Instructions for use STIMULOTON® (STIMULOTON®)

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Sertraline serotonin reuptake inhibitor . As a result, the concentration of this neurotransmitter increases, eliminating serotonin deficiency, which is the main cause of depressive conditions.

Does not produce a psychostimulating, sedative or m-anticholinergic effect. Has no affinity for serotonergic , muscarinic , GABA receptors and benzodiazepine receptors , does not inhibit MAO. Does not cause drug dependence and weight gain. There is also no cardiotoxic effect of the drug.

The antidepressant effect of the drug is observed by the end of the second week, and the initial effect is in the first week.

Pharmacokinetics

Absorbed from the gastrointestinal tract completely, but slowly. Cmax in the blood is determined after 5-8 hours. Bioavailability increases with simultaneous food intake. 98% bound to blood proteins. Excreted in breast milk. There is no data on the possibility of penetration through the placental barrier. Metabolized in the liver. Excreted in urine and feces. T 1/2 is 22-36 hours.

Pharmacological properties of the drug Stimuloton

The active ingredient of the drug, sertraline, selectively inhibits the reuptake of serotonin by synaptosomes in the brain. At a therapeutic dose, sertraline also inhibits the uptake of serotonin by human blood platelets. The antidepressant effect is noted at the end of the 2nd week of regular use of sertraline, and the maximum effect is observed after 6 weeks. Sertraline does not have stimulant, sedative, anticholinergic or cardiotoxic effects. The drug does not increase catecholaminergic activity and has no affinity for muscarinic (cholinergic), serotonin, dopamine, adrenergic, histamine, GABAergic and benzodiazepine receptors. When taken orally, it is quickly and almost completely absorbed in the gastrointestinal tract and undergoes biotransformation in the liver. The maximum concentration in the blood is achieved within 4.5–8.4 hours after administration. Blood protein binding - 98%. Intensively metabolized in the liver. The main route of excretion of metabolites is with urine and feces; 0.2% of sertraline is excreted unchanged by the kidneys. The half-life is 62–104 hours. If liver function is impaired, the half-life of sertraline and its AUC increase.

Indications for use

• depressive states;
• recurrent (repeating) depression ;
• prevention of episodes of depression;
• panic disorders;
• social phobia;
• state of anxiety and depression at the same time;
• obsessive-compulsive disorder;
• stress disorder after trauma.

Contraindications

• recurrent attacks of epilepsy ;
• taking MAO inhibitors ;
• age up to 18 years, except for patients with obsessive-compulsive disorder;
• hypersensitivity to the drug;
• pregnancy and breastfeeding.

Some caution should be exercised when prescribing Stimuloton for manic states , mental retardation, liver and kidney failure .

Special instructions for the use of the drug Stimuloton

Electroconvulsive therapy There are no data regarding the risks or benefits of electroconvulsive therapy and sertraline. Activation of mania and hypomania Like other antidepressants, the drug can cause mania or hypomania (up to 0.4% of patients). Suicide Patients with depression belong to a risk group for suicide attempts. From the start of treatment until the development of a pronounced clinical effect, such patients should be under close medical supervision. Use in children and adolescents under 18 years of age Stimuloton should not be used to treat children and adolescents under 18 years of age, with the exception of patients with OCD. If the drug is prescribed for clinical indications, it is necessary to monitor the patient for timely detection of suicide attempts. Epileptic seizures A direct connection between epileptic seizures and the use of sertraline has not been established. The drug should not be prescribed to patients with unstable epilepsy. If attacks occur, sertraline should be discontinued. Hepatic impairment Sertraline metabolism occurs primarily in the liver. Sertraline should be prescribed with caution to patients with impaired liver function. It is possible to reduce the dose or increase the interval between taking the drug. Renal failure Patients with impaired renal function do not need special dosage selection. Pregnancy and lactation Due to the lack of adequate clinical data during pregnancy, sertraline can be prescribed only when the benefit of the drug justifies the possible risk to the fetus or child. Sertraline is excreted into milk, so it is not recommended to use it during breastfeeding. Effect on the ability to drive vehicles and potentially dangerous mechanisms Sertraline monotherapy does not affect the psychomotor performance of patients. Clinical studies did not reveal any undesirable effects on the ability to drive vehicles or use other machinery.

Side effects of Stimuloton

All side effects are rare:

• drowsiness, dizziness , insomnia , headache, tremor , hallucinations , irritability , restlessness syndrome, agitation;
• dry mouth, stomach cramps, loss of appetite, flatulence , abdominal pain, nausea;
• heartbeat;
• weight loss;
• nosebleeds;
• blurred vision;
• dysmenorrhea , decreased potency, delayed ejaculation;
• skin hyperemia , rash, itching;
• increased sweating;
• increased AST and ALT;
• withdrawal syndrome.

