Melarena, 0.3 mg 30 pcs

Synthetic analogue of the pineal body hormone (epiphysis) melatonin; has adaptogenic, sedative, and hypnotic effects. It normalizes circadian rhythms.

Increases the concentration of gamma-aminobutyric acid (GABA) and serotonin in the midbrain and hypothalamus, changes the activity of pyridoxal kinase, 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 mental functions of the brain, on the emotional and personality sphere.

Promotes the organization of the biological rhythm and the normalization of night sleep. It improves the quality of sleep, accelerates falling asleep, reduces the number of night awakenings, improves the sense of well-being upon awakening, does not cause a feeling of dullness, weariness and fatigue upon awakening.

Makes dreams more vivid and emotionally rich.

Adapts the body to rapid change of time zones, reduces stress reactions, regulates neuroendocrine functions. Adapts the body of people sensitive to changes in weather conditions.

It shows immunostimulating and antioxidant properties. Inhibits secretion of gonadotropins, to a lesser extent – other adenohypophysis hormones (corticotropin, thyroid hormone, somatotropic hormone). It is not addictive and not dependent.

Pharmacokinetics

When administered orally it is quickly and completely absorbed, easily passes through the histo-hematic barriers including the blood-brain barrier. It has a short half-life.

Indications

Tablets 0.3 mg Prevention and course treatment: Desynchronosis (disturbance of the normal circadian rhythm) due to rapid movement between time zones of the Earth; in case of violation of the light regime, including for people engaged in shift work or rotational work. Meteosensitivity. Fatigue, sleep disturbances (including in elderly patients). Depressive syndrome. Tablets 3 mg Desynchronosis (disruption of the normal circadian rhythm) due to rapid movement between time zones of the Earth; in case of violation of the light regime, including for people engaged in shift work or rotational work. Sleep disorders.

Pharmacological effect

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.

Pharmacokinetics

When taken orally, it is quickly and completely absorbed and easily passes histohematic barriers, including the blood-brain barrier. Has a short half-life.

Special instructions

During the period of use of the drug Melarena®, 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 not recommended.

Active ingredient

Melatonin

Active components

Melatonin

Composition

1 film-coated tablet contains:

Active ingredient

Pregnancy

The drug is contraindicated for use during pregnancy and breastfeeding.

Contraindications

Hypersensitivity to melatonin and other components of the drug; autoimmune diseases, allergic diseases; lymphogranulomatosis, leukemia, lymphoma, myeloma, epilepsy, diabetes mellitus, chronic renal disease

failure; severe renal dysfunction (for a dosage of 3 mg); pregnancy, breastfeeding period; age under 18 years (efficacy and safety of use have not been established).

Use during pregnancy and lactation

The drug is contraindicated for use during pregnancy and breastfeeding.

Side Effects

The classification of adverse reactions by organs and systems is presented indicating the frequency of their occurrence: very often (≥1/10), often (≥1/100, 1/10), infrequently (≥1/1000, 1/100), rarely (≥1/10000, 1/1000), very rarely (1/10000), including isolated reports, frequency unknown (frequency cannot be estimated based on available data). Infectious and parasitic diseases Rare: herpes zoster. Blood and lymphatic system disorders Rare: leukopenia, thrombocytopenia. Immune system disorders Frequency unknown: hypersensitivity reactions Metabolic and nutritional disorders Rare: hypertriglyceridemia, hypokalemia, hyponatremia. Mental disorders Uncommon: irritability, nervousness, restlessness, insomnia, unusual dreams, nightmares, anxiety. Rarely: mood swings, aggression, agitation, tearfulness, symptoms of stress, disorientation, early morning awakening, increased libido, decreased mood, depression. Nervous system disorders Uncommon: migraine, headache, lethargy, psychomotor hyperactivity, dizziness, drowsiness. Rarely: fainting, memory impairment, impaired concentration, delirium, restless legs syndrome, poor sleep quality, paresthesia. Visual disturbances Rare: decreased visual acuity, blurred vision, increased lacrimation. Hearing and labyrinthine disorders Rare: vertigo, positional vertigo. Cardiovascular system disorders: Uncommon: arterial hypertension. Rarely: exertional angina, palpitations, hot flashes. Gastrointestinal disorders 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. Liver and biliary tract disorders Uncommon: hyperbilirubinemia. Skin and subcutaneous tissue disorders 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: angioedema, swelling of the oral mucosa, swelling of the tongue. Musculoskeletal and connective tissue disorders Uncommon: pain in the extremities. Rarely: arthritis, muscle spasms, neck pain, night cramps. Renal and urinary tract disorders Uncommon: glucosuria, proteinuria. Rarely: polyuria, hematuria, nocturia. Genital and breast disorders Uncommon: menopausal symptoms. Rarely: priapism, prostatitis. Frequency unknown: galactorrhea. General disorders and administration site disorders Uncommon: asthenia, chest pain. Rarely: fatigue, pain, thirst. Laboratory and instrumental data Uncommon: abnormal 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. If any of the side effects indicated in the instructions get worse, or you notice any other side effects not listed in the instructions, you should stop taking the drug and inform your doctor.

Interaction

Incompatible with mopoaminooxidase inhibitors (MAOIs), glucocorticosteroids, cyclosporine.

Enhances the effect of drugs that depress the central nervous system and beta-blockers.

Concomitant use with non-steroidal anti-inflammatory drugs (NSAIDs) is not recommended.

It is not recommended to take together with hormonal medications.

Overdose

There are no data on cases of melatonin overdose. There may be an increase in dose-dependent adverse reactions.

Treatment: gastric lavage, symptomatic therapy.

Functional features

Absorption Melatonin after oral administration is rapidly 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 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 binds mainly to albumin, α1-acid glycoprotein and high-density lipoproteins. The distribution volume Vd is 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. Excretion 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 No accumulation of melatonin was observed during long-term treatment. These data are consistent with the short half-life of melatonin in humans.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25° C.

Keep out of the reach of children.

Shelf life

2 years. Do not use the drug after the expiration date indicated on the package.

Manufacturer

Hemofarm LLC, Russia