Serenata - instructions for use, doses, side effects, contraindications

: White or almost white capsular shaped tablets, biconvex, film-coated with a dividing line on one side. Type in the fracture: white or almost white tablet.

Pharmacotherapeutic group:antidepressant

ATX: & nbsp

N.06.A.X Other antidepressants

N.06.A Antidepressants

N.06.A.B Selective serotonin reuptake inhibitors

Pharmacodynamics:

Sertralin is a selective serotonin reuptake inhibitor (5-HT).It has very little effect on the re-uptake of norepinephrine and dopamine. In therapeutic doses sertraline blocking the seizure of serotonin by 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:

Absorption of sertraline from the gastrointestinal tract is significant, but it is slow. The maximum concentration in the blood plasma is achieved in 4,5-8,4 hours after taking the drug inside. The equilibrium concentration of sertraline in blood plasma is reached within a week with a single daily intake.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%. The volume of distribution> 20l / kg.

Metabolism and excretion. Sertraline is subjected to intensive metabolism during the 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 equal amounts. About 0.2% of sertraline is excreted by the kidneys unchanged. The half-life of the drug is 22-36 hours and does not depend on age or sex. For N-desmethylsertraline, this indicator is 62-104 hours.

The half-life of sertraline and the area under the plasma concentration 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:

Depression of various etiologies (treatment and prevention),
Obsessive-compulsive disorder (OCD)
Panic disorders (with or without agarobobia).
Post-traumatic stress disorder (PTSD).

Contraindications:

Hypersensitivity to the active substance or other ingredients contained in the preparation,
joint use of sertraline and MAO inhibitors. When replacing one drug for another, one should refrain from taking antidepressants within 14 days, the joint use of sertraline with tryptophan or fenfluramine, unstable epilepsy, children under 6 years of age;
- pregnancy and lactation period (see "Specific indication"),

Carefully:

organic brain diseases (including mental retardation), manic conditions, epilepsy, hepatic and / or renal insufficiency, weight loss, in children older than 6 years.

Dosing and Administration:

Depression and OCD

Adults

The initial dose is 50 mg Sertraline once a day, in the morning or in the evening. The daily dose can be gradually, not earlier than a week, increase from 50 mg to a maximum daily dose of 200 mg.

Panic disorder and PTSD

The initial dose is 25 mg Sertraline once a day, in the morning or in the evening. After a week, the doctor can increase the dose to 50 mg sertraline once a day, and then gradually, not earlier than a week, the daily dose can be gradually increased from 50 mg 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 the full therapeutic effect, a regular intake of the drug is required within 2-4 weeks. In patients with obsessive-compulsive disorders, 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.

Children with OCD

For children from 6 to 12 years, the initial dose 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 from 12 to 17 years, the initial dose is 50 mg once a day, in the morning or in the evening. The daily dose can be gradually, not earlier than a week, increase from 50 mg to a maximum daily dose of 200 mg.To avoid an overdose, it is necessary to take into account the smaller body weight in children compared to adults, and with increasing doses

more than 50 mg / day, careful monitoring of this category of patients and at the first signs of an overdose to cancel the drug.

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

Patients with impaired liver function require special attention in the treatment of sertraline. In case of severe impairment of 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 specific dose is required (see "Specific indication").

Side effects:

Dry mouth, increased sweating, drowsiness, headache, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, decreased appetite (rarely - increase), up to anorexia, dyspeptic disorders (flatulence, nausea, vomiting, diarrhea), abdominal pain, weight loss, gait disturbance.

There may also be weakness, redness of the skin, visual impairment, ejaculation disorder, decreased libido.

During the treatment with sertraline, extrapyramidal disorders, dyskinesia, tremor, convulsions, menstrual irregularities, hyperprolactinemia, galactorrhea, skin rashes, and occasional erythema multiforme were noted. Motor disorders were more often observed in patients with indications of their presence in an anamnesis or with the concomitant use of antipsychotics.

When treatment with sertraline is discontinued, rare cases of withdrawal syndrome are described. There may be paresthesia, hypostases, symptoms of depression, hallucinations, aggressive reactions, psychomotor agitation, anxiety or symptoms of psychosis that can not be distinguished from the symptoms of the underlying disease.

Laboratory test data: rarely - in 0.8% of observations, with long-term use - there is an asymptomatic increase in the activity of transaminases in the blood serum. The abolition of the drug in this case leads to a normalization of the activity of the enzymes.

During treatment with sertraline, transient hyponatremia may occur. It often develops in elderly patients, as well as when taking diuretics or a number of other drugs. A similar side effect is associated with the syndrome of inadequate secretion of antidiuretic hormone.

