope
Melatonin (INN - Melatonin) is sold under various trade names such as Natrol, Solgar, Vita, Melaxen and others. Synthetic melatonin belongs to the pharmacotherapeutic group of hypnotics (adaptogenic) drugs. The drug is recommended for people with insomnia, a broken regimen and a predisposition to seasonal depression. Also, the tool is widely used to improve immunity and to accelerate adaptation during travel.
Forms and prices in pharmacies
Medicines based on synthetic melatonin are not uncommon. There are many different companies that produce this hormone with the addition of various auxiliary components.
The most popular melatonin-containing products:
- Melatonin Solgar. Available immediately in 3 dosage forms:
- tablets: 3, 5 or 10 mg of active ingredient in 1 piece, placed in glass containers of 120 or 60 pieces. in each;
- capsules: 3 mg melatonin + 100 mg theanine, 30 pcs. in one vial;
- drops: 10 mg / 1 ml, for oral administration.
- Melatonin Natrol. Sold in tablets with a concentration of 1, 3, 5, 6, 10 mg or in liquid form. One plastic bottle can contain 60, 90, 100 and 150 tablets.
- Melatonin Now Foods is available in capsules, lozenges and drops. One capsule may contain 3, 5 or 10 mg, the lozenge contains only 3 mg of the active ingredient. The drug is sold in plastic bottles of 60, 180 or 240 pcs. in each or in a 60 ml glass bottle.
These drugs can be purchased at pharmacies, or in sports nutrition stores and on the website of the iHerb manufacturer.
The price of drugs depends on the country of manufacture, the form of release and the amount of the hormone in the composition.
Composition of preparations with melatonin in tablets
The concentration of the active substance in one tablet depends on the company that produces the drug. But, as a rule, all manufacturers produce dosage forms containing 3, 5 and 10 mg of the hormone. Synthetic melatonin helps to normalize sleep, restore sleep and wakefulness by increasing the amount of GABA and serotonin, as well as inhibiting the synthesis of adenohypophysis hormones.
Auxiliary substances, as a rule, are: magnesium, vitamin B6, cellulose (microcrystalline), calcium, stearic acid, silicon dioxide. Melatonin preparations do not contain glycine, lactic acid and sugar, so the list of contraindications does not include many diseases of an allergic nature, diabetes mellitus.
Pharmacodynamics and pharmacokinetics
The pharmacological action of the drugs is based on inhibition of the synthesis of adenohypophysis hormones and an increase in the amount of serotonin and γ-aminobutyric acid in the brain regions. This effect helps to get rid of insomnia and normalize sexual function by restoring the rhythm of gonadotropic hormones and the circadian rhythm in general. The drug also reduces the negative impact of stress on the body, thus increasing the psychological and physical performance.
Melatonin has a membrane-stabilizing effect, which justifies its antioxidant properties. The ability of melatonin to normalize vascular permeability and improve microcirculation has a positive effect on the level of blood pressure, especially after psycho-emotional stress. Improves cellular immunity.
The hormone is rather unstable and quickly decomposes under the influence of enzymes. Metabolism of the substance occurs in the liver. Bioavailability - 40-50%. The maximum concentration in the body is observed already 20-60 minutes after taking the minimum dose of the drug. It is found in the breast milk of a woman and in the body of the fetus. Quite quickly excreted from the body (more than 50% in 45 minutes). Excretion route - with urine.
Why is melatonin called the "sleep hormone"?
Melatonin is a unique hormone because it not only influences the quality of a person's sleep, but also affects the production of almost all hormones in the body and maintains circadian rhythms. Some call it the “hormone of life and longevity” due to its antioxidant action, but many prefer a different name, namely the sleep hormone. Such an informal name is not at all connected with its effect on the quality and duration of sleep, as it might seem at first glance.
The fact is that most of the hormone (more than 70%) is synthesized by the pineal gland at night, with reduced illumination. Daylight interferes with synthesis. The most active hormone is synthesized at night in the period from 00:00 to 03:00 hours and only under the condition of full sleep. Otherwise, the amount of synthesized melatonin will decrease significantly, which can affect health and cause sleep problems in the future.
