Melatonin Evalar
Melatonin Evalar: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Melatonin Evalar
ATX code: N05CH01
Active ingredient: melatonin (Melatonin)
Manufacturer: CJSC "Evalar" (Russia)
Description and photo update: 2020-18-08
Prices in pharmacies: from 197 rubles.
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Melatonin Evalar is an adaptogenic drug that has a sedative and hypnotic effect.
Release form and composition
The drug is produced in the form of film-coated tablets: white or almost white, round, biconvex, the core is from white to white with a brown tint, the presence of single brown inclusions is possible (20 or 25 pcs. In blisters, in cardboard a pack of 1, 2, 3, 4 or 5 packages and instructions for the use of Melatonin Evalar).
1 tablet contains:
- active substance: melatonin - 3 mg;
- auxiliary components: croscarmellose sodium, microcrystalline cellulose, colloidal silicon dioxide, calcium hydrogen phosphate, magnesium stearate;
- composition of the film shell: polysorbate 80, hypromellose (hydroxypropyl methylcellulose), titanium dioxide, polyethylene glycol 4000 (macrogol 4000), talc.
Pharmacological properties
Pharmacodynamics
Melatonin Evalar is an adaptogenic drug that has a sedative and hypnotic effect, normalizes circadian rhythms. Its active substance, melatonin, is a synthetic analogue of the pineal hormone (pineal gland), synthesized from amino acids of plant origin. The effect of melatonin is due to an increase in the concentration of GABA (gamma-aminobutyric acid) and serotonin in the midbrain and hypothalamus, a change in the activity of pyridoxal kinase, which is involved in the synthesis of dopamine, GABA and serotonin.
By regulating the cycle "sleep - wakefulness", as well as changes in locomotor activity and body temperature that occur in the body during the day, Melatonin Evalar has a positive effect on the intellectual-mnestic functions of the brain and the emotional-personal sphere. The hypnotic effect contributes to the normalization of night sleep and the organization of the biological rhythm. Melatonin, along with an acceleration of falling asleep and a decrease in the number of nighttime awakenings, improves the quality of sleep, and makes dreams more emotionally rich and vivid. Against the background of the use of the drug, the state of health improves after waking up in the morning, there is no feeling of fatigue, lethargy or weakness.
Taking Melatonin Evalar allows the body to quickly adapt to the change of time zones, in meteosensitive people - to changes in weather conditions, helps to reduce stress reactions and correct neuroendocrine functions.
The manifestation of immunostimulating and antioxidant properties by melatonin has been established.
Melatonin Evalar is not addictive or drug dependence.
Pharmacokinetics
After oral administration, melatonin is rapidly absorbed in the gastrointestinal tract. Bioavailability is approximately 15%. When the drug is taken in a dose of 3 mg, the maximum concentration (C max) in the blood plasma is reached after 20 minutes, in saliva - after 60 minutes. With max in blood serum is observed after 20–90 minutes and can be 10 times higher than the nighttime level of endogenous melatonin in blood serum.
Simultaneous food intake slows down the absorption of melatonin.
The kinetics of melatonin is linear in the range from 2 to 8 mg.
Plasma protein binding in vitro - 60%. Melatonin predominantly binds to albumin, high-density lipoprotein and alpha-1-acid glycoprotein. The volume of distribution (V d) is approximately 35 liters. It overcomes the blood-brain barrier, penetrates into saliva and placenta. In the cerebrospinal fluid, the level of melatonin concentration is 2.5 times lower than the plasma level.
It is metabolized mainly in the liver. During the initial passage through the liver, melatonin undergoes significant biotransformation by hydroxylation and conjugation with sulfate and glucuronide to form the main metabolite, 6-sulfatoxymelatonin, which is pharmacologically inactive. Up to 85% of the dose taken can undergo pre-systemic metabolism. The following isozymes of the cytochrome P 450 system are presumably involved in the metabolic process: CYP1A1, CYP1A2 and, possibly, CYP2C19.
The half-life (T 1/2) averages 45 minutes.
It is excreted through the kidneys: no more than 10% - unchanged, about 90% - in the form of glucuronic and sulfate conjugate of 6-hydroxymelatonin.
