2 English reference tianeptine [Xiangya Medical Dictionary]
3 description of tianeptine 3. 1 drug name tianeptine
3.2 English name Tianeptine
3.3 The alias of tianeptine is tianeptine sodium; Tatilang; Tioprodi; ThinaputineTatinol sodium
3.4 classification of nervous system drugs >: antidepressants > tricyclic drugs
3.5 dosage form 12.5 mg
3.6 Pharmacological effects of tianeptine The sodium salt of tianeptine is a tricyclic antidepressant, which acts on the serotonin system and plays an antidepressant role. Animal experiments show that tianeptine can increase the spontaneous activity of hippocampal pyramidal cells, accelerate the recovery after functional inhibition, and accelerate the uptake of 5- hydroxytryptamine by cerebral cortex and hippocampal neurons.
3.7 Pharmacokinetics of tianeptine Gastrointestinal absorption is rapid and complete. After oral administration of 12.5mg, the peak plasma concentration can reach 0.79 ~ 1.8 h, and the peak plasma concentration is 246ng/ml. It is rapidly distributed in the body, and the protein binding rate is as high as 94%. It is metabolized in the liver by β oxidation and N demethylation. A very small amount of prototype compounds (8%) are excreted from the kidney, mainly its metabolites are excreted from the urine. The half-life is 2.5h The half-life of the elderly and patients with renal insufficiency is prolonged 1 hour after long-term medication, and no adverse reactions are found in patients with hepatic insufficiency.
3.8 The indications of tianeptine are used to treat all kinds of depression, such as neurogenic reactive depression, anxiety and depression caused by physical discomfort, especially gastrointestinal discomfort, and anxiety and depression caused by alcohol dependence patients during withdrawal.
3.9 contraindications of tianeptine 1. Allergic to tianeptine;
2./kloc-children under 0/5 years old;
3. Pregnant women.
3. 10 Precautions 1. (1) Patients with cardiovascular diseases; (2) patients with gastrointestinal diseases; (3) mental patients; (4) Severe renal insufficiency; (5) elderly patients; (6) lactating women.
2. Effect of drugs on the elderly: Long-term use of tianeptine in the elderly over 70 years old can prolong the clearance half-life by 65438±0h hours.
3. Patients who use monoamine oxidase inhibitors must stop taking drugs for 2 weeks before taking tianeptine; However, monoamine oxidase inhibitors can be used after 24 hours of stopping tianeptine.
4. Patients with depression have suicidal tendency and must be closely monitored, especially in the early stage of treatment. If you want general anesthesia, you must inform the anesthesiologist that the patient is taking tianeptine 24 or 48 hours before operation and stop taking it. If you need emergency surgery, you can still operate without stopping the drug in advance, but you should be closely monitored during the operation.
5. The dosage should be gradually reduced 7 ~ 14 days before drug withdrawal.
6. A few patients will have decreased alertness, and taking tianeptine will cause drowsiness, so drivers or machine operators need to pay special attention.
7. Over-treatment: stop treatment and closely monitor, immediately lavage the stomach, monitor the heart, lungs, metabolism and renal function, treat the possible abnormal situation symptomatically, pay special attention to ventilation, and correct the abnormal metabolism and renal function.
3. Adverse reactions of11tianeptine are rare, and usually include mild epigastric discomfort, abdominal pain, dry mouth, aversion to food, nausea, vomiting, constipation, flatulence, tachycardia, retrosternal pain, insomnia, lethargy, nightmares, weakness, dizziness, headache, syncope, tremor, fever, and so on.
3. The recommended dosage of12 tianeptine is 12.5mg each time, taken orally three times a day, in the morning, in the middle and in the evening.
3. 13 drug interaction 1. Avoid the combination with non-selective monoamine oxidase inhibitors, because the combination of the two may lead to shock or paroxysmal hypertension, high temperature, convulsion and death.
2. The combination of St. John's wort and tianeptine may lead to 5- hydroxytryptamine syndrome (hypertension, high fever, myoclonus and mental state change).
3. Salicylic acid can reduce the protein binding rate of tianeptine, so it is suggested to reduce the dose of tianeptine when taking large doses of salicylic acid at the same time.
3. 14 Expert opinion