Description
Latin name
STIMULOTON
Release form
film-coated tablets.
Packing
28 pcs
Pharmacological action
Pharmacodynamics
Antidepressant. Selective serotonin reuptake inhibitor. It has a weak effect on the reuptake of norepinephrine and dopamine. In therapeutic doses, sertraline also inhibits the uptake of serotonin by human blood platelets.
Does not have a stimulating, sedative or anticholinergic effect. The drug does not interact with m-holinano-, 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 drug dependence.
The antidepressant effect is noted towards the end of the second week of regular administration of the drug, while the maximum effect is achieved only after 6 weeks.
Pharmacokinetics
Absorption
Absorbed from the digestive tract slowly but almost completely. C max is achieved after 4.5-8.4 hours after ingestion. When taking the drug at the same time as eating, its bioavailability increases by 25%, C max is reached faster.
Distribution With a single daily dose of C ss, it is usually achieved after a week. It binds to blood plasma proteins by 98%. V d – 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 is biotransformed during the first passage through the liver, undergoing N-demethylation. Its main metabolite, N-desmethylsertraline, is less active than sertraline.
Excretion of
0.2% sertraline excreted unchanged in the urine, the rest in the form of metabolites with urine and feces in equal amounts. T 1/2 is 22-36 hours and does not depend on the age and gender of patients. T 1/2 of N-desmethylsertraline is 62-104 hours. Sertraline is not excreted by hemodialysis. Pharmacokinetics in special clinical cases of T1 / 2 and AUC of sertraline increase with impaired liver function. Regardless of the severity of renal failure, the pharmacokinetics of sertraline with its constant use does not change.
Indications
Depression of various etiologies (treatment and prevention)
obsessive-compulsive disorder
panic disorder (with or without agoraphobia)
post-traumatic stress disorder.
Contraindications
The simultaneous use of MAO inhibitors and the period of 14 days after their withdrawal
the simultaneous use of tryptophan or fenfluramine
unstable epilepsy
children under 6 years old
pregnancy and lactation (if breastfeeding is different to others).
Precautions: organic brain diseases (including those with mental retardation) manic epilepsy, liver and / or renal failure, weight loss in children over 6 years of age.
Use during pregnancy and lactation
There are no controlled results for the use of Stimuloton in pregnant women, therefore, the drug should be prescribed during pregnancy 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 Stimuloton should be advised to use effective contraceptives.
Sertraline is excreted in breast milk. There is no reliable data on the safety of its use during lactation. If necessary, the appointment of Stimuloton during lactation should be discontinued.
Composition
1 coated tablet contains:
Active substances: sertraline hydrochloride 111.9 mg, which corresponds to a sertraline content of 100 mg.
Excipients: hydroxypropyl cellulose, calcium hydrogen phosphate dihydrate, microcrystalline cellulose, sodium amylopectin glycolate.
Shell Composition: hypromellose 2910, macrogol 6000, titanium dioxide.
Dosage and administration of
For adults
For depression and obsessive-compulsive disorder
The drug is prescribed at a dose of 50 mg 1 time / day in the morning or evening. Gradually, no sooner than a week later, the daily dose can be increased to a maximum daily dose of 200 mg.
In patients with obsessive-compulsive disorder, it may take 8-12 weeks to achieve a good result. The minimum dose providing a therapeutic effect is retained in the future as a supporting one.
For panic and post-traumatic stress disorders
Treatment should be started with a dose of 25 mg 1 time / day in the morning or evening. After a week, the daily dose can be increased to 50 mg, and then gradually, no earlier than a week, the daily dose can be increased from 50 mg to a maximum daily dose of 200 mg.
A satisfactory therapeutic effect is usually achieved after 7 days from the start of treatment, however, to achieve the full therapeutic effect, regular administration of the drug is required for 2-4 weeks.
For children
For obsessive-compulsive disorders
For children aged 6 to 12 years, the drug is prescribed in an initial dose of 25 mg 1 time / day 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 initial dose is 50 mg 1 time / day in the morning or in the evening. Gradually, not earlier than after a week, the daily dose can be increased to a maximum daily dose of 200 mg. In order to avoid overdose, the smaller body weight of children than adults should be taken into account, and with an increase in the dose of more than 50 mg / day, careful monitoring of the children should be established and the drug should be discontinued at the first signs of an overdose.