Stimuloton tablet p/o 100 mg per bl. in pack No. 14x2

Name

Stimuloton.

Description

Film-coated tablets, white or almost white, oval, biconvex, engraved “E271” on one side and scored on the other, odorless.

Main active ingredient

Sertraline

Release form

Film-coated tablets, white or almost white, oval, biconvex, engraved “E271” on one side and scored on the other, odorless. 1 tab. sertraline hydrochloride 55.95 mg, which corresponds to the content of sertraline 50 mg Excipients: magnesium stearate - 2 mg, hyprolose (hydroxypropylcellulose) - 6.05 mg, sodium carboxymethyl starch (type A) - 20 mg, calcium hydrogen phosphate dihydrate - 24 mg, microcrystalline cellulose - 45 mg . Shell composition: hypromellose - 2.9 mg, macrogol 6000 - 0.8 mg, titanium dioxide (CI77891 EEC 171) - 1.3 mg. 10 pieces. - blisters (1) - cardboard packs. 10 pieces. - blisters (2) - cardboard packs. 10 pieces. - blisters (3) - cardboard packs. Film-coated tablets, white or almost white, oval, biconvex, engraved “E272” on one side and scored on the other, odorless. 1 tab. sertraline hydrochloride 111.9 mg, which corresponds to the content of sertraline 100 mg Excipients: magnesium stearate - 4 mg, hyprolose (hydroxypropylcellulose) - 12.1 mg, sodium carboxymethyl starch (type A) - 40 mg, calcium hydrogen phosphate dihydrate - 48 mg, microcrystalline cellulose - 90 mg . Shell composition: hypromellose - 5.8 mg, macrogol 6000 - 1.6 mg, titanium dioxide (CI77891 EEC 171) - 2.6 mg. 14 pcs. - blisters (1) - cardboard packs. 14 pcs. - blisters (2) - cardboard packs.

Dosage

50 mg per bl. in pack №10x3

special instructions

There are no data on the possible risks and benefits of simultaneous use of electroconvulsive therapy and Stimuloton. Like other antidepressants, Stimuloton® in some cases (approximately 0.4%) can cause mania or hypomania. Suicidal thoughts and attempts are often associated with depression; they are possible at any time before the onset of remission. Therefore, at the beginning of the course of treatment, until the optimal clinical effect develops, patients need careful medical supervision. In clinical trials of Stimuloton, epileptic seizures were observed in 0.08% of patients with depression (approximately 3/4000) and in 0.2% of patients with obsessive-compulsive disorder (4/1800). A strict connection between epileptic seizures and the use of Stimuloton has not been established. There is no data on the treatment of patients with epilepsy with Stimuloton. The drug should not be prescribed to patients with unstable epilepsy, and patients who do not have seizures should be monitored regularly. If seizures occur, Stimuloton® must be discontinued. Sertraline is metabolized mainly in the liver, so caution is required when prescribing Stimuloton to patients with liver disease. Use in pediatrics The use of Stimuloton is contraindicated for the treatment of children and adolescents under 18 years of age, with the exception of patients with obsessive-compulsive disorder. Increases in the likelihood of suicide and suicidal ideation, as well as hostility (mainly aggression, defiance and anger), have been observed more frequently in clinical trials among children and adolescents receiving antidepressants compared with groups receiving placebo. If the drug is prescribed for clinical indications, the patient should be monitored to identify suicidal symptoms. In addition, there are no long-term safety data in children and adolescents regarding growth, maturation, and cognitive and behavioral development. Effect on the ability to drive vehicles and operate machinery. The results of clinical studies have shown that monotherapy with Stimuloton does not affect indicators of psychomotor function. However, since other drugs used for similar indications may adversely affect psychomotor reactions, the ability to drive vehicles and machines should be determined individually depending on the patient's response to treatment and the use of concomitant therapy.

pharmachologic effect

Antidepressant. Selective serotonin reuptake inhibitor. It has a weak effect on the reuptake of norepinephrine and dopamine. In therapeutic doses, sertraline also blocks the uptake of serotonin by human blood platelets. Does not have a stimulating, sedative or anticholinergic effect. Sertraline has no affinity for m-cholinergic, serotonin, dopamine, histamine, adrenergic, GABA and benzodiazepine receptors. When using Stimuloton, there is no increase in body weight. The drug does not cause mental or physical drug dependence. The antidepressant effect is observed by the end of the second week of regular use of the drug, while the maximum effect is achieved only after 6 weeks.

