Composition, form of production and packaging
The tablets covered with a cover of white color, oval.
1 tab.
tianeptin sodium 12.5 mg
Excipients: corn starch - 2.5 mg, mannitol - 101 mg, magnesium stearate - 2.5 mg, talc - 6.5 mg.
The composition of the shell: sodium bicarbonate - 77 mcg, sodium carbellose - 158 mcg, beeswax white - 114 mcg, titanium dioxide 6.208 mg, ethyl cellulose 247 mcg, glyceryl monooleate 123 mcg, polysorbate 80-135 mcg, povidone 228 mcg, sucrose - 23.946 mg, silicon dioxide colloidal anhydrous - 108 mcg, talc - 13.656 mg.
30 pcs. - blisters (1) - packs of cardboard with control of the first opening.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
PHARMACHOLOGIC EFFECT
Antidepressant from the group of tricyclic derivatives.
In experiments on laboratory animals, tianeptine increases the spontaneous activity of pyramidal cells in the hippocampus and increases the rate of their recovery after functional inhibition; increases the reuptake of serotonin by the neurons of the cerebral cortex and hippocampus.
According to the nature of the clinical effect on mood disorders, it takes an intermediate position in the bipolar classification between sedative and stimulating antidepressants. In patients, tianeptine helps to reduce somatic symptoms (especially from the gastrointestinal tract) associated with anxiety or mood disorders.
Tianeptine has no effect on the cholinergic system (does not have anticholinergic action), sleep and the ability to concentrate.
PHARMACOKINETICS
Suction
After ingestion, tianeptine is quickly and completely absorbed from the digestive tract.
Distribution
Tianeptine is rapidly distributed in the body. Has a high degree of binding to proteins (approximately 94%).
Metabolism
Tianeptine is extensively metabolized in the liver by? -oxidation and N-demethylation.
Excretion
The half-life (T 1/2 ) of tianeptine is 2.5 hours. Tianeptine is excreted from the body by the kidneys: the bulk - in the form of metabolites, 8% - unchanged.
Pharmacokinetics in special clinical cases
In renal failure, as well as in patients older than 70 years, T 1/2 is increased by 1 h.
In patients with chronic alcoholism (including in the presence of liver cirrhosis), the pharmacokinetic parameters of the preparation do not change significantly.
INDICATIONS
- Depressive states.
DOSING MODE
The drug is prescribed inside, before meals, 12.5 mg (1 tab.) 3 times / day (morning, afternoon and evening).
For patients with chronic alcoholism with or without cirrhosis, a change in the dosage regimen is not required.
For elderly patients (over 70 years) and patients with renal failure, the dose should be reduced to 2 tablets / day.
SIDE EFFECT
The side effects found in the clinical trials of tianeptine are not very pronounced. Basically, this is nausea, constipation, abdominal pain, drowsiness, headache, dry mouth and dizziness.
During clinical trials and / or post-marketing period, the following side effects were noted against tianeptine at the following frequency: very often (? 1/10); often (? 1/100, <1/10); infrequently (? 1/1000, <1/100); rarely (? 1/10 000, <1/1000); very rarely (? 1/100 000, <1/10 000); an unknown frequency (the frequency can not be calculated from the available data).
From the cardiovascular system: often - tachycardia, extrasystole, chest pain, "hot flashes" of blood to the skin of the face.
Mental disorders: often - nightmarish dreams; rarely - the development of drug dependence and drug abuse, especially in patients younger than 50 with a history of drug or alcohol dependence; unknown frequency * - cases of suicidal thoughts and suicidal behavior were reported at the time of admission or shortly after discontinuation of the drug (see / section "Special instructions"). Confusion, hallucinations.
From the side of the central nervous system: often - insomnia, drowsiness, dizziness, headache, tremor, fainting (lipotomy); unknown frequency * - extrapyramidal disorders, dyskinesia
From the digestive system: often - abdominal pain, epigastric pain, dry mouth, nausea, vomiting, constipation, flatulence.
From the hepatobiliary system: an unknown frequency * - an increase in the activity of hepatic enzymes, hepatitis, which in extremely rare cases can occur in severe form.
From the side of the skin: infrequently - maculopapular or erythematous rash, hives, itching; unknown frequency * - acne, bullous dermatitis in extremely rare cases.
From the osteomuscular system and connective tissue: often - myalgia, pain in the lumbar region.
From the respiratory system: often - shortness of breath.
Metabolic disorders and diseases caused by metabolic disorders: often - anorexia; unknown frequency * - hyponatremia.
Common symptoms and disorders at the injection site: often - asthenia, a feeling of "coma" in the throat.
* Post-registration application experience .
