Amineptine

At Amineptine it is an atypical tricyclic antidepressant. This is because the preparation has a selective effect and only inhibits the re-uptake of the two messenger substances dopamine and norepinephrine in the nerve cells of the brain.

What is amineptine?

Amineptine was developed in 1978 by the pharmaceutical company Servier, which brought the preparation onto the market under the name Servier. Because amineptine acts primarily on dopamine, the mood-enhancing effect occurs faster than many other antidepressants.

Because the preparation also has a strong euphoric effect, there have been various cases of abuse or use as a doping agent. The manufacturer reacted to this in 1999 by taking the active ingredient off the market in Portugal and France. In 2005 the production of amineptine was stopped worldwide.

Pharmacological effect

The active ingredient amineptine mainly affects the brain metabolism. The preparation triggers a strong inhibition of the uptake of the neurotransmitter dopamine and the reuptake of norepinephrine is also strongly inhibited.

In addition, amineptine has a slight inhibitory effect on the neurotransmitter acetycholine, which occurs both in the brain and in the peripheral nervous system. The effect of histamine, which plays an important role in the human immune system, is also slightly weakened. Amineptine has the greatest effects on the happiness hormone dopamine.

Nerve cells that have a high proportion of dopamine are mainly located in the human midbrain. The hormone controls a multitude of functions within the human organism, for example dopamine also controls the blood flow to the internal organs. Noradrenaline, on the other hand, is very closely related to adrenaline and has a stimulating effect on the cardiovascular system.

This substance acts in the human body as both a hormone and a neurotransmitter. It fulfills this function in the central nervous system as well as in the sympathetic nervous system, which is part of the autonomic nervous system. The inhibitory function of amineptine increases the concentration of dopamine and noradrenaline in the human brain.

Medical application & use

Amineptine was originally developed to treat major depression. This is a mental disorder with various symptomatic manifestations. The main symptom in diagnostics is psychological depression, from which almost all patients who are affected by depression suffer.

Other typical symptoms of depression are inhibition of drive, inner restlessness and sleep disorders, the cause of which is a non-intact 24-hour rhythm. There are some gender-specific differences: depression is typical for female patients, while men tend to show aggressive behavior and increased irritability. According to estimates by the Federal Ministry of Health, around four million people in Germany are acutely affected by depression, and another ten million have suffered from depression at some point in their lives.

This means that depression is by far the most common mental disorder, although it is difficult to diagnose because of the relatively diffuse symptoms. Amineptine was also given to treat Parkinson's disease and attention deficit hyperactivity disorder. This is a psychological disorder that begins in childhood and continues into adulthood in the majority of affected patients.

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Risks & side effects

Because amineptine has liver-toxic properties, the administration of the drug can lead to liver inflammation as an undesirable side effect. Common side effects also include unwanted skin reactions such as acne.

Because amineptine is used as a doping agent in professional sports, the preparation is considered a marketable, but not a prescription narcotic drug in Germany. In addition, the preparation has a high potential for addiction. In combination with the drug cocaine, amineptine can even develop cross-tolerance. In Germany, where the drug was not brought onto the market anyway, possession is punishable unless the owner has the express permission of the Federal Opium Agency.

The preparation amineptine was developed in the late 1970s as a remedy for severe depression. It was later used against conditions like Parkinson's disease and ADHD. Because the preparation is highly addictive and was used as a doping agent in sports, amineptine has not been manufactured since 2005.