Депрефолт®

General characteristics. Structure:

Active agent: hydrochloride sertraline 55,95mg (in terms of sertraline - 50 mg) Auxiliary  a veshchestva:kremniya dioxide colloid, microcrystallic cellulose, sodium of a kroskarmelloz, коповидон, lactoses monohydrate, magnesium stearate, Opadray white Y-5-7068, a gipromelloza of ZSR, hydroxypropyl cellulose, titanium dioxide, macrogoal/PEG 400, a gipromelloza 50sr. 1 tablet of 100 mg contains:
Active agent: sertraline of a hydrochloride of 111,9 mg (in terms of sertraline - 100 mg) Excipients: silicon dioxide colloid, microcrystallic cellulose, sodium of a kroskarmelloz, коповидон, lactoses monohydrate, magnesium stearate, Opadray white Y-5-7068, gipromelloza of ZSR, hydroxypropyl cellulose, titanium dioxide, macrogoal/PEG 400, gipromelloza 50sr.

Description
Oval, biconvex, coated tablets, white or almost white color, with risky on the one hand, with side risks and with an engraving "50" (for tablets of 50 mg) and "100" (for tablets of 100 mg) on the other hand.

Pharmacological properties:

Pharmacodynamics. Action mechanism.
Sertraline - selective serotonin reuptake inhibitor (5-HT). It exerts very weak impact on the return capture of noradrenaline and a dopamine. In therapeutic doses sertraline blocks serotonin reuptake in thrombocytes of the person. It has no the stimulating, sedative or anticholinergic effect. Sertraline has no affinity to muskarinovy (holinergyachesky), serotonergic, dopaminergic, adrenergic, gistaminergichesky, to GAMK-or benzodiazepine receptors. The antidepressive effect is noted by the end of the second week of regular reception of sertraline whereas the maximum effect is reached only in 6 weeks. Unlike tricyclic antidepressants, at purpose of sertraline there is no increase in body weight. Sertraline does not cause mental or physical medicinal dependence.

Pharmacokinetics. Absorption of sertraline from digestive tract considerable, but happens slowly. The concentration maximum in a blood plasma is reached in 4,5-8,4 hours after administration of drug inside. Equilibrium concentration of sertraline in a blood plasma is reached within a week at single daily dose. Bioavailability during meal increases by 25%, at the same time time of achievement of the maximum concentration is shortened.
Distribution. The general linkng of sertraline with proteins of plasma makes 98%. Distribution volume> 20l/kg.
Metabolism and removal. Sertraline is exposed to intensive metabolism at the first passing through a liver, being exposed to N-demethylation. Its main metabolite - N-desmetilsertralin is less active in comparison with initial connection. Metabolites are allocated with urine and a stake in equal quantities. About 0,2% of sertraline are removed by kidneys in not changed look. Time of semi-removal of drug makes 22-36 hours and does not depend on age or a floor. For N-desmetilsertralina this indicator makes 62-104 hours.
Time of semi-removal of sertraline and the area under a concentration curve in a blood plasma (AUC) increase at an abnormal liver function. Irrespective of expressiveness of a renal failure the sertraline pharmacokinetics at its constant use does not change.
Sertraline gets into breast milk. There are no data on its ability to pass through a gematoplatsentarny barrier.
Sertraline is not dialyzed.

Indications to use:

- Depressions of various etiology (treatment and prevention),
- Obsessivno-kompulsivnye Frustration (OKF)
- Panic frustration (with an agarofobiya or without).
- Posttraumatic stressorny frustration (PTSR).

Route of administration and doses:

Depressions and ROC
Adults
The initial dose makes 50 mg once a day, in the morning or in the evening. A day dose it is possible gradually, not earlier, than in a week to increase from 50 mg, to the maximum daily dose in 200 mg (by 50 mg a week).

Children
For children from 6 to 12 years the initial dose makes 25 mg of sertraline once a day, in the morning or in the evening. In a week, it is possible to increase a dose to 50 mg once a day. For children from 12 to 17 years the initial dose makes 50 mg once a day, in the morning or in the evening. A day dose it is possible gradually, not earlier, than in a week to increase from 50 mg,
to the maximum daily dose in 200 mg.

