Tianeptine

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Tianeptine is mainly used in the treatment anxiety in depression disorders. In contrast to other ant.....

What is Tianeptine?

Tianeptine was discovered and patented by The French Society of Medical Research in the 1960s and since marketed across the globe. Tianeptine is a drug which is used as antidepressant and is mainly used in the treatment anxiety in depression disorders. In contrast to other antidepressants, Tianeptine increases serotonin uptake and is therefore known to reduce stress. A review of its use has shown its efficacy and favorable tolerability in patients suffering depression. Additionally, data shows that it has more potential for people suffering alcoholism [1].

How does Tianeptine work?

Tianeptine is a mixture of two isomeric tricyclic, synthetic chemical compounds, which is one of the aromatics, carboxylic acids and amines. Tianeptine is therapeutically effective by modulating glutamatergic synapses.

Tianeptine has a modulating effect on glutamatergic NMDA and AMPA receptors, and seems to prevent stress-related changes in the hippocampus and prefrontal cortex or can be undone respectively [2]. In an initial phase of treatment, Tianeptine was able to strengthen the reuptake of serotonin synaptic from the split in parts of the brain and increase extracellular dopamine concentration in the nucleus accumbens of the forebrain. Therefore, it was in the past referred to as a serotonin reuptake inhibitor as opposed to serotonin, a reuptake amplifier.

Effects of Tianeptine

Tianeptine is commonly approved for the treatment of mild, moderate and severe depression [3]. Off-label it can also be used for the treatment of anxiety disorders and obsessive-compulsive disorder.

Like other anti-depressives, Tianeptine blocks the uptake of norepinephrine and serotonin into axon terminals and may block some subtypes of serotonin, adrenergic, and histamine receptors. However the mechanism of its antidepressant effects is not entirely clear because therapeutic effects usually take weeks to develop and may only reflect compensatory changes in the central nervous system.

Studies on Tianeptine

Tianeptine is studied for various benefits to conditions of severe depression and was found to be a competing therapeutically effective supplement for alleviating depressive feelings. Furthermore interest lies within testing its ability to reduce tolerance to physical dependence on substances like alcohol or sedative drugs.

Recommended Dosage / Usage Instructions

Tianeptine was proved to be effective in terms of antidepressant and anxiolytic effects with a dosage of 25mg to 50 mg per day.

Side-Effects of Tianeptine

The most common side-effects of Tianeptine (occurring in more than 1 in 100 treated) include nightmares, insomnia, somnolence, dizziness, headaches, circulatory collapse, tremors, impaired vision, flushing, fast or unnatural palpitations, chest pain, difficulty breathing, dry mouth, constipation, abdominal pain, nausea, vomiting, bloating, diarrhea, heartburn, back pain, muscle pain and weakness.

Caution

Treatment with tianeptine can pose a risk for addicted patients in terms of high doses as well as tolerability [4].

References                   

[1] - Tianeptine reduces morphine antinociceptive tolerance and physical dependence - https://www.ncbi.nlm.nih.gov/pubmed/20679893

[2] - Computational analysis of the impact of chronic stress on intrinsic and synaptic excitability in the hippocampus - https://www.ncbi.nlm.nih.gov/pubmed/20457854

[3] - Tianeptine: a review of its use in depressive disorders - http://www.ncbi.nlm.nih.gov/pubmed/11463130

[4] - A case of tianeptine abuse - http://www.ncbi.nlm.nih.gov/pubmed/16528638

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