Melarena pills 0.3mg, 30pcs

Composition

1 film-coated tablet contains: Active ingredient melatonin-0.30 mg or 3.00 mg; Excipients: Calcium hydrophosphate dihydrate-67.37 / 64.67 mg, Microcrystalline cellulose-25.00 / 25.00 mg, Croscarmellose sodium-2.00 / 2.00 mg, Povidone-K 25 ‒ 3,33/ 3,33 Colloidal silicon dioxide-0.50 / 0.50 mg, Talc-1.00 / 1.00 mg, calcium stearate-0.50 / 0.50 mg; Shell: For a dosage of 0.3 mg: Hypromellose 62.50%, Triethyl Citrate 12.50%, Titanium dioxide 25.00% ‒ – 3.00 mg; For a dosage of 3 mg: Hypromellose 62.50%, Macrogol-400 12.50%, Titanium dioxide 24.21%, Aluminum FD & C blue No. 2 varnish (12-14%) 0.28%, Aluminum FD & C blue No. 1 varnish (11-13%) 0.48%, Quinoline yellow varnish 0.02%, iron oxide black dye 0.01% ‒ – 3.00 mg.

Pharmacological action

Synthetic analog of the pineal gland 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. Promotes the organization of biological rhythm and normalization of night sleep. Improves the quality of sleep, accelerates falling asleep, reduces the number of nighttime awakenings, improves well-being after waking up in the morning, does not cause feelings of lethargy, weakness and fatigue when waking up. It makes your dreams more vivid and emotionally intense. Adapts the body to fast jet lag, reduces stress responses, and regulates neuroendocrine functions. Adapts the body of weather-sensitive people to changes in weather conditions. It exhibits immunostimulating and antioxidant properties. Inhibits the secretion of gonadotropins, to a lesser extent-other hormones of the adenohypophysis (corticotropin, thyroid-stimulating hormone, somatotropic hormone). It is not addictive or addictive. Pharmacokinetics When taken orally, it is rapidly and completely absorbed, easily passes histohematic barriers, including the blood-brain barrier. It has a short half-life.

Active ingredients

Melatonin

Indications

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

Use during pregnancy and lactation

The drug is contraindicated for use during pregnancy and lactation.

Contraindications

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

failure; severe impairment of renal function (for dosage 3 mg); pregnancy, lactation; age to 18 years (efficacy and safety not established). Use during pregnancy and lactation The product is contraindicated for use during pregnancy and lactation.

Side effects

The classification of adverse reactions by organ and system is presented with an indication of the frequency of their occurrence: very common (≥1/10), common (≥1/100,1/10), infrequent (≥1/1000,1/100), rare (≥1/10000,1/1000), very rare (1/10000), including individual reports, frequency unknown (frequency cannot be estimated based on available data). Infectious and parasitic diseases are rare: herpes zoster. Disorders of the blood and lymphatic system are rare: leukopenia, thrombocytopenia. Immune system disorders Frequency unknown: hypersensitivity reactions Metabolic and nutritional disorders Rare: hypertriglyceridemia, hypokalemia, hyponatremia. Mental disorders are uncommon: irritability, nervousness, restlessness, insomnia, unusual dreams, nightmares, anxiety. Rare: mood swings, aggression, agitation, tearfulness, stress symptoms, disorientation, early morning awakening, increased libido, low mood, depression. Nervous system disorders Infrequently: migraine, headache, lethargy, psychomotor hyperactivity, dizziness, drowsiness. Rare: syncope, memory impairment, impaired concentration, delirium, restless legs syndrome, poor sleep quality, paresthesia. Visual disturbances are rare: decreased visual acuity, blurred vision, increased lacrimation. Hearing disorders and labyrinth disorders are rare: vertigo, positional vertigo. Disorders of the cardiovascular system Infrequently: arterial hypertension. Rarely: angina pectoris of tension, palpitation, hot flashes. Gastrointestinal disorders Infrequently: abdominal pain, abdominal pain in the upper abdomen, dyspepsia, ulcerative stomatitis, dry mouth, nausea. Rare: 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 Infrequently: hyperbilirubinemia. Skin and subcutaneous tissue disorders Infrequently: dermatitis, night sweats, pruritus and generalized pruritus, rash, dry skin. Rare: eczema, erythema, dermatitis of the hands, psoriasis, generalized rash, itchy rash, nail damage. Frequency unknown: angioedema, edema of the oral mucosa, edema of the tongue. Musculoskeletal and connective tissue disorders Infrequently: pain in the extremities. Rare: arthritis, muscle spasms, neck pain, night cramps. Renal and urinary tract disorders Infrequently: glucosuria, proteinuria. Rare: polyuria, hematuria, nocturia. Genital and breast disorders Uncommon: menopausal symptoms. Rare: priapism, prostatitis. Frequency unknown: galactorrhea. General disorders and disorders at the injection site Infrequently: asthenia, chest pain. Rarely: fatigue, pain, thirst. Laboratory and instrumental data Infrequently: deviation from the norm of laboratory parameters of liver function, weight gain. Rare: increased activity of “hepatic” transaminases, abnormal blood electrolyte levels, abnormal laboratory test results. If any of the side effects listed in the instructions are aggravated, or If you notice any other side effects that are not listed in the instructions, you should stop taking the drug and inform your doctor about this.

