Stimuloton - instructions for use, dose, side effects, contraindications

: active substance: 50 mg or 100 mg sertraline in 1 tablet (in the form of 55.95 mg and 111.90 mg sertraline hydrochloride, respectively); auxiliary substances: magnesium stearate, giprolose (hydroxypropylcellulose), sodium carboxymethyl starch (type A), calcium hydrophosphate dihydrate, microcrystalline cellulose; Shell: Macrogol 6000, titanium dioxide, hypromellose.

Description:

Tablets of 50 mg: white or almost white, biconvex tablets covered with a film shell, oval, engraved "E 271" on one side and with a risk - on the other side; without smell.

Tablets of 100 mg: white or almost white, biconvex tablets covered with a film shell, oval, engraved "E 272" on one side and with a risk - on the other side; without smell.

Pharmacotherapeutic group:antidepressant

ATX: & nbsp

N.06.A.X Other antidepressants

N.06.A Antidepressants

N.06.A.B Selective serotonin reuptake inhibitors

Pharmacodynamics:

Mechanism of action.

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

Pharmacokinetics:

Absorption of sertraline from the gastrointestinal tract is significant,but it is slow. The maximum concentration in the blood plasma is achieved in 4,5-8,4 hours after taking the drug inside. The equilibrium concentration of sertraline in blood plasma is reached within a week with a single daily intake. Bioavailability during meals increases 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> 20l / kg.

Metabolism and excretion. Sertraline is subjected to intensive metabolism during the first passage through the liver, undergoing N-demethylation. Its main metabolite, N-desmethylsertralin, is less active than the parent compound. Metabolites are excreted in urine and feces in equal amounts. About 0.2% of sertraline is excreted by the kidneys unchanged. The half-life of the drug is 22-36 hours and does not depend on age or sex. For N-desmethylsertraline, this indicator is 62-104 hours.

The half-life of sertraline and the area under the plasma concentration curve (AUC) increase with liver function impairment. Regardless of the severity of renal failure, the pharmacokinetics of sertraline does not change with its constant application. Sertraline penetrates into breast milk. Data on its ability to pass through the hematoplacental barrier is not present.

Sertraline is not dialyzed.

Indications:

Depression of various etiologies, incl. accompanied by a sense of anxiety (treatment and prevention)

Obsessive-compulsive disorder (OCD), treatment of OCD in children older than 6 years.

Panic disorders (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 the period within 14 days after its cancellation (and vice versa).

Unstable epilepsy.

Age to 18 years, except for patients with obsessive-compulsive disorder (due to lack of sufficient clinical experience).

Pregnancy and lactation period (see the section "Pregnancy and lactation period"),

Carefully:

organic brain diseases (including mental retardation), manic conditions, epilepsy, hepatic and / or renal insufficiency, weight loss, in children older than 6 years.

Pregnancy and lactation:

There are no controlled results of the use of sertraline in pregnant women, so it is necessary to prescribe them only if the expected benefit for the mother exceeds the potential risk for the fetus. Women of reproductive age who are supposed to be appointed sertraline, it should be recommended to use effective contraceptives. Sertraline is found in breast milk, and therefore treatment with this drug during breastfeeding is not recommended. There are no reliable data on the safety of its use during lactation, so if treatment is still necessary, then breast-feeding should be stopped.

Dosing and Administration:

Stimuloton should be taken once a day (morning or evening).

For adults suffering from depression or obsessive-compulsive disorder, the usual dose is 50 mg 1 time per day.

To reduce the frequency and severity of side effects in patients with panic disorders or post-traumatic stress disorder, it is recommended to start treatment with a dose of 25 mg once a day and a week later increase the dose to 50 mg once a day.

With an unsatisfactory therapeutic response and good tolerability, the daily dose can be increased by 50 mg for several weeks to a maximum daily dose of 200 mg. - Therapeutic effect can occur within 7 days. However, usually for a full manifestation of the antidepressant effect, it takes from 2 to 4 weeks. With obsessive-compulsive disorder, the therapeutic effect develops even more slowly. For maintenance therapy, the minimum effective dose should be given.

Children aged 13-18 years with obsessive-compulsive disorder Stimuloton should be prescribed starting with a dose of 50 mg per day. For children with obsessive-compulsive disorder at the age of 6-12 years, an initial dose of 25 mg per day is recommended, which in a week can be increased to 50 mg per day. With an unsatisfactory therapeutic response, you can then increase the dose weekly at 50 mg per day to a maximum daily dose of 200 mg. However, in order to avoid an overdose with a dose increase of over 50 mg, it should be borne in mind that the body weight in children is less than in adults. With prolonged maintenance therapy, the lowest effective doses should be given.

