Serenata, 30 pcs., 50 mg, film-coated tablets
Serenata is an antidepressant.
Sertraline is a selective serotonin (5-HT) reuptake inhibitor. It has a very weak effect on the reuptake of norepinephrine and dopamine. At therapeutic doses, sertraline blocks the uptake of serotonin by human platelets. It does not have stimulant, sedative or anticholinergic effects. Sertraline has no affinity for muscarinic (cholinergic), serotonergic, dopaminergic, adrenergic, histaminergic, GABA or benzodiazepine receptors.
The antidepressant effect is observed by the end of the second week of regular use of sertraline, while the maximum effect is achieved only after 6 weeks. Unlike tricyclic antidepressants, sertraline does not cause weight gain. Sertraline does not cause mental or physical drug dependence.
Pharmacokinetics Absorption of sertraline from the gastrointestinal tract is significant, but occurs slowly. Maximum concentration in blood plasma is achieved 4.5-8.4 hours after taking the drug orally. The equilibrium concentration of sertraline in blood plasma is achieved within a week with a single daily dose. Bioavailability during meals increases by 25%, while the time to reach maximum concentration is shortened. Distribution. The total binding of sertraline to plasma proteins is 98%. Volume of distribution >20 l/kg.
Metabolism and excretion. Sertraline undergoes extensive metabolism during its first passage through the liver, undergoing N-demethylation. Its main metabolite, N-desmethylsertraline, is less active than the parent compound. Metabolites are excreted in urine and feces in equal quantities. About 0.2% of sertraline is excreted unchanged by the kidneys. The half-life of the drug is 22-36 hours and does not depend on age or gender. For N-desmethylsertraline this figure is 62-104 hours. The half-life of sertraline and the area under the plasma concentration curve (AUC) increase with impaired liver function. Regardless of the severity of renal failure, the pharmacokinetics of sertraline does not change with its continuous use. Sertraline passes into breast milk. There is no data on its ability to pass through the blood-placental barrier. Sertraline is not dialysable.
Serenata
With the simultaneous use of the drug Serenata and MAO inhibitors, both selectively acting (selegiline) and with a reversible type of action (moclobemide), severe complications may develop, including serotonin syndrome. 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. With the simultaneous use of selective neuronal reuptake inhibitors of serotonin and MAO inhibitors, the following occur: hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular system), changes in mental status, including increased irritability, severe agitation, confusion, which in some cases can progress to delirium or coma.
When coumarin derivatives and sertraline are administered together, a significant increase in prothrombin time is observed (it is recommended to monitor the prothrombin time at the beginning of treatment with Serenata and after its discontinuation).
Pharmacokinetic interaction
Sertraline binds to plasma proteins. Therefore, the possibility of its interaction with other protein-binding drugs (for example, diazepam, tolbutamide and warfarin) should be considered.
When used simultaneously with cimetidine, a significant decrease in the clearance of sertraline is observed. With long-term treatment with sertraline at a dose of 50 mg/day, in case of simultaneous use, an increase in the plasma concentration of desipramine, which is metabolized with the participation of the CYP2D6 isoenzyme, is observed.
In vitro experimental studies of drug interactions have shown that metabolic processes occurring with the participation of CYP3A3/4 isoenzymes - beta-hydroxylation 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 also do not change with long-term administration of sertraline at the same dose. Thus, we can conclude that sertraline does not inhibit the activity of 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 does not change with simultaneous use of sertraline, however, in such cases, tremor is more often observed. As with the administration of other selective neuronal serotonin reuptake inhibitors, the combined use of sertraline with drugs that affect serotonergic transmission (for example, lithium) requires increased caution. When replacing one neuronal serotonin 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.
Sertraline causes minimal induction of liver microsomal enzymes. The simultaneous administration of sertraline and antipyrine at a dose of 200 mg leads to a significant decrease in T1/2 of antipyrine, although this occurs in only 5% of cases.
With simultaneous use, sertraline does not change the beta-adrenergic blocking effect of atenolol.
When simultaneous use of sertraline at a dose of 200 mg/day with glibenclamide or digoxin, no drug interactions were detected.
Serenata tablets ppo 50mg No. 30
Compound
Active substance: sertraline (in the form of hydrochloride) 50 mg.
Excipients: microcrystalline cellulose, sodium carboxymethyl starch, calcium hydrogen phosphate dihydrate, hydroxypropylcellulose, polysorbate, magnesium stearate.
Shell composition: hypromellose, propylene glycol, titanium dioxide.
Pharmacokinetics
Suction
After taking the drug orally, the absorption of sertraline from the gastrointestinal tract is significant, but occurs slowly. Cmax in blood plasma is achieved after 4.5-8.4 hours. Bioavailability during meals increases by 25%, while the time to reach Cmax is shortened.
