Pharmacodynamics
Antidepressant, naphthylamine derivative. Selective serotonin reuptake blocker in the brain. The neuronal uptake of norepinephrine and dopamine is practically not affected. It does not have a specific affinity for adrenergic and m-cholinergic receptors, GABA receptors, dopamine, histamine, serotonin or benzodiazepine receptors. Does not inhibit MAO. Causes anorexia, effective in obsessive conditions.
Pharmacokinetics
When oral administration of sertraline in doses of 50-200 mg 1 time / day for 14 days, Cmax in plasma is reached after 4.5-8.4 hours. The average T1 / 2 in young and old men and women is 22-36 hours. Accordingly, the elimination half-life is observed approximately two-fold cumulation of the active substance until equilibrium is reached after 1 week of treatment. Binding to plasma proteins is about 98%, Vd - 20 l / kg. Intensively metabolized during the first passage through the liver. The main metabolite found in plasma, N-desmethylsertraline, has weak pharmacological activity.
T1 / 2 of N-desmethylsertraline varies between 62-104 hours. It is excreted mainly through the intestines and with urine in equal amounts in the form of metabolites, less than 0.2% is excreted in the urine unchanged.
Contraindications
Concomitant use with MAO inhibitors, hypersensitivity to sertraline.
Pregnancy and lactation
Adequate and well-controlled studies of the safety of sertraline during pregnancy have not been conducted, therefore, use is possible only in cases where the expected benefits to the mother outweigh the possible risk to the fetus.
It is not known whether sertraline is excreted in breast milk, so it is not recommended for use during lactation. Separate studies have shown that in infants whose mothers received sertraline during feeding, their plasma levels are negligible or not determined, while the concentrations in breast milk exceed the concentrations in the mother's blood.
Women of childbearing age should use reliable methods of contraception during treatment with sertraline.
In experimental studies, no teratogenic and mutagenic effects of sertraline were detected. However, at doses approximately 2.5-10 times the maximum daily clinical dose, sertraline caused a delay in the ossification of the fetal bone tissue, possibly as a result of an effect on the maternal individual. With the introduction of sertraline in doses approximately 5 times the maximum clinical dose, a decrease in the survival rate of newborns was observed.
Side effects
From the side of the central nervous system: dizziness, drowsiness, headache, insomnia, feeling tired, weakness, tremor; rarely - manic or hypomanic state, anxiety, anxiety, visual impairment.
From the cardiovascular system: rarely - redness of the skin with a sensation of heat or heat, a feeling of palpitations.
From the digestive system: decreased appetite, diarrhea, dry mouth, nausea, cramps in the stomach or intestines, flatulence; rarely - constipation, vomiting.
From the side of metabolism: increased sweating.
From the reproductive system: rarely - decreased potency.
Allergic reactions: rarely - fever, skin rash, urticaria, or itching.
Interaction
With the simultaneous use of coumarin derivatives with anticoagulants, the prothrombin time significantly increases.
With the simultaneous use of sertraline can displace other drugs from the connection with plasma proteins, as a result of this, the plasma concentration of the corresponding active substance increases and the risk of side effects increases.
With simultaneous use with drugs whose metabolism occurs with the participation of the CYP2D6 isoenzyme, an increase in the plasma concentration of these drugs is possible due to inhibition of the CYP2D6 isoenzyme under the influence of sertraline.
With the simultaneous use of MAO inhibitors (including selegiline, moclobemide), the development of serotonin syndrome (hyperthermia, muscle rigidity, myoclonus, as well as manifestations of instability of the mental and physiological state of the body, up to the development of delirium and coma) is possible.
With simultaneous use with lithium salts, tremor may increase. With simultaneous use with desipramine, an increase in the concentration of desipramine in blood plasma is possible; with cimetidine - a significant decrease in sertraline clearance.
Dosage and administration
Inside - 50 mg 1 time / day, if necessary, the dose can be increased to 200 mg / day for several weeks. The effect manifests itself 7 days after the start of treatment, reaching a maximum after 2-3 weeks.
Special instructions
It is used with caution in case of drug abuse or dependence on history, impaired liver function, impaired renal function, epileptic seizures, weight loss.
Should not be used in patients undergoing electroshock therapy. The use of sertraline is possible no earlier than 14 days after the withdrawal of MAO inhibitors.
During the period of treatment do not allow the use of alcohol.
Safety in pediatrics has not been established.
Influence on the ability to drive vehicles and control mechanisms
During the treatment period, activities requiring increased attention and a high speed of psychomotor reactions should be avoided.
