Stimuloton: instructions for using the medicine, structure, Contraindications

Active material: Sertraline
When ATH: N06AB06
CCF: Antidepressant
ICD-10 codes (testimony): F31, F32, F33, F41.0, F41.2, F42, F43
When CSF: 02.02.04
Manufacturer: EGIS PHARMACEUTICALS Plc (Hungary)

Stimuloton: dosage form, composition and packaging

Pills, Film-coated white or nearly white, oval, lenticular, Engraved “E271” on one side and Valium – another, without smell.

Excipients: magnesium stearate, giproloza (hydroksypropyltsellyuloza), sodium carboxymethyl (Type A), calcium hydrogen phosphate dihydrate, microcrystalline cellulose.

The composition of the shell: macrogol 6000, Titanium dioxide, gipromelloza.

10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.

Pills, Film-coated white or nearly white, oval, lenticular, Engraved “E272” on one side and Valium – another, without smell.

Excipients: magnesium stearate, giproloza (hydroksypropyltsellyuloza), sodium carboxymethyl (Type A), calcium hydrogen phosphate dihydrate, microcrystalline cellulose.

The composition of the shell: macrogol 6000, Titanium dioxide, gipromelloza.

14 PC. – blisters (1) – packs cardboard.
14 PC. – blisters (2) – packs cardboard.

Stimuloton: pharmachologic effect

Antidepressant. Selective serotonin reuptake inhibitor. It has little effect on the reuptake of norepinephrine and dopamine. At therapeutic doses, sertraline blocks the uptake of serotonin and platelets in human blood.

Do not have a stimulatory, sedative or anticholinergic action. Sertraline has no affinity for the m-choline, serotonin, dopamine, histamine, adrenocorticotropin, GABA- and benzodiazepine receptors.

In applying Stimulotona^® no increase in body weight. The drug does not cause mental or physical drug dependence.

Antidepressant effect was seen at the end of the second week of the regular ingestion, while the maximum effect is achieved only through 6 weeks.

Stimuloton: pharmacokinetics

Absorption

Once inside absorbed from the gastrointestinal tract slowly, but almost completely. C_max achieved through 4.5-8.4 no. While taking the drug at the same time eating its bioavailability is increased by 25%, C_max achieved faster.

Distribution

With daily single dose of the drug C_ss It is usually achieved within a week. Binding to plasma proteins is 98%. V_d – more 20 l / kg. Sertraline is excreted in breast milk. Data about its ability to cross the placental barrier there.

Metabolism

Sertraline is extensively metabolized in the “first pass” through the liver, undergoing N-demethylation. Its main metabolite - N-desmetilsertralin less active, Cem sertraline.

Deduction

T_1/2 is 22-36 hours and does not depend on the age and sex of patients. T_1/2 N-desmetilsertralina is 62-104 no.

Displays in the form of metabolites in urine and faeces in equal amounts, 0.2% sertraline is excreted in the urine in unchanged form.

Pharmacokinetics in special clinical situations

T_1/2 sertraline and AUC values ​​increase with abnormal liver function. Pharmacokinetic study drug administration in a single dose showed an increase in T_1/2 and AUC sertraline in patients with mild cirrhosis.

Regardless of the severity of renal impairment the pharmacokinetics of sertraline in his constant use is not changed. Sertraline does not appear in hemodialysis.

Stimuloton: testimony

• depression of various etiologies, incl. accompanied by a sense of anxiety (Treatment and Prevention);
• obsessive-compulsive disorder, incl. in children older 6 years;
• panic disorder (with or without agoraphobia);
• post-traumatic stress disorder.

Stimuloton: dosing regimen

The drug is prescribed inside, 1 time / day (in the morning or evening).

Adults at depression and obsessive-compulsive disorders the drug is prescribed in a dose 50 mg 1 time / day.

At panic disorders and PTSD to reduce the frequency and severity of side effects is recommended to start treatment with a dose of 25 mg 1 time / day and a week later increase it to 50 mg 1 time / day.

When poor therapeutic response and tolerability daily dose can be increased by 50 mg for several weeks to a maximum daily dose 200 mg.

The therapeutic effect is achieved, usually within 7 days. However, for the full manifestation of antidepressant action requires regular intake of the drug for 2-4 weeks. With obsessive compulsive disorder therapeutic effect develops more slowly. For maintenance therapy should be given the minimum effective dose.

At obsessive-compulsive disorders children aged 13 to 18 years the drug is prescribed in an initial dose 50 mg 1 time / day. Children aged 6 to 12 years the drug is prescribed in an initial dose 25 mg 1 time / day, a week daily dose can be increased to 50 mg. When poor therapeutic response further dose can be increased weekly 50 mg / day to a maximum daily dose 200 mg. To avoid overdosing with increasing dose over 50 mg / day should be considered, that body weight in children less than, than in adults. When long-term maintenance therapy, the drug should be used in the lowest effective dose.

