Release form, composition and packing
Tablets, film-coated white, round with beveled edges and a notch on the one hand, on a break - a white rough mass.
1 tab. sertraline hydrochloride, 55.95 mg, which corresponds to the contents of sertraline 50 mg.
Excipients: magnesium stearate, hydroxypropyl cellulose, sodium starch glycolate, calcium dihydrogen phosphate, microcrystalline cellulose, talc. The composition of the shell: Opadry 03H28758 (hypromellose, titanium dioxide, talc, propylene glycol).
Tablets, film-coated white, round with beveled edges and a notch on the one hand, on a break - a white rough mass.
1 tab. sertraline hydrochloride, 111.9 mg, which corresponds to the contents of sertraline 100 mg.
Excipients: magnesium stearate, hydroxypropyl cellulose, sodium starch glycolate, calcium dihydrogen phosphate, microcrystalline cellulose, talc. The composition of the shell: Opadry 03H28758 (hypromellose, titanium dioxide, talc, propylene glycol).
Clinico-pharmacological group: Antidepressant.
Pharmacological action
Antidepressant. Specific serotonin reuptake inhibitor (5-HT) in neurons. On the metabolism of norepinephrine and dopamine affects only slightly. At therapeutic doses, sertraline blocks the capture of serotonin in human platelets.
The drug has no stimulating, sedative or anticholinergic action. Has no affinity for serotonin, dopamine, histamine, benzodiazepine, GABA, holino-and adrenoreceptors. Antidepressant effect is noted at the end of the second week of the regular intake Asentry, while the maximum effect is achieved only after 6 weeks. Unlike tricyclic antidepressants in the appointment Asentry no increase in body weight in some cases, noted its decline. The drug does not cause mental or physical drug dependence.
Pharmacokinetics
Suction
After receiving the drug inside sertraline slowly absorbed from the gastrointestinal tract, Cmax plasma levels reached after 4.5-8.4 hours
Distribution
Css installed within a week with a daily intake of 1 time per day. Linking sertraline plasma protein is 98%. Vd> 20 L / kg. Sertraline is excreted in breast milk. Data on its ability to penetrate through the placental barrier is not.
Metabolism and Elimination
Sertraline undergoes intense biotransformation in the "first pass" through the liver by N-demethylation. The main metabolite - N-desmetilsertralin - less active than the parent compound. Metabolites are excreted in urine and feces in equivalent amounts. About 0.2% of sertraline excreted by the kidneys unchanged. T1 / 2 of the drug is 22-36 hours and does not depend on age or sex of patients. For N-desmetilsertralina T1 / 2 - 62-104 hours
Pharmacokinetics in special clinical situations
T1 / 2 and AUC in plasma increase with impaired liver function. Pharmacokinetic parameters of sertraline in patients with both mild and moderate renal impairment (creatinine clearance 20-50 ml / min) or with severe renal impairment (creatinine clearance <20ml/min) do not change when it is used consistently. Sertraline does not appear in dialysis.
Statement
treatment and prevention of depression of various etiologies;
treatment of obsessive-compulsive disorder (OCD);
treatment of panic disorder;
posttraumatic stressful disorders (PTSD).
Dosing regimen
In depression and OCD in adults average initial dose is 50 mg 1 time per day, morning or evening. Daily dosage may be gradually, not a week before increasing to 50 mg to a maximum daily dose of 200 mg.
In panic disorder and PTSD Asentry initial dose is 25 mg 1 time per day, morning or evening. After a week can increase the dose to 50 mg 1 time per day, and then gradually, not earlier than one week, increasing to a maximum daily dose of 200 mg. The initial dose Asentry for children aged 6 to 12 years is 25 mg of sertraline, 1 time per day, morning or evening. After a week can increase the dose to 50 mg 1 time per day.
For children aged 12 to 17 years starting dose is 50 mg 1 time per day in the morning or evening.
