Welson
Welson: 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: Velson
ATX code: N05CH01
Active ingredient: melatonin (Melatonin)
Manufacturer: JSC "Pharmproekt" (Russia)
Description and photo update: 2020-25-06
Prices in pharmacies: from 385 rubles.
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Welson is an adaptogenic drug with a sedative and hypnotic effect.
Release form and composition
The product is produced in the form of film-coated tablets: round biconvex, the film shell is white, the core on a cross-section is from white to almost white with a brown tint (10 pcs. In a blister; in a cardboard box 3, 6 or 9 packages and instructions for use of Welson).
1 tablet contains:
- active substance: melatonin - 3 mg;
- additional components: microcrystalline cellulose, calcium hydrogen phosphate dihydrate, croscarmellose sodium, povidone K-25, calcium stearate, talc, colloidal silicon dioxide;
- film shell: Opadry white (03A280002) [microcrystalline cellulose, hypromellose (hydroxypropyl methylcellulose), macrogol (polyethylene glycol), titanium dioxide].
Pharmacological properties
Pharmacodynamics
Welson's active substance is a synthetic analogue of a hormone produced by the pineal gland (pineal gland). Normally, the production of melatonin in the pineal gland is subject to a certain diurnal rhythm. The secretion of this substance is synchronized with the day / night cycle, its plasma concentration reaches a maximum at night, and a minimum during the day. The absence of light is fixed by the retina of the eye, from there the signal enters the suprachiasmatic nucleus via the retinohypothalamic pathway, and then to the upper cervical ganglion (cervical ganglion). From the endings of the sympathetic nerve fibers that depart from the neurons of this node, norepinephrine is released into the parenchyma of the pineal gland, which activates the synthesis of melatonin. The secretion of the latter is suppressed by light.
Weakening of melatonin production and disturbance of circadian rhythms can occur when any of the links in the secretion of this hormone is affected.
The following conditions can cause a decrease in melatonin production:
- desynchrony (disorder of the sleep-wake cycle), arising from the effects of endogenous (sleep delay / advancing syndromes) and exogenous (sleep disturbances in the event of a change in time zones, shift work schedule) factors;
- increased exposure in the dark to artificial light sources (especially of the blue spectrum), such as screens of smartphones, computers, TVs;
- perimenopause and postmenopause in women;
- elderly age;
- taking benzodiazepines, non-steroidal anti-inflammatory drugs (NSAIDs), β-blockers;
- alcohol consumption and active smoking.
Welson promotes the normalization of circadian rhythms, demonstrates adaptogenic, hypnotic and sedative effects. Provides an increase in the concentration of serotonin and gamma-aminobutyric acid (GABA) in the hypothalamus and midbrain, regulates the activity of the enzyme pyridoxal kinase, which is involved in the production of GABA, serotonin and dopamine. The hormone is responsible for the sleep-wake cycle, diurnal changes in body temperature and physical activity; helps to improve the intellectual and mnestic functions of the brain and emotional and personal sphere.
Welson leads to the normalization of nighttime sleep and promotes the formation of a biological rhythm. Melatonin speeds up falling asleep, reducing the number of nighttime awakenings, and improves the quality of sleep. After waking up in the morning, the drug does not cause feelings of lethargy, fatigue and loss of strength. Reduces the level of stress reactions, regulates the functions of the neuroendocrine system. For patients sensitive to weather conditions, the tool helps to adapt to changes in weather conditions.
Taking melatonin does not lead to addiction and addiction.
Pharmacokinetics
After oral administration, melatonin is intensively absorbed from the gastrointestinal tract (GIT). The kinetics of the active substance in the dose range from 2 to 8 mg is linear. With oral administration of melatonin at a dose of 3 mg in saliva and blood plasma, the maximum concentration (C max) is recorded, respectively, after 60 and 20 minutes. The period of reaching C max in blood serum (T Cmax) is on average 60 minutes (interval 20–90 minutes). After using melatonin at a dose of 3–6 mg, serum C max is usually 10 times higher than the endogenous melatonin content in serum at night. Its absorption is slowed down with concomitant food intake.
After oral administration, the bioavailability of melatonin varies from 9 to 33%, and is approximately equal to 15%.
The connection of the active substance with plasma proteins in in vitro studies is 60%. Melatonin mainly binds to α 1 -acid glycoprotein, albumin, high density lipoproteins (HDL). Welson is intensively distributed in saliva and penetrates the blood-brain barrier, is detected in the placenta. The volume of distribution (V d) is approximately 35 liters, the level of the drug in the cerebrospinal fluid is 2.5 times lower than that in the plasma.
Metabolic transformation of melatonin mainly occurs in the liver with possible participation, according to the results of experimental studies, isoenzymes CYP1A1 and CYP1A2, as well as CYP2C19 of cytochrome P450. After ingestion, the active substance undergoes significant transformation during the initial passage through the liver, where it is hydroxylated, and conjugated with glucuronide and sulfate to form the main metabolite of 6-sulfatoxymelatonin, which is not active. The degree of presystemic metabolism is quite high - up to 85%.
