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Active ingredients
Sertraline
Release form
Pills
Composition
1 tablet contains: Active substance: sertraline hydrochloride 55.95 mg, which corresponds to the content of sertraline 50 mg. Additional substances: magnesium stearate, hydroxypropylcellulose, sodium starch glycolate, calcium dihydrophosphate, microcrystalline cellulose, talc. Composition of the shell: Opadry 03H28758 (hygromolate, microcrystalline cellulose, talc. talc, propylene glycol).
Pharmacological effect
Antidepressant. Specific serotonin reuptake inhibitor (5-HT) in neurons. The metabolism of norepinephrine and dopamine has little effect. At therapeutic doses, sertraline blocks serotonin uptake in human platelets. The drug does not have a stimulating, sedative or anticholinergic action. It does not have an affinity for serotonin, dopamine, histamine, benzodiazepine, GABA, cholino and adrenoreceptors. The antidepressant effect is noted by the end of the second week of regular administration of Ascentra, whereas the maximum effect is achieved only after 6 weeks. Unlike tricyclic antidepressants, it does not appear as Asentra weight gain; in some cases, a decrease in it has been noted. The drug does not cause mental or physical drug dependence.
Pharmacokinetics
Absorption After taking the drug inside sertraline is slowly absorbed from the gastrointestinal tract, Cmax in plasma is reached after 4.5-8.4 hours. The distribution of Css is established within a week with a daily intake of 1 time / day. The binding of sertraline to plasma proteins is 98%. Vd> 20 l / kg. Sertralin is excreted in breast milk. There is no data on its ability to penetrate the placental barrier. Metabolism and elimination Sertralin undergoes intensive biotransformation during the first passage through the liver by N-demethylation. The main metabolite, N-desmethylsertraline, is less active than the parent compound. Metabolites are excreted in urine and feces in equivalent amounts. About 0.2% of sertraline is excreted by the kidneys unchanged. T1 / 2 of the drug is 22-36 hours and does not depend on the age or gender of patients. For N-desmethylsertraline T1 / 2 - 62-104 hours. Pharmacokinetics in special clinical situations of T1 / 2 and AUC in the blood plasma increase with abnormal liver function. Parametlin parameters of sertraline pharmacokinetics in patients with mild and moderate renal impairment (CC 20-50 ml / min)and with severe impaired renal function (CC <20 ml / min) do not change with its constant use. Sertralin is not eliminated during dialysis.
Indications
Regular hygiene of the ears. Dissolution of sulfur plugs. Prevention of the formation of sulfur plugs.
Contraindications
Simultaneous intake of MAO inhibitors and within 14 days after their cancellation. Simultaneous use of tryptophan or fenfluramine. Unstable epilepsy. Baby under 6 years old. Pregnancy. Lactation (breastfeeding). Increased sensitivity to components of the drug. (including mental retardation), manic states, epilepsy, liver and / or renal failure, weight loss, for children over 6 years old.
Use during pregnancy and lactation
Adequate and strictly controlled clinical studies on the safety of sertraline use during pregnancy have not been conducted. The purpose of the drug is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. Women of childbearing age should be advised to use effective contraceptives during use. Sertralin is found in breast milk. If necessary, the appointment of the drug during lactation should stop breastfeeding due to the lack of reliable data on the safety of sertraline use during this period.
Dosage and administration
For depression and OCD in adults: the average initial dose is 50 mg 1 time per day, in the morning or in the evening. The daily dose can be gradually, not earlier than in a week, increased from 50 mg to a maximum daily dose of 200 mg. In panic disorders and PTSD: the initial dose of Asentra is 25 mg 1 time / day, in the morning or in the evening. After a week, you can increase the dose to 50 mg 1 time / day, and then gradually, not earlier than in a week, increase to a maximum daily dose of 200 mg. For children aged 6 to 12 years: the initial dose of Asentra is 25 mg of sertraline 1 time per day, in the morning or in the evening. A week later, you can increase the dose to 50 mg 1 time / day. For children aged 12 to 17 years: the initial dose is 50 mg 1 time per day, in the morning or in the evening. If necessary, the daily dose can be gradually, not earlier than in a week, increased from 50 mg to a maximum daily dose of 200 mg.To avoid overdose, lower body weight in children compared with adults should be taken into account, and increasing the dose to more than 50 mg / day requires careful monitoring of this category of patients: the first signs of overdose should be discontinued. A satisfactory therapeutic result is usually achieved after 7 days from the start of treatment. However, to achieve the full therapeutic effect requires regular intake of the drug for 2-4 weeks. In patients with OCD, it may take 8-12 weeks to achieve a good result. The minimum dose that provides a therapeutic effect is further maintained as supportive. In elderly patients: there is no need for special dose selection. In the event of abnormal liver function: the drug should be administered with caution. In severely impaired liver function, the dose of the drug should be reduced or the intervals between intakes should be increased. In patients with impaired renal function: a special correction of the dosage regimen is not required.
