medicalmeds.eu Medicines Antidepressant. Асентра®

Асентра®

Producer: Krka Slovenia

Code of automatic telephone exchange: N06AB06

Release form: Firm dosage forms. Tablets.

Indications to use: Depression. Alarm. Obsessivno-kompulsivnoye frustration. Panic frustration. Posttraumatic stressful frustration.

General characteristics. Structure:

Active ingredient: 55,95 mg of sertraline of a hydrochloride (that corresponds to 50 mg of sertraline).

Excipients: Excipients: calcium phosphate double-base, cellulose mikrokrisyotallichesky, sodium carboxymethylstarch, hypro rod (hydroxypropyl cellulose), talc, magnesium stearate.

Cover: Опадрай 03H28758 (mix of a gipromelloza, ready for use, titanium dioxide, talc and propylene glycol).

Antidepressive means, powerful specific inhibitor of the return serotonin reuptake. It is well transferred; has no the stimulating, sedative or anticholinergic effect, does not change psychomotor activity, has no cardiotoxicity, does not increase body weight, does not cause physical and mental dependence. It is applied to treatment of the depressions of different degree of manifestation including which are followed by feeling of alarm; continuation of treatment allows to warn a depression recurrence. It is shown for treatment of obssesivno-compulsive frustration (obsessional neurosis); long therapy gave lasting effect at obsessional neurosis. It is applied also at the panic frustration (which are followed or not followed by an agoraphobia and other phobias) and posttraumatic stressful frustration.

Pharmacological properties:

Pharmacodynamics. Sertraline - specific inhibitor of the return serotonin reuptake (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 (cholinergic), serotonergic, dopaminergic, adrenergic, gistaminergichesky, GAMK - or to 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 makes 98%. Distribution volume> 20 l/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 equivalent 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:

1. depressions of various etiology (treatment and prevention) including which are followed by feeling of alarm);
2. obsessivno-komlulsivny frustration (OKF);
3. panic frustration;
4. posttraumatic stressorny frustration (PTSR).

Route of administration and doses:

Inside, regardless of meal.

Depressions and SURROUNDING. Adults. The initial dose makes 50 mg of sertraline 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 frustration of PTSR. 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, 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. However 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.

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. To avoid overdose it is necessary to take into account smaller body weight at children in comparison with adults, and at increase in a dose more than 50 mg/days are necessary careful observation of this category of patients and at the first signs of overdose to cancel drug.

Elderly patients have no need for special selection of a dose. Patients with abnormal liver functions require special attention at treatment by sertraline. At heavy disorder of function of a liver a dose of drug it is necessary to reduce or increase intervals between introductions.
At patients with renal failures specially it is not required to select a dose.

Features of use:

With care: neurologic disturbances (including delay of intellectual development), maniacal states, epilepsy, liver and/or renal failure, decrease in body weight.

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.

It should be noted that 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 and before achievement of optimum clinical effect for patients it is necessary to establish constant medical observation.

Women of childbearing age during treatment have to use adequate methods of contraception.

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. Sertraline is found in breast milk in this connection, treatment by this drug during breastfeeding is not recommended. There are no reliable data about safety of its use in this case. If treatment nevertheless is necessary, then a breast it is better to stop feeding.

Purpose of sertraline, as a rule, is not followed by disturbance of psychomotor functions. However its use along with other drugs 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 digestive organs: dryness in a mouth, a loss of appetite (it is rare - increase), up to anorexia, dispepsichesky frustration (a meteorism, nausea, vomiting, diarrhea or an unstable chair, a lock), spasms in a stomach, an abdominal pain, pancreatitis, hepatitis, jaundice or a liver failure.

From a nervous system: drowsiness, headache, dizziness, tremor, sleeplessness, alarm, agitation, hypomania, mania, akathisia, paresthesias, symptoms of a depression, hallucination, aggression, excitement, uneasiness, psychosis, gait disturbances, extrapyramidal frustration, dyskinesia, tremor, spasms. Motive disturbances were more often noted at patients with instructions on their existence in the anamnesis or at the accompanying use of antipsychotic means.

From urinogenital system: ejaculation delay, decrease in a libido and/or libido, erectile dysfunction, anorgazmiya, disturbances of a menstrual cycle, gynecomastia, priapism, giperprolaktinemiya, galactorrhoea.

From a respiratory organs: suffocation or feeling of "squeezing of a thorax".

From cardiovascular system: heartbeat, stethalgia, arterial hypertension, arterial hypotension, puffiness, syncope and tachycardia (very seldom). From sense bodys: a vision disorder (including a sight illegibility). Allergic reactions: erubescence, small tortoiseshell, puffiness century, persons or lips, skin rash, generalized itch, multiformny exudative erythema. Datas of laboratory: reversible increase in activity of transaminases, thrombocytopenia, a leukopenia, a tranzitorny hyponatremia (the syndrome of inadequate secretion of antidiuretic hormone, is more often at elderly patients, and also at reception of diuretics or some other drugs).

Others: sporadic bleedings (including nasal), a hypothyroidism, the increased sweating, decrease in body weight, weakness, yawning, "inflows" of blood to the person.

At the treatment termination the syndrome of "cancellation" can arise sertraline.

Interaction with other medicines:

Inhibitors of a monoaminooxidase (IMAO). Heavy complications at simultaneous use of sertraline and IMAO are noted (including selectively operating IMAO with reversible type of action - селегелин and 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 neyronalny serotonin reuptake and IMAO arise: a hyperthermia, rigidity, spasms, 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 sertraline 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 CYP2C9 isoenzyme.

Sertraline does not influence concentration of diazepam in blood serum that speaks about lack of inhibition of CYP 2C19 isoenzyme. According to the researches in vitro sertraline practically does not influence or minimum CYP 1A2 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 serotonergic 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. Induction of mikrosomachny enzymes in 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.

Atenolol: at joint introduction sertraline does not change it (3-adrenoceptor blocking action.

Glibenclamide and digoxin: at administration of sertraline in a daily dose of 200 mg of medicinal interaction with these drugs it is not revealed.

Contraindications:

1.povyshennaya sensitivity to the active agent or other ingredients which are a part of drug;
2.sovmestnoye use of sertraline and MAO inhibitors (monoaminooxidase). When replacing one drug by another it is necessary to refrain from reception of antidepressants within 14 days;
3.sovmestnoye use of sertraline with tryptophane or fenfluraminy;
4.nestabilnaya epilepsy;
5.detsky age up to 6 years;
6.beremennost and lactation period.

Overdose:

Symptoms: a serotoninovy syndrome - nausea, vomiting, drowsiness, changes on an ECG, a mydriasis, tachycardia, agitation, dizziness, uneasiness, psychomotor excitement, diarrhea, the increased sweating, a myoclonus and a hyperreflexia.

Symptomatic treatment: ensuring normal passability of respiratory tracts (oxygenation and ventilation of the lungs) and monitoring of a cordial rhythm and vitals and systems. It is not recommended to cause vomiting. Administration of absorbent carbon and sorbitol can be more effective, than a gastric lavage. There are no specific antidotes. At sertraline the large volume of distribution, in this regard strengthening of a diuresis, carrying out dialysis, hemoperfusion or hemotransfusion can be ineffectual.