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Stimuloton (Sertralinum, Sertraline) - Antidepressant. Selective serotonin reuptake inhibitor. It has little effect on the reuptake of noradrenaline and dopamine. At therapeutic doses, sertraline inhibits the uptake of serotonin and human blood platelets.
It has no stimulating, sedative or anticholinergic action. The drug does not interact with the m-choline, serotonin, dopamine, histamine, adrenergic, GABA- and benzodiazepine receptors.
When 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 administration of the drug, while the maximum effect is achieved only after 6 weeks.
Precautions: organic brain disease (including with mental retardation); mania; epilepsy; liver and / or kidney failure; weight loss; Children over the age of 6 years.
It should be noted that in patients undergoing electroconvulsive therapy, sufficient experience with Stimulotona absent. The possible success or the risk of such combined treatment has not been studied.
Patients with depression are at risk for suicide attempts. This risk persists until the development of remission. Therefore, from the beginning of the treatment and to achieve optimal clinical response for patients should establish a permanent medical supervision.
If you cancel Stimulotona described rare cases of the syndrome, which manifests itself paresthesias, hypoesthesia, depressive symptoms, hallucinations, aggressive reactions, agitation, anxiety or psychotic symptoms that are indistinguishable from symptoms of the underlying disease.
Asymptomatic elevation of liver transaminases may occur after 9 weeks of treatment Stimulotonom. Removal of the drug, in this case leads to a normalization of enzyme activity.
It requires special care while appointing Stimulotona with drugs that bind to plasma proteins (diazepam, tolbutamide, warfarin).
Application for violations of liver function
Precautions should be prescribed with hepatic insufficiency. If abnormal liver function dose should be reduced or increased intervals between doses.
Application for violations of renal function
Precautions should be prescribed in patients with renal insufficiency. In patients with impaired renal function specially select a dose is not required.
Effects on ability to drive vehicles and other machines that require high concentration of attention
Appointment of sertraline is not accompanied by violation of psychomotor functions. However, its use in conjunction with other drugs may impair attention and motor coordination. Therefore, during treatment Stimulotonom drive vehicles, special equipment or practice associated with an increased risk of the activity is not recommended.
When depression and obsessive-compulsive disorders
The drug is administered at a dose of 50 mg 1 time / day in the morning or in the evening. Gradually, not earlier than one week daily dose can be increased to a maximum daily dose of 200 mg.
Patients with obsessive-compulsive disorder to achieve a good result may require 8-12 weeks. The minimum dose providing therapeutic effect is maintained in the future as a support.
When panic disorders and post-traumatic stress disorder
It is necessary to begin treatment with a dose of 25 mg 1 time / day in the morning or in the evening. A week later, the daily dose can be increased to 50 mg, and then gradually, not earlier than one week, the daily dose can be increased to a maximum of 50 mg daily dose of 200 mg.
Satisfactory therapeutic effect is usually achieved after 7 days of starting treatment, but to achieve the full therapeutic effect requires the regular intake of the drug for 2-4 weeks.
With obsessive-compulsive disorders
Children aged 6 to 12 years Reparata administered in an initial dose of 25 mg 1 time / day in the morning or in the evening. A week later, the daily dose can be increased to 50 mg.
For children aged 12 to 17 years starting dose is 50 mg 1 time / day in the morning or in the evening. Gradually, not earlier than one week, the daily dose can be increased to a maximum daily dose of 200 mg. To avoid overdose should take into account a lower weight children compared with adults, and by increasing the dose of 50 mg / day must be installed to closely monitor the children and stop the drug at the first sign of overdose.
In elderly patients there is no need for a special dose selection.
If abnormal liver function dose should be reduced or increased intervals between doses.
In patients with impaired renal function specially select a dose is not required.
CNS: drowsiness, headache, dizziness, tremors, insomnia, anxiety, agitation, hypomania, mania, gait disturbance, blurred vision, convulsions, dyskinesia, extrapyramidal syndromes.
From the digestive system: dry mouth, decreased appetite (rarely - increased) up to anorexia, flatulence, nausea, vomiting, diarrhea, abdominal pain; rarely - transient increase in liver transaminases.
From the reproductive system: ejaculation disorder, decreased libido, menstrual disorders.
From endocrine system: hyperprolactinemia, galactorrhea, increased sweating, weight loss.
Dermatological reactions: flushing of the skin, skin rash, erythema multiforme.
Other: possible weakness, reversible hyponatremia that develops more frequently in elderly patients, as well as when taking diuretics or several other drugs.
Motor disorders observed in patients with indications of their presence or history of concomitant use of antipsychotic drugs.
In an application Stimulotona with MAO inhibitors (including the selective MAO inhibitors with a reversible type of action - selegiline and moclobemide) may develop serotonin syndrome, which is expressed in the development of hyperthermia, muscle rigidity, myoclonus, lability of the autonomic nervous system, changes in mental status (including confusion, increased irritability, expressed excitement, which in some cases can go into delirious state and to whom).
Thus sertraline should not be administered together with inhibitors and for 14 days after their withdrawal. Similarly, after the abolition of sertraline for 14 days did not prescribe MAOIs.
Combined use Stimulotona with drugs depressing the central nervous system, should be performed only under medical supervision, and alcohol use is prohibited during treatment Stimulotonom.
In an application Stimulotona and coumarin derivatives showed a significant increase in prothrombin time - in these cases it is recommended to monitor the prothrombin time at the beginning of treatment Stimulotonom and after its cancellation.
In an application with Stimulotonom cimetidine significantly reduces the clearance of sertraline.
Prolonged use Stimulotona a dose of 50 mg / day accompanied by an increase desipramine concentrations.
Experiments on the interaction in vitro showed that the CYP3A4 isoenzyme carried beta-hydroxylation of endogenous cortisol metabolism of carbamazepine and terfenadine and long-term use of sertraline at a dose of 200 mg / day does not change. The concentration in the blood plasma tolbutamide, warfarin and phenytoin term use of sertraline in the same dose also varies.
The pharmacokinetics of lithium is not changed by concomitant administration of sertraline. However, the tremor occurs more frequently, which suggests the possibility of a pharmacodynamic interaction. The combined use of sertraline with drugs that affect the serotonergic transmission (eg, lithium), requires increased caution.
Sertraline causes minimal induction of liver enzymes. Co-administration of sertraline and antipyrine at a dose of 200 mg leads to a significant reduction in the half-life of antipyrine, although there is only 5% of cases.
In a joint application with atenolol Stimuloton does not affect its effectiveness.
When administered sertraline not detected in a daily dose of 200 mg of glibenclamide and with the co-drug interaction with digoxin.
Symptoms: serotonin syndrome with nausea, vomiting, somnolence, tachycardia, agitation, dizziness, agitation, diarrhea, sweating, myoclonus and hyperreflexia.
Treatment: There are no specific antidotes. It requires intensive supportive care and constant monitoring of the functions of vital organs. Induce vomiting is not recommended. Introduction of the activated carbon can be more effective than gastric lavage. It is necessary to maintain airway patency. At the large volume of distribution of sertraline, in this regard, increased diuresis, dialysis, hemoperfusion or blood transfusion may be inconclusive.
It should be noted that even when assigning high doses of sertraline in life-threatening symptoms are not detected. However, administration of high doses of sertraline in conjunction with other drugs or ethanol may lead to severe poisoning.
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