1 tabl powl. contains 12.5 mg of tianeptine sodium.
Action:
Antidepressant. It increases the potential of electrical activity of the hippocampus pyramidal cells and restores its activity after its prior inhibition by the disease. Tianeptine, in contrast to other tricyclic antidepressants, increases the re-uptake of serotonin in the cortex and nerve cells of the hippocampus. In addition, it increases the metabolism of Dopamine in the brain and inhibits the release of acetylcholine. Tianeptine occupies an intermediate position between stimulant and sedative antidepressants. It affects the somatic disorders, especially gastrointestinal, associated with phobias and mood disorders. It absorbs quickly and almost entirely in the gastrointestinal tract (bioavailability is 99%) and is not subject to the first-pass effect. Cmax achieved within 1-2 h after administration. In about 95-96% it is bound to plasma proteins. It is metabolized by β-oxidation and (to a lesser extent) via N-demethylation in the liver, as well as in other locations (eg in plasma, kidneys). The pentanoic acid derivative (MC5) is the main active metabolite, the propionic acid derivative (MC3) is an inactive metabolite. Biotransformation of tianeptine occurs without the participation of cytochrome P-450. It is excreted in the urine, mainly in the form of metabolites; in about 15% with bile. T0,5 tianeptine in the elimination phase is 2.5-3 h, whereas for the active metabolite MC5 - 7-8 h. In patients with renal insufficiency and in the elderly T0,5 the drug is longer.
Contraindications:
Hypersensitivity to tianeptine sodium or to any of the excipients. Concomitant use of non-selective MAO inhibitors.
Precautions:
The drug should not be used to treat children and adolescents <18 years - no data on the safety of use, depth. the effects of the drug on growth, maturation, cognitive and behavioral development, moreover, in children and adolescents treated with antidepressants, suicide (suicide attempts and suicidal thoughts) and hostility (especially aggression, oppositional and rebellious behavior) were more frequently observed; if a decision to treat is based on the existing clinical need, the patient should be closely monitored for signs of suicide. All patients treated with tianeptine should be monitored for signs of suicidal ideation and behavior (especially in the initial phase of treatment and after the change of the dose); this applies especially to patients <25 years of age and patients with history of suicidal behavior or thoughts. Tianeptine should be discontinued 24-48 h before general anesthesia. In the case of emergency procedures, surgery may be performed regardless of the time of the last dose, but the patient should be carefully monitored during the postoperative period. Patients with a history of drug or alcohol addiction should be closely monitored to avoid increasing the dose.
Pregnancy and lactation:
Do not use during pregnancy and breast-feeding.
Side effects:
Common: anorexia nervosa, nightmares, insomnia, lethargy, dizziness, headache, collapse, tremors, blurred vision, tachycardia, palpitations, tachycardia, precordial pain (chest pain), hot flushes, shortness of breath, dryness mouth, constipation, abdominal pain, nausea, vomiting, dyspepsia, diarrhea, bloating, heartburn, back pain, muscle pain, asthenia, throat suppression. Uncommon: rash (maculopapular or erythematous), pruritus, urticaria. Rare: drug abuse and addiction (especially in patients <50 years of age and with alcohol or drug addiction). There are data on individual cases regarding the perception of suicide attempts and suicidal behavior during or early after treatment with tianeptine.
Dosage:
Orally. Adults: the recommended dose is 1 tablet. 3 times a day (in the morning, noon and evening), before meals. No dose adjustment is needed for alcohol addicted patients with or without cirrhosis liver. In patients over 70 years.and in the case of renal failure the dose should be reduced to 2 tablets. per day.
(C)
