Stimuloton, 50 mg 30 pcs

Pharmacodynamics

An antidepressant. Selective serotonin reuptake inhibitor. It has a weak effect on norepinephrine and dopamine reuptake. In therapeutic doses, sertraline also inhibits serotonin uptake by human platelets.

The drug does not have stimulant, sedative or anticholinergic effects. The drug does not interact with m-choline, serotonin, dopamine, histamine, adreno-, GABA- and benzodiazepine receptors.

When using Stimuloton there is no increase in body weight. The drug does not cause mental or physical addiction.

The antidepressant effect is noted by the end of the second week of regular use of the drug, whereas the maximum effect is reached only after 6 weeks.

Pharmacokinetics

Absorption

Absorbed from the gastrointestinal tract slowly but almost completely. C _max is reached 4.5-8.4 h after oral administration. When the drug is taken simultaneously with meals its bioavailability is increased by 25%, C _max is reached faster.

Distribution

When the drug is taken once daily, C _ss is usually reached after one week. It is 98% bound to plasma proteins. V _d is greater than 20 L/kg. Sertraline is excreted with breast milk. There is no data on its ability to penetrate the placental barrier.

Metabolism

Sertraline is biotransformed on first passage through the liver, undergoing N-demethylation. Its main metabolite, N-desmethylsertraline, is less active than sertraline.

0.2% of sertraline is excreted unchanged in the urine, the remainder as metabolites with the urine and feces in equal amounts. T _1/2 is 22-36 h and is independent of the age and sex of patients. T _1/2 N-desmethylsertraline is 62-104 h. Sertraline is not excreted by hemodialysis. Pharmacokinetics in special clinical cases T_1/2 and AUC of Sertraline are increased in liver dysfunction. Regardless of the severity of renal impairment, the pharmacokinetics of sertraline are not altered by its continued use.

Indications

Active ingredient

Composition

Active ingredients:

Sertraline hydrochloride 55.95 mg, which corresponds to the content of sertraline 50 mg.

Auxiliary substances:

hydroxypropyl cellulose,

calcium hydrophosphate dihydrate,

microcrystalline cellulose,

sodium amylopectin glycolate.

Coating composition:

Hypromellose 2910, macrogol 6000, titanium dioxide.

How to take, the dosage

Adults

In depressive and obsessive-compulsive disorders

The drug is prescribed in a dose of 50 mg once daily in the morning or evening. Gradually, at the earliest after a week, the daily dose can be increased to a maximum daily dose of 200 mg.

In patients with obsessive-compulsive disorders, it may take 8-12 weeks to achieve good results. The minimum dose that provides a therapeutic effect is maintained thereafter as a maintenance dose.

In panic disorder and post-traumatic stress disorder

The treatment should be started with a dose of 25 mg once daily in the morning or evening. After a week, the daily dose may be increased to 50 mg, and then gradually, at the earliest after a week, the daily dose may be increased from 50 mg to a maximum daily dose of 200 mg.

Satisfactory therapeutic effect is usually achieved within 7 days of starting treatment, but regular use of the drug for 2-4 weeks is required to achieve full therapeutic effect.

Children

In obsessive-compulsive disorder

Children between 6 and 12 years of age are given an initial dose of 25 mg once daily in the morning or evening. After a week, the daily dose can be increased to 50 mg.

For children aged 12 to 17 years, the starting dose is 50 mg once daily in the morning or evening. Gradually, at the earliest after one week, the daily dose may be increased to a maximum daily dose of 200 mg. In order to avoid overdose, the lower body weight of children compared to adults should be taken into account, and if the dose is increased beyond 50 mg/day, children should be closely monitored and the drug should be stopped at the first sign of overdose.

There is no need for special dose selection in older patients.

In patients with liver dysfunction, the dose of the drug should be reduced or the intervals between doses should be increased.

In patients with impaired renal function there is no need to specifically adjust the dose.

Interaction

Simultaneous use of Stimuloton and MAO inhibitors (including selective MAO inhibitors with reversible type of action – selegiline and moclobemide) may cause serotonin syndrome, which is manifested by hyperthermia, muscle rigidity, myoclonus, labile autonomic nervous system, changes in mental status (including confusion, increased irritability, severe agitation, which in some cases may progress to delirium and coma).

Hence, sertraline should not be coadministered with MAO inhibitors or for 14 days after their withdrawal. Similarly, no MAOI inhibitors should be prescribed for 14 days after withdrawal of Sertraline.

The combined use of Stimuloton with CNS depressant drugs should only be performed under medical supervision, and alcohol should not be consumed during treatment with Stimuloton.

In concomitant use of Stimuloton and coumarin derivatives, a significant increase in prothrombin time has been observed – in these cases, it is recommended to monitor the prothrombin time at the beginning of treatment with Stimuloton and after its withdrawal.