If necessary, the daily dose can be gradually, not earlier than one week, increasing from 50 mg to a maximum daily dose of 200 mg. To avoid an overdose should be taken into account the smaller body weight in children than adults, and with increasing doses of 50 mg / day should be closely monitored for this category of patients: the first signs of an overdose of the drug should be discontinued. Satisfactory therapeutic result is achieved usually within 7 days of starting treatment. However, to achieve full therapeutic effect requires taking regular medication for 2-4 weeks.
In patients with OCD in order to achieve a good result may require 8-12 weeks. The minimum dose that provides therapeutic effect persists in the future as a support. Elderly patients do not need a special dose adjustment.
When hepatic dysfunction drug should be used with caution.
In severe hepatic dysfunction drug dose should be reduced or increased intervals between doses. In patients with impaired renal function special correction dosing regimen is not required.
Side effect
CNS and peripheral nervous system: dry mouth, increased sweating, drowsiness, headache, dizziness, tremor, anxiety, agitation, hypomania, mania, insomnia, decreased appetite (rare - increasing), until anorexia, weakness, motor restlessness .
From the digestive system: flatulence, nausea, vomiting, diarrhea, abdominal pain, rarely (0.8%) with prolonged use - asymptomatic increase of transaminase activity in serum (normalizing to remove the drug).
Other: blurred vision, redness of the skin, disorders of ejaculation, decreased libido, weight loss.
From the laboratory parameters: a reversible hyponatremia (often in the elderly, as well as taking diuretics or some other drug) associated with the syndrome of inappropriate secretion of ADH. Using the drug in individual cases were marked extrapyramidal disorders, dyskinesias, tremors, convulsions, menstrual disorders, hyperprolactinemia, galactorrhea, skin rash, occasionally - erythema multiforme. Movement disorders were more common in patients with indications of their presence in history, or with concomitant use of antipsychotic drugs.
Discontinuation of the drug withdrawal syndrome is rare. There are paresthesias, hypesthesia, symptoms of depression, hallucinations, aggressive reaction, psychomotor agitation, anxiety or psychotic symptoms. These manifestations are difficult to differentiate from symptoms of the underlying disease, and they may arise in the application and other antidepressants.
Contraindications
concomitant use of MAO inhibitors and within 14 days after their withdrawal;
concurrent use of tryptophan or fenfluramine;
unstable epilepsy;
Children under the age of 6 years;
pregnancy;
Lactation (breastfeeding);
hypersensitivity to the drug.
With carefully administered drug for neurological disorders (including mental retardation), manic states, epilepsy, liver and / or renal failure, weight loss, children over 6 years.
Pregnancy and lactation
Adequate and well-controlled clinical studies on safety of using sertraline during pregnancy has not been carried out. The drug is only possible if the intended benefits to the mother outweighs the potential risk to the fetus. Women of childbearing age during treatment should be encouraged to use effective contraception. Sertraline is detected in breast milk.
If necessary, use during lactation should stop breastfeeding due to lack of reliable data about the safety of sertraline in this period.
Use in hepatic dysfunction
When hepatic dysfunction drug should be used with caution. In severe hepatic dysfunction drug dose should be reduced or increased intervals between doses.
Use in renal impairment
In patients with impaired renal function special correction dosing regimen is not required.
Cautions
According to clinical studies the drug sertraline is effective and safe in treating depression in patients with myocardial infarction and in patients with unstable angina. Placebo-controlled trials demonstrated the efficacy and safety of sertraline in patients with diabetes. Sertraline is not prescribed in conjunction with MAO inhibitors, as well as within 14 days after cessation of treatment MAO inhibitors; after discontinuation of sertraline within 14 days of MAO inhibitors is not indicated.
Patients c depression are at risk for suicide attempts. This risk persists until the development of remission. Therefore, from the beginning of treatment and to achieve an optimal clinical effect should be to establish a permanent medical surveillance of the patient.
There is currently no adequate experience with sertraline in patients undergoing electroconvulsive therapy. The possible success or risk of such combination therapy has not been studied.
