What is the biological activity of Tianeptine sodium salt?

Introduction

Tianeptine sodium salt (TSS) is a facilitator of serotonin and norepinephrine reuptake. TSS is well known as an antidepressant drug and works by restoring serotonergic neurotransmission. Tianeptine sulfate is believed to present some diferences versus Tianeptine sodium salt: it is sold only through the Internet without prescrption, the daily dose is 25mg per day versus 12.5mg every 8 hours and it might be more potent and long lasting. Those differences were confirmed by the patient after the prescription of tianeptine sodium[1].

Biological activity

Antidepressant drugs such as norfluoxetine, clomipramine, and desimpramine caused a significant decrease in cell viability by inducing mitochondrial dysfunction-mediated caspase-3 activation; however, it is unknown whether TSS regulates anticancer activity during the invasion process. No cytotoxic effects or changes in mitochondrial potential were observed in TSS-treated cells[2].

Kim et al. investigated the effect of TSS on the expression of matrix metalloproteinase-9 (MMP-9) and invasion in three different human carcinoma cell lines. The findings showed that MMP-9 activity was significantly increased in response to tumour necrosis factor-α (TNF-α) and that TSS reduced TNF-α-induced MMP-9 activity in a dose-dependent manner. TSS also downregulated both MMP-9 expression and TNF-α-induced MMP-9 promoter activity. A matrigel invasion assay showed that TSS significantly attenuated invasive rates in TNF-α-stimulated LNCaP prostate carcinoma cells. Furthermore, TSS suppressed TNF-α-induced NF-κB activity, which is a potential transcriptional factor for regulating many invasive genes, including MMP-9, by suppressing IκB degradation and nuclear translocation of NF-κB subunits in LNCaP prostate carcinoma cells. TSS also downregulated TNF-α-induced phosphorylation of phosphatidyl-inositol 3 kinase (PI3K) and Akt, and a selective PI3K/Akt inhibitor, LY294002, diminished TNF-α-induced NF-κB activation followed by levels of MMP-9, suggesting that TSS also reduces MMP-9 expression by inhibiting the PI3K/Akt-mediated NF-κB pathway. These results indicate that TSS is a potential anti-invasive agent by suppressing TNF-α-induced MMP-9 expression via inhibiting PI3K/Akt-mediated NF-κB activity.

Side effects

While Tianeptine sodium salt can be beneficial for many, it is not without its side effects. Common side effects include nausea, dizziness, headaches, and dry mouth. These symptoms are generally mild and often subside as the body adjusts to the medication. However, more severe side effects can occur, such as confusion, fatigue, and changes in heart rate. In rare cases, it can lead to liver toxicity, making regular monitoring of liver function important for long-term users.

Among the more concerning aspects of Tianeptine is its potential for abuse and dependency. At higher doses, it can produce opioid-like effects, which has led to misuse in some populations. This risk underscores the importance of using Tianeptine strictly as prescribed and under medical supervision[3].

Contraindications for Tianeptine Sodium include individuals with a history of substance abuse, those with severe renal or hepatic impairment, and individuals with known hypersensitivity to the drug. Pregnant or breastfeeding women should also avoid using Tianeptine due to insufficient data on its safety in these populations.

Additionally, abrupt discontinuation of Tianeptine can lead to withdrawal symptoms such as anxiety, agitation, and rebound depression. Therefore, any decision to stop the medication should be done gradually and under the guidance of a healthcare professional.

References

[1] Á. Palma Conesa. “Use of tianeptine sulfate over-the-counter, literature review, and case report.” European Psychiatry (2023).

[2] What is Tianeptine Sodium used for? (patsnap.com)https://synapse.patsnap.com/article/what-is-tianeptine-sodium-used-for

[3] Rajapaksha Gedara Prasad Tharanga Jayasooriya . “Tianeptine sodium salt suppresses TNF-α-induced expression of matrix metalloproteinase-9 in human carcinoma cells via suppression of the PI3K/Akt-mediated NF-κB pathway.” Environmental toxicology and pharmacology 38 2 (2014): Pages 502-509.