Synthetic analogue pineal hormone (epiphysis); It has adaptogenic, sedative, hypnotic effect. Normalize circadian rhythms.
Increases concentration of gamma-aminobutyric acid (GABA), serotonin and average brain and hypothalamus, piridoksalkinazy modifies the activity 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 intellectual-mental functions of the brain, in the emotionally-personal sphere.
It contributes to the organization of biological rhythm and normalization of nocturnal sleep. Improves the quality of sleep, fall asleep faster, regulate neuroendocrine function. The body adapts to changes in the weather-sensitive people weather conditions.
One tablet film coating contains:
The active substance :
Melatonin – 3 mg.
calcium hydrogen phosphate dihydrate – 64.67 mg
microcrystalline cellulose – 25.00 mg,
Povidone K 25 – 3.33 mg
croscarmellose sodium – 2.00 mg,
talc – 1.00 mg,
colloidal silicon dioxide – 0.50 mg,
calcium stearate – 0.50 mg.
The composition of the shell :
Opadry white (03A280002) – 3.00 mg [hypromellose (hydroxypropyl) – 40%, microcrystalline cellulose – 32% titanium dioxide – 20%, macrogol (polyethylene glycol) – 8%].
When sleep disorders, including due to arrhythmia “sleep-wake” such as desynchronosis (sharp jetlag).
- hypersensitivity to the drug;
- autoimmune diseases;
- liver failure;
- severe renal insufficiency;
- Pregnancy and breast-feeding;
- the age of 18 years (the efficacy and safety has not been established).
Velson® The drug should be used with caution in patients with various degrees of renal insufficiency.
Classification side reactions organs and systems indicating the frequency of occurrence: very often (≥1 / 10), often (≥1 / 100, < 1/10), rare (≥1 / 1000, < 1/100), rarely (≥1 / 10000, < 1/1000), very rare (< 1/10000), including individual messages, frequency not known (frequency can not be estimated from available data).
Infectious and parasitic diseases: rare – herpes zoster.
Blood disorders and lymphatic system: rarely – leukopenia, thrombocytopenia.
Violations by the immune system: the frequency is unknown – a hypersensitivity reaction.
Violations by the Metabolism and nutrition: rarely – hypertriglyceridemia, hypokalemia, hyponatremia.
Mental disorders: rarely – irritability, nervousness, restlessness, insomnia, abnormal dreams, nightmares, anxiety; rarely – mood swings, aggression, agitation, crying, stress symptoms, disorientation, early morning awakening, increased libido, depressed mood, depression.
Disorders of the nervous system: Infrequent – Migraine, headache, lethargy, psychomotor hyperactivity, dizziness, drowsiness; rarely – fainting, memory impairment, impaired concentration, delirium, syndrome of “restless legs”, poor quality sleep, paraesthesia.
Violations by the organ of vision: rarely – blurred vision, blurred vision, increased lacrimation.
Violations by the organ of hearing and labyrinth disorders: rare – vertigo, positional vertigo.
Violations of the heart: rarely – angina, palpitations.
Violations by vessels: seldom – hypertension; rare – “tides”.
Disorders of the gastrointestinal tract: rare – abdominal pain, abdominal pain in the upper abdomen, indigestion, ulcerative stomatitis, dry mouth, nausea; rarely – gastroesophageal disease, gastrointestinal disorder or a disorder, bullous disease, ulcerative glossitis, vomiting, increased peristalsis, bloating, hypersecretion of saliva, bad breath, abdominal discomfort, dyskinesia of the stomach, gastritis.
Violations of the liver and biliary tract: rarely – hyperbilirubinemia.
Violations of the skin and subcutaneous tissue disorders: uncommon – dermatitis, night sweats, itching and generalized itching, rash, dry skin; rarely – eczema, erythema, dermatitis of hands, psoriasis, generalized rash, itchy rash, nail infections; frequency is unknown – angioedema, swelling of oral mucous membrane, edema language.
Violations by musculoskeletal and connective tissue disorders: rarely – pain in the extremities; rarely – arthritis, muscle spasms, neck pain, night cramps.
Violations of the kidneys and urinary tract: infrequently – glycosuria, proteinuria; rarely – polyuria, hematuria, nocturia.
Violations by the genitals and mammary glands: rarely – menopausal symptoms; rarely – priapism, prostatitis; the frequency is unknown – galactorrhea.
General disorders and at the injection site: rare – fatigue, chest pain; rarely – fatigue, pain, thirst.
Effect on results of laboratory and instrumental investigations: infrequently – abnormal liver function laboratory parameters, body weight gain; rarely – increased activity of “liver” transaminases, abnormal electrolytes in the blood, abnormal laboratory test results.