Pharmacokinetics

Absorption After oral administration, it is absorbed from the gastrointestinal tract slowly, but almost completely. Cmax is reached after 4.5-8.4 hours. When taking the drug simultaneously with food, its bioavailability increases by 25%, Cmax is achieved faster. Distribution With a single daily dose of the drug, Css is usually achieved within a week. Plasma protein binding is 98%. Vd - more than 20 l/kg. Sertraline is excreted in breast milk. There is no data on its ability to penetrate the placental barrier. Metabolism Sertraline undergoes extensive first-pass metabolism through the liver, undergoing N-demethylation. Its main metabolite, N-desmethylsertraline, is less active than sertraline. Elimination T1/2 is 22-36 hours and does not depend on the age and gender of patients. T1/2 of N-desmethylsertraline is 62-104 hours. It is excreted in the form of metabolites in urine and feces in equal amounts, 0.2% of sertraline is excreted in the urine unchanged. Pharmacokinetics in special clinical cases T1/2 and AUC of sertraline increase with impaired liver function. Pharmacokinetic studies with the administration of the drug in a single dose revealed an increase in T1/2 and AUC of sertraline in patients with liver cirrhosis. Regardless of the severity of renal failure, the pharmacokinetics of sertraline does not change with its continuous use. Sertraline is not eliminated by hemodialysis.

Indications for use

- depression of various etiologies, incl. accompanied by feelings of anxiety (treatment and prevention); — obsessive-compulsive disorders, incl. in children over 6 years old; - panic disorders (with or without agoraphobia); - post-traumatic stress disorder.

Directions for use and doses

The drug is prescribed orally, 1 time/day (morning or evening). For adults with depression and obsessive-compulsive disorders, the drug is prescribed at a dose of 50 mg 1 time / day. For panic disorders and post-traumatic stress disorders, to reduce the frequency and severity of side effects, it is recommended to start treatment with a dose of 25 mg 1 time / day and after a week increase it to 50 mg 1 time / day. If the therapeutic response is unsatisfactory and is well tolerated, the daily dose can be increased by 50 mg over several weeks to a maximum daily dose of 200 mg. The therapeutic effect is usually achieved within 7 days. However, for the full manifestation of the antidepressant effect, regular use of the drug is required for 2-4 weeks. In obsessive-compulsive disorder, the therapeutic effect develops even more slowly. For maintenance therapy, the minimum effective dose should be prescribed. For obsessive-compulsive disorders in children aged 13 to 18 years, the drug is prescribed at an initial dose of 50 mg 1 time / day. For children aged 6 to 12 years, the drug is prescribed at an initial dose of 25 mg 1 time / day; after a week, the daily dose can be increased to 50 mg. If the therapeutic response is unsatisfactory, the dose can then be increased weekly by 50 mg/day to a maximum daily dose of 200 mg. To avoid overdose, when increasing the dose to more than 50 mg/day, it should be taken into account that the body weight of children is less than that of adults. For long-term maintenance therapy, the drug should be prescribed in the minimum effective dose. In elderly patients, no dose adjustment is required. In patients with severe liver dysfunction, the dose of the drug should be reduced or the intervals between doses increased. In patients with impaired renal function, no special dose selection is required.

Use during pregnancy and lactation

There are no controlled results of the safety of using Stimuloton in pregnant women, therefore its use during pregnancy is contraindicated. Women of reproductive age who are to be prescribed Stimuloton should be advised to use effective contraception. Sertraline is excreted in breast milk. There is no reliable data on the safety of its use during lactation. If it is necessary to prescribe Stimuloton during lactation, breastfeeding should be stopped.

Precautionary measures

The drug should be prescribed with caution in case of organic diseases of the brain (including mental retardation), manic states, epilepsy, liver and/or kidney failure, weight loss, as well as children over 6 years of age with OCD.

