Stimuloton
Stimuloton: 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: Stimuloton
ATX code: N06AB06
Active ingredient: sertraline (sertraline)
Producer: EGIS Pharmaceuticals, PLC (Hungary)
Description and photo update: 2019-20-08
Prices in pharmacies: from 285 rubles.
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Stimuloton is an antidepressant.
Release form and composition
The dosage form of Stimuloton is film-coated tablets: a biconvex oval shape, almost white or white, engraved on one side "E271" (50 mg) or "E272" (100 mg), on the other - a dividing risk, odorless (50 mg each: 10 pieces in a blister, in a cardboard box 1, 2 or 3 blisters; 100 mg each: 14 pieces in a blister, in a cardboard box 1 or 2 blisters).
1 tablet contains:
- active substance: sertraline hydrochloride - 55.95 mg or 111.9 mg, which is equivalent to 50 mg or 100 mg of sertraline;
- auxiliary components: microcrystalline cellulose, magnesium stearate, sodium carboxymethyl starch (type A), hydroxypropyl cellulose (hyprolose), calcium hydrogen phosphate dihydrate;
- shell composition: titanium dioxide, macrogol 6000, hypromellose.
Pharmacological properties
Pharmacodynamics
Sertraline is a selective serotonin (5-HT) reuptake inhibitor, which at the same time very slightly alters the processes of dopamine and norepinephrine reuptake. In recommended doses, this substance prevents the uptake of serotonin by human platelets. For him, anticholinergic, sedative or stimulating action is uncharacteristic. Sertraline has no affinity for benzodiazepine, muscarinic (cholinergic), histaminergic, serotonergic, adrenergic, dopaminergic, or GABA receptors.
The antidepressant effect is observed by the end of the second week of regular intake of Stimuloton, while the maximum therapeutic effect is observed only after 6 weeks. Unlike tricyclic antidepressants, the use of sertraline does not increase body weight. It also does not provoke physical or mental drug dependence.
Pharmacokinetics
The degree of absorption of sertraline from the gastrointestinal tract is quite high, but this process is slow. The maximum concentration of the substance in the blood plasma is recorded 4.5–8.4 hours after oral administration of Stimuloton. Equilibrium concentration in blood plasma is achieved within a week with a daily intake of 1 time per day. When sertraline is taken with food, its bioavailability increases by 25%, and the time to reach the maximum concentration decreases.
The degree of binding of sertraline to blood plasma proteins is 98%. The volume of distribution exceeds 20 l / kg.
Sertraline is extensively metabolized during the first passage through the liver, participating in the processes of N-demethylation. Its main metabolite is N-desmethylsertraline, which is less active than the parent substance. Metabolites are determined in feces and urine in equal concentrations. Approximately 0.2% of sertraline is excreted unchanged through the kidneys. The half-life of the drug varies from 22 to 36 hours and does not change depending on the sex or age of the patient. For N-desmethylsertraline, this figure ranges from 62 to 104 hours. The area under the concentration-time curve (AUC) and elimination half-life increase in patients with liver dysfunction. Regardless of the severity of renal failure, the pharmacokinetic parameters of sertraline with its regular use remain unchanged.
Sertraline is determined in breast milk, but there is no information regarding its ability to cross the blood-placental barrier. It is also not eliminated from the body through dialysis.
Indications for use
- prevention and treatment of depression of various etiologies, including conditions accompanied by anxiety;
- post-traumatic stress disorder;
- panic disorder (with or without agoraphobia);
- obsessive-compulsive disorders, including in pediatric patients over 6 years old.
Contraindications
- unstable epilepsy;
- concomitant therapy with monoamine oxidase (MAO) inhibitors and within 14 days after their withdrawal;
- age up to 18 years, except for the treatment of obsessive-compulsive disorder;
- the period of pregnancy and breastfeeding;
- hypersensitivity to the components of the drug.
According to the instructions, Stimuloton should be prescribed with caution to patients with organic brain diseases (including mental retardation), epilepsy, manic conditions, renal and / or hepatic failure, with a decrease in body weight, obsessive-compulsive disorders in children over 6 years old.
Instructions for the use of Stimuloton: method and dosage
Stimuloton tablets are taken orally, in the morning or in the evening, 1 time per day.
Recommended dosage of Stimuloton for adults:
- depression, obsessive-compulsive disorders: 50 mg, the therapeutic effect develops slowly, the duration of treatment is prescribed by the doctor individually;
- panic or post-traumatic stress disorder: initial dose of 25 mg for one week, then 50 mg. With good tolerance to achieve the desired therapeutic response, a weekly dose increase of 50 mg is indicated until a maximum daily dose of 200 mg is reached. The clinical effect usually occurs within one week. Regular intake should be continued for at least 2-4 weeks. For maintenance therapy, the minimum effective dose should be used.
