Asentra, 50 mg, film-coated tablets, 28 pcs.

Release form and composition

The dosage form of Asentra is film-coated tablets: round, white, with beveled edges and a notch on one side; on the fracture there is a rough white mass (7 pieces in blisters, 4 blisters in a cardboard box).

Composition of 1 tablet:

• active substance: sertraline – 50 or 100 mg (sertraline hydrochloride – 55.95 or 111.9 mg);
• auxiliary components: hydroxypropylcellulose, magnesium stearate, calcium dihydrogen phosphate, sodium starch glycolate, talc, microcrystalline cellulose;
• Shell: Opadry 03H28758 (talc, hypromellose, titanium dioxide, propylene glycol).

Pharmacological properties

Pharmacodynamics

The active ingredient of Asentra is sertraline, an antidepressant, a specific inhibitor of serotonin (5-HT) reuptake in neurons. In therapeutic doses, it blocks the uptake of serotonin in human platelets. The antidepressant effect develops by the end of the second week of daily use of Asentra, the maximum effect is observed only after 6 weeks.

Asentra, unlike tricyclic antidepressants, does not cause weight gain. In some cases, on the contrary, it helps to reduce it.

Has no affinity for GABA, histamine, dopamine, serotonin, benzodiazepine, adrenergic and cholinergic receptors. Does not have a sedative, stimulating or anticholinergic effect. Does not cause physical or mental drug dependence.

The effect on the metabolism of dopamine and norepinephrine is insignificant.

Pharmacokinetics

After oral administration of Asentra, sertraline is slowly absorbed from the gastrointestinal tract. The maximum concentration of the drug in the blood is achieved after 4.5–8.4 hours.

When taking Asentra daily once a day, the equilibrium concentration of sertraline is established within approximately a week. Bonding with plasma proteins is 98%, volume of distribution is more than 20 l/kg. Sertraline passes into breast milk. The ability to penetrate the placental barrier has not been established.

Sertraline is extensively metabolized by N-demethylation during the first passage through the liver. The main metabolite formed as a result of biotransformation is the less active compound N-desmethylsertraline. About 0.2% of sertraline is excreted unchanged by the kidneys. Metabolites are excreted in approximately equal parts with feces and urine. The half-life does not depend on the gender and age of the patient, it is about 22–36 hours, for N-desmethylsertraline it is 62–104 hours.

In patients with impaired liver function, the half-life of the drug and the area under the concentration-time curve increase.

The pharmacokinetic parameters of sertraline in patients with impaired renal function (both mild and severe) do not change with continuous use of Asentra.

The drug is not eliminated by dialysis.

Instructions:

Clinical and pharmacological group

02.002 (Antidepressant)

Release form, composition and packaging

White film-coated tablets, round, with beveled edges and a notch on one side; on the fracture there is a white rough mass.

Excipients: magnesium stearate, hydroxypropylcellulose, sodium starch glycolate, calcium dihydrogen phosphate, microcrystalline cellulose, talc.

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

7 pcs. - blisters (4) - cardboard packs.

White film-coated tablets, round, with beveled edges and a notch on one side; on the fracture there is a white rough mass.

Excipients: magnesium stearate, hydroxypropylcellulose, sodium starch glycolate, calcium dihydrogen phosphate, microcrystalline cellulose, talc.

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

7 pcs. - blisters (4) - cardboard packs.

pharmachologic effect

Antidepressant. A specific inhibitor of serotonin (5-HT) reuptake in neurons. The metabolism of norepinephrine and dopamine is slightly affected. At therapeutic doses, sertraline blocks the uptake of serotonin into human platelets. The drug does not have a stimulating, sedative or anticholinergic effect. It has no affinity for serotonin, dopamine, histamine, benzodiazepine, GABA, cholinergic and adrenergic receptors.

The antidepressant effect is observed by the end of the second week of regular use of Asentra, while the maximum effect is achieved only after 6 weeks.