In elderly patients correction dose is not required.

In patients with severely impaired hepatic function dose should be reduced or increased intervals between doses.

In patients with impaired renal function special dose adjustment is not required.

Stimuloton: side effects

From the central and peripheral nervous system: rarely – drowsiness, fatiguability, dizziness, headache, tremor, insomnia, irritability, akathisia, hypomania, craze.

As with other antidepressants in the treatment of, there may be reactions, which are difficult to differentiate from symptoms of the underlying disease in t. no. paraesthesia, gipesteziya, depression, hallucinations, excitation, aggressiveness, ažitaciâ, anxiety, psychosis.

From the digestive system: dry mouth, loss of appetite or increased appetite (possibly due to elimination of Depression); rarely – anorexia, stomach cramps, stomach, bloating or pain, unstable chair, diarrhea, dyspepsia, nausea, vomiting.

Cardio-vascular system: rarely – heartbeat.

Metabolism: weight loss.

From the hematopoietic system: bleeding (incl. bow).

From the senses: rarely – visual impairment (including blurred vision)

On the part of the reproductive system: rarely – dysmenorrhoea, sexual dysfunction (delayed ejaculation, reduced potency and / or libido, anorgazmija).

Dermatological reactions: rarely – flushing of the skin, or “tides” blood to the face, increased perspiration.

From the laboratory parameters: in some cases (0.8%) – Asymptomatic elevations of ALT and ACT (These changes were observed within the first 9 weeks and stop taking the drug immediately after its cancellation); there are reports of reversible hyponatremia (presumably, this phenomenon is associated with the syndrome of inadequate secretion of ADH, as it is seen mainly in elderly patients, simultaneously receiving concomitant diuretics or other drugs).

Other: rarely – allergic reactions, zevota; in some cases, stopping the drug causes withdrawal.

Sometimes (a causal relationship with the drug did not significantly set) – movement disorders (extrapyramidal symptoms and gait disturbance), convulsions, menstrual irregularities, hyperprolactinemia, galactorrhea, skin rash (rarely – erythema multiforme exudative), itch. In most cases, motor disorders observed in patients, receiving concomitant antipsychotics (neuroleptics), as well as the presence of a long history of movement disorders.

Stimuloton: Contraindications

• simultaneous use of MAO inhibitors and period 14 days after their cancellation;
• unstable epilepsy;
• Age to 18 years (due to insufficient clinical experience with), except for patients with obsessive-compulsive disorder;
• pregnancy;
• lactation (breast-feeding);
• hypersensitivity to the drug.

FROM caution should be prescribed with organic brain diseases (incl. when mental retardation), manic states, epilepsy, hepatic and / or renal failure, weight reduction, as well as children over the age of 6 years with OCD.

Stimuloton: Pregnancy and lactation

Controlled results of safety of Stimulotona^® in pregnant women is not, so the appointment is contraindicated in pregnancy.

Women of reproductive age, which is expected to appoint Stimuloton^®, should be advised to use effective contraception.

Sertraline is excreted in breast milk. Reliable data on the safety of its use during lactation is not. The appointment Stimulotona^® lactation breastfeeding should be discontinued.

Stimuloton: Special instructions

Information about the possible risks and benefits of the simultaneous use of electroconvulsive therapy and Stimulotona^® no.

As with other antidepressants, Stimuloton^® in some cases (about 0.4%) can cause mania or hypomania.

Suicidal ideation and attempts are often associated with depression; they are possible at any time to remission. Therefore, at the beginning of treatment, to the development of an optimal clinical effect, patients need close medical supervision.

In clinical trials Stimulotona^® seizures have been observed in 0.08% patients with depression (about 3/4000) and 0.2% Patients with obsessive-compulsive disorder (4/1800). A strict connection with epileptic seizures taking Stimulotona^® not installed. There are no data on the treatment of Stimulotonom^® epileptics. The drug should not be prescribed to patients with unstable epilepsy, and patients, without seizures, You should be screened regularly. In the event of seizures Stimuloton^® should be abolished.

The metabolism of sertraline is mainly carried out in the liver, therefore caution is required when appointing Stimulotona^® Patients with liver disease.

Use in Pediatrics

Do not use this Stimulotona^® treatment children and adolescents under the age of 18 years, except in patients with obsessive-compulsive disorder. Increased likelihood of suicide and suicidal thoughts, and hostility (mainly aggression, rebelliousness and anger), in clinical trials is more common among children and adolescents, receiving antidepressants, compared with groups, receiving placebo. If clinically indicated drug appointed, should establish observation of the patient to detect suicidal symptoms. Besides, There are no long-term safety data in children and adolescents with respect to growth, maturation, as well as the development of cognition and behavior.

