Among the drugs that help the body fight stress and ensure healthy sleep, everyone is familiar with Melatonin. These are sleep pills. Let's consider the features of the drug, rules of administration, indications and contraindications, how it interacts with other drugs.
Melatonin 3 mg
Sleep is very important for our body. In our sleep, we gain strength for the next day and recover physically and mentally. When a person does not get enough sleep, he cannot work productively. Irritability, fatigue, and lack of attention appear. How can you get enough sleep without resorting to sleeping pills?
There are many natural substitutes for sleeping pills. Among the drugs that restore the sleep-wake cycle, Melatonin is well known, produced in the pineal gland and responsible for restoring strength, protecting the body from stress.
With a lack of melatonin in the body, a person becomes restless, irritable, sleep is disturbed, headaches may appear, and vice versa, if there is a lot of melatonin, memory problems appear, the person becomes more lethargic and lethargic.
Melatonin: indications for use
This is the main hormone of the pineal gland, therefore it is not a medicine, but as a supplement containing glycine and melatonin. Melatonin is a medical drug, a synthetic analogue, which is sold in tablet form.
Is Melatonin a dietary supplement or a medicine? This is a dietary supplement. In Europe and Asia, to buy Melatonin in a pharmacy, you need a prescription. In the USA it is sold freely as a dietary supplement - dietary supplement.
How does Melatonin affect the body?
- Helps with insomnia, regulates the sleep cycle.
- Regulates the functioning of the cardiovascular system.
- Regulates metabolic processes in the body.
- Works as antioxidant protection.
- Slowing down the aging process in the body.
- Eliminate headaches.
- Improvement, increase in stress resistance.
- Immunity increases.
It is also responsible for synchronizing the biological clock and setting it up. The drug helps people adapt to time zone changes, regulates neuroendocrine functions in the body, and reduces stress levels.
Melatonin is a hormone that, when taken, sends a signal to the brain to put a person to sleep. This means that after taking the drug it will help you fall asleep. If the cause of insomnia lies in overwork or stress, then this is the best drug.
Attention! The drug helps the body rest, but does not cure insomnia. For this purpose other drugs are prescribed. As part of therapeutic treatment, the attending physician determines the course of treatment for insomnia and determines the dosage of the drug in combination with others.
Melarena Tablets, box, 30 pcs, 3 mg, for oral administration, film-coated
Pharmacological properties
A synthetic analogue of the pineal body (epiphysis) hormone melatonin;
has an adaptogenic, sedative, hypnotic effect. Normalizes circadian rhythms. Increases the concentration of gamma-aminobutyric acid (GABA) and serotonin 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, reduces the number of night awakenings, improves well-being after waking up in the morning, does not cause a feeling of lethargy, weakness and fatigue when waking up. Makes dreams more vivid and emotionally rich. Adapts the body to rapid changes in time zones, reduces stress reactions, and regulates neuroendocrine functions. Adapts the body of weather-sensitive people to changes in weather conditions. Shows immunostimulating and antioxidant properties. Inhibits the secretion of gonadotropins, and to a lesser extent, other hormones of the adenohypophysis (corticotropin, thyroid-stimulating hormone, somatotropic hormone). Does not cause addiction or dependence.
Absorption
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 taken orally at a dose of 3 mg, Cmax in blood plasma and saliva is achieved after 20 minutes and 60 minutes, respectively. Time to reach maximum serum Tmax concentration is 60 minutes (normal range 20-90 minutes). After taking 3-6 mg melatonin, the maximum serum Cmax is typically 10 times the endogenous melatonin serum at night. Concomitant meals delay the absorption of melatonin.
Bioavailability
The bioavailability of melatonin when taken orally ranges from 9 to 33% (approximately 15%).
Distribution
In in vitro studies, the binding of melatonin to plasma proteins is 60%. Melatonin binds primarily to albumin, α1-acid glycoprotein, and high-density lipoproteins. Distribution volume Vd> about 35 liters. It is quickly distributed into saliva and passes through the blood-brain barrier and is detected in the placenta. The concentration in cerebrospinal fluid is 2.5 times lower than in plasma.
Biotransformation
Melatonin is metabolized primarily in the liver. After ingestion, melatonin undergoes significant transformation during its initial passage 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.
Selection
Melatonin is excreted from the body by the kidneys. The average half-life (T1/2) 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.
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 the area under the concentration-time curve (AUC) and Cmax were obtained in the elderly, which reflects the 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.
pharmachologic effect
After taking melatonin, it immediately begins to show its effect. It has hypnotic, sedative, antioxidant and adaptogenic effects. The drug is quickly absorbed into the stomach, enters the bloodstream and begins to act immediately.
It is actually a sleeping pill that exhibits its properties within 24 hours. Melatonin is produced from serotonin, but dulls the effects of the latter. The amount of melatonin produced by our body directly depends on the amount of serotonin. This means that if you don't spend much time outdoors, you may be prescribed Melatonin.
It turns out that the drug will be effective if there is a lack of the hormone in the body. At the same time, if insomnia is caused by pathologies of internal organs, then Melatonin will not help.