Overdose:

Severe symptoms with an overdose of sertraline was not detected even with the administration of the drug in large doses. However, with simultaneous administration with other drugs or ethanol, severe poisoning can 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. It requires intensive maintenance therapy and constant monitoring of vital body functions. It is not recommended to induce vomiting. The introduction of activated carbon can be more effective than gastric lavage. It is necessary to maintain airway patency. Sertraline has a large volume of distribution, in connection with this, increased diuresis, dialysis, hemoperfusion or blood transfusion may not be successful.

Interaction:

Inhibitors of monoamine oxidase (MAOI). Severe complications are noted with simultaneous use of sertraline and MAOI (including selectiveselegiline) MAAO and with a reversible type of action (moclobemide).Perhaps the development of serotonin syndrome. Similar complications, sometimes fatal, occur with the appointment of MAOI on the background of treatment with antidepressants that depress the neuronal capture of monoamines or immediately after their withdrawal.

With the simultaneous use of selective inhibitors of reverse neuronal seizure of serotonin and MAOA, hyperthermia, rigidity, myoclonus, lability in the autonomic nervous system (rapid fluctuations in respiratory and cardiovascular parameters system), changes in mental status, including increased

irritability, marked excitement, confusion, which in some cases can go into a delirious state or to whom.

Medicines that depress the central nervous system and ethanol. The combined use of sertraline and substances that depress the central nervous system requires close attention, and the use of alcoholic beverages during the treatment with sertraline is prohibited.

Coumarin derivatives - when co-administered with sertraline, there is a significant increase in prothrombin time - in these cases it is recommended to monitor prothrombin time inthe 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. Drugs metabolized by isoenzyme 2D6 cytochrome P450: prolonged treatment with sertraline at a dose of 50 mg per day is accompanied by an increase in the concentration of desipramine.

Drugs metabolized by other enzymatic systems of cytochrome P450. Experiments on in vitro interaction showed that the isoenzyme CYP ZAZ / 4 beta-hydroxylation of endogenous cortisol, as well as the metabolism of carbamazepine and terfenadine with long-term administration of sertraline at a dose of 200 mg per day did not change. 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 Do not depress isoenzyme CYP 2C9.

Sertraline does not affect the concentration of diazepam in the serum, indicating that there is no inhibition of isoenzyme СНЗ 2С19. According to in vitro studies sertraline practically does not influence or minimally inhibits isoenzyme CYP 1A2.

Lithium. The pharmacokinetics of lithium does not change with the concomitant administration of sertraline. However, tremor is observed more often when they are used together. 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 (for example, with 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 washing". However, care must be taken when changing the course of treatment. Tryptophan or fenfluramine should be avoided together with sertraline.

Induction of microsomal liver enzymes. 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 the periodhalf-life of antipyrine, although this occurs in only 5% of observations.

Atenolol: with co-administration sertraline does not change it (3-adrenoblocking effect.

Glibenclamide and digoxin: when sertraline was administered in a daily dose, 200 mg of drug interaction with these drugs was not detected.

Special instructions:

Sertraline should not be administered in conjunction with MAOI, nor within 14 days after discontinuation of MAOI treatment. Similarly, after the withdrawal of sertraline within 14 days, no MAOI is 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.

Pregnancy and breastfeeding:

Controlled results of the use of sertraline in pregnant women do not exist, therefore, it is only necessary to prescribe them a drug,if the expected benefit for the mother exceeds the potential risk to the fetus. Women of reproductive age who are supposed to be appointed sertraline, it should be recommended to use effective contraceptives. 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.

Effect on the ability to drive transp. cf. and fur:

Influence on the ability to drive vehicles and control mechanisms:

The appointment, sertraline, as a rule, is not accompanied by a disturbance of the 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.

Form release / dosage:

Tablets coated with a coating, 50 mg and 100 mg.

Packaging:

10 tablets in PVC / Al. blister.5 blisters or 3 blisters for 10 tablets and instructions for use are packed in a cardboard box.

4 tablets in PVC / Al. blister. 1 blister with instructions for use in a cardboard box (sample not for sale).

Storage conditions:

Store at a temperature below 25 ° C, in a place inaccessible to children.

Shelf life:2 years. Do not use after the time specified on the package

Terms of leave from pharmacies:On prescription

Registration number:LS-000063

Date of registration:05.02.2010

The owner of the registration certificate:Torrent Pharmaceuticals Co., Ltd.Torrent Pharmaceuticals Co., Ltd. India

Manufacturer: & nbsp

TORRENT PHARMACEUTICALS, Ltd. India

Information update date: & nbsp20.09.2015

Illustrated instructions

Instructions

Serenata (Serenata)