Effects on ability to drive vehicles and management mechanisms

Clinical studies have shown, Chto monotherapy Stimulotonom^® It does not affect the performance of psychomotor function. However, since other drugs, used for the same indications, may adversely affect the psychomotor reactions, the ability to drive and use machines should be determined individually depending on the patient's response to treatment and the use of concomitant therapy.

Stimuloton: overdose

Even the appointment of sertraline in high severe symptoms have been identified. However, administration of high doses of sertraline in conjunction with other drugs or ethanol may lead to severe poisoning.

Symptoms: serotonin syndrome with nausea, vomiting, sleepiness, taxikardiej, agitation, dizziness, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia.

Treatment: There are no specific antidotes. Require intensive supportive care, and constant monitoring of the functions of vital organs. Induce vomiting is not recommended. Introduction of the activated carbon may be more effective, than gastric lavage. It is necessary to maintain an open airway. In sertraline big V_d, In this regard, increased diuresis, dialysis, hemoperfusion or blood transfusion may be inconclusive.

Stimuloton: drug interaction

In an application Stimulotona^® MAO inhibitors, incl. with selegiline and reversible MAO inhibitor moclobemide, there are severe complications. Perhaps the development of serotonin syndrome. Several cases of death in the combination of antidepressants and MAO inhibitors, as well as the isolated administration of inhibitors of MAO, started immediately after the abolition of other antidepressants. With the combination of selective serotonin reuptake blockers and MAO inhibitors were observed pyrexia, rigidity, myoclonus, autonomic instability (sometimes with the rapid changes in the functions of respiration and circulation), changes in mental status (eg, confusion, irritability, sometimes with extreme agitation, which could lead to delirium or coma). Why not use this Stimulotona^® combined with MAO inhibitors, or for 14 days after discontinuation of MAO inhibitor, and less than 1 the day after the cancellation of a reversible inhibitor of MAO. Similarly, after the abolition of Stimulotona^® must be at least 14 days prior to the use of an irreversible inhibitor of MAO.

In studies in healthy volunteers with daily intake Stimulotona^® dose 200 mg / day was not observed the growing influence of ethanol, karʙamazepina, haloperidol, or phenytoin on cognitive function and psychomotor reactions. However, while taking sertraline medicines, affecting the CNS, should be used with extreme caution, the use of ethanol during treatment is contraindicated.

The binding to plasma proteins sertraline high, therefore it is necessary to consider the possibility of interactions with other drugs, binds to a protein (eg, diazepamom, tolbutamide and warfarin) plasma.

In an application Stimulotona^® cimetidine significantly reduces the clearance of sertraline.

In an application Stimulotona^® with coumarin derivatives showed a significant increase in prothrombin time (In such cases it is recommended to monitor the prothrombin time at the beginning of treatment with sertraline and after its cancellation).

Against the background of long-term therapy Stimulotonom^® dose 50 mg / day use of drugs, metabolized with the participation of the CYP2D6 isoenzyme, accompanied by a rise in their concentrations in blood plasma.

In studies of drug interactions in vivo shows, that long-term administration of sertraline at a dose of 200 mg / day did not affect the indirect isozymes CYP3A3 / 4 beta-hydroxylation of endogenous cortisol, the metabolism of carbamazepine or terfenadine. Long-term administration of sertraline at a dose of 200 mg / day did not affect the concentrations of tolbutamide, phenytoin and warfarin in the blood plasma. It means, that sertraline does not inhibit CYP2C9 activity at clinically relevant degree. Long-term administration of sertraline at a dose of 200 mg / day, and no effect on the diazepam concentration in plasma, in connection with which a clinically significant inhibition of CYP2C19 isoenzyme activity should also be excluded. Past studies have shown in vitro, Sertraline has no effect or minimal inhibitory effect on CYP1A2.

In an application Stimulotona^® and drugs lithium pharmacokinetics last unchanged. However, this combination of tremor occurs more often. As well as the appointment of other selective inhibitors of serotonin reuptake, when combined Stimulotona^® medicine, affecting serotonergic transmission (incl. with lithium), requires increased caution.

Time, required for complete excretion of the active agent before transferring the patient from one selective serotonin reuptake inhibitor on the other, definitely not. Therefore, such a transition should be carried out with extreme caution.

With the simultaneous use of other serotonergic agents (eg, tryptophan or fenfluramine) sertraline, and requires special care. Where possible these combinations should be avoided.

In clinical studies found only a small inducing effect of sertraline on liver enzymes. In an application Stimulotona^® dose 200 mg / day and phenazone, sertraline caused small (5%), but a significant decrease in T_1/2 fenazona. This is a slight decrease in T_1/2 phenazone was due to clinically insignificant changes in metabolism in the liver.

When combined sertraline does not alter beta-blocking effect of atenolol.

When combined Stimulotona^® dose 200 mg / day with glibenclamide and digoxin drug interactions have been identified.

Stimuloton: terms of dispensing from pharmacies

The drug is released under the prescription.

Stimuloton: terms and conditions of storage

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 5 years.