Melatonin tablets: instructions
Melatonin is not a vitamin, but a hormone, and dosage and administration must be approached carefully. Before taking the drug, you should consult your doctor. You need to start with small doses, gradually increasing them. The regimen is also prescribed by the attending physician. Melatonin is taken 30 minutes before bedtime with plenty of water. You should not take it before leaving home or before work, as you will feel drowsy and your attention will be dulled.
If you want to buy melatonin, instructions for use are included in the package with the drug and must be studied carefully. Do not forget that melatonin is a hormone, which means it requires caution in use.
Melatonin is available in drops and tablets. You can choose the shape that suits you best.
Melatonin, 3 mg, film-coated tablets, 20 pcs.
Evalar, Russia
Price from 180₽
There are contraindications. Specialist consultation is required.
How to use Melarena
The drug is intended for use by patients over 18 years of age; for adolescents and adults, taking synthetic melatonin can be harmful.
- In case of sleep quality disturbances or insomnia, it is recommended to take 1 tablet per day 40 minutes before going to bed.
- In severe forms of disorders, the daily dose can be increased to 6 mg. melatonin.
- Before long flights and as a preventive measure for attacks of meteosensitivity, you should take the medicine for 2-3 days until the body adapts to new conditions.
- Chronic sleep disorders require a continuous course of about 6–8 weeks.
If necessary, therapy can be continued after a break. It is not advisable to combine Melaren with NSAIDs, caffeine, hormonal medications, cyclosporine, or antihypertensive drugs. After taking the medicine, you should not drive or do work that requires mental or nervous stress. To increase the effectiveness of melatonin, you should avoid being in bright sunlight or artificial light after taking the pills.
Melarena can have a contraceptive effect on the female body, which is important to remember for patients planning pregnancy.
Contraindications
Despite the fact that Melatonin is a dietary supplement, it should not be taken by patients with liver failure, hypersensitivity to the main components of the drug, diseases or severe renal failure. Melatonin should not be taken by pregnant women, during breastfeeding, or by children under 12 years of age.
Melatonin has long been well known as a sleep pill. We do not recommend prescribing this drug for yourself, but should only take it after consultation with your doctor.
Overdose
Due to the wide distribution and availability in pharmacies, as well as the availability of a wide selection of medications for the treatment of insomnia, people began to abuse medications, which led to a number of side effects. This also applies to Melatonin. An overdose of Melatonin may cause some symptoms such as drowsiness, confusion, and anxiety. More serious violations include:
- disruption of the cardiovascular system;
- osteoporosis, which results in leaching of calcium from the bones;
- kidney problems due to water-salt imbalance;
- atrophy of muscles, especially the heart muscle - myocardium.
These and other side effects can occur with a severe overdose of the drug.
In order not to harm your health, the tablets should be taken according to the instructions. An overdose of Melatonin can lead to serious health problems, so you should not take it without a doctor's prescription.
Analogs
To normalize all processes and restore health, you can use melatonin analogs that contain the same hormone. Among melatonin analogues, there are drugs that can be used to treat insomnia. They have a similar mechanism of action, but have their own characteristics.
Let's look at what melatonin analogues are, how they work, and in what cases they should be taken.
If it is not possible to buy Melatonin, analogues can be considered as an alternative. Melatonin analogues are natural stimulators of sleep hormone production, including:
- Circadin is used to treat primary insomnia. (available by prescription only)
- Melarithm is similar in its effect to the action of melatonin, and is used for sleep disorders.
- Melarena is a sedative and adaptogenic medicine prescribed for insomnia.
- Melaxen is prescribed for insomnia in older people.
Melarithm, 3 mg, film-coated tablets, 30 pcs.
Obolenskoye, Russia
Price from 440₽
Melarena, 3 mg, film-coated tablets, 10 pcs.
STADA, Russia
Price from 207₽
Melaxen, 3 mg, film-coated tablets, 24 pcs.
Unipharm, USA
Price from 524₽
There are contraindications. Specialist consultation is required.
There are a huge number of drugs in the world that have a similar effect as the original Melatonin Evalar. They all contain the active substance, but in different dosages. In preparations containing a large dose of melatonin, it is in the form of a purified and stable form.
Such drugs are more effective than drugs containing only the sleep hormone. There are also preparations that contain only pure melatonin. If you want to save money, then buy analogues rather than melatonin.
In order to receive a drug containing a large dose of the sleep hormone, you need to buy the original drug, but do not forget to consult with your doctor before doing so.
Indications for use
The drug is in a lighter dosage - 0.3 mg. recommended to take:
- for the prevention of somnological disorders;
- to relieve attacks of meteosensitivity;
- with a tendency to depression;
- for sleep disorders caused by high fatigue, excessive nervous stress, anxiety;
- with age-related changes in sleep quality;
- during desynchronosis: disruption of natural unique rhythms in travelers, in people working in shifts, on a shift schedule.
Melaren in an increased dosage is recommended for severe persistent insomnia or desynchronosis caused by various reasons:
- with difficulties falling asleep;
- low quality of sleep;
- frequent awakenings, insomnia;
- daytime drowsiness, lethargy, apathy.
The choice of one form or another of the drug must be trusted by a doctor, since self-medication can aggravate existing sleep problems.