Distribution
With a single daily dose, Css in blood plasma is achieved within a week. 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 permeability through the placental barrier.
Metabolism and excretion
Sertraline is extensively metabolized during the “first pass” through the liver, undergoing N-demethylation. Its main metabolite, N-desmethylsertraline, is less active than the parent compound. Metabolites are excreted in urine and feces in equal quantities. About 0.2% of sertraline is excreted unchanged by the kidneys. T1/2 is 22-36 hours and does not depend on age or gender. For N-desmethylsertraline this figure is 62-104 hours.
Pharmacokinetics in special clinical situations
If liver function is impaired, T1/2 and AUC increase.
Regardless of the severity of renal failure, the pharmacokinetics of sertraline does not change with its continuous use.
Sertraline is not dialyzable.
Indications for use
- Depression of various etiologies (treatment and prevention);
- obsessive-compulsive disorders (OCD);
- panic disorder (with or without agoraphobia);
- post-traumatic stress disorder (PTSD).
Contraindications
- Unstable epilepsy;
- children under 6 years of age;
- pregnancy;
- lactation period;
- combined use of sertraline and MAO inhibitors (when replacing one drug with another, you should refrain from taking antidepressants for 14 days);
- combined use of sertraline with tryptophan or fenfluramine;
- hypersensitivity to the components of the drug.
The drug should be used with caution in case of organic diseases of the brain (including mental retardation), manic states, epilepsy, liver and/or kidney failure, and weight loss.
Directions for use and doses
For adults with depression and OCD, the drug is prescribed at an initial dose of 50 mg 1 time / day in the morning or evening. The daily dose can be gradually, no earlier than a week later, increased from 50 mg to a maximum daily dose of 200 mg.
For panic disorders and PTSD, the initial dose 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, the daily dose can be increased from 50 mg to a maximum daily dose of 200 mg.
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. When treating 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.
For children with OCD, the drug is prescribed depending on age. For children aged 6 to 12 years, the initial dose is 25 mg 1 time / day in the morning or evening. After a week, the dose can be increased to 50 mg 1 time / day. For children and adolescents aged 12 to 17 years, the initial dose is 50 mg 1 time / day, in the morning or evening. The daily dose can be gradually, no earlier than a week later, increased from 50 mg to a maximum daily dose of 200 mg. To avoid overdose, one should take into account the lower body weight in children compared to adults, and when increasing the dose to more than 50 mg/day, it is necessary to carefully monitor this category of patients and, at the first signs of an overdose, discontinue the drug.
In elderly patients, no special dose selection is required.
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 dose selection is required.
Storage conditions
Store at a temperature not exceeding 25°C, out of the reach of children.
Best before date
2 years. Do not use after the expiration date stated on the packaging.
special instructions
Sertraline should not be administered within 14 days of stopping treatment with MAO inhibitors. MAO inhibitors are not prescribed within 14 days after discontinuation of sertraline.
Patients receiving electroconvulsive therapy do not have sufficient experience with the use of the drug Serenata. The possible success or risk of this combination treatment has not been studied.
Patients suffering from 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, patients should be under constant medical supervision.
When using the drug Serenata simultaneously with drugs that have a depressant effect on the central nervous system, special caution and careful monitoring of the patient's condition are required.
Description
Antidepressant.
Use in children
The drug is contraindicated in children under 6 years of age.
The drug should be used with caution in children over 6 years of age.
For children with OCD, the drug is prescribed depending on age. For children aged 6 to 12 years, the initial dose is 25 mg 1 time / day in the morning or evening. After a week, the dose can be increased to 50 mg 1 time / day. For children and adolescents aged 12 to 17 years, the initial dose is 50 mg 1 time / day, in the morning or evening. The daily dose can be gradually, no earlier than a week later, increased from 50 mg to a maximum daily dose of 200 mg. To avoid overdose, one should take into account the lower body weight in children compared to adults, and when increasing the dose to more than 50 mg/day, it is necessary to carefully monitor this category of patients and, at the first signs of an overdose, discontinue the drug.
Pharmacodynamics
Antidepressant. Selective serotonin reuptake inhibitor (5-HT). It has a weak effect on the reuptake of norepinephrine and dopamine. At therapeutic doses, sertraline blocks the uptake of serotonin by human platelets. Sertraline has no affinity for muscarinic, serotonin, dopamine, adrenergic, histamine, GABA or benzodiazepine receptors. Does not have a stimulating, sedative or anticholinergic effect.
The antidepressant effect is observed by the end of the second week of regular use of sertraline, while the maximum effect is achieved only after 6 weeks.