Panic расстройства_и_ПТ_СР
The initial dose makes 25 mg once a day, in the morning or in the evening. In a week it is possible to increase a dose to 50 mg of sertraline once a day, and then gradually, not earlier, than in a week, the day dose can be increased gradually from 50 mg to the maximum daily dose in 200 mg.
The satisfactory therapeutic result is achieved usually in 7 days from an initiation of treatment. Achievement of full therapeutic effect requires regular administration of drug within 2-4 weeks. At patients with obsessivno-compulsive frustration for achievement of good result 8-12 weeks can be required. The minimum dose providing medical action remains further as supporting (preventive). Elderly patients
Correction of the mode of dosing is not required. Patients with abnormal liver functions
At heavy disorder of function of a liver it is necessary to reduce a dose of drug or to increase intervals between receptions.
Manumissions with a renal failure
At patients with renal failures specially it is not required to select a dose (see.
"Special instructions").

Features of use:

It is not necessary to appoint sertraline together with IMAO, and also within 14 days after the termination of treatment of IMAO. Similarly after cancellation of sertraline within 14 days do not appoint IMAO.
At the patients who are exposed to electroconvulsive therapy, sufficient experience of use of sertraline is absent. Possible success or risk of the similar combined treatment is not studied.
The patients having a depression are risk group concerning suicide attempts. This danger remains before remission development. Therefore from an initiation of treatment before achievement of optimum clinical effect for the patient it is necessary to establish constant medical observation.
At prolonged use in rare instances (0,8% of observations) there is a symptomless increase in activity транаминаз in blood serum. Drug withdrawal leads to normalization of activity of enzymes of a liver.
During treatment the tranzitorny hyponatremia can arise sertraline. It develops at elderly patients more often, and also at reception of diuretics or some other drugs. The similar side effect is connected with a syndrome of inadequate secretion of antidiuretic hormone.

Influence on ability to driving of motor transport or to control of mechanisms:
Drug use, as a rule, is not followed by disturbance of psychomotor functions. However its use along with other medicines can lead to disturbance of attention and coordination of movements. Therefore during treatment by sertraline to manage vehicles, the special equipment or to be engaged in the activity connected with the increased risk it is not recommended.

Side effects:

From TsNS: dizziness, drowsiness, a headache, sleeplessness, weakness, the increased sweating, a tremor, a hypomania, a mania, extrapyramidal frustration, alarm, agitation, a vision disorder are possible.
From cardiovascular system: seldom - erubescence with feeling of heat or heat, a heart consciousness.
From the alimentary system: dryness in a mouth, a loss of appetite, dispepsichesky frustration (a meteorism, nausea, vomiting, diarrhea), an abdominal pain, decrease in body weight.
From a metabolism: giperprolaktinemiya, galactorrhoea.
 From reproductive system: seldom - disturbances of a menstrual cycle, frustration of an ejaculation, decrease in a libido.
Allergic reactions: seldom - temperature increase, skin rash, a small tortoiseshell or an itch, a multiformny erythema.
At the treatment termination sertraline described exceptional cases of a withdrawal. There can be paresthesias, giposteziya, symptoms of a depression, hallucination, aggressive reactions, psychomotor excitement, concern or symptoms of psychosis which cannot be distinguished from symptoms of a basic disease.

Interaction with other medicines:

Inhibitors of a moioaminoksidaza (IMAO). Heavy complications at simultaneous use of sertraline and IMAO are noted (including IMAO which are selectively operating (селегилин) and with reversible type of action (моклобемид). Development of a serotoninovy syndrome is possible. Similar complications, sometimes from the death, arise at purpose of IMAO against the background of treatment by the antidepressants oppressing neyronalny capture of monoamines or right after their cancellation.
At simultaneous use of selective inhibitors of the return iyeyronaljny serotonin reuptake and IMAO arise: a hyperthermia, rigidity, a myoclonus, lability of the autonomic nervous system (bystry fluctuations of parameters of respiratory and cardiovascular system), changes of the mental status, including an acrimony, the expressed excitement, confusion of consciousness which in certain cases can pass into a delirious state or a coma.
Medicines, the oppressing central nervous system and ethanol. The combined use of sertraline and the substances oppressing the central nervous system requires close attention, and also the use of alcoholic drinks is forbidden during treatment by sertraline.
 Coumarin derivatives - at their joint appointment with ertraliny significant increase in a prothrombin time is noted - in these cases it is recommended to control a prothrombin time in an initiation of treatment sertraline and after its cancellation. Pharmacokinetic interaction Sertraline contacts proteins of a blood plasma. Therefore it is necessary to consider a possibility of its interaction with other drugs contacting proteins (for example: diazepam, Tolbutamidum and warfarin).
Cimetidinum: simultaneous use substantially reduces clearance of sertraline.
Medicines, metaboliziruyemy isoenzyme 2D6 of P450 cytochrome: prolonged treatment by sertraline in a dose of 50 mg a day is followed by increase in concentration of desipramine.
Medicines, metaboliziruyemy other fermental systems of P450 cytochrome. Experiments on studying of interaction of in vitro showed that the beta hydroxylation of endogenous cortisol which is carried out by CYP ZAZ/4 isoenzyme, and also metabolism of carbamazepine and a terfenadin at long purpose of sertraline in a dose of 200 mg a day do not change. Concentration in a blood plasma of Tolbutamidum, Phenytoinum and warfarin at long purpose of sertraline in the same dose also does not change. Thus, it is possible to make the conclusion that sertraline does not oppress CYP 2C9 isoenzyme. Sertraline does not influence concentration of diazepam in blood serum that speaks about lack of inhibition of SNZ 2S19 isoenzyme. According to the researches in vitro sertraline practically does not influence or minimum CYP IA2 isoenzyme oppresses.
Lithium. The pharmacokinetics of lithium does not change at the accompanying administration of sertraline. However, the tremor is observed more often at their combined use. Also as well as purpose of other selective inhibitors of the return neyronalny serotonin reuptake, combined use of sertraline with the medicines influencing serotonergic transfer (for example, with lithium), demands the increased care. The drugs influencing serototshergichesky transfer. When replacing one inhibitor of neyronalny serotonin reuptake by another there is no need for "the washing period". However it is required to be careful at treatment changes of course. It is necessary to avoid joint purpose of tryptophane or a fenfluramin with sertraline.
Iidushchiya of microsomal enzymes of a liver. Sertraline causes the minimum induction of enzymes of a liver. Co-administration of sertraline and antipyrine in a dose of 200 mg leads to reliable reduction of an elimination half-life of antipyrine though there is it in only 5% of observations.
Ateiolol: at joint administration of sertraline does not change it r-adren about the blocking action.
Glibeiklamid and digoxin: at administration of sertraline in a daily dose of 200 mg of medicinal interaction with these drugs it is not revealed.

Contraindications:

-  hypersensitivity to the active agent or other ingredients which are a part of drug
combined use of sertraline and MAO inhibitors. When replacing one drug by another it is necessary to refrain from reception of antidepressants within 14 days,
combined use of sertraline with tryptophane or fenfluraminy unstable epilepsy,
- children's age up to 6 years;

With care: organic diseases of a brain (including a delay of intellectual development), maniacal states, epilepsy, a liver and/or renal failure, decrease in body weight, at children are more senior than 6 years. Pregnancy and breastfeeding:
There are no controlled results of use of sertraline for pregnant women therefore they need to appoint drug if the expected advantage for mother exceeds potential risk for a fruit. Women of reproductive age which is supposed to appoint sertraline should recommend to use effective contraceptive remedies. Sertraline is found in breast milk. Use of drug during breastfeeding is not recommended. If treatment nevertheless is necessary, then a breast it is better to stop feeding.

Overdose:

Heavy symptoms at overdose of sertraline it is not revealed even at purpose of drug in high doses. However at simultaneous introduction with other drugs or ethanol there can be a serious poisoning.
The overdose can cause a serotoninovy syndrome with nausea, vomiting, drowsiness, tachycardia, agitation, the dizziness, psychomotor excitement, diarrhea increased by sweating, a myoclonus and a hyperreflexia.
Treatment: there are no specific antidotes. The intensive maintenance therapy and constant observation of the vital functions of an organism is required. It is not recommended to cause vomiting. Administration of absorbent carbon can be more effective, than a gastric lavage. It is necessary to maintain passability of respiratory tracts. At sertraline the large volume of distribution, in this regard strengthening of a diuresis, carrying out dialysis, hemoperfusion or hemotransfusion can be ineffectual.

Storage conditions:

At a temperature not above 25 °C. To store in the place, unavailable to children. Period of validity 3 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated. 50 mg and 100 mg. On 10 tablets in the blister. On 1. 2 or 3 blisters with the application instruction in a pack.
On 10, 20, 40, 60 blisters together with application instructions in a cardboard box
(for hospitals).