Tablets, film-coated white, round with beveled edges and a notch on the one hand, on a break - a white rough mass.
1 tab. sertraline hydrochloride, 55.95 mg, which corresponds to the contents of sertraline 50 mg.
Excipients: magnesium stearate, hydroxypropyl cellulose, sodium starch glycolate, calcium dihydrogen phosphate, microcrystalline cellulose, talc. The composition of the shell: Opadry 03H28758 (hypromellose, titanium dioxide, talc, propylene glycol).
Tablets, film-coated white, round with beveled edges and a notch on the one hand, on a break - a white rough mass.
1 tab. sertraline hydrochloride, 111.9 mg, which corresponds to the contents of sertraline 100 mg.
Excipients: magnesium stearate, hydroxypropyl cellulose, sodium starch glycolate, calcium dihydrogen phosphate, microcrystalline cellulose, talc. The composition of the shell: Opadry 03H28758 (hypromellose, titanium dioxide, talc, propylene glycol).
Clinico-pharmacological group: Antidepressant.
Pharmacological action
Antidepressant. Specific serotonin reuptake inhibitor (5-HT) in neurons. On the metabolism of norepinephrine and dopamine affects only slightly. At therapeutic doses, sertraline blocks the capture of serotonin in human platelets.
The drug has no stimulating, sedative or anticholinergic action. Has no affinity for serotonin, dopamine, histamine, benzodiazepine, GABA, holino-and adrenoreceptors. Antidepressant effect is noted at the end of the second week of the regular intake Asentry, while the maximum effect is achieved only after 6 weeks. Unlike tricyclic antidepressants in the appointment Asentry no increase in body weight in some cases, noted its decline. The drug does not cause mental or physical drug dependence.
Pharmacokinetics
Suction
After receiving the drug inside sertraline slowly absorbed from the gastrointestinal tract, Cmax plasma levels reached after 4.5-8.4 hours
Distribution
Css installed within a week with a daily intake of 1 time per day. Linking sertraline plasma protein is 98%. Vd> 20 L / kg. Sertraline is excreted in breast milk. Data on its ability to penetrate through the placental barrier is not.
Metabolism and Elimination
Sertraline undergoes intense biotransformation in the "first pass" through the liver by N-demethylation. The main metabolite - N-desmetilsertralin - less active than the parent compound. Metabolites are excreted in urine and feces in equivalent amounts. About 0.2% of sertraline excreted by the kidneys unchanged. T1 / 2 of the drug is 22-36 hours and does not depend on age or sex of patients. For N-desmetilsertralina T1 / 2 - 62-104 hours
Pharmacokinetics in special clinical situations
T1 / 2 and AUC in plasma increase with impaired liver function. Pharmacokinetic parameters of sertraline in patients with both mild and moderate renal impairment (creatinine clearance 20-50 ml / min) or with severe renal impairment (creatinine clearance <20ml/min) do not change when it is used consistently. Sertraline does not appear in dialysis.
Statement
treatment and prevention of depression of various etiologies;
treatment of obsessive-compulsive disorder (OCD);
treatment of panic disorder;
posttraumatic stressful disorders (PTSD).
Dosing regimen
In depression and OCD in adults average initial dose is 50 mg 1 time per day, morning or evening. Daily dosage may be gradually, not a week before increasing to 50 mg to a maximum daily dose of 200 mg.
In panic disorder and PTSD Asentry initial dose is 25 mg 1 time per day, morning or evening. After a week can increase the dose to 50 mg 1 time per day, and then gradually, not earlier than one week, increasing to a maximum daily dose of 200 mg. The initial dose Asentry for children aged 6 to 12 years is 25 mg of sertraline, 1 time per day, morning or evening. After a week can increase the dose to 50 mg 1 time per day.
For children aged 12 to 17 years starting dose is 50 mg 1 time per day in the morning or evening.
