Stimuloton tablets p / o 50mg, No. 30

• Depression of various etiologies, incl. accompanied by feelings of anxiety (treatment and prevention)

• Obsessive-compulsive disorder (OCD), treatment for OCD in children over 6 years of age.

• Panic disorder (with and without agoraphobia).

• Post-traumatic stress disorder (PTSD).

Stimuloton should be taken once a day (morning or evening).
For adults with depression or obsessive-compulsive disorder, the usual dose is 50 mg once a day.
To reduce the frequency and severity of side effects in patients with panic disorder or PTSD, it is recommended to start treatment with a dose of 25 mg once a day and increase the dose to 50 mg once a day after a week.
With an unsatisfactory therapeutic response and good tolerance, the daily dose can be increased by 50 mg over several weeks to a maximum daily dose of 200 mg.
The therapeutic effect can occur within 7 days. However, it usually takes 2 to 4 weeks for the full manifestation of the antidepressant effect. In obsessive-compulsive disorder, the therapeutic effect develops even more slowly. For maintenance therapy, the minimum effective dose should be prescribed.
Children aged 13-18 years with obsessive-compulsive disorder should be prescribed Stimuloton starting at a dose of 50 mg per day. For children with obsessive-compulsive disorder aged 6-12 years, an initial dose of 25 mg per day is recommended, which can be increased to 50 mg per day after a week. If the therapeutic response is unsatisfactory, then the dose can be increased weekly by 50 mg per day to a maximum daily dose of 200 mg. However, in order to avoid overdose when the dose is increased over 50 mg, it should be borne in mind that the body weight in children is less than in adults. With long-term maintenance therapy, the lowest effective dose should be prescribed.
Special groups:
No need for dose adjustment for elderly patients.
Patients with impaired liver functionrequire special attention during treatment with sertraline. In severe liver dysfunction, the dose of the drug should be reduced or the intervals between doses should be increased. In patients with impaired renal function, it is not required to specifically select a dose (see 'Special instructions' ).

active substance: 50 mg of sertraline in 1 tablet (in the form of 55.95 mg of sertraline hydrochloride, respectively);
excipients: magnesium stearate, hyprolose (hydroxypropyl cellulose), sodium carboxymethyl starch (type A), calcium hydrogen phosphate dihydrate, microcrystalline cellulose;
shell: macrogol 6000, titanium dioxide, hypromellose.

• Hypersensitivity to any component of the drug.

• Simultaneous reception of any MAO inhibitor, as well as a period within 14 days after its cancellation (and vice versa).

• Unstable epilepsy.

• Age up to 18 years, with the exception of patients with obsessive-compulsive disorder (due to lack of sufficient clinical experience).

• Pregnancy and lactation (see section 'Pregnancy and lactation').

With caution:
organic brain diseases (including mental retardation),
manic conditions,
epilepsy,
hepatic and / or renal failure,
weight loss,
in children over 6 years old.

Tradename:

STIMULOTON Ѓ

International non-proprietary name:

sertraline

Dosage form:

film-coated tablets

Composition:

active substance: 50 mg or 100 mg of sertraline in 1 tablet (in the form of 55.95 mg and 111.90 mg of sertraline hydrochloride, respectively);
excipients: magnesium stearate, hyprolose (hydroxypropyl cellulose), sodium carboxymethyl starch (type A), calcium hydrogen phosphate dihydrate, microcrystalline cellulose;
shell: macrogol 6000, titanium dioxide, hypromellose.

Description:

Tablets 50 mg: white or almost white, biconvex film-coated tablets, oval in shape, engraved with 'E 271' on one side and with a line on the other side; without smell.
Tablets 100 mg: white or almost white, biconvex film-coated tablets, oval in shape, engraved with 'E 272' on one side and with a line on the other side; without smell.

Pharmacotherapeutic group:

antidepressant.

ATX code: N06A B06

Pharmacological properties

Pharmacodynamics

Mechanism of action.
Sertraline is a selective serotonin reuptake inhibitor (5-HT). It has very little effect on the reuptake of norepinephrine and dopamine. In therapeutic doses, sertraline blocks the uptake of serotonin by human platelets. It has no stimulating, sedative or anticholinergic effect. Sertraline has no affinity for muscarinic (cholinergic), serotonergic, dopaminergic, adrenergic, histaminergic, GABA or benzodiazepine receptors.
The antidepressant effect is noted by the end of the second week of regular administration of sertraline, while the maximum effect is achieved only after 6 weeks. Unlike tricyclic antidepressants, there is no increase in body weight with the administration of sertraline. Sertraline does not cause mental or physical drug dependence.