Efficiency and application
Melatonin-based preparations have proven their effective effect on human sleep: like sleeping pills, the hormone reduces the period of falling asleep and the number of night awakenings, but at the same time helps to feel alert and full of energy after waking up, unlike other sedatives. Some studies have proven that the substance reduces the number of free radicals, thereby slowing down aging and reducing the risk of cancer.
Medicines containing melatonin are especially useful for people who travel often, it allows them to adapt to a new country as easily as possible and enter into the usual rhythm of life. Many experts also advise elderly people suffering from mild insomnia to take melatonin, since over the years the amount of the natural hormone synthesized significantly decreases.
Indications and contraindications
As a rule, drugs are used for disturbed sleep patterns, difficulty falling asleep and reduced performance, both mental and physical.
Other indications for use are:
- Constant stress.
- Seasonal depressions.
- Chronic insomnia with concomitant hypertension.
- Premenstrual syndrome.
- Reduced immunity.
- High blood pressure and cholesterol.
- Violation of the sleep-wake rhythm.
- Problems with falling asleep in people over 67 years of age due to an age-related decrease in the synthesis of the natural sleep hormone.
Despite all the safety, there are a number of diseases in which you should refrain from taking the hormone.
Contraindications:
- allergy to any substance in the composition;
- epileptic status;
- diabetes;
- oncological diseases of the blood and lymph;
- endocrine diseases and hormone therapy;
- autoimmune diseases.
The use of melatonin in severe allergies or autoimmune diseases can stimulate a person's immunity, which will only aggravate the course of the underlying disease. Patients with concomitant liver diseases should take the drug with caution, due to its slow metabolism.
With prolonged therapy with melatonin, a decrease in blood pressure is observed, so people with low blood pressure are prescribed medication with extreme caution. May cause drowsiness, which is the reason why, until the optimal therapeutic dose is established, it is necessary to give up driving and other work that requires increased attention.
During pregnancy
Until now, there is no accurate data on the effect of a synthetic hormone on the fetus, so the drug in this group is not prescribed during pregnancy and breastfeeding. Women of childbearing age should also avoid taking melatonin, as large doses of the hormone can exhibit properties similar to contraceptives.
For kids
Children are not prescribed melatonin, because the child's body synthesizes a sufficient amount of the hormone, and its additional intake can lead to an overdose. Also, taking melatonin-containing drugs before the age of 18 can cause growth retardation and sexual development of the child due to inhibition of the synthesis of sex hormones and growth hormone.
Harm and benefit
Melatonin-based medicines have low toxicity and rarely cause adverse reactions. Only a minority of people taking synthetic melatonin have experienced the following side effects:
- Irritability and hyperexcitability.
- Nightmares.
- Tearfulness.
- Agitation.
- Depression.
- Increased sexual desire.
- Shingles.
- Changes in blood composition (leukopenia, thrombocytopenia).
- Strong heartbeat.
- Angina.
- Violation of memory and attention.
- Deterioration in the quality of sleep.
- Fatigue and drowsiness.
- Headache and dizziness.
- Decreased visual acuity.
- Gastrointestinal disorders (dry mouth, ulcers, bad breath, heartburn, abdominal pain, bloating, constipation).
- Liver dysfunction.
- Allergy (rash, itching, erythema, urticaria, damage to the nail plate).
- Heartache.
- Thirst.
- Obesity.
An overdose is almost impossible. With long-term use of large doses of the drug, some patients noted a lengthening of the sleep phase, increased fatigue, impaired orientation in space and memory impairment. Reducing the dose or canceling the drug eliminates all symptoms caused by an excess of the hormone in the body.
Despite a number of possible side reactions, melatonin preparations are among the safest, but at the same time effective medicines. A large number of studies have been able to prove the positive effect of melatonin on human sleep. In addition, the antioxidant and immunostimulating effect of the hormone on the body was also recorded. In this regard, melatonin is also used as a prophylactic anticarcinogenic drug.
The greatest effectiveness of the drug is noted by travelers, whom it helps to adapt to different time zones and climatic conditions. In general, melatonin helps to adapt to an unusual or stressful life situation, improves the quality of sleep and helps to enter the wakefulness phase immediately after waking up.
Instructions for use of medications with melatonin
The instructions for preparations containing melatonin recommend taking the hormone 25-40 minutes before a night's sleep. The drug is not recommended for daily use, as this can cause disruption of the sleep / wakefulness rhythm.
