Expiration date: 02/2026

Release form and composition:

The tablets covered with a cover white or nearly so white color, round, biconcave.

1 tablet contains sertraline (hydrochloride) 50 mg

Other ingredients: calcium phosphate, sodium carboxymethyl starch, microcrystalline cellulose, aerosil, polyvinylpyrrolidone (povidone) and calcium stearate, hydroxypropylmethylcellulose, polyethylene glycol 4000, titanium dioxide, talc.

Pharmachologic effect:

Antidepressant. Selective serotonin reuptake inhibitor (5-HT) in neurons. On the reuptake of norepinephrine and dopamine affects slightly. At therapeutic doses, sertraline blocks the uptake of serotonin human platelets.

It has no stimulating, sedative and anticholinergic actions. The drug has no affinity for serotonin, dopamine, histamine, benzodiazepine, GABA-, m nicotinic acetylcholine receptor and adrenoceptor.

Antidepressant effect was seen at the end of the second week of the regular administration of the drug, the maximum effect is achieved after 6 weeks.

Unlike tricyclic antidepressants when assigning Thorin no increase in body weight.

The drug does not cause mental or physical drug dependence.

Pharmacokinetics:

Suction

Once inside slowly absorbed from the gastrointestinal tract, Cmax achieved within 4.5-8.4 hours in plasma. The bioavailability when taken with food increased by 25%, while Cmax achievement decreases.

Distribution

Css installed within a week with a daily intake of 1 times / day. sertraline Plasma protein binding is 98%.

Vd is more than 20 l / kg. Sertraline is excreted in breast milk is not known whether sertraline penetrates through the placental barrier.

Metabolism and excretion

Sertraline undergoes intensive biotransformation on first passage through the liver by N-demethylation. The main metabolite - N-desmetilsertralin less active than the parent compound. The metabolites are excreted with urine and faeces in equal amounts. About 0.2% of sertraline excreted by the kidneys unchanged. T1 / 2 hours 22-36 of the drug is not dependent on the patient age or gender. For N-desmetilsertralina T1 / 2 - 62-104 hours.

Pharmacokinetics in special clinical situations

T1 / 2 and AUC in plasma increases with abnormal liver function.

Parameters pharmacokinetics of sertraline in patients with a mild to moderate dysfunction (creatinine clearance 20-50 ml / min) or with severe renal impairment (KKt20ml / min) do not change both at once, and with regular use of the drug. Thus, in patients with renal insufficiency, there is no need for a special selection dose.

Sertraline is not displayed during dialysis.

Testimony:

• Depression different etiology (treatment and prevention)
  
• Obsessive-compulsive disorder
  
• Panic disorder (with or without agoraphobia)
  
• Post-traumatic stress disorder.
  

Dosage and administration:

For adults with depression and obsessive-compulsive disorders the initial dose Torina is 50 mg 1 time / day in the morning or in the evening. If necessary, the dose can be gradually (1 per week) increased to a maximum daily dose of 200 mg.

When panic disorders and post-traumatic stress disorders, the initial dose is 25 mg 1 time / day, morning or evening. After a week, you can increase the dose to 50 mg 1 time / day, and then gradually (1 per week) increased to a maximum daily dose of 200 mg.

Satisfactory therapeutic results achieved typically after 7 days of starting treatment. However, to achieve full therapeutic effect requires the regular intake of the drug for 2-4 weeks. Patients with obsessive-compulsive disorder to achieve a therapeutic effect may require 8-12 weeks. The minimum dose providing therapeutic effect is maintained in the future as a support.

For children aged 6 to 12 years with obsessive-compulsive disorders the initial dose Torina is 25 mg 1 time / day, morning or evening. After a week, you can increase the dose to 50 mg 1 time / day.

For children aged 12 to 17 years starting dose is 50 mg 1 time / day in the morning or in the evening. If necessary, the dose can be gradually (1 per week) increased to a maximum daily dose of 200 mg. With increasing doses of over 50 mg / day is necessary to ensure close supervision of children and the first signs of an overdose of the drug to cancel.

In the elderly there is no need a special dose adjustment.

When violations of liver function The drug should be used with caution. In severe hepatic dysfunction dose should be reduced or increased intervals between doses.

Patients with impaired renal function, a special correction dosing regime is not required.

Side effects:

From the central and peripheral nervous system: drowsiness, headache, dizziness, tremors, insomnia, anxiety, agitation, hypomania, mania, gait disturbance, weakness, visual disturbances, extrapyramidal disorder, dyskinesia, seizures.

From the digestive system: dry mouth, decreased appetite (rarely - increased) up to anorexia, flatulence, nausea, vomiting, diarrhea, abdominal pain, rarely (0.8%), with prolonged use - asymptomatic increase of transaminases in serum (normalizes to remove the drug).

On the part of the endocrine and reproductive system: ejaculation disorder, decreased libido, menstrual disorders, hyperprolactinemia, galactorrhea.

Dermatological reactions: skin rash, rarely - erythema multiforme.

Other: increased sweating, weight loss, redness of the skin.

From the laboratory parameters: - reversible hyponatremia (usually in the elderly, as well as when taking diuretics or some other drugs) related to the syndrome of inappropriate secretion of ADH.