In elderly patients, there is no need for special dose selection.
In case of impaired liver function, the dose should be reduced or the intervals between doses should be increased.
In patients with impaired renal function, a special dose is not required.
Side effects of the
From the side of the central nervous system: drowsiness, headache, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, impaired gait, impaired vision, convulsions, dyskinesias, extrapyramidal syndromes.
From the digestive system: dry mouth, decreased appetite (rarely, increase) up to anorexia, flatulence, nausea, vomiting, diarrhea, abdominal pain, rarely – transient increase in the activity of hepatic transaminases.
From the reproductive system: ejaculation disorders, decreased libido, menstrual irregularities.
From the endocrine system: hyperprolactinemia, galactorrhea, increased sweating, weight loss.
Dermatological reactions: hyperemia of the skin, skin rash, erythema multiforme.
Other: possible weakness, reversible hyponatremia, which develops more often in elderly patients, as well as when taking diuretics or several other drugs.
Movement disorders were observed in patients with indications of their presence in history or with concomitant use of antipsychotic drugs.
Drug Interaction
With the simultaneous use of Stimulotton with MAO inhibitors (including selective MAO inhibitors with reversible type of action – selegiline and moclobemide), the development of serotonin syndrome, which is expressed in the development of hypertension, (including confusion, heightened irritability, intense arousal, which in some cases can go into a delirious state and to whom).
Therefore, sertraline should not be co-administered with MAO inhibitors or within 14 days of withdrawal. Similarly, after the withdrawal of sertraline for 14 days do not prescribe MAO inhibitors.
Combined use of Stimuloton with CNS depressant drugs should only be performed under the supervision of a physician and alcoholic beverages should not be used during treatment with Stimuloton.
With the simultaneous use of Stimuloton and coumarin derivatives, a significant increase in prothrombin time is observed – in these cases, it is recommended to control prothrombin time at the start of Stimuloton treatment and after its withdrawal.
When used with Stimuloton, cimetidine significantly reduces sertraline clearance.
Long-term use of Stimuloton at a dose of 50 mg / day is accompanied by an increase in the concentration of desipramine.
In vitro interaction studies have shown that the CYP3A4 isoenzyme beta-hydroxylation of endogenous cortisol, as well as the metabolism of carbamazepine and terfenadine, with long-term administration of sertraline at a dose of 200 mg / day, do not change. The plasma concentration of tolbutamide, phenytoin and warfarin does not change with prolonged use of sertraline at the same dose.
The pharmacokinetics of lithium do not change with concomitant administration of sertraline. However, tremor is observed more frequently, suggesting the possibility of pharmacodynamic interaction. Co-administration of sertraline with medicines that affect serotonergic transmission (eg, lithium) requires extreme caution.
Sertraline causes minimal induction of liver enzymes. Simultaneous administration of sertraline and antipyrine at a dose of 200 mg leads to a significant reduction in the elimination half-life of antipyrine, although this occurs in only 5% of observations.
When used with Atenolol, Stimuloton does not affect its effectiveness.
No drug interaction was detected with the administration of sertraline at a daily dose of 200 mg together with glibenclamide and digoxin.
Overdose
Symptoms: serotonin syndrome with nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, sweating, myoclonus and hyperreflexia.
Treatment: There are no specific antidotes. Intensive maintenance therapy and constant monitoring of vital organ functions are required. Causing vomiting is not recommended. The introduction of activated carbon may be more effective than gastric lavage. It is necessary to maintain the airway. Sertraline has a large volume of distribution, and therefore an increase in diuresis, dialysis, hemoperfusion or blood transfusions may not be successful.
It should be noted that even with the administration of sertraline in large doses life-threatening symptoms are not detected. However, administration of sertraline in high doses at the same time as other drugs or ethanol can lead to severe poisoning.
Storage conditions
Store at a temperature of 15 ° to 25 ° C.
Keep out of the reach of children.
Expiration
3 years.
Deystvuyuschee substances
sertraline
pharmacy terms for
tablet dosage form
Formulation