Interaction with other drugs

When using Stimuloton simultaneously with MAO inhibitors, incl. with selegiline and the reversible MAO inhibitor moclobemide, severe complications are observed. Serotonin syndrome may develop. Several cases of death have been reported with the combination of other antidepressants and MAO inhibitors, as well as with the isolated administration of MAO inhibitors, started immediately after discontinuation of other antidepressants. When a selective serotonin reuptake blocker and an MAO inhibitor were combined, hyperthermia, rigidity, myoclonus, autonomic instability (sometimes with rapid changes in respiratory and circulatory function), mental status changes (for example, confusion, irritability, sometimes with extreme agitation, which could lead to delirium or coma). Therefore, the use of Stimuloton in combination with MAO inhibitors or within 14 days after discontinuation of a MAO inhibitor, as well as less than 1 day after discontinuation of a reversible MAO inhibitor, is contraindicated. Similarly, after discontinuation of Stimuloton, at least 14 days must pass before starting the use of an irreversible MAO inhibitor. In studies in healthy volunteers, with daily intake of Stimuloton at a dose of 200 mg/day, there was no increase in the effect of ethanol, carbamazepine, haloperidol or phenytoin on cognitive functions and psychomotor reactions. However, while taking sertraline, drugs that affect the central nervous system should be used with extreme caution; the use of ethanol during treatment should be avoided. Sertraline is highly bound to plasma proteins and the potential for interaction with other plasma protein-bound drugs (eg diazepam, tolbutamide and warfarin) must be considered. With simultaneous use of Stimuloton with cimetidine, the clearance of sertraline is significantly reduced. With the simultaneous use of Stimuloton with coumarin derivatives, a significant increase in prothrombin time is observed (in such cases, it is recommended to monitor the prothrombin time at the beginning of treatment with sertraline and after its discontinuation). During long-term therapy with Stimuloton at a dose of 50 mg/day, the use of drugs metabolized with the participation of the CYP2D6 isoenzyme is accompanied by an increase in their concentrations in the blood plasma. In vivo drug interaction studies have shown that long-term administration of sertraline at a dose of 200 mg/day does not affect the endogenous beta-hydroxylation of cortisol mediated by CYP3A3/4 isoenzymes or the metabolism of carbamazepine or terfenadine. Long-term administration of sertraline at a dose of 200 mg/day does not affect the concentrations of tolbutamide, phenytoin and warfarin in blood plasma. This means that sertraline does not inhibit CYP2C9 activity to a clinically significant extent. Long-term administration of sertraline at a dose of 200 mg/day does not affect the concentration of diazepam in the blood plasma, and therefore clinically significant inhibition of the activity of the CYP2C19 isoenzyme should also be excluded. In vitro studies have shown that sertraline has no or minimal inhibitory effect on CYP1A2. With simultaneous use of Stimuloton and lithium preparations, the pharmacokinetics of the latter does not change. However, with this combination, tremor is observed more often. Just as when prescribing other selective serotonin reuptake inhibitors, increased caution is required when combining Stimuloton with drugs that affect serotonergic transmission (including lithium drugs). The time required for complete elimination of the active substance from the body before transferring a patient from one selective serotonin reuptake inhibitor to another has not been determined. Therefore, such a transition should be made with extreme caution. Particular caution is required when other serotonergic substances (e.g. tryptophan or fenfluramine) and sertraline are used concomitantly. Such combinations should be avoided whenever possible. In clinical studies, only a slight inducing effect of sertraline on liver enzymes was found. With simultaneous use of Stimuloton at a dose of 200 mg/day and phenazone, sertraline caused a small (5%) but significant decrease in T1/2 of phenazone. This small decrease in T1/2 of phenazone was due to a clinically insignificant change in liver metabolism. When used together, sertraline does not change the beta-blocking effect of atenolol. When combining Stimuloton at a dose of 200 mg/day with glibenclamide and digoxin, no drug interactions were detected.

Contraindications

- simultaneous use of MAO inhibitors and a period of 14 days after their discontinuation; - unstable epilepsy; - age under 18 years (due to lack of sufficient clinical experience), with the exception of patients with obsessive-compulsive disorders; - pregnancy; - lactation period (breastfeeding); - hypersensitivity to the components of the drug.

Compound

1 tab. sertraline hydrochloride 55.95 mg, which corresponds to the content of sertraline 50 mg Excipients: magnesium stearate - 2 mg, hyprolose (hydroxypropylcellulose) - 6.05 mg, sodium carboxymethyl starch (type A) - 20 mg, calcium hydrogen phosphate dihydrate - 24 mg, microcrystalline cellulose - 45 mg . Shell composition: hypromellose - 2.9 mg, macrogol 6000 - 0.8 mg, titanium dioxide (CI77891 EEC 171) - 1.3 mg. 10 pieces. - blisters (3) - cardboard packs.

Overdose

Even when sertraline was prescribed in high doses, no severe symptoms were detected. However, administration of sertraline in high doses simultaneously with other drugs or ethanol can lead to severe poisoning. Symptoms: serotonin syndrome with nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia. Treatment: There are no specific antidotes. Intensive supportive care and constant monitoring of vital organ functions are required. Inducing vomiting is not recommended. The administration of activated carbon may be more effective than gastric lavage. The airway must be maintained. Sertraline has a large Vd, and therefore increased diuresis, dialysis, hemoperfusion or blood transfusion may be ineffective.

