Melarena, 0.3 mg 30 pcs

How to take, the dosage

Oral. Tablets of 0.3 mg 1 tablet once a day for 30-40 minutes before bedtime. Course of treatment is determined individually (from 6 to 8 weeks). Repeated courses are possible. Tablets 3 mg in violation of sleep, desynchronosis – 1 tablet once a day for 30-40 minutes before bedtime. In application as adaptogen in change of time zones, 1 tablet 1 day before flight and during the next 2-5 days – 1 tablet 30-40 minutes before sleep. The maximum daily dose is 6 mg. Elderly patients As we age, melatonin metabolism decreases, which should be considered when choosing a dosing regimen for elderly patients. Taking this into account, in elderly patients it is possible to take the drug 60-90 minutes before sleep. Renal failure The effect of varying degrees of renal failure on the pharmacokinetics of melatonin has not been studied, so melatonin should be used with caution in these patients. In patients with severe renal insufficiency, the use of the drug is not recommended. Liver failure There is no experience in using melatonin in patients with hepatic impairment. Significantly elevated plasma concentrations of endogenous melatonin during the day have been observed in patients with hepatic impairment. In patients with hepatic impairment, use of the drug is not recommended.

Interaction

Incompatible with monoamine oxidase inhibitors (MAOIs), glucocorticosteroids, cyclosporine.

Increases the effect of drugs that depress the central nervous system and beta-adrenoblockers.

It is not recommended to take simultaneously with nonsteroidal anti-inflammatory drugs (NSAIDs).

It is not recommended to take together with hormonal drugs.

Special Instructions

During the use of Melaren® , it is recommended to avoid exposure to bright light. Women who want to get pregnant should be informed about the weak contraceptive effect of the drug. There are no clinical data on the use of melatonin in patients with autoimmune diseases; therefore, the use in this category of patients is not recommended.

Synopsis

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

Features

Absorption Melatonin is rapidly absorbed in the gastrointestinal tract after oral administration. The absorption rate may be reduced by 50% in the elderly. The kinetics of melatonin in the 2-8 mg range are linear. When administered orally at a dose of 3 mg, Cmax in plasma and saliva is reached in 20 minutes and 60 minutes, respectively. Time to reach maximum serum Tmax concentration is 60 minutes (normal range 20-90 minutes). After ingestion of 3-6 mg of melatonin, the maximum serum Cmax concentration is typically 10 times that of endogenous melatonin in serum at night. Concomitant food intake delays melatonin absorption. Bioavailability The bioavailability of oral 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 albumin, α1-acid glycoprotein and high-density lipoproteins. Vd distribution volume is about 35 liters. Rapidly distributed in saliva and passes through the blood-brain barrier, determined in the placenta. Concentration in cerebrospinal fluid is 2.5 times lower than in plasma. Biotransformation Melatonin is metabolized mainly in the liver. After ingestion, melatonin undergoes significant transformation during primary passage through the liver, where it is hydroxylated and conjugated with sulfate and glucuronide to form 6-sulfatoxymelatonin; the presystemic metabolism rate can reach 85%. Experimental studies suggest that CYP1A1, CYP1A2 isoenzymes and possibly CYP2C19 of the cytochrome P450 system are involved in the metabolism of melatonin. The main metabolite of melatonin, 6-sulfatoxymelatonin, is inactive. Melatonin is excreted by the kidneys. The average half-life (T1/2) of melatonin is 45 minutes. Excretion is with the urine, about 90% as sulfate and glucuron conjugates of 6-hydroxymelatonin, and about 2-10% is excreted unchanged. Pharmacokinetic parameters are influenced by age, caffeine intake, smoking, taking oral contraceptives. Accelerated absorption and impaired elimination are observed in patients in critical condition. Elderly patients Melatonin metabolism is known to slow with age. At different doses of melatonin, higher values of 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. No cumulation of melatonin was noted in patients with impaired renal function during long-term treatment. These data are consistent with the short half-life of melatonin in humans.

Contraindications

Hypersensitivity to melatonin and other drug components; autoimmune diseases, allergic diseases; lymphogranulematosis, leukemia, lymphoma, myeloma, epilepsy, diabetes, chronic renal

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

Application during pregnancy and lactation

The drug is contraindicated during pregnancy and lactation.

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Side effects

Classification of adverse reactions by organs and systems is given with indication of their frequency: very frequently (≥1/10), frequently (≥1/100, 1/10), infrequently (≥1/1000, 1/100), rarely (≥1/10000, 1/1000), very rarely (1/10000), including individual reports, frequency is 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 nutrition disorders Rare: hypertriglyceridemia, hypokalemia, hyponatremia. Mental disorders Infrequent: irritability, nervousness, anxiety, insomnia, unusual dreams, nightmares and anxiety. Rare: mood swings, aggression, agitation, tearfulness, stress symptoms, disorientation, early morning awakening, increased libido, decreased mood, depression. Nervous system disorders Infrequent: migraine, headache, lethargy, psychomotor hyperactivity, dizziness, somnolence. Rare: fainting, memory impairment, impaired concentration, delirium, “restless legs” syndrome, poor quality of sleep, paresthesias. Visual disorders Rarely: decreased visual acuity, blurred vision, increased lacrimation. Hearing organ and labyrinth disorders Rarely: vertigo, positional vertigo. Cardiovascular system disorders Infrequent: arterial hypertension. Rare: angina pectoris, palpitations, hot flashes. Gastrointestinal disorders Infrequent: abdominal pain, abdominal pain in the upper abdomen, dyspepsia, ulcerative stomatitis, dry mouth, nausea. Rare: gastroesophageal disease, gastrointestinal disturbance or disorder, bullous stomatitis, ulcerative glossitis, vomiting, increased peristalsis, abdominal bloating, salivary hypersecretion, bad breath, abdominal discomfort, gastric dyskinesia, gastritis. Liver and biliary tract disorders Infrequent: hyperbilirubinemia. Skin and subcutaneous tissue disorders Infrequent: dermatitis, night sweats, itching and generalized itching, rash, dry skin. Rare: eczema, erythema, hand dermatitis, psoriasis, generalized rash, itching rash, nail lesions. Frequency unknown: angioedema, oral mucous membrane edema, tongue swelling. Musculoskeletal and connective tissue disorders Infrequent: pain in extremities. Rare: arthritis, muscle spasm, neck pain, night cramps. Renal and urinary tract disorders Infrequent: glucosuria, proteinuria. Rare: polyuria, hematuria, nycturia. Genital and breast disorders Infrequent: menopausal symptoms. Rare: priapism, prostatitis. Infrequent unknown: galactorrhea. General disorders and disorders at the site of administration Infrequent: asthenia, chest pain. Rare: fatigue, pain, thirst. Laboratory and instrumental data Infrequent: abnormal laboratory values of liver function, increased body weight. Rare: increased “hepatic” transaminase activity, abnormal blood electrolyte content, abnormal laboratory test results. If any of the side effects mentioned in the instructions are aggravated, or if you notice any other side effects not specified in the instructions, you should stop taking the drug and inform your doctor.

Overdose

There are no data on cases of melatonin overdose. Increased dose-dependent adverse reactions are possible.

Treatment: gastric lavage, symptomatic therapy.

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Pregnancy use

The drug is contraindicated in pregnancy and during breast-feeding.

Similarities

Melaxen, Sonnovan, Melarena, Melatonin, Wellson, Strengthen Your Immunity by Evalar