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

Excipients: calcium phosphate dibasic, microcrystalline cellulose, sodium carboxymethyl starch, giprolose (hydroxypropylcellulose), talc, magnesium stearate.

SHELL: Opadray 03Н28758 (ready-to-use mixture of hypromellose, titanium dioxide, talc and propylene glycol).

Description:

Round tablets covered with a film shell of white color, with a bevelled edge and with a notch on one side.

Pharmacotherapeutic group:Antidepressant

ATX: & nbsp

N.06.A.X Other antidepressants

N.06.A Antidepressants

N.06.A.B Selective serotonin reuptake inhibitors

Pharmacodynamics:Mechanism of action

Sertraline is a specific inhibitor of serotonin reuptake (5-HT).It has very little effect on the re-uptake of norepinephrine and dopamine. In therapeutic doses sertraline blocks the seizure of serotonin in 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 the blood plasma is reached within a week with a single daily intake. Bioavailability during meals increases by 25 %, while the time to reach the maximum concentration is shortened.

Distribution. The total binding of sertraline to proteins is 98%. The volume of distribution> 20 l / kg.

Metabolism and excretion. Sertraline is subjected to intensive metabolism during the first passage through the liver, undergoing N-detylation. His main metabolite - N-desmethylsertralin is less active than the starting compound. Metabolites are excreted in urine and feces in equivalent amounts. About 0.2 % 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 in the violation of liver function. 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), including those accompanied by a sense of anxiety);

- obsessive-compulsive disorder (OCD);

- panic disorder;

- post-traumatic stress disorder (PTSD).

Contraindications:

- Hypersensitivity to the active substance or other ingredients included in the preparation;

- joint use of sertraline and MAO inhibitors (monoamine oxidase). When replacing one drug with another, one should refrain from taking antidepressants within 14 days;

- joint use of sertraline with tryptophan or fenfluramine;

- unstable epilepsy;

- children's age till 6 years;

- pregnancy and lactation.

Carefully:

Neurological disorders (including mental retardation), manic conditions, epilepsy, hepatic and / or renal failure, weight loss, children older than 6 years.

Pregnancy and lactation:

There are no controlled results of the use of sertraline in pregnant women, so it is necessary to prescribe them only if the expected benefit for the mother exceeds the potential risk for the fetus. 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.

Dosing and Administration:Inside, regardless of food intake.

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, increased from 50 mg to a maximum daily dose of 200 mg.

Panic disorder of PTSD

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, 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, the drug should be taken regularly for 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 further preserved as a supporting one.

Children

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, increased from 50 mg to a maximum daily dose of 200 mg. To avoid overdosage, less weight in children should be taken into account compared with adults, and with an increase in the dose of more than 50 mg / day, careful monitoring of this category of patients is necessary and at the first signs of an overdose, discontinue the drug.

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

Patients with impaired hepatic function require special attention in the treatment of sertraline. In severe liver function disorder, the dose of the drug should be reduced or the intervals between administrations should be increased.

In patients with impaired renal function specially to select a dose is not required.

Side effects:

On the part of the digestive system: dry mouth, decreased appetite (rarely increased), up to anorexia, dyspeptic disorders (flatulence, nausea, vomiting, diarrhea or unstable stools, constipation), stomach cramps, abdominal pain, pancreatitis, hepatitis, jaundice or liver failure.

From the nervous system: drowsiness, headache, dizziness, tremor, insomnia, anxiety, agitation, hypomania, mania, akathisia, paresthesia, symptoms of depression, hallucinations, aggressiveness, agitation, anxiety, psychosis, gait disorders, extrapyramidal disorders, dyskinesias, tremors, convulsions. Motor disorders were more often observed in patients with indications of their presence in an anamnesis or with the concomitant use of antipsychotics.

From the genitourinary system: ejaculation delay, decreased libido and / or libido, erectile dysfunction, anorgasmia, menstrual disorders, gynecomastia, priapism, hyperprolactinaemia, galactorrhea.

On the part of the respiratory system: choking or feeling "squeezing the chest."

From the cardiovascular system: heart palpitations, chest pain, hypertension, arterial hypotension, swelling, fainting and tachycardia (very rarely).

From the sense organs: impaired vision (including blurred vision).

Allergic reactions: redness of the skin, urticaria, swelling of the eyelids, face or lips, skin rash, generalized itching, multiforme exudative erythema.

Laboratory data: reversible increase in transaminase activity, thrombocytopenia, leukopenia, transient hyponatremia (syndrome of inadequate secretion of antidiuretic hormone, more often in elderly patients, as well as with the intake of diuretics or a number of other drugs).

Other: sporadic bleeding (including nasal), hypothyroidism, increased sweating, weight loss, weakness, yawning, "tides" of blood to the face.

With the cessation of sertraline treatment, a "cancellation" syndrome may occur.

Overdose:

Symptoms: serotonin syndrome - nausea, vomiting, drowsiness, ECG changes, mydriasis, tachycardia, agitation, dizziness, anxiety, psychomotor agitation, diarrhea, increased sweating, myoclonus and hyperreflexia.

Treatment symptomatic: ensuring the normal patency of the airways (oxygenation and ventilation of the lungs) and monitoring the heart rate and vital organs and systems. It is not recommended to induce vomiting. The introduction of activated charcoal and sorbitol can be more effective than gastric lavage. There are no specific antidotes. 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 selective MAOIs with reversible type of action - selegiline and 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 arise: hyperthermia, stiffness, convulsions, myoclonus, lability in the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular system), changes in mental status, including increased irritability, marked agitation, confusion, which in some cases may go into a delirious state or to whom.

Medicines that depress the central nervous system and ethanol. The combined use of sertraline and substances depressing the central nervous system requires close attention, as well as the use of alcohol during the treatment with sertraline.

Coumarin derivatives - when they are co-administered with sertraline, there is a significant increase in prothrombin time - in these cases it is recommended to monitor prothrombin time at the 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.

Medicines metabolized by isoenzyme 2D6 cytochrome P450: long-term 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 the study of interaction in vitro showed that the isoenzyme CYP 3A3 / 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 do 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 does not depress isoenzyme CYP2C9.

Sertraline does not affect the concentration of diazepam in serum, indicating that there is no inhibition of isoenzyme CYP 2C19. According to research in vitro 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 enzymes in the liver. Sertraline causes minimal induction of liver enzymes. Simultaneous administration of sertraline and antipyrin at a dose of 200 mg leads to a significant decrease in the half-life of antipyrine, although this occurs in only 5% of cases.

Atenolol: when co-administered sertraline does not change its β-adrenergic blocking action.

Glibenclamide and digoxin: with the introduction of sertraline in a daily dose of 200 mg of drug interaction with these drugs is not revealed.

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.

Women of childbearing age during treatment should use adequate methods of contraception.

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

The appointment of sertraline, as a rule, is not accompanied by a violation of 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, film-coated, 50 mg and 100 mg.

Packaging:

7 tablets in a blister pack. For 4 blisters in a cardboard pack together with instructions for use.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:П N014474 / 01

Date of registration:10.04.2008 / 31.05.2017

Expiration Date:Unlimited

The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO

Manufacturer: & nbsp

KRKA, d.d. Slovenia

Representation: & nbspKRKA KRKA Slovenia

Information update date: & nbsp11.10.2017

Illustrated instructions

Instructions

Asentra® (Asentra®)