Unlike tricyclic antidepressants, Asentra does not cause weight gain; in a number of cases its decrease was noted.

The drug does not cause mental or physical drug dependence.

Pharmacokinetics

Suction

After taking the drug orally, sertraline is slowly absorbed from the gastrointestinal tract, Cmax in blood plasma is reached after 4.5-8.4 hours.

Distribution

Css is established within a week when taken once a day daily. The binding of sertraline to plasma proteins is 98%. Vd >20 l/kg.

Sertraline is excreted in breast milk. There is no data on its ability to penetrate the placental barrier.

Metabolism and excretion

Sertraline undergoes intensive biotransformation during the “first pass” through the liver by N-demethylation. The main metabolite, N-desmethylsertraline, is less active compared to the parent compound. Metabolites are excreted in urine and feces in equivalent quantities. About 0.2% of sertraline is excreted unchanged by the kidneys. T1/2 of the drug is 22-36 hours and does not depend on the age or gender of patients. For N-desmethylsertraline T1/2 - 62-104 hours.

Pharmacokinetics in special clinical situations

T1/2 and AUC in blood plasma increase with impaired liver function.

The pharmacokinetic parameters of sertraline in patients with both mild and moderate renal impairment (CR 20-50 ml/min) and severe renal impairment (CR <20 ml/min) do not change with its continuous use.

Sertraline is not eliminated by dialysis.

Dosage

For depression and OCD in adults, the average initial dose is 50 mg 1 time / day, in the morning or evening. The daily dose can be gradually increased, no earlier than after a week, from 50 mg to a maximum daily dose of 200 mg.

For panic disorders and PTSD, the initial dose of Asentra is 25 mg 1 time / day, in the morning or evening. After a week, you can increase the dose to 50 mg 1 time / day, and then gradually, no earlier than a week later, increase to a maximum daily dose of 200 mg.

The initial dose of Asentra for children aged 6 to 12 years is 25 mg sertraline 1 time / day, in the morning or evening. After a week, you can increase the dose to 50 mg 1 time / day. For children aged 12 to 17 years, the initial dose is 50 mg 1 time / day in the morning or evening. If necessary, the daily dose can be gradually, no earlier than after a week, increased from 50 mg to a maximum daily dose of 200 mg. To avoid an overdose, the lower body weight of children compared to adults should be taken into account, and when increasing the dose to more than 50 mg/day, careful monitoring of this category of patients is necessary: ​​at the first signs of an overdose, the drug should be discontinued.

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

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

In case of liver dysfunction, the drug should be prescribed with caution. In case of severe liver dysfunction, the dose of the drug should be reduced or the intervals between doses increased.

In patients with impaired renal function, no special adjustment of the dosage regimen is required.

Overdose

Symptoms: serotonin syndrome may occur with nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, increased sweating, myoclonus, hyperreflexia. No severe symptoms were detected even when using the drug in high doses. However, when taken simultaneously with other drugs or ethanol, severe poisoning can occur, sometimes fatal.

Treatment: There are no specific antidotes. If necessary, intensive supportive care and monitoring of the vital functions of the body. The introduction of activated carbon may be more effective than gastric lavage; inducing artificial vomiting is not recommended. The airway must be maintained. Forced diuresis, dialysis, hemoperfusion or blood transfusion may be unsuccessful (due to the large volume of distribution of sertraline).

Drug interactions

With the simultaneous use of sertraline and MAO inhibitors (including selectively acting MAO inhibitors with a reversible type of action - selegiline and moclobemide), the development of serotonin syndrome is possible: hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system (rapid fluctuations in parameters of the respiratory and cardiovascular system), changes mental status, including increased irritability, severe agitation, confusion, which in some cases can develop into a delirious state or coma (this combination is contraindicated). Similar complications (sometimes fatal) occur when MAO inhibitors are prescribed during treatment with antidepressants that inhibit the neuronal uptake of monoamines or immediately after their withdrawal.