Melatonin is excreted from the body by the kidneys - approximately 90% is excreted in the urine in the form of glucuronic and sulfate conjugates of 6-hydroxymelatonin, and approximately 2-10% is excreted unchanged. The average half-life (T 1/2) is 45 minutes.
Welson's pharmacokinetic parameters are influenced by age, smoking, caffeine consumption, and oral contraceptive use. In a critical condition, there is an acceleration of absorption and a violation of the elimination of the drug.
Indications for use
Welson is recommended for use in sleep disorders, including those associated with sleep-wake rhythm disturbances, including desynchrony.
Contraindications
Absolute:
- severe renal failure;
- autoimmune diseases;
- liver failure;
- age up to 18 years;
- pregnancy and lactation;
- hypersensitivity to any of Welson's constituents.
Since the effect on the pharmacokinetics of melatonin in mild and moderate renal failure has not been studied, if patients with this pathology have this pathology, it is necessary to use an adaptogenic agent with caution.
Welson, instructions for use: method and dosage
Welson tablets are taken orally. They should be taken with a sufficient amount of liquid.
Recommended dosage regimen:
- sleep disorders, desynchrony: once a day at a dose of 3 mg (1 tablet) 30-40 minutes before going to bed;
- change of time zones as an adaptogenic agent: 1 day before the planned flight and then for 2-5 days, 3 mg (1 tablet) 30-40 minutes before bedtime.
The maximum daily dose of Welson should not exceed 6 mg.
Side effects
The incidence of side effects by systemic organ classes [scale: (≥ 1/10) - very often, (from ≥ 1/100 to <1/10) - often, (from ≥ 1/1000 to <1/100) - infrequently, (from ≥ 1/10 000 to <1/1000) - rarely, (<1/10 000, including individual messages) - extremely rare; the frequency cannot be calculated based on the available data - with an unknown frequency]:
- lymphatic system and blood: rarely - thrombocytopenia, leukopenia;
- immune system: with unknown frequency - hypersensitivity reactions;
- parasitic and infectious lesions: rarely - herpes zoster;
- nervous system: infrequently - drowsiness, lethargy, psychomotor hyperactivity, headache, migraine, dizziness; rarely - poor sleep quality, impaired concentration and / or memory, paresthesia, restless legs syndrome, fainting, delirium;
- cardiovascular system: infrequently - arterial hypertension; rarely - hot flashes, palpitations, exertional angina;
- organ of hearing, labyrinth disorders: rarely - vertigo, positional vertigo;
- organ of vision: rarely - increased lacrimation, blurred vision, decreased visual acuity;
- mental disorders: infrequently - anxiety, insomnia, irritability, nervousness, unusual dreams, anxiety, nightmares; rarely - early morning awakening, mood changes, tearfulness, agitation, aggression, stress symptoms, low mood, disorientation, increased libido, depression;
- metabolism: rarely - hypokalemia, hyponatremia, hypertriglyceridemia;
- digestive tract: infrequently - nausea, dry mouth, dyspepsia, ulcerative stomatitis, abdominal pain, including pain in the upper abdomen; rarely - salivary hypersecretion, bloating, bad breath, vomiting, abdominal discomfort, gastrointestinal upset / disorder, increased peristalsis, gastric dyskinesia, ulcerative glossitis, gastritis, bullous stomatitis, gastroesophageal disease;
- hepatobiliary system: infrequently - hyperbilirubinemia;
- urinary system: infrequently - proteinuria, glucosuria; rarely - hematuria, polyuria, nocturia;
- musculoskeletal system and connective tissue: infrequently - pain in the limbs; rarely - night cramps, muscle spasm, neck pain, arthritis;
- genitals and mammary gland: infrequently - symptoms of menopause; rarely - prostatitis, priapism; with an unknown frequency - galactorrhea;
- skin and subcutaneous fat: infrequently - night sweats, dry skin, rash, dermatitis, itching (including generalized); rarely - erythema, nail lesions, hand dermatitis, itchy rash, eczema, generalized rash, psoriasis; with an unknown frequency - swelling of the tongue and / or oral mucosa, Quincke's edema;
- general disorders: infrequently - painful sensations in the chest, asthenia; rarely - fatigue, thirst, pain;
- laboratory results: infrequently - increased body weight, abnormal liver function indicators; rarely - a change in the level of electrolytes in the blood, an increase in the activity of hepatic transaminases, a deviation from the normal results of laboratory tests.
Overdose
According to published data, taking the drug in a daily dose not exceeding 300 mg did not lead to clinically significant side effects. When using Welson for several weeks at doses of 3000–6600 mg, disorders such as hyperemia, diarrhea, abdominal cramps, scotoma and headache were recorded.
Loss of consciousness was noted in the case of taking Welson in doses up to 1000 mg. Overdose of melatonin may cause drowsiness. In this condition, gastric lavage, intake of activated carbon, symptomatic therapy are recommended.
The clearance of melatonin after oral administration is not expected to exceed 12 hours.
special instructions
After taking the tablets, you need to beware of exposure to bright light, since the latter can weaken the effectiveness of the therapy.