The agent is taken orally, 1 tablet or capsule, or 0.5-1 ml of drops, which can be consumed both in pure form and diluted in any liquid. The recommended single dose is 3 mg. In the case of an upcoming long trip, you can take a small dose of medication (up to 1.5 mg), this will help you fall asleep on the road. The maximum single dose is 10 mg. The maximum course of treatment is 2 months, with the possibility of repetition, after a seven-day break. It is advisable to take a break for a week after a month.
In the case of using the drug for prevention purposes, the daily dose and duration of treatment is determined by the specialist, based on data on the patient's condition. On average, intake is limited to 1 tablet half an hour before bedtime for one month. Elderly people with chronic sleep disorders or high blood pressure are prescribed 1.5 mg of medication once a day. With insufficient therapeutic effect, the dose may be increased to 3 mg per day. The course of treatment can take from 3 to 6 months, with a weekly interval once a month.
Compatibility with drugs and alcohol
Melatonin enhances the effect of drugs that depress the human NS. In this regard, it is not recommended to take it together with:
- β-blockers;
- benzodiazepine derivatives (for example, with);
- sleeping pills (Zaleplon, Zopiclone, Zolpidem);
- neuroleptics (for example, with Aminazine pilyule_nervi-247);
- Thioridazine and Imipramine.
Such interactions adversely affect the activity of the nervous system, reduce concentration, impair memory and coordination. Also, the drug is not compatible with MAO inhibitors, cyclosporine and NSAIDs (including ibuprofen, and).
Medicines that reduce the synthesis of vitamin B6 inhibit not only the synthesis of natural melatonin, but also its absorption. In view of this, it is worth avoiding the simultaneous use of loop diuretics, oral contraceptives, estrogens, theophylline, penicillamine and hydralazine with melatonin-containing agents. Fluvoxamine and cimetidine increase the concentration of the hormone in the blood by slowing down its metabolism. It is not recommended to take melatonin during hormone therapy, because under the influence of hormones, the level of the substance in the body increases. Nicotine and alcohol significantly reduce the effectiveness of the drug, so during treatment you should refrain from smoking and ethanol-containing products.
Melatonin analogues
Analogues are selected according to the composition, mechanism of action and pharmacological group.
The most popular synthetic analogues of the hormone are:
- . In addition to the hormone, magnesium, cellulose, calcium, pharmaceutical glaze, talc and alcohol (isopropyl alcohol) are present in the composition. Melaxen facilitates falling asleep, normalizes sleep cycles and prevents frequent nocturnal awakenings. The drug is well tolerated by the body and rarely causes complications. As a rule, the drug is prescribed for insomnia, which arose against the background of stress or an age-related lack of natural melatonin in the body. Melaxen is available in the form of white or almost white film-coated tablets. Method of application - oral. The recommended dose is 3 mg (1 tablet) an hour or 2 before bedtime.
- The psychostimulant Phenibut is sold in the form of flat-cylindrical tablets. One tablet contains 250 mg of aminophenylbutyric acid, milk sugar, calcium stearate, gelatin, starch. The drug has a high pharmacological activity, due to which it is used for asthenia, emotional instability, anxiety-depressive conditions, insomnia, kinetosis, stuttering, enuresis, tics and chronic withdrawal syndrome. All analogues of Phenibut pilyule_ana-091 based on this active substance have these pharmacological properties. Phenibut irritates the gastric mucosa, therefore it is prohibited for use in patients with gastric and duodenal ulcers.
- on the territory of Russia is sold under the brand name "Luminal". Available in the form of tablets containing 5, 50 or 100 mg of phenobarbital. Refers to antiepileptic drugs with a hypnotic effect. Phenobarbital is usually prescribed for serious conditions such as epilepsy, spasm paralysis, and eclampsia. Despite the hypnotic effect, experts do not recommend taking the drug as a cure for insomnia due to its strong inhibitory effect on the central nervous system. Phenobarbital is prohibited for use by people prone to suicidal thoughts and actions.
Also, similar drugs include:
All of the listed medicines, except Melarena, do not contain melatonin, but are effective for insomnia. Anvifen, Diazepam and Midazolam are available exclusively by prescription.