Side effect

From the central nervous system and peripheral nervous system: rarely - drowsiness, fatigue, dizziness, headache, tremor, insomnia, irritability, akathisia, hypomania, mania. As with treatment with other antidepressants, reactions may occur that are difficult to differentiate from symptoms of the underlying disease, including. paresthesia, hypoesthesia, depression, hallucinations, agitation, aggressiveness, agitation, anxiety, psychosis. From the digestive system: dry mouth, decreased appetite or increased appetite (possibly due to the elimination of depression); rarely - anorexia, cramps in the stomach, abdomen, flatulence or pain, unstable stools, diarrhea, dyspepsia, nausea, vomiting. From the cardiovascular system: rarely - palpitations. Metabolism: weight loss. From the hematopoietic system: bleeding (including nosebleeds). From the senses: rarely - visual disturbances (including blurred vision). From the reproductive system: rarely - dysmenorrhea, sexual dysfunction (delayed ejaculation, decreased potency and/or libido, anorgasmia). Dermatological reactions: rarely - skin hyperemia or “flushes” of blood to the face, increased sweating. From the laboratory parameters: in some cases (0.8%) - an asymptomatic increase in AST and ALT (these changes were observed during the first 9 weeks of taking the drug and stopped immediately after its discontinuation); There are reports of reversible hyponatremia (presumably this phenomenon is associated with the syndrome of insufficient ADH secretion, since it was observed mainly in elderly patients receiving concomitant diuretics or other drugs). Other: rarely - allergic reactions, yawning; in some cases, stopping the drug causes withdrawal syndrome. Sometimes (a causal relationship with the drug has not been reliably established) - motor disorders (extrapyramidal symptoms and gait disturbances), convulsions, menstrual irregularities, hyperprolactinemia, galactorrhea, skin rash (rarely - erythema multiforme), itching. In most cases, movement disorders were observed in patients taking concomitant antipsychotic drugs (neuroleptics), as well as in those with a long history of movement disorders.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Buy Stimuloton tablet p/o 100 mg in bl. in pack No. 14x2 in the pharmacy

Price for Stimuloton tablet p/o 100 mg per bl. in pack No. 14x2

Instructions for use for Stimuloton tablet p/o 100 mg per bl. in pack No. 14x2

Instructions for use of Stimuloton (Method and dosage)

The tablets are taken orally, 1 time per day. The time of admission does not matter (morning or evening).

Treatment of depression and obsessive-compulsive disorder: 50 mg for adults.

For panic disorders, treatment begins with 25 mg, after 7 days the dose is increased to 50 mg. In these conditions, if necessary, the dose is increased by 25–50 mg once a week to the MS dose of 200 mg. The effect of treatment occurs within a week; for a full and lasting antidepressant effect, it takes from 2 weeks to 1 month. The minimum effective dose is prescribed as maintenance therapy.

Children from 13 to 18 years old with obsessive-compulsive disorder - 50 mg. For children 6 to 12 years of age with this condition, 25 mg is recommended, increasing to 50 mg every other week. In the future, it is allowed to increase the dose by 50 mg every week up to an MS dose of 200 mg. Since children have less body weight, the possibility of overdose must be taken into account. For maintenance therapy, the minimum effective doses are selected.

Instructions for use of Stimuloton contain information on the dosage of the drug in certain groups: elderly patients and patients with impaired renal function - the dose is not adjusted, severe liver dysfunction - the dose is reduced.

Instructions for use STIMULOTON® (STIMULOTON®)

Serotonin syndrome (SS) or neuroleptic malignant syndrome (NMS)

During treatment with SSRI drugs, including sertraline, the development of SS or NMS with possible fatal outcome has been reported. Concomitant use of SSRIs with other serotonergic drugs (including other serotonergic antidepressants, amphetamine, triptans), with drugs that inhibit serotonin metabolism (including MAOIs, such as methylene blue), with antipsychotics and other dopamine antagonists, and with opioids increases the risk of developing CVD or ZNS. Due to the possible development of signs and symptoms of SS or NMS, patients should be carefully monitored (see section Contraindications).

Switching from other selective serotonin reuptake inhibitors, antidepressants or anti-obsessive medications

There is limited controlled experience regarding the optimal timing of switching from other selective serotonin reuptake inhibitors, antidepressants or anti-obsessive medications to sertraline. The transition should be made with caution and under close medical supervision, especially when taking long-acting drugs such as fluoxetine.

Other serotonergic drugs, such as tryptophan, fenfluramine, and 5-HT agonists

Co-administration of sertraline with other drugs that enhance serotonergic neurotransmission, such as amphetamine, tryptophan or fenfluramine, or 5-HT agonists, as well as herbal drugs such as St. John's wort ( hypericum perforatum

), should be monitored and avoided if possible due to the potential for pharmacodynamic interactions.

Prolongation of the QTc/ari interval

In the post-registration period, there have been reports of QTc prolongation and torsade de pointes (TdP) while taking sertraline. In most cases, this was observed in patients with other risk factors for prolongation of the QTc interval and torsade de pointes. Prolongation of the QTc interval was confirmed in a QTc study in healthy volunteers, with a statistically significant increase in effect (increased effect/response ratio). Therefore, in patients with additional risk factors for prolongation of the QTc interval (such as heart disease, hypokalemia or hypomagnesemia, prolongation of the QTc interval in the family analysis, bradycardia, and taking drugs that cause prolongation of the QTc interval), sertraline should be prescribed with caution (see sections Pharmacological action and Drug interactions).