Interaction

Incompatible with mopoamine oxidase (MAO) inhibitors, glucocorticosteroids, cyclosporine. Increases the effect of drugs that depress the central nervous system and beta-blockers. Concomitant use with nonsteroidal anti-inflammatory drugs (NSAIDs) is not recommended. It is not recommended to take it together with hormonal medications.

How to take, course of use and dosage

Inside. Tablets of 0.3 mg 1 tablet once a day for 30-40 minutes before bedtime. The duration of treatment is determined individually (from 6 to 8 weeks). Repeated courses are possible. Tablets of 3 mg For sleep disorders, desynchronosis-1 tablet once a day for 30-40 minutes before bedtime. When used as an adaptogen when changing time zones-1 day before the flight and in the next 2-5 days-1 tablet 30-40 minutes before bedtime. The maximum daily dose is 6 mg. Elderly patients With age, melatonin metabolism decreases, which should be taken into account when choosing a dosage regimen for elderly patients. Taking this into account, elderly patients can take the drug 60-90 minutes before bedtime. Renal insufficiency The effect of varying degrees of renal insufficiency on the pharmacokinetics of melatonin has not been studied, so melatonin should be used with caution in such patients. In patients with severe renal insufficiency, the use of the drug is not recommended. Hepatic insufficiency There is no experience of using melatonin in patients with impaired liver function. In patients with impaired liver function, significantly increased plasma concentrations of endogenous melatonin were observed during the daytime. The drug is not recommended for patients with hepatic insufficiency.

Overdose

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

Treatment: gastric lavage, symptomatic therapy.

Description

Round, biconvex tablets, film-coated from white to almost white (for a dosage of 0.3 mg) or blue (for a dosage of 3 mg) color. The core is white to almost white in color.

Functional features

Absorption Melatonin after oral use is rapidly absorbed in the gastrointestinal tract. In the elderly, the absorption rate 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 reached after 20 minutes and 60 minutes, respectively. The time to reach the maximum concentration of Tmax in blood serum is 60 minutes (normal range is 20-90 minutes). After taking 3-6 mg of melatonin, the maximum concentration of Cmax in the blood serum is usually 10 times greater than the endogenous melatonin in the blood serum at night. Concomitant food intake delays melatonin absorption. Bioavailability The oral bioavailability of melatonin ranges from 9 to 33% (approximately 15%). Distribution In vitro studies, the binding of melatonin to plasma proteins is 60%. Melatonin mainly binds to albumin, α1-acid glycoprotein, and high-density lipoproteins. The Vd distribution volume is about 35 liters. It is rapidly distributed in saliva and passes through the blood-brain barrier, and is detected in the placenta. The concentration in the cerebrospinal fluid is 2.5 times lower than in plasma. Biotransformation Melatonin is primarily metabolized in the liver. After ingestion, melatonin undergoes a 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 presystemic metabolism can reach 85%. Experimental studies suggest that the cytochrome P450 isoenzymes CYP1A1, CYP1A2, and possibly CYP2C19 are involved in melatonin metabolism. The main metabolite of melatonin,6-sulfatoxymelatonin, is inactive. Melatonin is released 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% is excreted unchanged. Pharmacokinetic parameters are affected by age, caffeine intake, smoking, and oral contraceptive use. Patients in critical condition have accelerated absorption and impaired elimination. Older 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 a reduced melatonin metabolism in this group of patients. Patients with impaired renal function During long-term treatment, melatonin accumulation was not observed. These findings are consistent with the short human melatonin half-life.

Special instructions

During the use of Melarena®, it is recommended to avoid exposure to bright light. It is necessary to inform women who want to get pregnant about the presence of a weak contraceptive effect of the drug. There are no clinical data on the use of melatonin in patients with autoimmune diseases, and therefore the use in this category of patients is not recommended.

Form of production

Film-coated tablets,0.3 mg,3 mg. 10 tablets in a contour cell package made of polyvinyl chloride film laminated with Aklar® material, and aluminum foil printed varnished or aluminum foil printed varnished and aluminum foil laminated with polyvinyl chloride and polyamide film. 1 or 3 contour cell packages together with instructions for use in a cardboard pack.

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25° C. Keep out of reach of children.

Shelf

life is 2 years. Do not use the product after the expiration date indicated on the package.

Active ingredient

Melatonin

Dosage form

Tablets

Purpose

For adults

Indications

Depression, Jet Lag, Weather Sensitivity, Insomnia