In healthy volunteers, the use of sertraline at a dose of 200 mg / day does not affect the effect of ethanol, carbamazepine or haloperidol, as well as mental activity and psychomotor activity (however, the combined administration of sertraline and drugs that depress the central nervous system requires close attention, and simultaneous use with ethanol and ethanol-containing drugs is contraindicated).

When indirect anticoagulants (coumarin derivatives) are co-administered with sertraline, a significant increase in prothrombin time is observed (monitoring of prothrombin time is required at the beginning of sertraline use and after its discontinuation).

Pharmacokinetic interaction

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

Concomitant use of the drug with cimetidine significantly reduces the clearance of sertraline.

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

In vitro experiments have shown that the beta-hydroxylation of endogenous cortisol carried out by the CYP3A3/4 isoenzyme, as well as the 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, we can conclude that sertraline does not inhibit the CYP2C9 isoenzyme.

Sertraline does not affect the concentration of diazepam in the blood serum, which indicates the absence of inhibition of the CYP2C19 isoenzyme.

According to in vitro studies, sertraline has virtually no effect or minimal inhibition of the CYP1A2 isoenzyme.

The pharmacokinetics of lithium do not change statistically significantly with concomitant administration of sertraline; but tremor is observed more frequently, suggesting the possibility of a pharmacodynamic interaction (this combination requires caution). Sertraline should also be administered with caution with other drugs that affect serotonergic transmission.

When replacing one neuronal uptake inhibitor with another, there is no need for a washout period. However, caution is required when changing the course of treatment. Co-administration of tryptophan or fenfluramine with sertraline should be avoided.

Clinical studies have shown that sertraline causes minimal induction of liver enzymes. Simultaneous 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 in only 5% of observations).

When administered together, sertraline does not affect the beta-blocking effect of atenolol.

When sertraline was administered in a daily dose of 200 mg, no drug interactions with glibenclamide and digoxin were detected.

Use during pregnancy and lactation

Adequate and strictly controlled clinical studies on the safety of sertraline during pregnancy have not been conducted. Prescribing the drug is possible only if the expected benefit to the mother outweighs the potential risk to the fetus.

Women of childbearing age should be advised to use effective contraception during the period of use of the drug.

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

Side effects

From the central nervous system and peripheral nervous system: dry mouth, increased sweating, drowsiness, headache, dizziness, tremor, anxiety, agitation, hypomania, mania, insomnia, decreased appetite (rarely increased), up to anorexia, weakness, restlessness .

From the digestive system: flatulence, nausea, vomiting, diarrhea, abdominal pain; rarely (0.8%) with long-term use - an asymptomatic increase in transaminase activity in the blood serum (normalized when the drug is discontinued).

Other: visual disturbances, redness of the skin, ejaculation disorders, decreased libido, weight loss.

From laboratory parameters: reversible hyponatremia (more often in elderly people, as well as when taking diuretics or a number of other drugs) associated with the syndrome of inappropriate ADH secretion.

When using the drug in isolated cases, extrapyramidal disorders, dyskinesia, tremor, convulsions, menstrual irregularities, hyperprolactinemia, galactorrhea, and skin rash were noted; occasionally - erythema multiforme. Motor disorders were more often observed in patients with indications of their presence in the anamnesis or with concomitant use of antipsychotic drugs.

When you stop using the drug, withdrawal syndrome rarely occurs. Paresthesia, hypoesthesia, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety or symptoms of psychosis are possible. These manifestations are difficult to differentiate from the symptoms of the underlying disease, and they can occur when using other antidepressants.

Storage conditions and periods

The drug should be stored out of the reach of children at temperatures up to 25°C. Shelf life: 2 years.

Indications

— treatment and prevention of depression of various etiologies;

— treatment of obsessive-compulsive disorders (OCD);

- treatment of panic disorders;

- post-traumatic stress disorder (PTSD).

Contraindications

- simultaneous use of MAO inhibitors and within 14 days after their withdrawal;

- simultaneous use of tryptophan or fenfluramine;

- unstable epilepsy;

- children under 6 years of age;

- pregnancy;

- lactation (breastfeeding);

- hypersensitivity to the components of the drug.

