Tianeptine for 5-HT system, sedation, anti-acetylcholine and cardiotoxicity for depression

Pharmacological Effect

1. The antidepressant mechanism of this product is different from that of traditional TCA. It can increase the uptake of 5-HT in the synaptic cleft, but has a weaker effect on the reuptake of 5-HT and NA. May have the effect of enhancing 5-HT neuronal transmission. It has no affinity for M receptors, H1, α1 and α2-NA receptors.
2. The antidepressant efficacy of this product is similar to that of TCA, and its safety and tolerability are better than TCA (tricyclic antidepressants). The efficacy of this product is similar to that of SSRI fluoxetine.
3. Animal drug experiments have shown that it can: increase the spontaneous activity of pyramidal cells in the hippocampus and accelerate the recovery of its function after inhibition; increase the reabsorption of 5-hydroxytryptamine by neurons in the cerebral cortex and hippocampus.

Toxicology Research

- Acute, subacute and long-term toxicity tests: no changes in biology, liver function, pathological anatomy.
- Reproductive toxicity and teratogenicity test: Tianeptine has no effect on the reproductive ability of the treated parents and on the fetus and offspring.
- Mutagenicity test: Tianeptine has no mutagenic effect.

Side Effect

- Epigastric pain, abdominal pain, dry mouth, anorexia, nausea, vomiting, constipation, flatulence;
- Insomnia, drowsiness, nightmares, weakness;
- Tachycardia, extrasystoles, precordial pain;
- dizziness, headache, fainting, tremors, flushing of the face;
- Shortness of breath, feeling of congestion in the throat;
- Myalgia, back pain, etc.