Pharmacokinetic parameters are impaired by smoking, caffeine intake and oral contraceptives. Accelerated absorption and impaired elimination can be observed in critically ill patients.
In the elderly, the metabolism of melatonin slows down, the rate of its absorption may be 50% lower than in young people.
With long-term treatment of patients with impaired renal function, the accumulation of melatonin was not recorded.
Indications for use
The use of Melatonin Evalar is indicated for sleep disorders, including those that are caused by disturbances in the sleep-wake rhythm with a sharp change in time zones.
Contraindications
Absolute:
- autoimmune diseases;
- severe renal failure;
- liver failure;
- period of pregnancy;
- breast-feeding;
- age up to 18 years;
- hypersensitivity to drug components.
Melatonin Evalar should be taken with caution in case of mild to moderate renal failure.
Melatonin Evalar, instructions for use: method and dosage
Melatonin Evalar tablets are taken orally 0.5 hours before going to bed.
Recommended dosage: 1 pc. (With 3 mg) once a day.
With desynchronosis (time zone change syndrome), the drug as an adaptogen is taken 1 day before the intended flight and continues for the next 2-5 days.
The maximum daily dose is 2 pcs.
Elderly patients should take the tablet 1-1.5 hours before bedtime.
Side effects
The classification of undesirable side effects of Melatonin Evalar was made in accordance with the following gradation of frequency of occurrence: very often - more than 1/10; often - more than 1/100, but less than 1/10; infrequently - more than 1/1000, but less than 1/100; rarely - more than 1/10 000, but less than 1/1000; very rarely - less than 1/10 000; frequency not established - the available data do not allow to establish the frequency of development of adverse reactions.
- on the part of the blood and lymphatic system: rarely - thrombocytopenia, leukopenia;
- from the nervous system: infrequently - lethargy, drowsiness, headache, dizziness, migraine, psychomotor hyperactivity; rarely - poor sleep quality, fainting, impaired concentration, memory impairment, delirium, dreaming (oneiric) condition, restless legs syndrome, paresthesia;
- mental disorders: infrequently - insomnia, irritability, anxiety, nervousness, anxiety, nightmares, unusual dreams; rarely - early morning awakening, low or unstable mood, agitation, tearfulness, aggression, stress symptoms, increased libido, disorientation, depression;
- from the gastrointestinal tract: infrequently - dry mouth, ulcerative stomatitis, nausea, dyspepsia, abdominal pain in the upper abdomen, abdominal pain; rarely - bad breath, ulcerative glossitis, salivary hypersecretion, bullous stomatitis, vomiting, bloating, increased peristalsis, abdominal discomfort, gastrointestinal disturbance or disorder, stomach dyskinesia, gastroesophageal disease, gastritis;
- from the hepatobiliary system: infrequently - hyperbilirubinemia;
- from the immune system: the frequency is not established - hypersensitivity reactions;
- on the part of the cardiovascular system: infrequently - arterial hypertension; rarely - hot flashes, palpitations, exertional angina;
- from the organ of hearing and labyrinth disorders: rarely - positional vertigo, vertigo;
- on the part of the organ of vision: rarely - increased lacrimation, blurred vision, decreased visual acuity;
- from the musculoskeletal system: infrequently - pain in the limbs; rarely - muscle spasm, arthritis, night cramps, neck pain;
- from the genitals and breast: infrequently - menopausal symptoms; rarely - prostatitis, priapism; frequency not established - galactorrhea;
- from the urinary system: infrequently - proteinuria, glucosuria; rarely - nocturia, polyuria, hematuria;
- from the side of metabolism and nutrition: rarely - hypokalemia, hyponatremia, hypertriglyceridemia;
- infectious and parasitic pathologies: rarely - herpes zoster;
- dermatological reactions: infrequently - sweating at night, itching and generalized itching, dry skin, rash, dermatitis; rarely - itchy rash, generalized rash, erythema, hand dermatitis, nail lesions, psoriasis, eczema; frequency not established - edema of the oral mucosa, Quincke's edema, tongue edema;
- general disorders: infrequently - chest pain, asthenia; rarely - thirst, fatigue, pain;
- laboratory and instrumental disorders: infrequently - an increase in body weight, impaired liver function indicators; rarely - an increase in the activity of liver transaminases, deviation from the normal results of laboratory tests, a violation of the level of electrolytes in the blood.
