Amineptine (antidepressant): Uses, Indications And Side Effects
Amineptine is an old antidepressant drug which was marketed for the treatment of major depression.
Its stimulant effects and addictive potential led governments to prohibit its sale and consumption twenty years ago. This medication is no longer used and is on the list of controlled substances.
In this article we explain what amineptine is and what are the main characteristics of the group of antidepressants to which it belongs what is its mechanism of action, and what type of side effects does it produce.
Amineptine is an atypical antidepressant drug from the group of tricyclic antidepressants It was developed and introduced into the market by the French company Servier, in the seventies, to treat severe clinical depression of endogenous origin. After its launch, it gained some popularity because, apart from the effects of an antidepressant drug, it also produced exciting effects, short-lived but very pleasant, according to what the patients themselves experienced.
The stimulating effects caused by this medication led many people to make recreational use of it; Furthermore, after its commercialization spread in several European countries, numerous cases of hepatotoxicity arose due to abusive use, some of them of considerable severity, which led the authorities to suspend the authorization for its sale.
In 1999, the marketing of amineptine was banned in Spain, sold under the name Survector, a measure that spread to several European countries. However, the United States Food and Drug Administration (FDA), a key institution worldwide when it comes to allowing certain drugs to be marketed or not, never approved amineptine for sale in its country.
Currently, amineptine (in its hydrochloride form) is included in list II of controlled and controlled substances of the UN.
Tricyclic antidepressants
Amineptine belongs to the group of tricyclic antidepressants. These types of drugs were discovered in the 1950s and, for a few decades, they have been the first option when it comes to the pharmacological treatment of clinical depression. Although they are still used for mood disorders (along with MAOIs or lithium, for example), they have currently been replaced by another group of antidepressants.
Tricyclic antidepressants share some chemical characteristics with phenothiazines, a group of antipsychotic (or neuroleptic) medications used to relieve psychotic symptoms and distress in emotional disturbances and serious mental disorders, despite their marked side effects.
It is precisely due to the large number of side effects that tricyclic antidepressants cause that Today it is preferred to use other types of antidepressants, such as selective serotonin reuptake inhibitors (SSRIs) or serotonin and norepinephrine reuptake inhibitors (SNRIs), two groups of antidepressants that generate fewer and milder adverse reactions.
Mechanism of action
Amineptine exerts its effects through the inhibition of dopamine reuptake and, to a lesser extent, norepinephrine. One of the peculiarities of the drug is that it also induces the release of dopamine, which explains its stimulating effects; However, the release of dopamine is relatively mild when compared to other exciting drugs, such as amphetamine, since its predominant effect seems to be the inhibition of the reuptake of said neurotransmitter, rather than its release.
Unlike dopamine, amineptine does not cause the release of norepinephrine and, therefore, acts only as an inhibitor of its reuptake. Tricyclic antidepressants usually interact with serotonin, adrenergic, dopamine, histamine and acetylcholine (muscarinic type) receptors; However, this does not occur with amineptine, since its interaction is very weak or practically non-existent.
Amineptine shares some of the side effects of tricyclic antidepressants (such as insomnia or irritability) and, given its particular pharmacological profile, it also causes organic complications and its own adverse reactions that are detailed below.
1. Dermatological problems
Cases of severe acne have been reported in people who have consumed excessively amineptine. Specifically, the case of a 54-year-old woman was described whose excessive use of this drug caused an acneiform eruption, characterized by the appearance of papules and pustules in seborrheic areas.
Several cases have also been described of women who, after continued consumption of amineptine, suffered severe acne on the face, back and chest, the severity of which varied with the dose.
2. Psychiatric disorders
Another side effect that the consumption of amineptine can produce is psychomotor excitement, although its appearance is very infrequent. This includes: insomnia, irritability, nervousness and suicidal ideation.
3. Potential for abuse and dependency
Although the risk of addiction is low, several cases of dependence on amineptine have been reported in several centers in France. In a study carried out with 155 addicted people, it was observed that they were predominantly women, and that two thirds of them had known risk factors for addiction.
However, research carried out in the 1980s with people addicted to opiates and schizophrenic patients did not find addiction to amineptine in any of the subjects. In another study, in which eight cases of dependence on amineptine were analyzed, it was found that the gradual withdrawal of the drug was achieved without problems in six of the people, and in the other two symptoms of anxiety, psychomotor agitation and bulimia were observed. .
Amineptine may rarely cause hepatitis (cytolytic and cholestatic). It has been suggested that hepatitis induced by this drug, which is sometimes preceded by a rash, may be due to an allergic reaction and resolves upon discontinuation of use. Furthermore, it is known that amineptine does not usually elevate transaminases, alkaline phosphatase, and bilirubin.
Mixed hepatitis, which is very rare, usually occurs between days 15 and 30 of treatment with this antidepressant. This is often preceded by abdominal pain (sometimes severe), nausea, vomiting, rash and jaundice (variable). The evolution of the condition is usually favorable if treatment with amineptine is discontinued.
In Spain, in the mid-nineties, a case was identified in which acute pancreatitis and mixed hepatitis were associated, after three weeks of treatment with the drug.
5. Cardiovascular problems
Although it occurs rarely, after the consumption of amineptine, arterial hypotension, palpitations (hard, rapid and/or irregular heartbeats) and vasomotor episodes or syncope (which occur with temporary loss of consciousness, with spontaneous recovery and without sequelae) may occur.