Activation of hypomania or mania

Manic/hypomanic symptoms have been reported in a small number of patients taking approved antidepressants and anti-obsessive medications, including sertraline. Therefore, sertraline should be used with caution in patients with a history of mania/hypomania. Such patients require medical supervision. Sertraline should be discontinued if the patient enters a manic phase.

Schizophrenia

Patients with schizophrenia may experience worsening psychotic symptoms.

Seizures

Epileptic seizures may occur during treatment with sertraline. Sertraline should not be prescribed to patients with unstable epilepsy; In patients with controlled epilepsy, sertraline should be used under close supervision. If seizures occur, sertraline should be discontinued.

Suicide/suicidal ideation/suicide attempts or clinical deterioration

Depression is associated with an increased risk of suicidal ideation, self-harm and suicide (suicide attempts). This risk persists until remission occurs. Because During the first few weeks from the start of treatment, there may be no improvement in the condition; at the initial stage of treatment, patients should be under constant monitoring. There is clinical experience of increasing the risk of suicide in the early stages of recovery.

Other mental illnesses for which sertraline is prescribed may also be associated with an increased risk of suicidal events. In addition, such diseases may accompany major depressive disorder. The same precautions should be taken when treating patients with major depressive disorder and other mental illnesses.

Patients with a history of suicidality or who demonstrate a significant degree of suicidal ideation should be adequately monitored before initiating treatment. A meta-analysis of placebo-controlled clinical trials of antidepressants in adult patients with mental disorders found an increased risk of suicidal behavior with antidepressants compared with placebo in patients under 25 years of age.

Drug treatment should be accompanied by careful monitoring of patients, especially those at increased risk, especially early in treatment and after dose changes. Patients and caregivers should be advised to monitor the condition for clinical worsening, suicidal behavior and ideation, and unusual changes in behavior, and to seek prompt medical attention if symptoms occur.

Use of the drug in children and adolescents under 18 years of age

Sertraline is not generally used to treat children and adolescents under the age of 18 years, with the exception of patients with obsessive-compulsive disorder aged 6-17 years. Suicidal behavior (suicide attempts, suicidal ideation) and hostility (mainly aggression, oppositional behavior and anger) were observed more frequently in clinical trials in children and adolescents treated with antidepressants compared with placebo. If treatment is prescribed based on clinical need, the patient should be closely monitored for suicidal symptoms. In addition, long-term safety studies of sertraline in children and adolescents regarding growth, puberty, cognitive and behavioral development are currently poorly studied. In the post-registration period, inhibition of growth and puberty has been reported in rare cases. Clinical significance and causality have not yet been established (see section on non-clinical safety studies). Physicians should monitor their young patients during long-term treatment for disturbances in these body systems.

Abnormal bleeding/hemorrhage

Bleeding events, including skin bleeding (such as ecchymosis and purpura), and other bleeding events, including gastrointestinal or gynecological bleeding that are life-threatening, have been reported during treatment with SSRI drugs. Patients taking SSRIs, in particular their concomitant use with drugs that affect platelet function (for example, anticoagulants, atypical antipsychotics and phenothiazines, most tricyclic antidepressants, acetylsalicylic acid and nonsteroidal anti-inflammatory drugs (NSAIDs)), and patients should be carefully monitored. with a known history of blood diseases (see section Drug interactions).

Hyponatremia

Hyponatremia may occur as a result of treatment with selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs), including sertraline. In many cases, hyponatremia is the result of syndrome of inappropriate antidiuretic hormone secretion (SIADH). Cases of serum sodium levels decreasing to 110 mmol/L have been reported. Elderly patients are at increased risk of developing hyponatremia when treated with SSRIs and SNRIs. Also, patients taking diuretics or patients with hypovolemia may be at increased risk (see Dosage Regimen "Use in Elderly Patients"). Discontinuation of sertraline should be considered in patients with symptomatic hyponatremia, and appropriate medical intervention should be instituted. Signs and symptoms of hyponatremia include headache, difficulty concentrating, memory loss, confusion, weakness, and unsteadiness that may lead to falls. Signs and symptoms associated with more severe and/or acute cases include hallucinations, fainting, seizures, coma, respiratory arrest, and death.

Withdrawal symptoms observed when stopping treatment with sertraline

Withdrawal symptoms when stopping treatment are common, especially if treatment is stopped abruptly (see Side Effects section). In clinical studies conducted in patients taking sertraline, the incidence of withdrawal reactions was 23% in those who discontinued sertraline, compared with 12% in those who continued treatment with sertraline.