Contraindications:

• Simultaneous reception of MAO inhibitors and the period up to 14 days after their withdrawal
  
• The simultaneous use of tryptophan or fenfluramine
  
• Unstable epilepsy
  
• Children up to age 6 years
  
• pregnancy
  
• Lactation (breastfeeding)
  
• Hypersensitivity to sertraline and other ingredients.
  

Pregnancy and lactation:

Adequate and well-controlled clinical safety trials of sertraline during pregnancy was conducted. Appointment of the drug is only possible if the intended benefits to the mother outweighs the potential risk to the fetus.

Women of childbearing age during treatment should be advised to use effective contraception.

If necessary, the appointment during lactation should stop breastfeeding due to lack of reliable data on the safety of sertraline in this period.

Special instructions:

Precautions should use the drug in patients with organic brain diseases (including in mental retardation), and manic states, epilepsy, liver and / or kidney failure, reduction of body weight.

Sertraline not administered jointly with inhibitors and for 14 days after cessation of treatment MAO inhibitors after discontinuation of sertraline for 14 days did not designate MAO inhibitors.

In appointing the drug should take into account the lack of sufficient experience in the use of sertraline in patients receiving electroconvulsive therapy. A possible outcome or risk of such combined treatment has not been studied.

Upon termination of use of the drug may (rarely) the development of the syndrome. May appear paresthesia, gipostezii, depressive symptoms, hallucinations, aggressive reaction, agitation, anxiety or psychotic symptoms. These manifestations are difficult to distinguish from the main symptoms of the disease, and may occur in the application and other antidepressants.

C 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 should be to establish a permanent medical supervision of the patient.

Combined appointment of Thorin and drugs which depress the central nervous system requires close attention, and the simultaneous application of ethanol and drugs etanolosoderzhaschimi contraindicated.

Use in Pediatrics

Be wary of the drug in children under the age of 6 years.

Effects on ability to drive vehicles and management mechanisms

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, while taking Thorin is not recommended to perform work that requires attention and speed of psychomotor reactions.

Overdose:

Symptoms of serotonin syndrome may occur with nausea, vomiting, somnolence, tachycardia, agitation, dizziness, agitation, diarrhea, sweating, myoclonus, hyperreflexia. Severe symptoms are observed even when using the drug in high doses. However, severe poisoning can occur when taken with other drugs or ethanol.

Treatment: There are no specific antidotes. If necessary - intensive supportive care and monitoring of the condition of the vital functions of the body. Injection of activated carbon can be more effective than gastric lavage, artificial cause vomiting is not recommended. It is necessary to maintain airway patency. Forced diuresis, dialysis, hemoperfusion or blood transfusion may be ineffective (because of the large volume of distribution of sertraline).

Drug Interactions:

With simultaneous use of Thorin and MAO inhibitors (including the selective MAO inhibitors with a reversible type of action - selegiline and moclobemide) may develop serotonin syndrome: hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular system), change mental status, including increased irritability, marked agitation, confusion, which in some cases can go into delirious state or coma (this combination is contraindicated).

The joint appointment with Thorin anticoagulants has been a significant increase in prothrombin time (prothrombin time monitoring is required at the beginning of the use of sertraline and after its cancellation).

Pharmacokinetic interactions

In a joint application Sertraline can interact with other drugs that bind to plasma proteins (diazepam, tolbutamide and warfarin).

The simultaneous use of the drug cimetidine significantly reduces the clearance of sertraline.

Long-term use of sertraline at a dose of 50 mg / day with desipramine (the drug is metabolized with the participation of isoenzyme CYP2D6) accompanied by an increase desipramine plasma concentration.

In experiments in vitr established that carried CYP3A3 / 4 betagidroksilirovanie endogenous cortisol, as well as the metabolism of carbamazepine and long-term administration of terfenadine with sertraline at a dose of 200 mg / day does not change.

plasma concentrations of tolbutamide, phenytoin and warfarin in long-term appointment of sertraline at a dose of 200 mg / day does not change, therefore, it can be concluded that sertraline does not inhibit CYP2C9.

Sertraline has no effect on the concentration of diazepam in blood serum, which indicates the absence of inhibition of CYP2C19.

According to studies in vitr sertraline has virtually no effect or minimally inhibits CYP1A2.

The pharmacokinetics of lithium is not changed by concomitant administration of sertraline, however tremor occurs more often when they are used together, which suggests the possibility of a pharmacodynamic interaction (such a combination requires caution).

In clinical studies have shown that sertraline causes minimal induction of liver enzymes. Co-administration of sertraline at a dose of 200 mg and antipyrine leads to a significant decrease in T1 / 2 of antipyrine (this change is detected only 5% of cases).

If co-administration of sertraline has no effect on the beta-adrenoceptor blocking action of atenolol.

With the introduction of sertraline in a daily dose of 200 mg drug interactions with glibenclamide and digoxin have been identified.

Conditions and terms:

List B. The drug should be stored in a dry, dark, place inaccessible to children at temperature not exceeding 25 ° C. Shelf life - 2 years.