The drug is prescribed with caution for neurological disorders (including mental retardation), manic states, epilepsy, liver and/or renal failure, weight loss, and children over 6 years of age.

special instructions

According to clinical studies, the drug sertraline is effective and safe in the treatment of depression in patients who have suffered a myocardial infarction and in patients with unstable angina. Placebo-controlled studies have shown the effectiveness and safety of sertraline in patients with diabetes mellitus.

Sertraline is not prescribed together with MAO inhibitors, or within 14 days after stopping treatment with MAO inhibitors; After discontinuation of sertraline, MAO inhibitors are not prescribed for 14 days.

Patients with depression are at risk for suicide attempts. This danger persists until remission develops. Therefore, from the start of treatment until the optimal clinical effect is achieved, constant medical monitoring of the patient should be established.

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.

Impact on the ability to drive vehicles and operate machinery

The administration of sertraline is not accompanied by impairment of psychomotor functions. However, its use simultaneously with other drugs can lead to impairment of attention and coordination of movements. Therefore, driving or engaging in activities associated with increased risk is not recommended during sertraline therapy.

Use for renal impairment

The drug is prescribed with caution in case of renal failure.

Use for liver dysfunction

In case of liver dysfunction, the drug should be prescribed with caution. In case of severe liver dysfunction, the dose of the drug should be reduced or the intervals between doses increased.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Contraindications

Absolute:

• unstable epilepsy;
• combination therapy with tryptophan or fenfluramine, as well as with monoamine oxidase inhibitors (MAO) and for 2 weeks after their discontinuation;
• age up to 6 years;
• pregnancy and breastfeeding;
• hypersensitivity to the components of the drug.

Relative (Asentra tablets should be used with caution in the presence of the following conditions/diseases):

• epilepsy;
• neurological disorders, including mental retardation;
• liver/renal failure;
• manic states;
• weight loss;
• children's age from 6 years.

Analogues of the drug Asentra

The drug has analogues both in chemical composition and therapeutic effect. Absolute analogues of Asentra are:

1. Adyuvin is a sertraline-based product. Available in tablets. The composition and mechanism of action are absolutely identical to the analog product. However, it is cheaper in price. The method of application is similar to that for Asentra therapy. Indications and contraindications are similar.
2. Zoloft is a complete repetition of the composition of Asentra at a more affordable price. Pharmacokinetics are the same. The medication is actively being studied by American scientists to confirm the emergence of drug addiction that occurs against the background of its uncontrolled use.
3. Misol is a medicine of the Turkish pharmaceutical industry. The instructions for its use completely repeat the instructions for Asentra. Contraindicated if the patient has an allergic reaction to the components of the drug.

Instructions for use of Asentra: method and dosage

Asentra tablets are taken orally. The daily dose is taken in 1 dose (morning or evening).

Recommended dosage regimen for adults:

• OCD, depression: initial average daily dose – 50 mg in 1 dose. The dose is increased gradually (not earlier than after 7 days). Maximum – 200 mg per day;
• panic disorders and PTSD: initial daily dose – 25 mg. After 7 days, the dose can be doubled, after which it can be gradually (no earlier than 7 days) increased to a maximum of 200 mg per day.

Recommended dosage regimen for children:

• 6–12 years: initial daily dose – 25 mg. After 7 days, the dose can be doubled;
• 12–17 years: initial daily dose – 50 mg.

If necessary, gradually increase the dose (not earlier than after 7 days). Maximum – 200 mg per day.

It is necessary to take into account the lower weight of children compared to adults (to avoid overdose). When prescribing daily doses above 50 mg, careful monitoring is required; at the first symptoms of an overdose, therapy is canceled.

As a rule, a satisfactory therapeutic effect is observed after 7 days from the start of using Asentra, and a complete one – after 2–4 weeks. For OCD, good results can take 8–12 weeks to develop. The smallest dose that provides a therapeutic effect is subsequently retained as a maintenance dose.