Overdose
A symptom of a melatonin overdose may be the development of drowsiness. Taking the drug up to 300 mg per day did not cause clinically significant adverse reactions. In case of a significant overdose (a dose of melatonin up to 1000 mg), involuntary loss of consciousness was recorded.
Treatment: immediate gastric lavage, taking activated charcoal, prescribing symptomatic therapy. It should be borne in mind that after oral administration, the clearance of melatonin is assumed within 12 hours.
special instructions
During the period of application of Melatonin Evalar, exposure to bright light is not recommended.
It should be borne in mind that smoking can reduce the concentration of melatonin.
Influence on the ability to drive vehicles and complex mechanisms
The use of Melatonin Evalar negatively affects the ability of patients to perform potentially hazardous activities that are associated with increased concentration of attention and the speed of psychomotor reactions, including driving and complex mechanisms.
Application during pregnancy and lactation
The use of Melatonin Evalar is contraindicated during the period of gestation and breastfeeding.
Women wishing to become pregnant should take into account the weak contraceptive effect of the drug.
Pediatric use
Melatonin Evalar tablets are not prescribed for patients under 18 years of age.
With impaired renal function
Melatonin Evalar is contraindicated in patients with severe renal failure.
It is recommended to take the drug with caution in case of mild and moderate renal failure.
For violations of liver function
It is contraindicated to use Evalar Melatonin for liver failure.
Use in the elderly
Elderly patients should take Melatonin Evalar 1 tablet 1–1.5 hours before bedtime.
Drug interactions
- fluvoxamine: a combination with fluvoxamine, which contributes to a significant increase in the concentration of melatonin, should be avoided, as the AUC (area under the concentration-time pharmacokinetic curve) of the latter increases 17 times, and C max - 12 times;
- cimetidine, 5- and 8-methoxypsoralen, estrogens (including contraceptives, hormone replacement therapy drugs): each of these drugs inhibits the metabolism of melatonin, which leads to an increase in its level in blood plasma, therefore, it is recommended to be careful;
- quinolones: it is possible to increase the exposure of melatonin against the background of concomitant therapy with quinolones;
- carbamazepine, rifampicin: inducers of the CYP1A2 isoenzyme contribute to a decrease in the plasma concentration of melatonin;
- agonists or antagonists of antidepressants, adrenergic and opioid receptors, prostaglandin inhibitors, tryptophan, benzodiazepines, ethanol: the effect of these drugs on the pharmacodynamics or pharmacokinetics of melatonin has not been studied, but it should be borne in mind that they have an effect on the secretion of endogenous melatonin;
- ethanol: helps to reduce the effectiveness of the drug;
- zaleplon, zopiclone, zolpidem and other hypnotics of the benzodiazepine and non-benzodiazepine series: melatonin potentiates the sedative effect of these drugs, promotes the progression of memory, attention and coordination disorders;
- Imipramine: Combining imipramine with melatonin increases feelings of calmness and makes it difficult to complete specific tasks.
- thioridazine: in combination with thioridazine, an increase in the feeling of clouding in the head is observed.
Analogs
Melatonin Evalar analogs are Melatonin-SZ, VELSON, Kakspal Neo, Meladapt, Melaxen, Melaxen Balance, Melarena, Melarithm, Sonnovan, Circadin, Doxylamin, Donormil, Reslip, Slipzon, Sanval, SOMNOL, Relaxon, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Available without a prescription.
Reviews about Melatonin Evalar
Reviews about Melatonin Evalar are mostly positive. Patients, pointing out the effectiveness of the drug, report that taking the drug provides quick and easy falling asleep, healthy sound sleep and good vigor in the morning. Its advantages include plant origin, the absence of side effects and addiction.
There are individual reviews in which patients give a negative assessment of the effect of this sleeping pill. They complain of a complete lack of desire to sleep and note the appearance of a rapid heartbeat.
Price for Melatonin Evalar in pharmacies
The price for Melatonin Evalar for a pack containing 20 tablets can range from 208 rubles.
Melatonin Evalar: prices in online pharmacies
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Drug name Price Pharmacy |
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Melatonin Evalar tab. p.p. 3 mg 20 pcs. 197 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
