Tianeptine: uses and side effects of this drug

Major depression is one of the most common mental disorders in the population, being the search for therapeutic alternatives for its treatment something of great relevance. The use of psychotropic drugs is one of these alternatives, with many substances classified as antidepressants and having between them mechanisms of action that may differ to a greater or lesser extent extent.

Some of these substances may even have an effect through a mechanism of action that may seem contrary to that of most of these types of drugs. This is what happens with tianeptine, about which we are going to talk in this article.

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What is tianeptine

Tianeptine is a psychotropic drug synthesized in the seventies, which was created in order to combat depressive symptoms. This antidepressant has interesting properties, and it has been shown that it has a level of efficacy similar to that of substances such as fluoxetine, also presenting a rapid action having the first effects about a week or two after first use (antidepressants generally take about a month). It has also been used as an adjuvant treatment to improve the efficacy of other antidepressants, as well as other disorders such as

anxiety and stress.

Sometimes it has been classified as tricyclic because it has the same chemical structure, but the truth is that its mechanism of action does not correspond to that of this group. In fact, it could rather be classified differentially in a new category: by its mechanism of action, opposite to that of specific serotonin reuptake inhibitors or SSRIs, tianeptine is the main representative of the enhancers of the reuptake of serotonin or PSRS.

Despite its efficacy and usefulness, tianeptine is not usually particularly well known or used because it has a risk relatively high degree of dependency (even being classified as a narcotic in countries like France), not being authorized as an antidepressant in many countries considering that the balance between risks and benefits was at best slightly favorable. However, if it is sold by other means, because has nootropic effects and improves memory. In our country, it began to be marketed as an antidepressant in 2015, but other alternatives are often used as first-line treatment.

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Mechanism of action

Tianeptine is a unique antidepressant due to its peculiar mechanism of action. And it is that unlike other antidepressants as popular as the SSRIs, which inhibit the reuptake of serotonin in such a By increasing the amount of this hormone in the brain, tianeptine works by greatly enhancing this hormone. reuptake.

Although it might seem that this mechanism of action is counterproductive, the truth is that tianeptine is effective in the treatment of depressive symptoms. And it is that despite the fact that the amount of serotonin present in the synaptic space is reuptaken, it seems that it also acts intensifying communication between neurons of the serotonergic pathways. The drug itself does not appear to bind to any receptor.

In addition, it also reduces the levels of corticotropin and glucocorticoids, which make it useful in the fight against stress. It also reduces the activity of the hypothalamic-pituitary-adrenocortical axis. It also contributes to increasing the levels of acetylcholine in the brain (among other reasons because it reduces the level of serotonin). Finally, it also seems to modify the function and transmission of glutamate, normalizing in stressful situations.

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Applications and indications

Tianeptine is a psychoactive drug that has been used in different disorders and with different applications. The first and most noteworthy is its indication in major depression and other depressive disorders, in which, as mentioned, have an efficacy comparable to that of drugs as popular as SSRIs.

It is also very useful in the treatment of disorders linked to anxiety and even somatic disorders, also not having any negative effect on the level of consciousness. It has been shown to be very useful for the treatment of stress, also preserving areas such as the hypothalamus from damage derived from its continued experience.

Finally, tianeptine is also marketed as a dietary supplement in some countries due to its ability to facilitate the increase in acetylcholine levels, which favors attention and learning and facilitates memorization and recall.

Side effects and contraindications

Tianeptine is a drug that has a considerable level of efficacy. Unlike other drugs, it does not generate sexual alterations, nor does it increase weight. It has not been detected to cause arrhythmias or heart problems, and the fact that it does not cause drowsiness is especially well known. However, its consumption can generate different side effects.

Among the side effects that we can find, tianeptine could generate vertigo and dizziness, tremor, abdominal pain, headache and cold symptoms. Also asthmatic crises, anorexia or loss of appetite, pain, palpitations, tachycardia, flushing and asthenia. In subjects with a history of psychotic episodes, it can facilitate their reappearance. Likewise, one of the great risks of this drug is that it has a great potential to generate dependency, and the subject who consumes it may become addicted. This is one of the main factors why its use has not become popular and in fact it is not marketed in different countries.

As main contraindications, it should be noted that Subjects who are taking MAOI-type antidepressants should not take this type of drug., or before the application of an anesthetic. It is also contraindicated in subjects with addiction problems (although it is used in depressions associated with alcoholism), subjects with positive psychotic symptoms and/or manic episodes. Pregnant, lactating mothers or minors should be very careful, as well as people with kidney problems.

Bibliographic references:

• McEwen, B.S.; Chattarji, S.; Diamond, D.M.; Jay, T.M.; Reagan, L.P.; Svenningson, P. & Fuchs, E. (2010). The neurobiological properties of Tianeptine (Stablon): from monoamine hypothesis to glutamatergic modulation. Mol Psychiatry.; 15(3): 237–49. doi: 10.1038/mp.2009.80.
• Watanabe, Y.; Gould, E.; Daniels, D.C.; Cameron, H. & McEwen, B.S. (1992). Tianeptine attenuates stress-induced morphological changes in the hippocampus. European Journal of Pharmacology; 222: 157-16.
• Dungeon, B.; Molina, v. & Uribe, F. (2016). Tianeptine: why hasn't it been classified as a narcotic in Spain? Rev. psychiatrist Health ;ent; 9 (3): 176-177.