In case of functional renal impairment and elderly patients, the dosage regimen should not be adjusted. In patients with severe liver dysfunction, Asentra is prescribed with caution, and the dose should be reduced or the interval between doses should be increased.

What do patients say?

But patients’ opinions about the medication are not always so positive. Although, in fairness, it must be said that negative reviews are rare. Most often, people say that the medication helped them in a certain life situation.

Patients who take the pills for a long time fully confirm the doctors’ opinion about the drug “Asentra”. Reviews from patients indicate that the medicine perfectly relieves anxiety, fears, and panic conditions. An effective remedy in the fight against psychosis. People claim that treatment with the drug allows you to restore a good mood and improve your mood.

However, patients pay special attention to the accumulative ability of the drug. After all, many people who have started treatment with this medication claim that Asentra tablets do not help. Patients who experienced a beneficial effect from treatment indicate that they felt the first results only after 2 weeks. And some people much later. After all, most often the issue of increasing the dosage is decided after 2 weeks. This allows you to avoid such an unpleasant condition as an overdose.

When talking about this drug, one cannot help but dwell on the side effects. Patients testify that during therapy, undesirable manifestations may indeed appear. It’s hard to say exactly what side effects will occur. It depends on the body. But it should be clearly understood that unpleasant reactions may well occur during therapy. You should not wait for all the symptoms indicated in the annotation to appear. If you have the first negative signs, be sure to consult a doctor.

Side effects

• digestive system: diarrhea, flatulence, vomiting, nausea, abdominal pain; rarely (with long-term therapy) - asymptomatic increase in transaminase activity in the blood serum (transient in nature, disappears after discontinuation of treatment);
• central and peripheral nervous system: insomnia, drowsiness, motor restlessness, dry mouth, increased sweating, hypomania, headache, tremor, dizziness, agitation, anxiety, weakness, mania, decreased appetite (in rare cases, increased) up to anorexia;
• laboratory parameters: reversible hyponatremia (in most cases in elderly patients, as well as during therapy with diuretics or some other drugs), associated with the syndrome of inappropriate secretion of antidiuretic hormone (ADH);
• others: decreased libido, redness of the skin, visual disturbances, ejaculation disorders, weight loss.

In isolated cases, the development of the following adverse reactions was observed during therapy: skin rash, convulsions, extrapyramidal disorders, tremor, dyskinesia, menstrual irregularities, galactorrhea, hyperprolactinemia; occasionally - erythema multiforme. Motor disorders were more often observed in patients with a complicating medical history or in patients with combined use of Asentra with antipsychotic drugs.

Withdrawal syndrome after cessation of treatment is usually rare. Symptoms: aggressive reactions, psychomotor agitation, paresthesia, symptoms of depression/psychosis, hypoesthesia, hallucinations, anxiety. These disorders are difficult to differentiate from the symptoms of the underlying disease, and they can develop with the use of other antidepressant drugs.

Overdose

In case of overdose, serotonin syndrome may develop, accompanied by symptoms such as nausea and vomiting, diarrhea, agitation, dizziness, drowsiness, psychomotor agitation, tachycardia, increased sweating, hyperreflexia, myoclonus. Severe signs of intoxication were not detected even when taking Asentra in high doses. However, in the case of simultaneous use of other drugs or ethanol, severe poisoning, even death, can occur.

There is no specific antidote for sertraline. Taking activated charcoal may be more effective than gastric lavage. Inducing vomiting is not recommended. Intensive supportive therapy is indicated, as well as monitoring the state of vital functions of the body. The airway must be maintained. Dialysis, forced diuresis, hemoperfusion, and blood transfusion are likely to be ineffective due to the large volume of distribution of sertraline.

special instructions

According to clinical studies, Asentra is safe and effective in the treatment of depression in patients who have suffered a myocardial infarction, as well as in patients with unstable angina and diabetes mellitus.