Pharmacokinetics

Absorption of sertraline from the gastrointestinal tract is significant, but occurs slowly.
The maximum concentration in blood plasma is reached 4.5-8.4 hours after ingestion of the drug. The equilibrium concentration of sertraline in blood plasma is achieved within a week with a single daily intake. Bioavailability during food intake is increased by 25%, while the time to reach maximum concentration is shortened.
Distribution.
The total binding of sertraline to plasma proteins is 98%. The volume of distribution is> 20 l / kg.
Metabolism and excretion.
Sertraline is extensively metabolized during the first passage through the liver, undergoing N-demethylation. Its main metabolite, N-desmethylsertraline, is less active than the parent compound. Metabolites are excreted in urine and feces in equal amounts. About 0.2% of sertraline is excreted unchanged by the kidneys. The half-life of the drug is 22-36 hours and does not depend on age or gender. For N-desmethylsertraline, this figure is 62-104 hours.
The half-life of sertraline and the area under the plasma concentration curve (AUC) increase with impaired liver function. Regardless of the severity of renal failure, the pharmacokinetics of sertraline with its constant use does not change. Sertraline passes into breast milk. There is no data on its ability to pass through the blood-placental barrier.
Sertraline is not dialyzed.

Indications for use:

• Depression of various etiologies, incl. accompanied by feelings of anxiety (treatment and prevention)

• Obsessive-compulsive disorder (OCD), treatment for OCD in children over 6 years of age.

• Panic disorder (with and without agoraphobia).

• Post-traumatic stress disorder (PTSD).

Contraindications:

• Hypersensitivity to any component of the drug.

• Simultaneous reception of any MAO inhibitor, as well as a period within 14 days after its cancellation (and vice versa).

• Unstable epilepsy.

• Age up to 18 years, with the exception of patients with obsessive-compulsive disorder (due to lack of sufficient clinical experience).

• Pregnancy and lactation (see section 'Pregnancy and lactation').

With caution:
organic brain diseases (including mental retardation),
manic conditions,
epilepsy,
hepatic and / or renal failure,
weight loss,
in children over 6 years old.

Pregnancy and lactation

There are no controlled results of the use of sertraline in pregnant women, therefore, it is worth prescribing the drug to them only if the expected benefit to the mother outweighs the potential risk to the fetus. Women of reproductive age who are expected to be prescribed sertraline should be advised to use effective contraceptives. Sertraline is found in breast milk and is therefore not recommended during breastfeeding. There is no reliable data on the safety of its use during lactation, therefore, if treatment is still necessary, then it is better to stop breastfeeding.

Method of administration and dosage

Stimuloton should be taken once a day (morning or evening).
For adults with depression or obsessive-compulsive disorder, the usual dose is 50 mg once a day.
To reduce the frequency and severity of side effects in patients with panic disorder or PTSD, it is recommended to start treatment with a dose of 25 mg once a day and increase the dose to 50 mg once a day after a week.
With an unsatisfactory therapeutic response and good tolerance, the daily dose can be increased by 50 mg over several weeks to a maximum daily dose of 200 mg.
The therapeutic effect can occur within 7 days. However, it usually takes 2 to 4 weeks for the full manifestation of the antidepressant effect. In obsessive-compulsive disorder, the therapeutic effect develops even more slowly. For maintenance therapy, the minimum effective dose should be prescribed.
Children aged 13-18 years with obsessive-compulsive disorder should be prescribed Stimuloton starting at a dose of 50 mg per day. For children with obsessive-compulsive disorder aged 6-12 years, an initial dose of 25 mg per day is recommended, which can be increased to 50 mg per day after a week. If the therapeutic response is unsatisfactory, then the dose can be increased weekly by 50 mg per day to a maximum daily dose of 200 mg. However, in order to avoid overdose when the dose is increased over 50 mg, it should be borne in mind that the body weight in children is less than in adults. With long-term maintenance therapy, the lowest effective dose should be prescribed.
Special groups:
No need for dose adjustment for elderly patients.
Patients with impaired liver functionrequire special attention during treatment with sertraline. In severe liver dysfunction, the dose of the drug should be reduced or the intervals between doses should be increased. In patients with impaired renal function, it is not required to specifically select a dose (see 'Special instructions' ).

