Pharmacological properties
Sertraline ((1 s-cis) -4-(3,4-dichlorophenyl) -1,2,3,4-tetrahydro-n-methyl-1-naphthalenamine hydrochloride) is a selective serotonin reuptake inhibitor in the brain, is a derivative of naphthylamine. It has practically no effect on the neuronal uptake of noradrenaline and dopamine. It does not have specific affinity for adreno- and m-cholinoreceptors, GABA receptors, dopamine, histamine, serotonin or benzodiazepine receptors. It does not inhibit MAO. It causes anorexia, and is effective in obsessive-compulsive disorders.
When taken orally in doses of 50-200 mg 1 time per day for 14 days, the maximum concentration in the blood is reached after 4.5-8.5 hours. The average half-life is 22-36 hours, thus an approximately twofold accumulation of sertraline is observed before reaching an equilibrium state after 1 week of treatment. Binding to blood plasma proteins is about 98%, the volume of distribution is 20 l/kg of body weight. It is intensively metabolized during the first passage through the liver. The main metabolite of sertraline - N-desmethylsertraline - is almost 20 times inferior in activity to sertraline in vitro and is virtually inactive in models of depression in vivo. Sertraline and N-desmethylsertraline are actively biotransformed in the body, the metabolites formed are excreted with feces and urine in equal amounts. Unchanged sertraline is excreted in the urine in insignificant amounts (0.2%). Food intake does not significantly affect the bioavailability of the drug. The pharmacokinetics of sertraline in the elderly and adolescents do not differ significantly from the pharmacological profile of the drug in adults.
Indication
Treatment of depressive states of various genesis in patients with mono- and bipolar affective disorders. Prevention of relapses of depressive episodes.
Application
The recommended dose of the drug for adults is 50 mg once a day, if necessary, the dose can be increased to 200 mg/day for several weeks. The effect appears 7 days after the start of treatment, reaching a maximum after 2-3 weeks.
Patients with impaired liver and kidney function Sertraloft should be prescribed in lower doses. The initial dose of Sertraloft for the treatment of children aged 12-17 years with obsessive-compulsive disorders should not exceed 50 mg/day, subsequently, with insufficient therapeutic efficacy, the dose can be increased, but not more than 100 mg/day. Given the rather long half-life of the drug, the dose should not be changed more often than once a week. In elderly patients, Sertraloft is used in the same doses as for young patients.
Contraindication
Hypersensitivity to sertraline, pregnancy and breastfeeding, children's age (up to 12 years), simultaneous use of MAO inhibitors; severe liver and kidney dysfunction; convulsive states (unstable epilepsy).
Side effects
From the side of the central nervous system: dizziness, drowsiness, headache, insomnia, fatigue, weakness, tremor are possible; rarely - manic or hypomanic state, anxiety, restlessness, visual disturbances.
From the cardiovascular system: rarely - skin hyperemia with a feeling of heat or warmth, tachycardia.
On the part of the digestive system: possible loss of appetite, diarrhea, dry mouth, nausea, stomach or intestinal spasm, flatulence; rarely - constipation, vomiting.
Other: increased sweating, decreased potency, allergic reactions (fever, skin rash, itching) are possible. During treatment with Sertraloft, an asymptomatic increase in the activity of aminotransferases (AST and ALT) is possible. These disorders are rare and quickly disappear after drug withdrawal. In elderly patients and patients receiving diuretics and other drugs, hyponatremia may develop. After sertraline withdrawal, sodium levels return to normal.
Special instructions
Use with caution in case of drug abuse or dependence in history, liver and kidney dysfunction, epileptic seizures, weight loss. Should not be taken by patients who have undergone electroconvulsive therapy. Sertraloft can be used no earlier than 14 days after discontinuation of MAO inhibitors.
Sertraline is not recommended for use in patients with unstable epilepsy, and patients with controlled epilepsy should be closely monitored during treatment. If seizures occur, the drug should be discontinued.
Women of reproductive age should use adequate methods of contraception during treatment with Sertraloft. The use of the drug during breastfeeding is possible only on the advice of a doctor; it is recommended to decide on the termination of breastfeeding.
During treatment, you should refrain from drinking alcohol and avoid activities that require increased attention and quick reactions.
When Sertraloft is used simultaneously with drugs that have a high degree of protein binding, especially with digitoxin and warfarin, it is possible to increase the concentration of free (unbound) active substances in the blood plasma and increase the risk of developing the corresponding undesirable side effects. Sertraloft cannot be used in combination with MAO inhibitors, including selective (selegiline) and reversible (moclobemide), as well as in patients who have recently stopped taking an antidepressant and started taking an MAO inhibitor. Sertraloft can be used no earlier than 14 days after the end of treatment with MAO inhibitors. Caution should be exercised when replacing sertraline with other selective serotonin reuptake inhibitors, especially if the patient has been receiving drugs with a long half-life (for example, fluoxetine). It is necessary to avoid simultaneous administration of sertraline and carbamazepine, haloperidol or phenytoin. Simultaneous administration of sertraline and alcohol is contraindicated.
Sertraline should not be used concomitantly with tricyclic antidepressants, H1 and H2 receptor blockers, tranquilizers, coumarin anticoagulants, sulfonylurea derivatives, and digoxin.
When used simultaneously with cimetidine, a significant decrease in sertraline clearance is possible. Sertraline inhibits the biochemical activity of cytochrome P450 2D6, therefore, an increase in the plasma concentration of drugs metabolized by this enzyme, including tricyclic antidepressants and class IC antiarrhythmic drugs, is possible.
When Sertraline is used concomitantly with lithium, a pharmacodynamic interaction is possible, which is believed to be associated with serotonergic mechanisms and is clinically manifested by increased tremor; however, the pharmacokinetics of lithium are not significantly changed.
Overdose
Possible increase in side effects of the drug.
Treatment: ensuring airway patency (oxygenation and ventilation of the lungs), gastric lavage, administration of emetics, activated charcoal with sorbitol. Monitoring of heart and liver function is necessary.
Storage conditions
In a dry, dark place at a temperature not exceeding 25 °C.
