Instructions Vita-melatonin tablets 3 mg blister No. 30
Composition
active ingredient: melatonin;
1 tablet contains 3 mg of melatonin;
Excipients: lactose monohydrate, microcrystalline cellulose, potato starch, calcium stearate.
Dosage form
Pills.
Main physicochemical properties: flat-cylindrical tablets with beveled edges and a score, white or almost white in color.
Pharmacotherapeutic group
Hypnotics and sedatives. Melatonin receptor agonists. ATC code N05C H01.
Pharmacological properties
Pharmacodynamics
Vita-melatonin® is a synthetic analogue of the pineal neuropeptide melatonin. The main effect of Vita-melatonin® is to inhibit the secretion of gonadotropins. To a lesser extent, the drug inhibits the secretion of other hormones of the adenohypophysis - corticotropin, thyrotropin, somatotropin. In addition, under the influence of melatonin in the midbrain and hypothalamus, the content of GABA and serotonin increases.
The above processes lead to the normalization of circadian rhythms, changes in sleep and wakefulness, the rhythmicity of gonadotropic effects and sexual function, increase mental and physical performance, and reduce the manifestations of stress reactions.
The drug has antioxidant properties, which determines its membrane-stabilizing effect. Normalizes the permeability of the vascular wall and increases its resistance, improves microcirculation. The drug improves only the impaired functional state of the endothelium, without affecting the normal function of the endothelium. Melatonin reduces systolic pressure and heart rate in elderly patients at rest, reduces the increase in blood pressure during psycho-emotional stress. The drug normalizes the autonomic nervous regulation of the cardiovascular system mainly at night, which contributes to the improvement of the impaired diurnal profile of blood pressure.
Vita-melatonin®, by stimulating cellular immune responses, has an immunomodulatory effect on the body.
Pharmacokinetics
After oral administration, melatonin undergoes significant transformation during the first pass through the liver. The bioavailability of the drug is 30-50%. When administered orally at a dose of 3 mg, the maximum concentration in serum and saliva is reached after 20 and 60 minutes, respectively.
Melatonin crosses the blood-brain barrier and is detected in the placenta. The average half-life of melatonin is 45 minutes. It is excreted from the body by the kidneys.
Indication
For the prevention and treatment of circadian rhythm disorders "sleep-wake" when changing time zones, manifested by increased fatigue; sleep disorders, including chronic insomnia of functional origin, insomnia in the elderly (including with concomitant hypertension and hypercholesterolemia); to increase mental and physical performance, as well as to alleviate stress reactions and depressive states of a seasonal nature. High blood pressure and hypertension (stages I-II) in elderly patients (as part of complex therapy).
Contraindication
Hypersensitivity to the components of the drug. Autoimmune diseases, lymphogranulomatosis, leukemia, lymphoma, myeloma, epilepsy, diabetes mellitus. Simultaneous use of monoamine oxidase inhibitors, corticosteroids, cyclosporine.
Interaction with other medicinal products and other types of interactions
Drugs that block β-adrenergic receptors, clonidine, dexamethasone, fluvoxamine and some other drugs can change the secretion of endogenous melatonin. Vita-melatonin® can affect the effectiveness of hormonal drugs (estrogens, androgens, etc.), increase the binding of benzodiazepines to specific receptors, therefore their simultaneous use requires medical supervision.
Melatonin may enhance the sedative properties of benzodiazepines and non-benzodiazepine hypnotics such as zaleplon, zolpidem and zopiclone. There is clear evidence of a pharmacodynamic interaction between melatonin and zolpidem within one hour of co-administration. Co-administration results in greater impairment of attention, memory and coordination compared to zolpidem alone.
Vita-melatonin® may potentiate the antitumor effect of tamoxifen.
The dopaminergic and serotoninergic effects of methamphetamine may be enhanced when used simultaneously with Vita-melatonin®.
Vita-melatonin® may potentiate the antibacterial effect of isoniazid.
Melatonin can be used with lisinopril in concomitant antihypertensive therapy in patients with functional insufficiency of the pineal gland, enhancing its effect.
Melatonin has been shown to induce CYP3A in vitro at concentrations exceeding therapeutic levels. The clinical significance of this finding is unknown. Induction may result in decreased plasma concentrations of concomitantly administered drugs.
Patients receiving 5- or 8-methoxypsoralen, which increases melatonin levels by inhibiting its metabolism, should be carefully monitored.
Patients receiving cimetidine, a CYP2D inhibitor that increases melatonin plasma levels by inhibiting its metabolism, should be carefully monitored.
Smoking may reduce melatonin levels by inducing CYP1A2.
Patients receiving estrogens (e.g. contraceptives or hormone replacement therapy) should be carefully monitored, as melatonin levels are increased due to inhibition of its metabolism by CYP1A1 and CYP1A2.
CYP1A2 inhibitors, such as quinolones, may enhance the effects of melatonin.
CYP1A2 inducers, such as carbamazepine and rifampicin, may contribute to a decrease in melatonin plasma concentrations.
Application features
Do not use in women planning pregnancy due to the specific contraceptive effect of melatonin.
