Asentra, 50 mg 28 pcs.

An antidepressant. Specific inhibitor of serotonin reuptake (5-NT) in neurons. Effects on norepinephrine and dopamine metabolism are insignificant.

In therapeutic doses, sertraline blocks serotonin uptake in human platelets. The drug has no stimulant, sedative or anticholinergic effect.

It has no affinity for serotonin, dopamine, histamine, benzodiazepine, GABA, choline and adrenoreceptors.

The antidepressant effect is noted by the end of the second week of regular Asentra administration, while the maximum effect is not reached until 6 weeks.

In contrast to tricyclic antidepressants, there is no increase in body weight when prescribing Asentra; in some cases a decrease in body weight has been noted.

The drug does not cause mental or physical drug dependence.

Indications

Active ingredient

Composition

1 tablet contains:

Active ingredients:

Sertraline hydrochloride 55.95 mg, corresponding to a sertraline content of 50 mg.

Auxiliary substances:

magnesium stearate,

hydroxypropyl cellulose,

sodium starch glycolate,

calcium dihydrophosphate,

microcrystalline cellulose,

talc.

Coating composition:

Opadry 03H28758 (hypromellose, titanium dioxide, talc, propylene glycol).

How to take, the dosage

In depression and OCD in adults: the average starting dose is 50 mg once daily, morning or evening. The daily dose can be gradually increased from 50 mg to a maximum daily dose of 200 mg, at the earliest after one week.

In panic disorder and PTSD: The initial dose of Asentra is 25 mg once daily, morning or evening. After a week, the dose may be increased to 50 mg once daily, and then gradually, at the earliest after a week, increased to a maximum daily dose of 200 mg.

For children aged 6 to 12 years: the starting dose of Asentra is 25 mg of sertraline once daily, morning or evening. After a week, the dose may be increased to 50 mg once daily. For children aged 12 to 17 years: the initial dose is 50 mg once daily in the morning or evening. If necessary, the daily dose may be gradually increased from 50 mg to a maximum daily dose of 200 mg, at the earliest after one week. To avoid overdose, the lower body weight in children compared to adults should be taken into account, and if the dose is increased above 50 mg/day, this category of patients should be closely monitored: at the first sign of overdose the drug should be discontinued.

Satisfactory therapeutic results are usually achieved after 7 days of treatment. However, regular use of the drug for 2-4 weeks is required to achieve full therapeutic effect. In patients with OCD, it may take 8-12 weeks to achieve a good result. The minimum dose that provides a therapeutic effect is maintained thereafter as maintenance.

In elderly patients: no special dose adjustment is necessary.

In patients with hepatic impairment: The drug should be prescribed with caution. In severe hepatic impairment, the dose of the drug should be reduced or the intervals between doses should be increased.

In patients with impaired renal function: No special dosing adjustment is necessary.

Interaction

The simultaneous use of sertraline and MAO inhibitors (including selectively acting MAO inhibitors with reversible type of action – selegiline and moclobemide) may result in serotonin syndrome: hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system (rapid fluctuations of respiratory and cardiovascular system parameters), changes in mental status, including increased irritability, pronounced agitation, confusion of consciousness, which in some cases may progress to delirium or coma (this combination is contraindicated). Similar complications (sometimes fatal) occur when prescribing MAO inhibitors during treatment with antidepressants that inhibit monoamine neuronal uptake or immediately after their withdrawal.

In healthy volunteers, administration of Sertraline at a dose of 200 mg/day has no effect on the effects of ethanol, carbamazepine, or haloperidol, or on mental performance and psychomotor activity (however, the combined administration of Sertraline and CNS depressant drugs requires close attention, and concomitant use with ethanol and ethanol-containing medications is contraindicated).

In co-administration of indirect anticoagulants (coumarin derivatives) with sertraline a significant increase in prothrombin time has been noted (prothrombin time control is required at the beginning of use of sertraline and after its withdrawal).

Pharmacokinetic interaction

When used concomitantly, sertraline may interact with other drugs that bind to plasma proteins (diazepam, tolbutamide and warfarin).

The concomitant use of the drug with cimetidine significantly reduces the clearance of sertraline.

The long-term use of sertraline at a dose of 50 mg/day with desipramine (a drug metabolized by CYP2D6 isoenzyme) is associated with increased plasma concentrations of desipramine.

In in vitro experiments it was found that betahydroxylation of endogenous cortisol, and metabolism of carbamazepine and terfenadine do not change with long-term administration of Sertraline at a dose of 200 mg/day.

The plasma concentrations of tolbutamide, phenytoin and warfarin do not change with long-term administration of Sertraline at a dose of 200 mg/day, therefore it can be concluded that Sertraline does not inhibit CYP2C9 isoenzyme.

