Instruction for use: Asentra

Dosage form: feel-coated tablets

Active substance: Sertaline*

ATX

N06AB06 Sertalin

Pharmacological groups:

Antidepressant

The nosological classification (ICD-10)

F32 Depressive episode: Adynamic subdepression; Astheno-adynamic subdepressive states; Asthenoadressive disorder; Astheno-depressive disorder; Asthenodepressive state; Astheno-depressive state; Major Depressive Disorder; Vyaloapatichesky depression with retardation; Double Depression; Depressive pseudodement; Depressive illness; Depressive mood disorder; Depressive disorder; Depressive mood disorder; Depressive state; Depressive disorders; Depressive syndrome; Depressive syndrome larviated; Depressive syndrome in psychoses; Depressed masks; Depression; Depression Depletion; Depression with the phenomena of inhibition within the framework of cyclothymia; Depression is smiling; Involutional depression; Involutionary melancholy; Involutional depression; Manic-depressive disorder; Masked Depression; Melancholic Attack; Neurotic depression; Neurotic depression; Shallow Depression; Organic depression; Organic depressive syndrome; Simple depression; Simple melancholic syndrome; Psychogenic depression; Reactive depression; Reactive depression with moderate psychopathological symptoms; Reactive depressive states; Reactive depression; Recurrent depression; Seasonal depressive syndrome; Severostatic depression; Senile Depression; Symptomatic Depression; Somatogenic depression; Cyclotymic depression; Exogenous depression; Endogenous depression; Endogenous Depressive Conditions; Endogenous Depression; Endogenous depressive syndrome

F41.0 Panic disorder [episodic paroxysmal anxiety]: Panic state; Panic attack; Panic; Panic disorders

F41.2 Mixed anxiety and depressive disorder: Depression with anxiety-depressive components; Mixed anxiety-depressive conditions; Anxiety Depression; Anxious and depressing mood; Anxiety-depressive state; Anxious-depressive conditions; Anxiety-depressive syndrome; Anxious-Neurotic Conditions

F42 Obsessive-compulsive disorder: Obsessive-compulsive syndrome; Obsessive compulsive states; Obsessive-compulsive syndrome; The Obsession Syndrome; The obsession neurosis; Obsessive-compulsive neurosis; Obsessions

F43.1 Post-traumatic stress disorder: Combat fatigue; Catastrophe Syndrome; The survivor's syndrome; Traumatic isolation; Traumatic neurosis; Traumatic syndrome; Post-Traumatic Stress Disorder

Composition and release form

Tablets, coated with a coating.

sertraline hydrochloride 55.95 mg

(corresponding to 50 mg of sertraline); 111.9 mg

(corresponding to 100 mg of sertraline)

auxiliary substances: calcium dihydrogen phosphate; ICC; magnesium stearate; sodium carboxymethyl starch; hydroxypropyl cellulose; talc.

composition of the shell: Opadry 03H28758 (ready-to-use mixture of hypromellose, titanium dioxide, talc, propylene glycol)

in packs of contour cells for 7 pcs .; in a pack of cardboard 4 packs.

Description of dosage form

Round tablets covered with a film shell of white color, with a bevelled edge and with a notch on one side.

Pharmachologic effect

Mode of action - antidepressant.

Pharmacodynamics

Mechanism of action. Sertraline is a specific inhibitor of serotonin reuptake (5-HT). It has very little effect on the re-uptake of norepinephrine and dopamine. In therapeutic doses, sertraline blocks the seizure of serotonin in human platelets. It has no stimulating, sedative or anticholinergic action. Sertraline does not have an affinity for muscarinic (cholinergic), serotonergic, dopaminergic, adrenergic, histaminergic, GABA or benzodiazepine receptors.

The antidepressant effect is noted towards the end of the second week of regular sertraline intake, whereas the maximum effect is achieved only after 6 weeks. Unlike tricyclic antidepressants, sertraline does not increase body weight. Sertraline does not cause mental or physical drug dependence.

Pharmacokinetics

Absorbed in the gastrointestinal tract to a large extent, but slowly. Cmax in the blood plasma is reached after 4,5-8,4 hours after taking the drug inside. The equilibrium concentration of sertraline in the blood plasma is reached within a week with a single daily intake. Bioavailability when taken with food rises by 25%, while the time to reach maximum concentration is shortened.

Distribution. The total binding of sertraline to proteins is 98%. The volume of distribution is> 20 l / kg.

Metabolism and excretion. Sertraline undergoes intensive metabolism upon first passage through the liver, undergoing N-demethylation. Its main metabolite, N-desmethylsertralin, is less active than the parent compound.

Metabolites are excreted in urine and feces in equivalent amounts. About 0.2% of sertraline is excreted by the kidneys unchanged. T1 / 2 of the drug is 22-36 hours and does not depend on age or gender. For N-desmethylsertraline, this value is 62-104 hours.