Special groups:

There is no need for dose adjustment for elderly patients.

Patients with impaired liver function require special attention in the treatment of sertraline. In case of severe impairment of liver function, the dose of the drug should be reduced or the intervals between doses should be increased. In patients with impaired renal function, no specific dose is required (see "Specific indication").

Side effects:

Allergic reactions, bleeding (including nasal), palpitations, dry mouth, decreased appetite or increased appetite (possibly due to the elimination of depression).

Drowsiness, fatigue, dizziness, headache, tremor, insomnia, irritability, akathisia, weight loss, anorexia, stomach or abdominal cramps, flatulence or pain, unstable stools, diarrhea, dyspepsia, nausea, vomiting, and visual impairment were rarely observed. including blurred vision), skin hyperemia or "flushes" of blood to the face, yawning, increased sweating, dysmenorrhea, impaired sexual function (delay in ejaculation, decreased potency and / or libido, anorgasmia), hypomania, mania.

Sometimes - although a causal relationship with the drug is not reliably established - during the course of treatment with the drug, motor disorders (extrapyramidalsymptoms and disorders of gait), seizures, menstrual irregularities, hyperprolactinemia, galactorrhea, skin rash (rarely multiforme exudative erythema) and itching. In most cases, motor disorders were observed in patients taking concomitant neuroleptic drugs, as well as in the presence of a long history of motor disorders.

In rare cases, discontinuation of the drug causes withdrawal syndrome.

As with other antidepressants, there may be some symptoms, including paresthesia, hypesthesia, depression, hallucinations, agitation, aggressiveness, agitation, anxiety, and psychosis, which are difficult to differentiate from the symptoms of the underlying disease. Laboratory indicators: in rare cases (0.8%) asymptomatic increase of transaminases (ACT and ALT) was noted. These changes were observed during the first 9 weeks of taking the drug and stopped immediately after it was discontinued. There have also been reports of reversible hyponatremia. Presumably, this phenomenon is associated with the syndrome of insufficient secretion of antidiuretic hormone (ADH), as it was mainly observed in elderly patients concomitantly receiving concomitant diuretics or other drugs.

Overdose:

Severe symptoms with an overdose of sertraline was not detected even with the administration of the drug in large doses. However, with simultaneous administration with other drugs or ethanol, severe poisoning can 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. It requires intensive maintenance therapy and constant monitoring of vital body functions. It is not recommended to induce vomiting. The introduction of activated carbon can be more effective than gastric lavage. It is necessary to maintain airway patency. Sertraline has a large volume of distribution, in connection with this, increased diuresis, dialysis, hemoperfusion or blood transfusion may not be successful.

Interaction:

Inhibitors of monoamine oxidase (MAOI): simultaneous use of sertraline with

inhibitors of MAO, including selegilin and a reversible inhibitor of moclobemide, leads to severe complications.Perhaps the development of serotonin syndrome. Several deaths of the patient were noted in the combination of other antidepressants and MAO inhibitors, as well as with the isolated administration of MAO inhibitors, started immediately after the abolition of other antidepressants. Hyperthermia, stiffness, myoclonia, autonomic instability (sometimes with rapid changes in respiratory and circulatory functions), changes in mental state (for example, confused consciousness, irritability, sometimes with extreme agitation, which could lead to delirium or coma). therefore sertraline never be used in combination with MAO inhibitors, or within 14 days after the abolition of the MAO inhibitor, and also less than 1 day after the reversal of the reversible MAO inhibitor. Similarly, after the withdrawal of sertraline, at least 14 days must elapse before the introduction of the irreversible MAO inhibitor.

Substances depressing the central nervous system and alcohol: in healthy volunteers, daily intake of sertraline 200 mg per day did not enhance the effects of alcohol, carbamazepine, haloperidol or phenytoin on cognitive functions and psychomotor activity.However, during the administration of sertraline, drugs that affect the central nervous system should be used with great care, and alcohol use during drug intake should be avoided.

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

Cimetidine: simultaneous use significantly reduces the clearance of sertraline. Coumarin derivatives - when combined with sertraline, there is a significant increase in prothrombin time - in these cases it is recommended to monitor prothrombin time at the beginning of treatment with sertraline and after its withdrawal.

