Major depression is one of the most common mental disorders in the population, and the search for therapeutic alternatives for its treatment is of great relevance. The use of psychotropic drugs is one of these alternatives, with many substances classified as antidepressants and among them having mechanisms of action that may differ to a greater or lesser extent.
Some of these substances can even have an effect through a mechanism of action that may seem contrary to that of the majority of this type of drugs. This is what happens with tianeptine which we are going to talk about in this article.
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 to have a level of effectiveness similar to that of substances such as fluoxetine, also presenting a rapid action by having the first effects around one or two weeks after the first consumption (generally, antidepressants take around one month). It has also been used as an adjuvant treatment to improve the effectiveness of other antidepressants, as well as other disorders such as anxiety and stress.
It has sometimes 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: due to its mechanism of action, opposite to that of specific serotonin reuptake inhibitors or SSRIs, Tianeptine is the main representative of serotonin reuptake enhancers or PSRS
Despite its effectiveness and usefulness, tianeptine is not usually particularly known or used because it has a relatively high risk of generating dependence (even being classified as a narcotic in countries such as France), and is not authorized as an antidepressant in many countries. The balance between risks and benefits was considered to be at best slightly favourable. However, if it is sold through 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 usually used as first-line treatment.
Mechanism of action
Tianeptine is a unique antidepressant due to its peculiar mechanism of action. And unlike other popular antidepressants such as SSRIs, which inhibit the reuptake of serotonin in such a way that the amount of this hormone in the brain increases, tianeptine works by greatly enhancing said reuptake.
Although it may seem that this mechanism of action is counterproductive, the truth is that tianeptine is effective in the treatment of depressive symptoms. And despite the fact that the amount of serotonin present in the synaptic space is recaptured, it apparently also acts intensifying the communication between neurons of the serotonergic pathways The drug itself does not appear to bind to any receptors.
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, also appears to modify glutamate function and transmission normalizing in stressful situations.
Tianeptine is a psychotropic drug that has been used in different disorders and with different applications. The first and most notable is its indication in major depression and other depressive disorders, in which, as mentioned, it has an efficacy comparable to that of such popular drugs 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 proven to be very useful for the treatment of stress, also preserving damage derived from its continued experience in areas such as the hypothalamus.
Finally, Tianeptine is also marketed as a dietary supplement in some countries due to its ability to facilitate an increase in acetylcholine levels, which promotes attention and learning and facilitates memorization and remembering.
Side effects and contraindications
Tianeptine is a drug that has a considerable level of effectiveness. Unlike other drugs, it does not cause sexual alterations or increase weight. It has not been detected to cause arrhythmias or cardiac problems, and it is especially known that it does not cause drowsiness. However, its consumption can cause different side effects.
Among the side effects that we can find, tianeptine could cause vertigo and dizziness, tremor, abdominal pain, headache and cold symptoms Also asthma attacks, anorexia or loss of appetite, pain, palpitations, tachycardia, suffocation and asthenia. In subjects with a history of psychotic outbreaks, it may facilitate their recurrence. 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 antidepressants should not consume 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 depression that occurs with alcoholism), subjects with positive psychotic symptoms and/or manic episodes. Pregnant women, nursing mothers or minors, as well as people with kidney problems, should be very careful.