Side effects

Allergic reactions, bleeding (including nosebleeds), palpitations, dry mouth, decreased appetite or increased appetite (possibly due to elimination of depression).
Rarely observed: drowsiness, fatigue, dizziness, headache, tremors, insomnia, irritability, akathisia, weight loss, anorexia, stomach or abdominal cramps, flatulence or pain, unstable stools, diarrhea, dyspepsia, nausea, vomiting, visual disturbances ( including blurred vision), flushing of the skin or 'hot flushes' of blood to the face, yawning, increased sweating, dysmenorrhea, impaired sexual function (delayed ejaculation, decreased potency and / or libido, anorgasmia), hypomania, mania.
Sometimes- although the causal relationship with the drug has not been reliably established - during the course of treatment with the drug, movement disorders (extrapyramidal symptoms and gait disturbances), convulsions, menstrual irregularities, hyperprolactinemia, galactorrhea, skin rash (rarely exudative erythema multiforme) and itching were observed. In most cases, movement disorders were observed in patients taking concomitant neuroleptic drugs, as well as in the presence of a long history of movement disorders.
In rare cases, discontinuation of the drug causes a withdrawal syndrome.
As with treatment with other antidepressants, some symptoms may occur, including paresthesia, hypoesthesia, depression, hallucinations, agitation, aggressiveness, agitation, anxiety, psychosis, which are difficult to differentiate from the symptoms of the underlying disease.
Laboratory indicators: in rare cases (0.8%), there was an asymptomatic increase in transaminases (ACT and ALT). These changes were observed during the first 9 weeks of taking the drug and stopped immediately after discontinuation. Reversible hyponatremia has also been reported. Presumably, this phenomenon is associated with the syndrome of insufficient secretion of antidiuretic hormone (ADH), since it is mainly observed in elderly patients who are simultaneously receiving concomitant diuretics or other drugs.

Overdose

Sertraline overdose did not show severe symptoms even when the drug was prescribed in high doses. However, when administered simultaneously with other drugs or ethanol, severe poisoning may occur.
Overdose can cause serotonin syndrome with nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia.
Treatment:there are no specific antidotes. Requires intensive supportive therapy and constant monitoring of vital body functions. Inducing vomiting is not recommended. The administration of activated charcoal may be more effective than gastric lavage. The airway must be kept clear. Sertraline has a large volume of distribution, in this regard, increased diuresis, dialysis, hemoperfusion or blood transfusion may be ineffective.

Interaction with other medicinal products

Monoamine oxidase inhibitors (MAOIs): the simultaneous use of sertraline with MAO inhibitors, including selegiline and the reversible inhibitor moclobemide, leads to severe complications. Development of serotonin syndrome is possible. Several cases of patient death were noted with a combination of other antidepressants and MAO inhibitors, as well as with the isolated administration of MAO inhibitors, started immediately after the withdrawal of other antidepressants. With the combination of a selective serotonin reuptake blocker and an MAO inhibitor, hyperthermia, rigidity, myoclonus, autonomic instability (sometimes with rapid changes in respiratory and circulatory functions), changes in mental state (for example, confusion, irritability, sometimes with extreme agitation were observed, which could lead to delirium or coma).Therefore, sertraline should never be used in combination with MAO inhibitors or within 14 days after the withdrawal of the MAO inhibitor, and also less than 1 day after the withdrawal of the reversible MAO inhibitor.
Similarly, after discontinuation of sertraline, at least 14 days must elapse before the administration of an irreversible MAO inhibitor begins.

Substances that depress the central nervous system and alcohol:
in healthy volunteers, daily sertraline 200 mg per day did not increase the effects of alcohol, carbamazepine, haloperidol or phenytoin on cognitive function and psychomotor activity. However, drugs that affect the central nervous system should be used with great caution while taking sertraline, and alcohol should be avoided while taking the drug.

Sertraline binds to plasma proteins. Therefore, it is necessary to take into account the possibility of its interaction with other drugs that bind to proteins (for example: diazepam, tolbutamide and warfarin).

Cimetidine: concomitant use significantly reduces sertraline clearance.

Coumarin derivatives - when administered together with sertraline, there is a significant increase in prothrombin time - in these cases, it is recommended to control the prothrombin time at the beginning of treatment with sertraline and after its cancellation.

Drugs metabolized by cytochrome P450 isoenzyme 2D6: long-term treatment with sertraline at a dose of 50 mg per day is accompanied by an increase in the concentration of these drugs.

Drugs metabolized by other cytochrome P450 enzymes: in vivo
interaction studies have shown that long-term administration of sertraline 200 mg per day did not affect endogenous beta-hydroxylation of cortisol or metabolism of carbamazepine or terfenadine mediated by CYP3A3 / 4 isoenzymes . Long-term administration of sertraline 200 mg per day did not affect plasma levels of tolbutamide, phenytoin, and warfarin . This means that sertraline does not suppress CYP2C9 activity to a clinically significant extent. Long-term administration of doses of 200 mg per day did not affect diazepam levels either.in blood plasma, therefore, clinically significant sertraline inhibition of CYP2C19 should also be excluded. Conducted in vitro studies have shown that sertraline has no effect or minimal inhibitory effect on CYP 1A2.