When using Vita-melatonin®, bright lighting should be avoided.
In patients with liver cirrhosis, the level of melatonin metabolism is reduced, so the drug should be used with caution in these patients.
The drug can be used in patients with high blood pressure (especially systolic) and hypercholesterolemia. With prolonged use, Vita-melatonin® reduces cholesterol levels in patients with hypercholesterolemia, but does not affect cholesterol levels in patients with normal serum levels. The drug reduces insulin and glucose levels in blood plasma, so it can be used in patients with hypertension and hypercholesterolemia accompanied by insulin resistance (HOMA index above 3 standard units).
It is prescribed with caution in cases of hormonal disorders and/or hormone therapy, as well as in patients with allergic diseases.
Melatonin causes drowsiness. The drug should be used with caution if the potential drowsiness may be associated with a risk or danger to the patient's health.
It is not recommended for use in patients with autoimmune diseases.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Simultaneous intake of alcohol reduces the effectiveness of melatonin.
Ability to influence reaction speed when driving vehicles or other mechanisms
Given that the drug causes drowsiness, while taking the drug you should refrain from driving vehicles and performing other work that requires concentration.
Use during pregnancy or breastfeeding
The drug is not used during pregnancy and breastfeeding due to the lack of clinical data.
Method of administration and doses
For treatment, Vita-melatonin® is prescribed internally to adults at a dose of 3 mg to 6 mg (1-2 tablets) per day. The tablets should be taken 30 minutes before bedtime every day, preferably at the same time.
The course of treatment lasts until the physiological rhythm of "sleep-wakefulness" is restored, but not more than 1 month.
In the case of prophylactic use, the dose of the drug and the duration of its use are determined by the doctor depending on the individual characteristics of the patient and the course of the disease. Usually, 1-2 tablets are taken per day 30 minutes before bedtime, preferably at the same time, for 2 months with a week break between courses (course of use - 1 month).
For the treatment of chronic sleep disorders (including concomitant hypertension and/or hypercholesterolemia) in elderly patients, the drug is prescribed in a minimum effective dose of 1.5 mg (½ tablet) once a day, the tablets are taken 30 minutes before bedtime. If the effectiveness is insufficient, the dose is increased to 3 mg. The drug should be discontinued gradually, reducing the dose over 1-2 weeks.
The same regimen is used by elderly patients with high blood pressure and hypertension. The drug can be used for 3-6 months with 1-week intervals between monthly courses of treatment.
Renal insufficiency. There are no studies on the effect of varying degrees of renal insufficiency on the pharmacokinetics of melatonin, therefore melatonin should be used with caution in such patients.
Hepatic impairment. There is no experience with the use of melatonin in patients with hepatic impairment. Published data suggest markedly increased levels of endogenous melatonin during the daytime as a result of reduced clearance in such patients. Therefore, melatonin is not recommended for use in patients with hepatic impairment.
Children
There is no experience with the use of the drug in pediatric patients.
Overdose
Several cases of melatonin overdose have been described (single dose of 24-30 mg of melatonin). Overdose may cause disorientation, prolonged sleep, and anterograde memory loss. Treatment is symptomatic.
Adverse reactions
In some cases, adverse reactions may occur when using the drug.
Infections and infestations: shingles.
Cardiovascular system: angina pectoris, palpitations.
On the part of the psyche: irritability, increased excitability, anxiety, insomnia, unusual dreams, mood swings, aggressiveness, agitation, tearfulness, early morning awakening, increased libido, depression.
From the side of the central nervous system: migraine, increased psychomotor activity, dizziness, drowsiness, memory impairment, impaired attention, impaired sleep quality, paresthesia.
On the part of the organs of vision: decreased visual acuity, blurred vision, increased lacrimation.
From the side of the organs of hearing and vestibular apparatus: dizziness when changing body position.
Vascular disorders: flushing.
Gastrointestinal: abdominal pain, constipation, dry mouth, oral mucosal ulcers, vomiting, abnormal bowel sounds, flatulence, increased salivation, bad breath, gastroesophageal reflux.
Metabolic: hypertriglyceridemia, hypocalcemia, hyponatremia.
From the hepatobiliary system: hyperbilirubinemia, increased activity of liver enzymes, impaired liver function, deviations from the norm of laboratory test data.
Skin and subcutaneous tissue disorders: night sweats, dermatitis, eczema, erythema, itchy rash; itching, dry skin, psoriasis, nail disorders.
Musculoskeletal and connective tissue disorders: pain in extremities, muscle spasms, neck pain, arthritis.
From the genitourinary system: glycosuria, proteinuria, menopausal symptoms, polyuria, hematuria, nocturia, priapism, prostatitis.
General disorders: asthenia, chest pain, fatigue, thirst.
Other disorders: weight gain, changes in electrolyte levels.
Expiration date
3 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
10 tablets in a blister; 3 blisters in a pack.
Vacation category
According to the recipe.
Producer
JSC "KYIV VITAMIN FACTORY".
Location of the manufacturer and its business address
04073, Ukraine, Kyiv, Kopylivska St., 38.