Drugs metabolized by isoenzyme 2D6 cytochrome P450: prolonged 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 prolonged administration of sertraline at 200 mg per day did not affect the endogenous beta-hydroxylation of cortisol or the metabolism of carbamazepine or terfenadine mediated by CYP3A3 / 4 isozymes.Long-term administration of sertraline at 200 mg per day did not affect the levels of tolbutamide, phenytoin and warfarin in the blood plasma. It means that sertraline does not inhibit the activity of CYP2C9 in a clinically significant degree. Long-term doses of 200 mg per day did not affect diazepam levels in the blood plasma, and therefore clinically significant suppression of sertraline CYP2C19 should also be excluded. In vitro studies have shown that sertraline does not affect or has a minimal inhibitory effect on CYP 1A2.

Lithium. The pharmacokinetics of lithium does not change with the concomitant administration of sertraline. However, tremor is observed more often when they are used together. As well as the appointment of other selective inhibitors of reverse neuronal seizure of serotonin, a joint

the use of sertraline with drugs, influencing on

serotonergic transmission (for example, with lithium), requires increased caution. Serotonergic agents: the duration of the washout period required before transferring the patient from one selective serotonin reuptake inhibitor to another is not determined.Therefore, such a transition should be carried out with extreme caution.

Simultaneous administration of other serotonergic substances (eg, tryptophan or fenfluramine) and sertraline requires extreme caution. If possible, such combinations should be avoided.

Induction of microsomal enzymes: in clinical trials, only

a slight inducing effect of sertraline on hepatic enzymes. With the simultaneous use of sertraline at 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 combined sertraline does not change the beta-blocking effect of atenolol.

Glibenclamide and digoxin: when sertraline was administered in a daily dose, 200 mg of drug interaction with these drugs was not detected.

Special instructions:

There are no data on the possible risks and benefits of simultaneous 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 the optimal clinical effect, patients need careful medical supervision.

Stimuloton should not be used to treat children and adolescents under the age of 18, except for patients with obsessive-compulsive disorder. Increased likelihood of suicide and suicidal thoughts, as well as hostility (mainly aggression, disobedience and anger), in clinical trials are more likely to occur among children and adolescents receiving antidepressants, compared with groups receiving a placebo. If, on clinical grounds, the drug is prescribed, patient monitoring should be established to detect suicidal symptoms. In addition, there are no long-term safety data for children and adolescents regarding growth, maturation, and development of cognitive scope and behavior.

In clinical trials of sertraline epileptic seizures were observed in 0.08% of depressed patients (approximately 3/4000) and in 0.2% of patients with obsessive-compulsive disorders (4/1800).Strict communication of epileptic seizures with sertraline is not established. There are no data on the treatment of sertraline in patients with epilepsy. This drug should not be prescribed to patients with unstable epilepsy, and patients who do not have seizures should be screened regularly. When seizures occur sertraline necessary cancel.

Liver failure: the metabolism of sertraline is mainly carried out in the liver. Pharmacokinetic studies with single dose administration revealed elongation sertraline half-life and increased area under the concentration-time curve in patients with mild cirrhosis. Therefore, caution is necessary in the appointment of sertraline in liver diseases; for such patients, the possibility of reducing the dose or increasing the interval between doses of the drug should be considered.

Renal insufficiency: Sertraline Pharmacokinetics after administration of a single dose or multiple dose had no significant changes in patients with moderate (creatinine clearance 20 - 50 ml / min) or severe (less than 20 ml / min) of renal insufficiency.These studies showed that there is no need to adjust the dose of sertraline for kidney disease.

Effect on the ability to drive transp. cf. and fur:

Impact on the ability to drive vehicles and mechanisms The results of clinical studies have shown that sertraline monotherapy does not affect the psychomotor performance of patients. However, since other drugs used for similar indications can adversely affect psychomotor activity, the patient's ability to control vehicles and mechanisms should be determined individually, depending on the patient's response to treatment and the use of concomitant therapy.

Form release / dosage:Tablets film-coated 50 mg, 100 mg.

Packaging:

Tablets covered film shell 50 mg: by 10 tablets in blister from PVC / PVDC / al.foil. 1, 2, or 3 blisters in a cardboard box together with instruction for medical use.

Tablets covered film shell 100 mg: for 14 tablets in blister from PVC / PVDC / al.foil. 1 or 2 blisters in cardboard pack together with instruction by

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 expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N013940 / 01

Date of registration:08.04.2009

The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Manufacturer: & nbsp

EGIS Pharmaceutical Plant, ZAO Hungary

Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Information update date: & nbsp20.09.2015

Illustrated instructions

Instructions

Stimuloton® (Stimuloton®)