T1 / 2 sertraline and the area under the plasma concentration-time curve (AUC) increase with liver function impairment. Regardless of the severity of renal failure, the pharmacokinetics of sertraline does not change with its constant application. Sertraline penetrates into breast milk. Data on its ability to pass through the hematoplacental barrier is not present.

Sertraline is not dialyzed.

Indications of the preparation Asentra

treatment and prevention of depressions of various etiologies, incl. accompanied by a sense of anxiety;

obsessive-compulsive disorder (OCD);

panic disorder;

post-traumatic stress disorder (PTSD).

Contraindications

hypersensitivity to the active substance or other ingredients included in the preparation;

joint use of sertraline and MAO inhibitors (monoamine oxidase). When replacing one drug with another, one should refrain from taking antidepressants within 14 days;

joint use of sertraline with tryptophan or fenfluramine;

unstable epilepsy;

pregnancy;

lactation period;

children's age till 6 years.

Carefully:

neurological disorders (including delayed mental development);

manic states;

epilepsy;

hepatic and / or renal insufficiency;

decreased body weight;

children age over 6 years.

Application in pregnancy and lactation

There are no controlled results of the use of sertraline in pregnant women, so it is necessary to prescribe them only if the expected benefit for the mother exceeds the potential risk for the fetus.

Sertraline is found in breast milk, and therefore treatment with this drug during breastfeeding is not recommended. In this case there are no reliable data on the safety of its application. If treatment is still necessary, then breast-feeding should be stopped.

Side effects

On the part of the digestive organs: dry mouth, decreased appetite (rarely - increase), up to anorexia, dyspeptic disorders (flatulence, nausea, vomiting, diarrhea or unstable stool, constipation), stomach cramps, abdominal pain, pancreatitis, hepatitis, jaundice or liver failure.

From the nervous system: drowsiness, headache, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, akathisia, paresthesia, symptoms of depression, hallucinations, aggressiveness, agitation, anxiety, psychosis, gait disorders, extrapyramidal disorders, dyskinesias, tremor , convulsions. Motor disorders were more often observed in patients with indications of their presence in an anamnesis or with the concomitant use of antipsychotics.

On the part of the genitourinary system: delay in ejaculation, decreased libido, erectile dysfunction, anorgasmia, menstrual irregularities, gynecomastia, priapism, hyperprolactinaemia, galactorrhea.

On the part of the respiratory system: choking or feeling chest compressions.

From the cardiovascular system: palpitation, chest pain, arterial hypertension, arterial hypotension, swelling, fainting and tachycardia (very rarely).

From the sense organs: visual impairment (including blurred vision).

Allergic reactions: redness of the skin, hives, swelling of the eyelids, face or lips, skin rash, generalized itching, multiforme exudative erythema.

Laboratory data: reversible increase in transaminase activity, thrombocytopenia, leukopenia, transient hyponatremia (syndrome of inadequate secretion of antidiouric hormone, more often in elderly patients, and also with diuretics or a number of other drugs).

Other: sporadic bleeding (including nasal), hypothyroidism, increased sweating, weight loss, weakness, yawning, flushing of blood to the face. With the cessation of sertraline treatment, a "cancellation" syndrome may occur.

Interaction

MAO inhibitors. There are serious complications with the simultaneous use of sertraline and MAO inhibitors (including selective MAO inhibitors with a reversible type of action - selegiline and moclobemide). Perhaps the development of serotonin syndrome. Similar complications, sometimes fatal, occur with the appointment of MAO inhibitors against the background of treatment with antidepressants that inhibit neuronal capture of monoamines or immediately after their withdrawal.

With the simultaneous use of selective inhibitors of reverse neuronal seizure of serotonin and MAO inhibitors, hyperthermia, rigidity, convulsions, myoclonus, lability in the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular system), changes in mental status, including increased irritability, marked agitation, confusion consciousness, which in some cases can go into a delirious state or to whom.

Drugs that depress the central nervous system and ethanol. Combined use of sertraline and substances depressing the central nervous system requires close attention, it is also forbidden to drink alcohol during treatment with sertraline.

Derivatives of coumarin. When they are co-administered with sertraline, there is a significant increase in PV. In these cases, it is recommended to monitor the PV at the beginning of treatment with sertraline and after its withdrawal.

Pharmacokinetic interaction

Sertraline binds to blood plasma proteins. Therefore, it is necessary to consider the possibility of its interaction with other drugs that bind to proteins (for example, diazepam, tolbutamide and warfarin).

Cimetidine. Simultaneous use significantly reduces the clearance of sertraline.

LS metabolized by isoenzyme 2D6 cytochrome P450. Long-term treatment with sertraline at a dose of 50 mg / day is accompanied by an increase in the concentration of desipramine.

LS, metabolized by other enzymatic systems of cytochrome P450. Experiments on in vitro interaction showed that the isoenzyme CYP3A3 / 4 beta-hydroxylation of endogenous cortisol, as well as the metabolism of carbamazepine and terfenadine, do not change with the long-term administration of sertraline at a dose of 200 mg / day. The concentration in the blood plasma of tolbutamide, phenytoin and warfarin in the long-term administration of sertraline in the same dose also does not change. Thus, it can be concluded that sertraline does not inhibit the isoenzyme CYP2C9.