Lithium. The pharmacokinetics of lithium does not change with the concomitant administration of sertraline. However, tremors are more common when they are used together. As well as the appointment of other selective serotonin reuptake inhibitors, the combined use of sertraline with drugs that affect serotonergic transmission (for example, with lithium) requires increased caution.

Serotonergics: The
length of the washout period required before transferring a patient from one selective serotonin reuptake inhibitor to another has not been determined. Therefore, this transition should be done with extreme caution.

The simultaneous administration of other serotonergic substances (for example, tryptophan or fenfluramine) and sertraline requires special care. Such combinations should be avoided whenever possible.

Induction of microsomal enzymes:
In clinical trials, only a slight inducing effect of sertraline on liver enzymes was found. With the simultaneous use of sertraline 200 mg per day and phenazone, sertraline caused a small (5%) but significant decrease in the half-life of phenazone. This slight decrease in the half-life of phenazone was due to a clinically insignificant change in liver metabolism.

Atenolol: When used together, sertraline does not alter the beta-blocking effect of atenolol.

Glibenclamide and digoxin: with the introduction of sertraline in a daily dose of 200 mg, drug interactions with these drugs were not detected.

special instructions

There are no data on the possible risks and benefits of concomitant use of electroconvulsive therapy (ECT) and sertraline.
Like other antidepressants, sertraline can cause mania or hypomania in a small percentage of patients (approximately 0.4%).
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, before the development of an optimal clinical effect, patients need careful medical supervision.
Stimuloton should not be used to treat children and adolescents under the age of 18, with the exception of patients with obsessive-compulsive disorder. An increase in the likelihood of suicide and suicidal thoughts, as well as hostility (mainly aggression, rebelliousness and anger), in clinical trials, is more often observed among children and adolescents receiving antidepressants compared with groups receiving placebo. If, according to clinical indications, the drug is prescribed, the patient should be monitored to detect suicidal symptoms. In addition, there is a lack of long-term safety data in children and adolescents regarding growth, maturation, and cognitive and behavioral development.
In clinical trials of sertraline, epileptic seizureswere observed in 0.08% of patients with depression (approximately 3/4000) and in 0.2% of patients with obsessive-compulsive disorders (4/1800). A strict connection between epileptic seizures and sertraline intake has not been established. There are no data on the treatment of patients with epilepsy with sertraline. This drug should not be given to patients with unstable epilepsy, and patients who do not have seizures should be monitored regularly. If seizures occur, sertraline should be discontinued.
Liver failure:the metabolism of sertraline is mainly carried out in the liver. Single-dose pharmacokinetic studies have shown an increase in sertraline half-life and an increase in the area under the concentration-time curve in patients with mild cirrhosis. Therefore, caution is needed when prescribing sertraline for liver disease; for such patients, the possibility of reducing the dose or increasing the interval between doses of the drug should be considered.
Renal failure:the pharmacokinetics of sertraline after administration of a single dose or multiple dosing did not show significant changes in patients with moderate (creatinine clearance 20-50 ml / min) or severe (less than 20 ml / min) renal impairment. These studies have shown that there is no need to adjust the dose of sertraline in kidney disease.

¬ли¤ние на способность управлени¤ транспортными средствами и механизмами

–езультаты клинических исследований показали, что монотерапи¤ сертралином не вли¤ет на показатели психомоторной де¤тельности пациентов. ќднако поскольку другие препараты, примен¤емые по аналогичным показани¤м, могут отрицательно вли¤ть на психомоторную де¤тельность, способность пациента управл¤ть транспортными средствами и механизмами следует определ¤ть индивидуально в зависимости от реакции пациента на лечение и применени¤ сопутствующей терапии.

‘орма выпуска

Film-coated tablets 50 mg: 10 tablets in a PVC / PVDC / aluminum foil blister. 1, 2 or 3 blisters in a cardboard box along with instructions for medical use.
Film-coated tablets 100 mg: 14 tablets in a PVC / PVDC / aluminum foil blister. 1 or 2 blisters in a cardboard box along with instructions for medical use.

Storage conditions

Store at a temperature not exceeding 25 ? C.
Keep out of the reach of children.

Shelf life

5 years. Do not use after the expiration date printed on the package.

Conditions of dispensing from pharmacies

On prescription.