CONTRAINDICATIONS
- hypersensitivity to tianeptine and other components of the drug;
- simultaneous use of monoamine oxidase inhibitors (MAO). When switching from therapy with MAO inhibitors to tianeptine treatment, a break of at least two weeks is necessary. When switching from tiapentin to MAO inhibitors, it is sufficient to take a break for 24 hours;
- use of the drug in children and adolescents under 18 due to lack of data on the safety and efficacy of Coaxil in this age group. It was shown that the use of other antidepressants in children and adolescents was accompanied by an increase in the frequency of suicidal behavior (suicidal attempts and suicidal thoughts) and manifestations of hostility (mainly aggression, negative behavior and rage) compared with the placebo group.
- use of the drug in patients with a deficiency of sugar-isomaltase, intolerance to fructose, glucose-galactose malabsorption, because the preparation contains sucrose.
With caution: patients with alcohol or drug dependence in the history.
PREGNANCY AND LACTATION
Taking tianeptine during pregnancy is not recommended.
During pregnancy it is desirable to maintain mental balance. If medication is needed for this, then it is possible to start or continue the previously initiated treatment, preferably in the monotherapy regime.
The results of studies of Coaxil В® in laboratory animals are encouraging, but the experience of clinical use is insufficient.
Given these data, tianeptine is not recommended for pregnancy. If the life indications need to start or continue therapy with Coaxil В® during pregnancy, the pharmacological properties of the drug should be considered when monitoring the newborn.
There are no clinical data on the effect on fertility in humans.
Due to the fact that tricyclic antidepressants penetrate into breast milk, it is not recommended to breast-feed during the treatment period.
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with renal failure should reduce the daily dose to 25 mg (2 tab.).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
For patients with chronic alcoholism with or without cirrhosis, a change in the dosage regimen is not required.
APPLICATION FOR CHILDREN
The drug is contraindicated in children and adolescents under 18 years.
APPLICATION IN ELDERLY PATIENTS
For elderly patients (over 70 years), the dose should be reduced to 2 tablets / day.
SPECIAL INSTRUCTIONS
In the depressed state, the risk of suicidal thoughts, self-harm and suicidal behavior is increased. The risk persists until a distinct remission occurs. Patients should be under close medical supervision until the condition improves (after the start of therapy, it may take several weeks before the condition improves). Clinical experience indicates that the risk of suicide may increase in the early stages of the onset of remission.
Patients with a history of suicidal events, as well as patients who had suicidal intent before initiating therapy, are at risk for suicide and should be closely monitored during therapy.
The results of the meta-analysis of clinical trials of antidepressants in patients with mental disorders indicate an increased risk of suicidal behavior in patients under 25 years of age when taking antidepressants compared with placebo.
During the treatment period, patients, especially those at risk, should be under close medical supervision, especially at the beginning of therapy and when changing the dose of the drug. Patients (and caregivers) should be informed of the need for immediate medical attention if the condition worsens, suicidal and unusual behavior, and when suicidal thoughts occur.
If general anesthesia is required, the anesthetist should be warned that the patient is taking Coaxil В® . The drug should be withdrawn 24 or 48 hours prior to surgery. In the case of emergency surgical care, the operation can be performed without first discontinuing the drug, but under strict control of the patient's condition during the operation.
When discontinuing therapy with Coaxil В® , as with any psychotropic drugs, the dose should be reduced gradually, within 7-14 days.
Do not exceed the recommended dose of the drug.
Patients with drug or alcohol dependence should be under close medical supervision to avoid exceeding the recommended dose of the drug.
Impact on the ability to drive vehicles and manage mechanisms
In some patients, the ability to concentrate and the speed of psychomotor reactions may decrease, and therefore, during the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities requiring increased concentration of attention and speed of psychomotor reactions.
OVERDOSE
The experience of tianeptine overdose (the maximum amount was 2,250 mg per dose) revealed the following signs and symptoms : confusion, convulsions, drowsiness, dry mouth and respiratory failure, which were noted mainly when tianeptine was combined with alcohol.
Treatment: in all cases of overdose, stop taking the drug and carry out medical supervision of the patient. If necessary, the following activities should be carried out:
- if the drug was taken less than 2 hours before admission, it is recommended to wash the stomach if, for a longer time, it is necessary to take activated charcoal;
- to control the functions of the cardiovascular and respiratory systems, the function of the kidneys, the indices of homeostasis;
- conduct symptomatic therapy (eg, artificial ventilation, correction of metabolic disorders and renal dysfunction).
Specific antidotes for tianeptine are unknown.
DRUG INTERACTION
Unwanted combination of drugs
When used simultaneously with nonselective MAO inhibitors, collapse or sudden increase in arterial pressure, hyperthermia, seizures, and death can occur.
Simultaneous use with mianserin is undesirable, because with this combination of drugs on the experimental model an antagonistic effect was detected.
It is not recommended simultaneous use of Coaxil with ethanol.
TERMS OF RELEASE FROM PHARMACY
The drug is only released to hospitals.
TERMS AND CONDITIONS OF STORAGE
Refers to the list of III psychotropic substances, whose turnover in the Russian Federation is limited.
The drug should be stored at a temperature not higher than 30 В° C, out of the reach of children. Shelf life - 3 years. Do not use after the expiration date printed on the package.