If necessary, the daily dose can be gradually, not earlier than one week, increasing from 50 mg to a maximum daily dose of 200 mg. To avoid an overdose should be taken into account the smaller body weight in children than adults, and with increasing doses of 50 mg / day should be closely monitored for this category of patients: the first signs of an overdose of the drug should be discontinued. Satisfactory therapeutic result is achieved usually within 7 days of starting treatment. However, to achieve full therapeutic effect requires taking regular medication for 2-4 weeks.
In patients with OCD in order to achieve a good result may require 8-12 weeks. The minimum dose that provides therapeutic effect persists in the future as a support. Elderly patients do not need a special dose adjustment.
When hepatic dysfunction drug should be used with caution.
In severe hepatic dysfunction drug dose should be reduced or increased intervals between doses. In patients with impaired renal function special correction dosing regimen is not required.
Side effect
CNS and peripheral nervous system: dry mouth, increased sweating, drowsiness, headache, dizziness, tremor, anxiety, agitation, hypomania, mania, insomnia, decreased appetite (rare - increasing), until anorexia, weakness, motor restlessness .
From the digestive system: flatulence, nausea, vomiting, diarrhea, abdominal pain, rarely (0.8%) with prolonged use - asymptomatic increase of transaminase activity in serum (normalizing to remove the drug).
Other: blurred vision, redness of the skin, disorders of ejaculation, decreased libido, weight loss.
From the laboratory parameters: a reversible hyponatremia (often in the elderly, as well as taking diuretics or some other drug) associated with the syndrome of inappropriate secretion of ADH. Using the drug in individual cases were marked extrapyramidal disorders, dyskinesias, tremors, convulsions, menstrual disorders, hyperprolactinemia, galactorrhea, skin rash, occasionally - erythema multiforme. Movement disorders were more common in patients with indications of their presence in history, or with concomitant use of antipsychotic drugs.
Discontinuation of the drug withdrawal syndrome is rare. There are paresthesias, hypesthesia, symptoms of depression, hallucinations, aggressive reaction, psychomotor agitation, anxiety or psychotic symptoms. These manifestations are difficult to differentiate from symptoms of the underlying disease, and they may arise in the application and other antidepressants.
Contraindications
concomitant use of MAO inhibitors and within 14 days after their withdrawal;
concurrent use of tryptophan or fenfluramine;
unstable epilepsy;
Children under the age of 6 years;
pregnancy;
Lactation (breastfeeding);
hypersensitivity to the drug.
With carefully administered drug for neurological disorders (including mental retardation), manic states, epilepsy, liver and / or renal failure, weight loss, children over 6 years.
Pregnancy and lactation
Adequate and well-controlled clinical studies on safety of using sertraline during pregnancy has not been carried out. The drug is only possible if the intended benefits to the mother outweighs the potential risk to the fetus. Women of childbearing age during treatment should be encouraged to use effective contraception. Sertraline is detected in breast milk.
If necessary, use during lactation should stop breastfeeding due to lack of reliable data about the safety of sertraline in this period.
Use in hepatic dysfunction
When hepatic dysfunction drug should be used with caution. In severe hepatic dysfunction drug dose should be reduced or increased intervals between doses.
Use in renal impairment
In patients with impaired renal function special correction dosing regimen is not required.
Cautions
According to clinical studies the drug sertraline is effective and safe in treating depression in patients with myocardial infarction and in patients with unstable angina. Placebo-controlled trials demonstrated the efficacy and safety of sertraline in patients with diabetes. Sertraline is not prescribed in conjunction with MAO inhibitors, as well as within 14 days after cessation of treatment MAO inhibitors; after discontinuation of sertraline within 14 days of MAO inhibitors is not indicated.
Patients c depression are at risk for suicide attempts. This risk persists until the development of remission. Therefore, from the beginning of treatment and to achieve an optimal clinical effect should be to establish a permanent medical surveillance of the patient.
There is currently no adequate experience with sertraline in patients undergoing electroconvulsive therapy. The possible success or risk of such combination therapy has not been studied.
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