In concomitant use with Stimulotone, cimetidine significantly reduces the clearance of sertraline.

Long-term use of Stimulotone at a dose of 50 mg/day is accompanied by an increase in desipramine concentrations.

The experiments on study of interaction in vitro showed that beta-hydroxylation of endogenous cortisol by CYP3A4 isoenzyme, and metabolism of carbamazepine and terfenadine do not change with long-term use of Sertraline at a dose of 200 mg/day. Plasma concentrations of tolbutamide, phenytoin and warfarin also do not change with long-term use of Sertraline at the same dose.

The pharmacokinetics of lithium are not altered by concomitant administration of sertraline. However, tremor is observed more frequently, which suggests a possible pharmacodynamic interaction. Co-administration of sertraline with drugs affecting serotonergic transmission (e.g., lithium) requires increased caution.

Sertraline causes minimal induction of liver enzymes. Concomitant administration of sertraline and antipyrine at a dose of 200 mg results in a significant decrease in the half-life of antipyrine, although this occurs in only 5% of observations.

When coadministered with atenolol Stimulotone does not affect its effectiveness.

When administering sertraline at a daily dose of 200 mg together with glibenclamide and digoxin, no drug interaction was found.

Special Instructions

It should be noted that there is insufficient experience with Stimuloton in patients undergoing electroconvulsive therapy. The possible success or risk of such combined treatment has not been studied.

Depressed patients are at risk for suicide attempts. This risk persists until remission develops. Therefore, ongoing medical monitoring of patients should be established from the initiation of treatment until optimal clinical effect is achieved.

Rare cases of withdrawal syndrome, manifested by paresthesias, hypoesthesia, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety or symptoms of psychosis that cannot be distinguished from symptoms of the underlying disease, have been described when Stimulotone is withdrawn.

Asymptomatic increases in hepatic transaminase activity may appear 9 weeks after the start of treatment with Stimuloton. Withdrawal of the drug in this case leads to normalization of enzyme activity.

Particular caution is required when Stimuloton is concomitantly prescribed with drugs that bind to plasma proteins (diazepam, tolbutamide, warfarin).

The use in liver function disorders

With caution should be prescribed in cases of hepatic impairment. If liver function is impaired, the dose of the drug should be reduced or the intervals between doses should be increased.

The use in renal impairment

Precaution should be used in patients with renal impairment. There is no need to specifically adjust the dose in patients with renal impairment.

Impact on ability to drive vehicles and other mechanisms requiring increased concentration

The administration of Sertraline is not accompanied by impairment of psychomotor functions. However, its use simultaneously with other drugs may lead to impairment of attention and coordination of movements. Therefore, during treatment with Stimulotone, it is not recommended to drive vehicles, operate special equipment, or engage in high-risk activities.

Contraindications

With caution: organic brain disease (including mental retardation); manic states; epilepsy; hepatic and/or renal insufficiency; weight loss; children over 6 years of age.

Side effects

CNS disorders: drowsiness, headache, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, gait disturbances, visual disturbances, seizures, dyskinesia, extrapyramidal syndromes.

Digestive system disorders: dry mouth, decreased appetite (rarely – increased) up to anorexia, flatulence, nausea, vomiting, diarrhea, abdominal pain; transient increase of liver transaminases activity is rare.

Social system disorders: disorders of ejaculation, decreased libido, menstrual cycle disorders.

Endocrine system disorders: hyperprolactinemia, galactorrhea, increased sweating, decreased body weight.

Dermatological reactions: skin hyperemia, skin rash, erythema multiforme.

Others: weakness, reversible hyponatremia may occur, which develops more often in elderly patients and also while taking diuretics or a number of other drugs.

Motor disorders have been reported in patients with a history of these or with concomitant use of antipsychotic drugs.

Overdose

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 therapy and constant monitoring of the functions of vital organs is required. Inducing vomiting is not recommended. Injection of activated charcoal may be more effective than gastric lavage. Airway patency should be maintained. Sertraline has a large volume of distribution, so increasing diuresis, performing dialysis, hemoperfusion, or blood transfusion may be ineffective.

It should be noted that even with high doses of Sertraline, there are no life-threatening symptoms. However, administration of Sertraline in high doses simultaneously with other drugs or ethanol may lead to severe poisoning.

Pregnancy use

There are no controlled effects of Stimuloton in pregnant women; therefore, the drug should only be prescribed in pregnancy if the expected benefits to the mother exceed the potential risk to the fetus.

Women of reproductive age who are expected to receive Stimuloton should be advised to use effective contraception.

Sertraline is excreted with breast milk. There are no reliable data on the safety of its use during lactation. Breastfeeding should be discontinued if Stimuloton is to be administered during lactation.

Similarities