Sertraline has no effect on the serum concentration of diazepam, indicating no inhibition of the CYP2C19 isoenzyme.

In in vitro studies, Sertraline has little or no effect on the CYP1A2 isoenzyme.

The pharmacokinetics of lithium are not statistically significantly altered by concomitant administration of sertraline; however, tremor is observed more frequently, suggesting a possible pharmacodynamic interaction (this combination requires caution). Caution should also be exercised when prescribing sertraline with other drugs affecting serotonergic transmission.

There is no need for a “washout period” when replacing one neuronal takeover inhibitor with another. However, caution is required when changing the course of treatment. Co-prescribing tryptophan or fenfluramine with sertraline should be avoided.

In clinical studies, sertraline has been shown to cause minimal induction of liver enzymes. Concomitant administration of sertraline at a dose of 200 mg and antipyrine leads to a significant decrease in T1/2 of antipyrine (this change is found in only 5% of observations).

When administered concomitantly, sertraline has no effect on the beta-adreno-blocking effect of atenolol.

There are no drug interactions with glibenclamide and digoxin when sertraline is administered at a daily dose of 200 mg.

Special Instructions

According to clinical studies, sertraline is effective and safe in the treatment of depression in patients with myocardial infarction and unstable angina pectoris. Placebo-controlled studies have shown the efficacy and safety of sertraline in diabetic patients.

Sertraline is not coadministered with MAO inhibitors or for 14 days after stopping treatment with MAO inhibitors; no MAO inhibitors are prescribed for 14 days after withdrawal of Sertraline.

Patients with depression are at risk for suicide attempts. This risk persists until remission develops. Therefore, constant medical monitoring of the patient should be established from the beginning of treatment until optimal clinical effect is achieved. Currently, there is insufficient experience with the use of sertraline in patients undergoing electroconvulsive therapy. The possible success or risk of this combination treatment has not been studied.

The effect on the ability to drive and operate machinery

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 therapy with Sertraline it is not recommended to drive vehicles or engage in activities associated with increased risk.

Contraindications

With caution: the drug is prescribed in neurological disorders (including mental retardation), manic states, epilepsy, hepatic and/or renal failure, weight loss, children over 6 years.

Side effects

CNS and peripheral nervous system: dry mouth, increased sweating, drowsiness, headache, dizziness, tremor, anxiety, agitation, hypomania, mania, insomnia, decreased appetite (rarely – increase), up to anorexia, weakness, motor anxiety.

Digestive system disorders: flatulence, nausea, vomiting, diarrhea, abdominal pain; rarely (0.8%) with long-term use – asymptomatic increased serum transaminase activity (normalizing with discontinuation of the drug).

Others: visual disturbances, reddening of the skin, disorders of ejaculation, decreased libido, weight loss.

Laboratory disorders: reversible hyponatremia (more often in elderly patients and also while taking diuretics or some other drugs) associated with ADH inadequate secretion syndrome.

In single cases during the use of the drug extrapyramidal disorders, dyskinesia, tremors, convulsions, menstrual disorders, hyperprolactinemia, galactorrhea, skin rash; rarely – erythema multiforme have been noted. Motor disorders were more often observed in patients with indications of their presence in the anamnesis or with concomitant use of antipsychotic drugs.

When discontinuing the drug, withdrawal syndrome rarely occurs. Paresthesias, hypoesthesias, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety or symptoms of psychosis are possible. These manifestations are difficult to differentiate from symptoms of the underlying disease and may also occur with other antidepressants.

Overdose

Symptoms: serotonin syndrome with nausea, vomiting, somnolence, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, increased sweating, myoclonus, hyperreflexia may occur. Severe symptoms have not been detected even when the drug is used in high doses. However, when concomitantly taken with other drugs or ethanol, severe poisoning may occur, sometimes with fatal outcome.

Treatment: there are no specific antidotes. If necessary – intensive supportive therapy and monitoring of vital body functions. Administration of activated charcoal may be more effective than gastric lavage, artificial vomiting is not recommended. Airway patency must be maintained. Forced diuresis, dialysis, hemoperfusion, or blood transfusion may be ineffective (due to the large volume of sertraline distribution).

Pregnancy use

There have been no adequate and strictly controlled clinical studies on the safety of Sertraline in pregnancy. Administration of the drug is possible only if the expected benefits to the mother exceed the potential risk to the fetus.

Women of childbearing age should be advised to use effective contraception while using the drug.

Sertraline is detected in breast milk. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped due to the lack of reliable data about the safety of Sertraline use during this period.

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