The recommended dosage of Stimuloton for pediatric patients in the treatment of obsessive-compulsive disorders:
- children aged 6 to 12 years: the initial dose is 25 mg, after a week of therapy, the dose is shown to be increased to 50 mg;
- children aged 13 to 18 years: initial dose - 50 mg.
If the therapeutic effect is insufficient, the dose of Stimuloton can be increased by 50 mg once a week, but not more than 200 mg per day. Doses above 50 mg in children should be used with extreme caution to prevent overdose. For long-term maintenance therapy, the minimum effective dose must be used.
In case of impaired renal function and for elderly patients, dose adjustment is not required.
In case of severe liver dysfunction, the dose should be reduced or the interval between Stimuloton doses should be increased.
Side effects
- from the nervous system: rarely - headache, drowsiness, dizziness, fatigue, tremor, irritability, insomnia, hypomania, mania, akathisia; possibly - reactions similar to the symptoms of the underlying disease, including depression, paresthesia, hypesthesia, hallucinations, aggressiveness, agitation, agitation, psychosis, anxiety;
- on the part of the cardiovascular system: rarely - palpitations;
- from the digestive system: decreased or increased appetite, dry mouth; rarely - stomach and abdominal cramps, nausea, vomiting, anorexia, diarrhea, flatulence or pain, unstable stools, dyspepsia;
- from the hematopoietic system: bleeding (including nosebleeds);
- dermatological reactions: rarely - flushing of the face, flushing of the skin, increased sweating;
- from the side of metabolism: weight loss;
- on the part of the reproductive system: rarely - decreased potency, delayed ejaculation, decreased libido, anorgasmia, dysmenorrhea;
- from the senses: rarely - blurred vision, visual impairment;
- laboratory parameters: in some cases - an asymptomatic increase in aspartate aminotransferase (ACT) and alanine aminotransferase (ALT) (observed during the first nine weeks of taking Stimuloton, immediately stops after discontinuation of the drug), reversible hyponatremia (more often in elderly patients who are on concomitant diuretic therapy or by other means);
- others: rarely - yawning, allergic reactions; in some cases - withdrawal syndrome; (the relationship of the following undesirable effects with the reception of Stimuloton has not been reliably established) rarely - exudative erythema multiforme; sometimes - convulsions, movement disorders (gait disturbance, extrapyramidal symptoms), hyperprolactinemia, menstrual irregularities, galactorrhea, pruritus, rash.
Overdose
Even when taking Stimuloton in high doses, severe symptoms associated with an overdose of sertraline are usually not observed. However, its combination with ethanol or other drugs can cause severe intoxication.
The consequence of an overdose in some cases is serotonin syndrome, the signs of which are hyperreflexia, myoclonus, nausea, vomiting, diarrhea, excessive sweating, psychomotor agitation, agitation, dizziness, tachycardia.
There are no specific antidotes to sertraline. Continuous monitoring of vital body functions and intensive supportive therapy are recommended. Do not induce vomiting. Taking activated charcoal can have a more significant effect than gastric lavage. It is also necessary to monitor the patency of the airways. Sertraline has a large volume of distribution, therefore, in case of an overdose, blood transfusion, forced diuresis, and hemoperfusion and dialysis may not lead to the desired result.
special instructions
There is no information about the possibility of using electroconvulsive therapy while using Stimuloton.
In some cases, the development of mania or hypomania is possible.
Depression-related suicidal thoughts and attempts can occur at any stage of treatment before remission occurs. Therefore, careful medical supervision of the patient is required from the beginning of the course of treatment until the moment of stable clinical effect.
Women of childbearing age should be warned about the need to use reliable contraception during the entire period of use of Stimuloton.
Movement disorders in most cases are observed in patients who are simultaneously taking antipsychotics (neuroleptics) or with a long history of movement disorders.
In clinical studies, rare cases of epileptic seizures have been observed in patients with depression and with obsessive-compulsive disorders. The exact relationship of their appearance with the administration of sertraline has not been established. Patients with epilepsy who do not have seizures should be examined regularly, and if seizures occur, Stimuloton therapy should be discontinued.
During the period of treatment, you should not drink alcohol or take ethanol-containing drugs.
Since the use of antidepressants in children and adolescents contributes to the development of hostility, rebelliousness, aggression, anger and increases the likelihood of suicide and suicidal thoughts, when prescribing Stimuloton for the treatment of obsessive-compulsive disorder, children must be carefully monitored for the timely detection of suicidal symptoms.
The drug should be used in pediatrics with extreme caution due to the lack of data on long-term safety in relation to growth, maturation, the formation of the cognitive sphere, and child behavior.