From the start of using Asentra until the optimal clinical effect is achieved, constant medical monitoring of the patient’s condition is necessary, since patients with depression are at risk for suicide attempts (the danger exists until the development of remission).

There is no sufficient experience with the use of Asentra in patients undergoing electroconvulsive therapy (the safety/efficacy profile of combination therapy has not been studied).

Impact on the ability to drive vehicles and complex mechanisms

The combined use of Asentra with other drugs can cause the development of disturbances in attention and coordination of movements, and therefore, during the period of therapy, performing work associated with increased risk and driving vehicles is not recommended.

Indications for use

Despite the fact that the medication is a fairly effective antidepressant, do not take this medication at your own discretion. Self-medication rarely achieves the desired results. Most often, therapy chosen without a doctor ends in the development of many unpleasant conditions.

Before starting treatment, be sure to consult a specialist whether Asentra is suitable for you or not.

Instructions for use recommend taking the medicine for the following conditions:

• depression of various etiologies (for therapeutic and preventive purposes);
• obsessive-compulsive disorders (OCD);
• post-traumatic stress disorder (PTSD);
• panic states.

Use during pregnancy and lactation

Strictly controlled and adequate clinical studies regarding the safety of taking sertraline in pregnant women have not been conducted, therefore the use of Asentra during this period is not recommended. A doctor can decide to prescribe a drug only in cases where the expected benefits are clearly higher than the potential risks.

Women of reproductive age are recommended to use reliable contraceptive methods during treatment.

Sertraline passes into breast milk. There are no data on the safety of sertraline in infants. In this regard, breastfeeding should be discontinued if antidepressant therapy is required during lactation.

Drug interactions

When Asentra is used in combination with certain drugs/substances, the following effects may develop:

• drugs that depress the central nervous system: development of interaction (combined use requires caution);
• MAO inhibitors: the occurrence of serotonin syndrome: myoclonus, rigidity, hyperthermia, lability of the autonomic nervous system, changes in mental status, including severe agitation, increased irritability, confusion, which in some cases can turn into a delirious state or coma (combined use is contraindicated). Similar disorders (in some cases with fatal outcomes) develop when MAO inhibitors are prescribed during treatment with antidepressant drugs that inhibit the neuronal uptake of monoamines, or immediately after their withdrawal;
• indirect anticoagulants (coumarin derivatives): a significant increase in prothrombin time (at the beginning of therapy and after discontinuation of Asentra, monitoring of prothrombin time is necessary);
• ethanol and drugs containing ethanol: development of interaction (combined use is contraindicated);
• cimetidine: significant reduction in the clearance of sertraline;
• drugs that bind to plasma proteins (diazepam, tolbutamide and warfarin): development of interaction;
• lithium and other drugs affecting serotonergic transmission: development of interaction (combined use requires caution);
• desipramine (long-term use of sertraline in a daily dose of 50 mg): an increase in its plasma concentration;
• antipyrine: significant reduction in its half-life;
• tryptophan, fenfluramine: development of interaction (combined use should be avoided).

Reviews about the drug

As a medication recommended by the International Psychiatric Association, Asentra has earned numerous positive reviews from specialists, although patients are not so clear in their assessment of this new generation antidepressant.

Psychiatrists

1. Ignatiy Sviridov, psychiatrist of the highest category: “Given the unstable economic and social situation in the country and society, every year there is an increase in the percentage of patients with depressive disorders. I often prescribe Asentra to my patients. It gives a wonderful effect. It is enough to carry out a two-week course of therapy and the most striking signs of the disease will begin to recede. In my practice, I had to refuse to prescribe it because, while using it, the patient developed a narcotic syndrome leading to addiction.”
2. Evgenia Ismailova, psychiatrist, candidate of medical sciences: “I prescribe Asentra to my patients. The medicine is relatively new, but it has already shown its effectiveness in many tests. I see positive dynamics during treatment with him. I recommend my colleagues to use it in their practice.”