The risk of developing withdrawal symptoms may depend on several factors, including the duration of treatment and dosage, and the rate at which the dosage is tapered. Dizziness, sensory disturbances (including paresthesia), sleep disturbances (including insomnia and vivid dreams), restlessness and anxiety, nausea and/or vomiting, tremor and headache are the most common reactions. In general, these symptoms are mild to moderate, but in some patients they can be severe.

They usually occur within the first few weeks after stopping treatment, but such conditions have rarely been reported in patients who accidentally missed a dose of the drug. In most cases, such symptoms are self-limiting and resolve within 2 weeks, although in some patients they may continue (2-3 months or more). It is therefore recommended to gradually reduce the dose of sertraline before stopping treatment over several weeks or months according to the patient's needs (see Dosage Regimen).

Akathisia/psychomotor agitation

Sertraline use has been associated with the development of akathisia, characterized by a subjective feeling of discomfort or restlessness and a need to move, often accompanied by an inability to sit or stand still. These symptoms most often occur during the first few weeks of treatment. Increasing the dose in patients with such symptoms may be detrimental.

Liver dysfunction

Sertraline is extensively metabolized in the liver. Pharmacokinetic studies with a single dose in patients with moderate liver cirrhosis revealed an increase in T1/2 of sertraline, a threefold increase in AUC and Cmax compared with those in healthy people. No significant differences in plasma protein binding were observed in either group. Caution is required when treating patients with impaired liver function with sertraline. In such patients, the dose should be reduced or the interval between doses of sertraline should be increased. Sertraline should not be prescribed to patients with severe liver disease (see Dosage Regimen).

Renal dysfunction

Sertraline is intensively metabolized and is therefore excreted unchanged in the urine. In studies involving patients with mild or moderate renal impairment (creatinine clearance 30-60 ml/min) and severe renal impairment (creatinine clearance less than 10-29 ml/min), the pharmacokinetic parameters of sertraline (AUC0-24 or Cmax) did not differ significantly from the control group . Therefore, patients with renal failure do not require dose adjustment.

Use of the drug in elderly patients

More than 700 elderly patients (>65 years) took part in clinical studies. The nature and frequency of adverse reactions in elderly patients did not differ from the same indicators in young patients. However, the use of selective serotonin reuptake inhibitors and serotonin-norepinephrine reuptake inhibitors, including sertraline, has been associated with cases of clinically significant hyponatremia in elderly patients who may be at risk for this side effect (see Hyponatremia earlier in this section).

Diabetes

In patients with diabetes mellitus, treatment with SSRIs may alter glycemic control and dosage adjustments of insulin and/or concomitant hypoglycemic medications may be necessary.

Electroconvulsive therapy

Clinical studies evaluating the risks and benefits of concomitant use of electroconvulsive therapy and sertraline have not been conducted.

Grapefruit juice

It is not recommended to drink grapefruit juice during treatment with sertraline (see section Drug interactions).

Preclinical safety studies

Preclinical studies have not identified a specific hazard to humans, as evidenced by traditional pharmacological safety studies, repeated dose toxicity studies, genotoxicity and carcinogenicity studies. Reproductive toxicity studies in animals have shown no evidence of teratogenicity or adverse effects on fertility. The observed fetotoxicity was likely related to maternal toxicity. Postpartum survival and fetal weight were reduced only during the first days after birth. Early postnatal mortality was shown to be caused by intrauterine exposure at day 15 of gestation. Delays in postpartum development of litters of treated females are likely due to exposure to females and are therefore not related to human risk.

Experiments conducted in rodents and non-rodents showed no effects on fertility.

Impact on the ability to drive vehicles and machinery

Clinical pharmacology studies have shown that sertraline has no effect on psychomotor functions. However, because psychotropic drugs can affect the mental and physical abilities needed to perform potentially hazardous tasks, such as operating vehicles or machinery, the patient should take appropriate precautions.

Overdose

Stimuloton, even in large doses, does not cause severe overdose symptoms. But when it is prescribed with psychotropic drugs, cases of poisoning are observed. Overdose is manifested by the appearance of serotonin syndrome :

• movement disorders (muscle twitching, tremors , bruxism , ataxia );
• autonomic disorders (chills, profuse sweating, nausea, abdominal pain, stool upset, tachycardia , blood pressure fluctuations);
• mental disorders ( disorientation , agitation, hypomania , confusion ).

There are no antidotes. Intensive therapy and monitoring of cardiac activity and respiratory function are carried out. Gastric lavage is not very effective; sorbents .

Interaction

Drugs that affect the central nervous system ( Carbamazepine , Haloperidol , Phenytoin ) should be used with caution. You must abstain from drinking alcohol.