The use of Welson is not recommended for persons with autoimmune diseases, due to the lack of clinical data on the treatment of sleep disorders with melatonin in this category of patients.
Influence on the ability to drive vehicles and complex mechanisms
The adaptogenic drug causes drowsiness, therefore, during the period of administration, it is necessary to refrain from driving vehicles and operating other potentially dangerous and complex mechanisms.
Application during pregnancy and lactation
For the treatment of pregnant and breastfeeding women, Welson tablets cannot be used.
Patients planning a pregnancy need to remember that the drug has a weak contraceptive effect.
Pediatric use
Welson is contraindicated for persons under 18 years of age, due to the lack of data indicating its effectiveness and safety in children and adolescents.
With impaired renal function
In the presence of impaired renal function, prolonged use of melatonin does not lead to its accumulation, which is consistent with a short T 1/2 in humans. In patients with severe renal failure, drug therapy is contraindicated; with mild to moderate degrees, Welson must be taken with caution.
For violations of liver function
Due to the fact that Welson's metabolism occurs mainly in the liver, when its function is impaired, the level of endogenous melatonin increases. In the daytime, in patients with cirrhosis of the liver, the concentration of the drug increases significantly.
Treatment with the drug is contraindicated in patients with hepatic impairment.
Use in the elderly
In elderly patients, the rate of absorption of melatonin can be reduced by 50%, as well as its biotransformation slowed down. When using different doses of Welson in elderly people, higher values of C max and values of the area under the concentration-time curve (AUC) were recorded, indicating a reduced metabolism in this age group. As a result, elderly patients can take the drug 1-1.5 hours before bedtime.
Drug interactions
Melatonin in concentrations significantly exceeding therapeutic ones induces the CYP3A isoenzyme in vitro. The clinical significance of this phenomenon has not been precisely established. If signs of induction appear, it may be necessary to reduce the doses of the funds simultaneously received with it.
Interaction reactions are possible with the combined use of melatonin with the following drugs (combinations require special care):
- cimetidine (inhibitor of CYP2D isoenzymes): increases the plasma content of melatonin in the blood;
- 5- and 8-methoxypsoralen: the concentration of melatonin in the blood increases as a result of inhibition of its metabolism;
- inhibitors of the isoenzyme CYPA2, including quinolones: increased exposure to melatonin;
- estrogen-containing agents: the plasma concentration of melatonin increases due to inhibition of the metabolic process with the participation of CYP1A1 and CYP1A2 isoenzymes;
- rifampicin, carbamazepine and other inducers of the CYP1A2 isoenzyme: the plasma level of Welson decreases;
- fluvoxamine: the content of melatonin in the blood increases significantly (the value of AUC and C max increases 17 and 12 times, respectively), due to inhibition of its biotransformation by isoenzymes CYP1A2 and CYP2C19; you want to avoid this combination;
- nicotine: a decrease in the concentration of melatonin in smokers is possible as a result of the induction of the isoenzyme CYP1A2;
- ethanol: Welson's effectiveness is weakened;
- imipramine + thioridazine: the feeling of calmness may increase, difficulty in performing some tasks in comparison with imipramine monotherapy may be recorded, as well as the risk of an increase in the feeling of clouding in the head when compared with the use of thioridazine alone;
- zolpidem, zaleplon, zopiclone and other benzodiazepine and non-benzodiazepine hypnotics: the sedative effect of these substances is enhanced; combined use can provoke progressive impairment of memory, attention and coordination when compared with zolpidem monotherapy.
There are a large number of publications on the effect of the following drugs on the secretion of endogenous melatonin: antidepressants, agonists / antagonists of opioid and adrenergic receptors, benzodiazepines, prostaglandin inhibitors, tryptophan, ethanol. The mutual influence of these drugs on the dynamics and kinetics of melatonin has not been studied.
Analogs
Welson's analogs are Melatonin Evalar, Melarena, Circadin, Meladapt, Melarithm, Melatonin-SZ, Sonnovan, Kakspal Neo, Melaxen, etc.
Terms and conditions of storage
It is required to save the drug in a place protected from light, out of the reach of children, at a temperature not exceeding 25 ° C.
Shelf life is 4 years.
Terms of dispensing from pharmacies
Available without a prescription.
Reviews about Welson
The reviews about Welson found on specialized sites are mostly positive. Patients note that the drug promotes faster falling asleep, relaxes, soothes and quickly provides a full healthy sleep. It does not cause morning sluggishness, fatigue and weakness. Welson has also proven itself well as an adaptogen in case of jet lag.
Sometimes there are complaints about the rather high cost of Welson, but at the same time, tablets from one package are enough for a long period, and they have a long shelf life. The disadvantages include a large number of possible undesirable effects, many indicate the frequent absence of the drug in pharmacies.
Price for Welson in pharmacies
The price of Welson in the form of film-coated tablets can be per pack containing 30 pcs. - 430-450 rubles.
Welson: prices in online pharmacies
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Drug name Price Pharmacy |
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Welson 3 mg film-coated tablets 30 pcs. 385 r Buy |
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Welson tablets p.o. 3mg 30 pcs. 452 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