Sertraline does not affect the concentration of diazepam in the serum, indicating that there is no inhibition of isoenzyme CYP 2C19. According to in vitro studies, sertraline has virtually no effect or minimally inhibits the isoenzyme CYP 1A2.

Lithium. The pharmacokinetics of lithium does not change with the concomitant administration of sertraline. However, when combined, tremor is more common. As well as the appointment of other selective inhibitors of reverse neuronal seizure of serotonin, the joint use of sertraline with drugs that affect serotonergic transmission (eg, lithium) requires increased caution.

Drugs affecting serotonergic transmission. When replacing one inhibitor of neuronal seizure of serotonin with another, there is no need for a period of "laundering". However, care must be taken when changing the course of treatment. Tryptophan or fenfluramine should be avoided together with sertraline.

Induction of microsomal enzymes in the liver. Sertraline causes minimal induction of liver enzymes. Simultaneous administration of sertraline and antipyrine at a dose of 200 mg leads to a significant decrease in T1 / 2 antipyrine, (differs only 5% of observations).

Atenolol. With the co-administration of sertraline does not change its beta-adrenergic blocking effect.

Glibenclamide and digoxin. With the introduction of sertraline in a daily dose of 200 mg of drug interaction with these drugs is not revealed.

Dosing and Administration

Inside.

With depression and OCD in adults, the average initial dose is 50 mg once a day, in the morning or in the evening. Daily dose can be gradually, not earlier than a week, increase from 50 mg to a maximum daily dose of 200 mg.

In panic and post-traumatic stress disorders, the initial dose of Asentra is 25 mg once a day, in the morning or in the evening. In a week, you can increase the dose to 50 mg once a day, and then gradually, not earlier than a week, raise to a maximum daily dose of 200 mg.

A satisfactory therapeutic result is achieved usually after 7 days from the start of treatment. However, in order to achieve a complete therapeutic effect, the drug should be taken regularly for 2-4 weeks. In patients with OCD, it may take 8-12 weeks to achieve a good result. The minimum dose providing the therapeutic effect is preserved as a supporting one in the future.

The initial dose of Asentra for children aged 6 to 12 years is 25 mg sertraline once a day, in the morning or in the evening. After a week, you can increase the dose to 50 mg once a day. For children aged 12 to 17 years, the initial dose is 50 mg once a day in the morning or evening. If necessary, the daily dose can be gradually, not earlier than a week, increased from 50 mg to a maximum daily dose of 200 mg. To avoid overdose, less weight in children should be taken into account compared with adults, and with a dose increase of more than 50 mg / day, careful monitoring of this category of patients is necessary and at the first signs of an overdose, the drug should be discontinued.

In elderly patients, there is no need for a special dose selection.

For violations of liver function, the drug should be administered with caution. In case of severe violations of the liver function, the dose of the drug should be reduced or the intervals between doses should be increased.

In patients with impaired renal function, no special correction of the dosing regimen is required.

Overdose

Symptoms: serotonin syndrome - nausea, vomiting, drowsiness, ECG changes, mydriasis, tachycardia, agitation, dizziness, anxiety, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia.

Treatment: symptomatic maintenance of normal patency of the respiratory tract (oxygenation and ventilation of the lungs) and monitoring of the heart rhythm and vital organs and systems. It is not recommended to induce vomiting. The use of activated charcoal and sorbitol can be more effective than gastric lavage. There are no specific antidotes. Sertraline has a large volume of distribution, in connection with this, increased diuresis, dialysis, hemoperfusion or blood transfusion may be unsuccessful.

Special instructions

Sertraline should not be administered together with MAO inhibitors, and also within 14 days after discontinuation of treatment with MAO inhibitors. Similarly, after the withdrawal of sertraline within 14 days, MAO inhibitors are not prescribed.

It should be noted that in patients undergoing electroconvulsive therapy, there is no sufficient experience with sertraline. The possible success or risk of such a combined treatment has not been studied. Patients suffering from depression are at risk for suicide attempts. This danger persists until the development of remission. Therefore, from the beginning of treatment and until the optimal clinical effect is achieved, patients should be provided with permanent medical supervision.

Women of childbearing age during treatment should use adequate methods of contraception.

Impact on the ability to drive vehicles and manage mechanisms. The appointment of sertraline, as a rule, is not accompanied by a violation of psychomotor functions. However, its use simultaneously with other drugs can lead to disruption of attention and coordination of movements. Therefore, during the treatment with sertraline, it is not recommended to drive vehicles, special equipment or engage in activities involving an increased risk.

Storage conditions for Asentra

At a temperature of no higher than 25 ° C, in the original packaging.

Keep out of the reach of children.

Shelf life of Asentra

5 years.

Do not use after the expiry date printed on the package.