Tianeptine (sodium salt) 12.5 mg for one coated tablet.
Excipients/Inactive Ingredients: D-mannitol, maize starch, talc, magnesium stearate.
Coating: ethylcellulose, glycerol oleate, SEPIFILM SE 700 White (povidone, sodium carmellose, anhydrous colloidal silica, talc, sucrose, polysorbate 80, titanium dioxide, sodium hydrogen carbonate), white beeswax.
Pharmacotherapeutic group: Other Antidepressants. ATC code: N06AX14.
Pharmacology: Pharmacodynamics: Tianeptine is an antidepressant.
In animals, tianeptine has the following properties: tianeptine increases the spontaneous activity of pyramidal cells in the hippocampus and accelerates their recovery after functional inhibition; tianeptine increases the rate of serotonin re-uptake by neurons in the cortex and hippocampus.
In man, tianeptine is characterised by: marked action on somatic complaints, especially gastrointestinal complaints related to anxiety and mood disturbances.
Moreover, tianeptine has no effect on: sleep and alertness; the cholinergic system (no anticholinergic symptoms).
Pharmacokinetics: Gastrointestinal absorption is rapid and complete.
Distribution is rapid, and is associated with a high level of protein binding (approximately 94%).
The molecule is extensively metabolised in the liver by the processes of beta-oxidation and N-demethylation.
The elimination of tianeptine is characterised by a short terminal half-life of 2½ h and by essentially renal excretion of the metabolites.
In elderly subjects: pharmacokinetics studies performed in chronically treated elderly patients (aged over 70 years) demonstrated an increase of one hour in the elimination half-life.
In subjects with hepatic insufficiency: studies have shown that the effects of chronic alcoholism on the pharmacokinetic parameters are negligible, even when the alcoholism is associated with cirrhosis of the liver.
In subjects with renal insufficiency: studies have shown an increase of one hour in the elimination half-life.
Toxicology: Preclinical safety data: A study demonstrated in rats a decrease in reproductive performance in females (increase in pre-implantation losses) at a maternotoxic dose of 45 mg/kg/day.
Major depressive episodes (i.e. typical).
The recommended dosage is one 12.5 mg tablet three times a day (morning, midday and evening) at the beginning of the main meals.
In chronic alcoholics, whether cirrhotic or not, no alteration of the dosage is necessary.
In subjects aged over 70 years, and in subjects with renal insufficiency, the dosage should be restricted to 2 tablets per day.
Symptoms: The experience concerning acute tianeptine intoxication cases (maximum quantity: 2250 mg, ingested in a single administration) have mainly revealed alertness disorders that may even cause coma, especially in case of multiple intoxication.
Treatment: There is no known specific tianeptine antidote. In case of acute intoxication, a symptomatic treatment and routine monitoring must be implemented. Medical monitoring in a specialised setting is recommended.
Hypersensitivity to tianeptine or to any of the excipients listed in Description.
Children and adolescents under 15 years old.
Association with MAOIs (see Interactions).
A wash-out period of two weeks is necessary between treatment with MAOIs and treatment with tianeptine. A wash-out period of only 24 hours is required when replacing tianeptine with a MAOI.
If general anaesthesia is necessary, the anaesthetist should be informed of the treatment, and the drug discontinued 24 or 48 hours prior to surgery.
In an emergency, surgery may be performed without an intervening wash-out period; peroperative monitoring should be performed.
As with any psychotropic drug, this medicinal product should not be taken with alcoholic beverages or medicines containing alcohol.
As with all psychotropic agents, if the treatment is to be interrupted, the dosage should be gradually reduced over a period of 7 to 14 days.
If there is a history of drug dependence or alcohol dependence, the patients must be kept under very close surveillance in order to avoid any increase in dosage.
Do not exceed the recommended doses.
This medicinal product contains sucrose. Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take this medicine.
Suicide/suicidal thoughts or clinical worsening: Depression is associated with an increased risk of suicidal thoughts, self-harm and suicide (suicidal behaviour). This risk persists until a significant remission has been obtained. Clinical improvement may not be obtained until after several weeks of treatment, so patients must be closely monitored until this improvement has been achieved. Clinical experience shows that the risk of suicide can increase during the very early stages of recovery.
Patients with a history of suicidal behaviour or those expressing significant suicidal thoughts before starting the treatment face a higher risk of the onset of suicidal thoughts or suicidal behaviour, and must be closely monitored during treatment. A meta-analysis of placebo-controlled clinical trials of the use of antidepressants in adults displaying psychiatric disorders has revealed an increase in the risk of suicidal behaviour in patients under 25 years of age who were being treated with antidepressants compared to those receiving a placebo. Careful monitoring of patients, and particularly of high-risk patients, must accompany use of this medication, particularly at the beginning of treatment and at times of dose changes.
The patients (and their family and friends) must be alerted to the need to monitor for the onset of clinical worsening, the appearance of suicidal thoughts/behaviour and any abnormal change of behaviour, and to seek medical advice immediately if such symptoms present.
Effects on ability to drive and use machines: Some patients may experience diminished alertness. The attention of drivers and machine-operators in particular should thus be drawn to the risk of somnolence with this product.
Use in Children: STABLON is contraindicated in children and adolescents under 15 years of age (see Contraindications) and should not be used in adolescents between 15 and 18 years of age. Suicidal type (suicide attempts and suicidal thoughts) and hostile type (mainly aggressiveness, opposition behaviour and anger) behaviours have been observed more frequently during clinical studies in children and adolescents treated with antidepressants compared to those treated with placebo. However, if treatment is clinically necessary, the patient must be closely monitored to detect the appearance of suicidal symptoms. Furthermore, there is no long term safety data in children and adolescents concerning the effects on growth, sexual maturation and cognitive and behavioural development.
Pregnancy: It is preferable to maintain a good psychological balance throughout pregnancy. If medical treatment is necessary to ensure this balance, treatment should be initiated or continued at an effective dose throughout pregnancy and if possible as monotherapy.
Animal data is reassuring but clinical data is still insufficient. In consideration of this data, it is preferable not to use tianeptine during pregnancy whatever the term. If initiation or continuation of treatment by tianeptine proves to be vital during pregnancy, the pharmacological profile of the molecule should be taken into account when monitoring the newborn baby.
Breast-feeding: Tricyclic antidepressants are excreted into breast milk, and thus breast-feeding is not recommended during treatment.
Fertility: A study demonstrated in rats a decrease in reproductive performance in females (increase in pre-implantation losses) at a maternotoxic dose. The clinical impact is unknown.
Summary of the safety profile:
Side effects reported with tianeptine in clinical trials are of moderate intensity. They consist mainly of nausea, constipation, abdominal pain, somnolence, headache, dry mouth and dizziness.
Tabulated list of undesirable effects:
The following undesirable effects have been reported during clinical trials and/or post-marketing use with tianeptine and are ranked using the following frequency: Very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10,000, <1/1000); very rare (<1/10,000), and not known (cannot be estimated from the available data). (See table.)
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Reporting of suspected adverse reactions:
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system.
Combinations that are inadvisable: Irreversible MAOIs (iproniazide): because of the risk of cardiovascular collapse or paroxysmal hypertension, hyperthermia, convulsions, death.
Special precautions for disposal and other handling: No special requirements.
Incompatibilities: Not applicable.
To be stored at a temperature below 30 °C (climatic zones III and IV).
Shelf life: 36 months.
N06AX14 - tianeptine ; Belongs to the class of other antidepressants.
Coated tab 12.5 mg x 30's.