Prescribing monoamine oxidase inhibitors with simultaneous administration of sertraline leads to significant complications in the form of the development of serotonin syndrome . After discontinuation of the drug, treatment with MAO inhibitors begins only after 2 weeks.

Since the active substance binds to blood proteins, this pharmacokinetic feature must be taken into account when prescribing Diazepam , Warfarin and other drugs that also bind to proteins.

Cimetidine reduces the clearance of sertraline.

Tremor is observed when used in combination with lithium , and coumarin increase PT (prothrombin time). Concomitant use with other serotonergic drugs ( Tryptophan , Fenfluramine ) should be avoided.

Drug interactions Stimuloton

MAO inhibitors According to available data, the combined use of sertraline with MAO inhibitors, including selegiline and the reversible inhibitor moclobemide, leads to serious consequences. When these drugs were combined, hyperthermia, muscle rigidity, myoclonus, lability of the autonomic nervous system, and mental status changes, including irritability, agitation, which may progress to delirium or coma, were noted. Therefore, sertraline should never be prescribed together with MAO inhibitors or within 14 days after their discontinuation, or less than 1 day after discontinuation of a reversible MAO inhibitor. Similarly, after discontinuation of sertraline therapy, at least 14 days must elapse before starting the use of a reversible MAO inhibitor. CNS depressants and alcohol Daily use of sertraline 200 mg/day does not enhance the effect of alcohol, carbamazepine, haloperidol or phenytoin on cognitive function and psychomotor activity. Protein-Bound Drugs Since sertraline is bound to plasma proteins, the possibility of interaction with other protein-bound drugs must be considered. Cimetidine Concomitant use significantly reduces the clearance of sertraline, however, the clinical significance of this has not been established. Coumarin derivatives Coumarin derivatives significantly increase prothrombin time, therefore it is necessary to monitor prothrombin time at the beginning of treatment and after its discontinuation. Drugs metabolized by the cytochrome P450 isoenzyme Long-term treatment with sertraline at a dose of 50 mg/day is accompanied by an increase in the concentration of despramine (a compound used to assess the activity of the 2D6 isoenzyme of cytochrome P450) in the blood plasma. Lithium A study in healthy volunteers showed that pharmacokinetics do not change significantly when lithium is administered concomitantly with sertraline. However, compared with the placebo group, the incidence of tremor was higher, suggesting a possible pharmacodynamic interaction. Serotonergic agents The length of the washout period required before switching a patient from one selective serotonin reuptake inhibitor to another has not yet been determined and requires extreme caution. It is advisable to avoid simultaneous administration of tryptophan or fenfluramine and sertraline. Induction of microsomal enzymes Studies have revealed a slight inducing effect of sertraline on liver enzymes. Atenolol When used concomitantly, sertraline does not change the β-blocking effect of atenolol. Glibenclamide and digoxin No interactions have been identified.

Analogs

Level 4 ATC code matches:
Actaparoxetine

Plizil

Fluxen

Paroxin

Surlift

Asentra

Elycea

Fluoxetine

Lenuksin

Escitalopram

Adepress

Selectra

Citalopram

Cipramil

Zoloft

Paroxetine

Prozac

Paxil

Rexetine

Fevarin

Aleval , Asentra , Zoloft , Serenata , Sirlift , Thorin , Deprefault , Deprefault , Sertraline hydrochloride .

Reviews about Stimuloton

Reviews about Stimuloton on forums indicate the effectiveness of the drug and the absence of addiction to it when prescribed correctly.

According to patients who took the drug, tension and anxiety gradually go away, there is no excitement or worry about any reason:

“Stimuloton helps! He brought me back to life."

“I’ve been taking Stimuloton for 5 years in a small dose, everything is fine,” “...it started helping me on the second day—the panic attacks stopped.”

“I took the pills for about 6 months, my psychological state improved significantly, I didn’t feel any addiction...”, “...I didn’t feel any addiction either.”

Negative reviews, although there are few of them, are associated with the appearance of side effects, among which the most prominent ones are the appearance of insomnia, fatigue, sweating, apathy and loss of appetite.

Stimuloton price, where to buy

You can buy it in pharmacies in Moscow and other cities. The price of Stimuloton depends on the dose of the drug and the number of tablets in the package. The cost of the drug 50 mg No. 10 ranges from 348 rubles. up to 419 rubles, and the drug 100 mg No. 28 - from 1285 rubles. up to 1648 rub.

• Online pharmacies in UkraineUkraine

Pharmacy24

• Stimuloton 50 mg No. 30 tablets ZAT FZ EGIS/VAT Pharmaceutical plant EGIS, Ugorshchina/Ugorshchina
  234 UAH.order
• Stimuloton 100 mg No. 28 tablets ZAT FZ Egis, Ugorshchina

  383 UAH. order