Side effects
CNS and peripheral nervous system: dry mouth, sweating, drowsiness, headache, dizziness, tremor, anxiety, agitation, hypomania, mania, insomnia, loss of appetite (rarely - increased), up to anorexia, weakness, motor restlessness From the digestive system: flatulence, nausea, vomiting, diarrhea, abdominal pain; rarely (0.8%) with long-term use - asymptomatic increase in transaminase activity in the blood serum (normalizing with the abolition of the drug). Other: visual disturbances, redness, ejaculation disorders, decreased libido, weight loss. From laboratory indicators: reversible hyponatremia (more often in the elderly, as well as when taking diuretics or a number of other drugs) associated with the syndrome of inadequate secretion of ADH. When using the drug in isolated cases, extrapyramidal disorders were noted dyskinesias, tremor, convulsions, menstrual disorders, hyperprolactinemia, galactorrhea, skin rash; occasionally - erythema multiforme. Movement disorders were more frequently observed in patients with indications of their presence in history or with concomitant use of antipsychotic drugs. Discontinuation syndrome rarely occurs when the drug is discontinued. Paresthesias, hypesthesia, symptoms of depression, hallucinations, aggressive reactions, agitation, anxiety, or symptoms of psychosis are possible.These manifestations are difficult to differentiate from the symptoms of the underlying disease, and they can occur when other antidepressants are used.
Overdose
Symptoms: Serotonin syndrome may occur with nausea, vomiting, drowsiness, tachycardia, agitation, dizziness, psychomotor agitation, diarrhea, sweating, myoclonus, hyperreflexia. Severe symptoms were not detected even with the use of the drug in high doses. However, when taken simultaneously with other drugs or ethanol, severe poisoning can occur, sometimes fatal. Treatment: There are no specific antidotes. If necessary, intensive supportive therapy and monitoring of the state of vital body functions. The introduction of activated carbon may be more effective than gastric lavage, artificial vomiting is not recommended. It is necessary to maintain airway patency. Forced diuresis, dialysis, hemoperfusion, or blood transfusion may be unsuccessful (due to the large volume of distribution of sertraline).
Interaction with other drugs
With simultaneous use of sertraline and MAO inhibitors (including selectively acting MAO inhibitors with a reversible type of action - selegiline and moclobemide), serotonin syndrome may develop: hyperthermia, rigidity, myoclonus, lability of the autonomic nervous system (rapid fluctuations in the parameters of the respiratory and cardiovascular systems), changes mental status, including irritability, marked excitement, confusion, which in some cases can turn into a delirious state or anyone (this combination is contraindicated). Similar complications (sometimes fatal) occur when prescribing MAO inhibitors during treatment with antidepressants that inhibit the neuronal seizure of monoamines or immediately after their withdrawal. In healthy volunteers, the use of sertraline 200 mg / day does not affect the effect of ethanol, carbamazepine or haloperidol, and also on mental activity and psychomotor activity (however, the combined prescription of sertraline and drugs that depress the central nervous system requires close attention,a simultaneous use with ethanol and ethanol-containing drugs is contraindicated). When administering indirect anticoagulants (coumarin derivatives) with sertraline together, a significant increase in the prothrombin time is observed (control of the prothrombin time is required at the beginning of sertraline and after its withdrawal). Pharmacokinetic interaction. other drugs that bind to plasma proteins (diazepam, tolbutamide and warfarin). The use of the drug with cimetidine significantly reduces the clearance of sertraline. Long-term administration of sertraline 50 mg / day with desipramine (a drug that is metabolized by the CYP2D6 isoenzyme) is accompanied by an increase in the concentration of desipramine in the blood plasma. In vitro experiments established that carried out by the CYP3A3 isoenzyme / 4 betahydroxylation of endogenous cortisol, as well as the metabolism of carbamazepine and terfenadine with a prolonged appointment of sertraline at a dose of 200 mg / day do not change. The concentration in plasma cr With long-term administration of sertraline at a dose of 200 mg / day, tolbutamide, phenytoin and warfarin do not change, therefore, it can be concluded that sertraline does not inhibit the CYP2C9 isoenzyme. Sertralin does not affect the serum diazepam concentration, which indicates the absence of CYP2C19 isoenzyme inhibition. According to in vitro studies, sertraline has virtually no effect or is minimally inhibited by the CYP1A2 isoenzyme. The lithium pharmacokinetics are not statistically significantly altered with the concomitant administration of sertraline; but tremor occurs more often, which suggests the possibility of pharmacodynamic interaction (this combination requires caution). Sertraline should also be used with caution with other drugs that affect serotonergic transmission. When replacing one inhibitor of neuronal uptake with another, there is no need for a laundering period. However, care is required when changing the course of treatment. Co-administration of tryptophan or fenfluramine with sertraline should be avoided. In clinical studies, sertraline has been shown to cause minimal induction of liver enzymes.The simultaneous administration of sertraline 200 mg and antipyrine leads to a significant decrease in antipyrine T1 / 2 (this change is detected only in 5% of observations). When co-administered sertraline does not affect the beta-adrenoceptor blocking effect of atenolol. interactions with glibenclamide and digoxin were not detected.
special instructions
According to clinical studies, the drug sertraline is effective and safe in the treatment of depression in patients after myocardial infarction and in patients with unstable angina. Placebo-controlled studies have shown the efficacy and safety of sertraline in patients with diabetes mellitus. Sertralin is not administered together with MAO inhibitors, and also for 14 days after discontinuation of treatment with MAO inhibitors; after the abolition of sertraline, MAO inhibitors are not prescribed for 14 days. Patients with depression are at risk for suicidal attempts. This danger persists until the development of remission. Therefore, from the start of treatment and until the optimum clinical effect is achieved, permanent medical observation of the patient should be established. Currently, there is not enough experience with sertraline in patients undergoing electroconvulsive therapy. The possible success or risk of such a combination treatment has not been studied. Effect on the ability to drive motor vehicles and control mechanisms The purpose of sertraline is not accompanied by impaired psychomotor functions. However, its use simultaneously with other drugs can lead to impaired attention and coordination of movements. Therefore, it is not recommended to drive vehicles during sertraline therapy or engage in activities associated with increased risk.