If any of these instructions side effects are compounded, or if you notice any other side effects not mentioned in the instructions, tell your doctor.
How to accept, acceptance rate and dosage
Inside, drinking plenty of fluids.
Sleep disorders: 1 to 3 mg once a day for 30-40 minutes before bedtime.
When desynchronosis as adaptogena jet lag: 1 day before the flight and the next 2-5 days to 3 mg for 30-40 minutes before sleep.
The maximum daily dose – 6 mg.
With age there is a decrease metabolism of melatonin, which should be considered when selecting the dosing regimen for elderly patients. With this in mind in elderly patients can receive medication for 60-90 minutes before bedtime.
Patients with impaired renal function
Effect of varying degrees of renal impairment on the pharmacokinetics of melatonin has not been studied, however, melatonin should be taken with caution in these patients. Patients with severe renal impairment is not recommended to use the drug.
In the dark place at a temperature not higher than 25 ° C.
Keep out of the reach of children.
It is known that in concentrations much higher than therapeutic, melatonin induces isoenzyme CYP3A in vitro. The clinical significance of this phenomenon is not fully elucidated. In the case of induction symptoms should consider lowering the dose at the same time used drugs.
At concentrations much higher than therapeutic, melatonin does not induce isozymes group CYP1A in vitro. Therefore, melatonin interaction with other drugs due to the effect of melatonin on CYP1A isozymes group apparently insignificant.
The metabolism of melatonin, mainly mediated by CYP1A isozymes. Therefore, melatonin may be interactions with other drugs due to the effect of melatonin on CYP1A isozymes group.
Use caution in patients taking fluvoxamine, which increases the concentration of melatonin (increase in AUC and Cmax 17 times to 12 times) by inhibiting its metabolism cytochrome P450 (CYP): CYP1A2 and CYP2C19. such combinations should be avoided.
Use caution in patients taking 5- and 8-methoxy-psoralen, which increases the concentration of melatonin from inhibition of its metabolism.
Use caution in patients receiving cimetidine (an inhibitor of isozyme CYP2D), because it increases the concentration of melatonin in the plasma due to inhibition of the latter.
Smoke can reduce the concentration of melatonin by induction of isoenzyme CYP1A2.
Use caution in patients taking estrogens (e.g., contraception or hormone replacement therapy), which increase the concentration of melatonin by inhibiting their metabolism isozymes CYP1A1 and CYP1A2.
Inhibitors isoenzymes CYPA2, e.g., quinolones, capable of increasing the exposure of melatonin.
Isoenzyme inducers of CYP1A2, such as carbamazepine and rifampicin, can reduce the plasma concentration of melatonin.
In recent literature has lots of data concerning the effect of agonists / antagonists of adrenergic receptors and opioid, antidepressants, prostaglandin inhibitors, benzodiazepines, tryptophan and alcohol on endogenous melatonin secretion. Study the mutual influence of these drugs on the dynamics and kinetics of melatonin are not carried out.
During the reception, melatonin should not drink alcohol, because it reduces the effectiveness of the drug.
Melatonin potentiates the sedative effect of benzodiazepine and non-benzodiazepine hypnotics, such as zaleplon, zolpidem and zopiclone. In the clinical study were clear signs transitory pharmacodynamic interaction between melatonin and zolpidem hour after receiving them. The combined use can lead to a progressive disorder of attention, memory and coordination compared with monotherapy zolpidem.
During the research, melatonin was administered together with thioridazine and imipramine, drugs that affect the central nervous system. In none of the cases did not reveal clinically significant pharmacokinetic interaction. However, the simultaneous use of melatonin resulted in increased feelings of tranquility and difficulty in performing certain tasks in comparison with mono therapy with imipramine, as well as to strengthen the sense of “cloud in my head”, in comparison with monotherapy thioridazine.
During the period of Velson® drug is recommended to avoid exposure to bright light.
It is necessary to inform women wishing to become pregnant, about the presence of a weak drug contraceptive effect.
There are no clinical data on the use of melatonin in patients with autoimmune diseases, and therefore, is not recommended in these patients.
According to literature data, the use of melatonin in a daily dose of 300 mg not causing clinically significant adverse reactions. Hyperemia observed, abdominal cramps, diarrhea, headache and scotoma in the application of melatonin in doses of 3000-6600 mg for several weeks. In the application of very high doses of melatonin (1 g) was observed involuntary loss of consciousness.
Symptoms: an overdose may develop drowsiness.
Treatment: gastric lavage, activated charcoal, symptomatic therapy. The clearance of the active substance is assumed within 12 hours after ingestion.