Unlike tricyclic antidepressants, sertraline does not cause weight gain. Sertraline does not cause mental or physical drug dependence.
Side effects
From the digestive system: dry mouth, decreased appetite (rarely increased), up to anorexia, dyspeptic disorders (flatulence, nausea, vomiting, diarrhea), abdominal pain; with long-term use in 0.8% of cases - an asymptomatic increase in transaminase activity in the blood serum (when the drug is discontinued, enzyme activity normalizes).
From the central nervous system and peripheral nervous system: drowsiness, headache, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, gait disturbances, weakness. During treatment with sertraline, extrapyramidal disorders, dyskinesias, tremor, convulsions, and visual disturbances were noted. Motor disorders were more often observed in patients with indications of their presence in the anamnesis or with concomitant use of antipsychotic drugs.
From the endocrine system: ejaculation disorders, decreased libido, menstrual irregularities, hyperprolactinemia, galactorrhea.
Metabolism: increased sweating, weight loss; 0.8% (more often in elderly patients, as well as when taking diuretics or a number of other drugs) - transient hyponatremia (this side effect is associated with the syndrome of inappropriate ADH secretion).
Dermatological reactions: redness of the skin, skin rash; rarely - erythema multiforme.
When stopping treatment: rarely - withdrawal syndrome: possible paresthesia, hypoesthesia, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety or symptoms of psychosis that cannot be distinguished from the symptoms of the underlying disease.
Use during pregnancy and breastfeeding
Adequate and strictly controlled clinical studies of the safety of Serenata during pregnancy have not been conducted. Prescribing the drug to pregnant women is contraindicated.
Women of reproductive age who are expected to undergo treatment with Serenata should use effective methods of contraception.
Sertraline is excreted in breast milk. There are no reliable data on the safety of sertraline use during lactation. Therefore, if it is necessary to prescribe the drug, breastfeeding should be stopped.
Interaction
With the simultaneous use of the drug Serenata and MAO inhibitors, both selectively acting (selegiline) and with a reversible type of action (moclobemide), severe complications may develop, including serotonin syndrome. 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. With the simultaneous use of selective neuronal reuptake inhibitors of serotonin and MAO inhibitors, the following occur: hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular system), changes in mental status, including increased irritability, severe agitation, confusion, which in some cases can progress to delirium or coma.
When coumarin derivatives and sertraline are administered together, a significant increase in prothrombin time is observed (it is recommended to monitor the prothrombin time at the beginning of treatment with Serenata and after its discontinuation).
Pharmacokinetic interaction
Sertraline binds to plasma proteins. Therefore, the possibility of its interaction with other protein-binding drugs (for example, diazepam, tolbutamide and warfarin) should be considered.
When used simultaneously with cimetidine, a significant decrease in the clearance of sertraline is observed. With long-term treatment with sertraline at a dose of 50 mg/day, in case of simultaneous use, an increase in the plasma concentration of desipramine, which is metabolized with the participation of the CYP2D6 isoenzyme, is observed.
In vitro experimental studies of drug interactions have shown that metabolic processes occurring with the participation of CYP3A3/4 isoenzymes - beta-hydroxylation 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 also do not change with long-term administration of sertraline at the same dose. Thus, we can conclude that sertraline does not inhibit the activity of 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 does not change with simultaneous use of sertraline, however, in such cases, tremor is more often observed. As with the administration of other selective neuronal serotonin reuptake inhibitors, the combined use of sertraline with drugs that affect serotonergic transmission (for example, lithium) requires increased caution. When replacing one neuronal serotonin 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.
Sertraline causes minimal induction of liver microsomal enzymes. The simultaneous administration of sertraline and antipyrine at a dose of 200 mg leads to a significant decrease in T1/2 of antipyrine, although this occurs in only 5% of cases.
With simultaneous use, sertraline does not change the beta-adrenergic blocking effect of atenolol.
When simultaneous use of sertraline at a dose of 200 mg/day with glibenclamide or digoxin, no drug interactions were detected.
Overdose
Symptoms: no severe symptoms of sertraline overdose were detected even when the drug was prescribed in high doses. However, when taken simultaneously with other drugs or ethanol, severe poisoning may occur. Overdose can cause serotonin syndrome with nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia.
Treatment: There are no specific antidotes. Intensive supportive care and constant monitoring of vital body functions are required. Inducing vomiting is not recommended. The administration of activated carbon may be more effective than gastric lavage. The airway must be maintained. Sertraline has a large Vd, so increasing diuresis, dialysis, hemoperfusion, or blood transfusion may not be effective.
Impact on the ability to drive vehicles and operate machinery
The administration of sertraline, as a rule, 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, during treatment with sertraline, driving vehicles, special equipment or engaging in activities associated with increased risk is not recommended.