Influence on the ability to drive vehicles and complex mechanisms
With monotherapy, the use of Stimuloton does not affect the patient's psychomotor functions. When combined with other means, recommendations on the patient's ability to drive vehicles and mechanisms in each case should be given by the attending physician individually.
Application during pregnancy and lactation
Controlled studies of the use of Stimuloton in pregnant women have not been conducted, therefore, the appointment of a drug is allowed only in cases where the potential benefit of treatment for the mother significantly outweighs the possible risks to the fetus. Patients of reproductive age who are going to take sertraline must use reliable methods of contraception.
Sertraline is determined in breast milk, so its use during lactation is not recommended. Since there are no reliable data on the safety of its intake by lactating women, breastfeeding should be discontinued before starting the course of therapy.
Pediatric use
There is no sufficient clinical experience in the use of Stimuloton in pediatrics, therefore, the drug is not prescribed to children and adolescents under the age of 18. The exception is children over 6 years of age with OCD (obsessive-compulsive disorders), this category of patients should be taken with caution.
With impaired renal function
Care is required when prescribing Stimuloton to patients with renal failure. There is no need to specifically adjust the dose in the presence of impaired renal function.
For violations of liver function
Care must be taken when prescribing Stimuloton to patients with hepatic insufficiency. In the presence of liver dysfunctions, it is necessary to adjust the dose downward, or increase the intervals between doses of the drug.
Use in the elderly
Elderly patients do not need to adjust the Stimuloton dose.
Drug interactions
Combination therapy with MAO inhibitors, including selegiline and the reversible MAO inhibitor moclobemide, causes severe complications, so this combination is contraindicated. It is allowed to start taking sertraline at least 1 day after the withdrawal of the reversible MAO inhibitor.
With the simultaneous use of Stimuloton:
- cimetidine significantly reduces sertraline clearance;
- diazepam, warfarin, tolbutamide and other plasma protein-binding agents should be used with caution, since sertraline has a high plasma protein binding;
- carbamazepine, ethanol, phenytoin, haloperidol do not affect psychomotor reactions and cognitive functions at the maximum dose (200 mg) of sertraline;
- atenolol does not change its beta-blocking action;
- glibenclamide and digoxin do not change their properties and do not violate the therapeutic effect of sertraline used in the maximum dose;
- coumarin derivatives contribute to a significant increase in prothrombin time, therefore, it is necessary to control prothrombin time both at the beginning of treatment with sertraline and after its cancellation;
- carbamazepine, terfenadine do not change their metabolic rate;
- cortisol does not interfere with endogenous beta-hydroxylation;
- lithium preparations increase the risk of tremor.
With long-term use of Stimuloton at a dose of 50 mg per day, concomitant therapy with drugs metabolized with the participation of the CYP2D6 isoenzyme causes an increase in their concentrations in blood plasma.
To a clinically significant extent, sertraline does not inhibit the activity of the CYP2C9 isoenzyme, has a minimal inhibitory effect, or does not affect the CYP1A2 isoenzyme.
Combinations with tryptophan, fenfluramine, and other serotonergic substances should be avoided, and in case of urgent need for their simultaneous administration with sertraline, it is recommended to be especially careful.
Analogs
Stimuloton's analogues are: Aleval, Thorin, Serlift, Asentra, Serenata, Zoloft, Paroxetine, Selektra, etc.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Stimuloton
Almost all the reviews about Stimuloton that are found on the network confirm the effectiveness of the drug. When used in therapeutic doses, addiction does not develop. Patients claim that after the start of treatment, feelings of internal tension and anxiety disappear, the severity of emotional experiences and internal anxiety decreases, panic attacks disappear (almost a few days after the start of the course of therapy). Some patients take Stimuloton for a long time (up to 5 years), noting an improvement in their psychological state.
There are also negative reviews associated with adverse reactions when taking the drug. These mainly include decreased appetite, insomnia, fatigue, lethargy, and excessive sweating.
Price for Stimuloton in pharmacies
On average, the price of Stimuloton with a dosage of 50 mg varies from 381 to 415 rubles (for a pack containing 10 tablets) or from 857 to 934 rubles (for a pack containing 30 tablets). A drug in a dosage of 100 mg will cost about 1,405-1536 rubles (for a package containing 28 tablets).
Stimuloton: prices in online pharmacies
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Drug name Price Pharmacy |
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Stimuloton 50 mg film-coated tablets 10 pcs. 285 r Buy |
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Stimuloton tablets p.p. 50mg 10 pcs. 344 r Buy |
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Stimuloton 50 mg film-coated tablets 30 pcs. 815 RUB Buy |
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Stimuloton tablets p.p. 50mg 30 Pcs. 822 RUB Buy |
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Stimuloton tablets p.p. 100mg 28 pcs. 1307 RUB Buy |
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Stimuloton 100 mg film-coated tablets 28 pcs. 1307 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!
