Amineptine is an atypical tricyclic antidepressant. This is because the drug has a selective effect and only inhibits the reuptake of the two neurotransmitters dopamine and norepinephrine in the nerve cells of the brain.
What is amineptine?
Amineptine is an atypical tricyclic antidepressant. Amineptine was developed in 1978 by the pharmaceutical company Servier, which marketed the drug under the name Servier. Because amineptine acts predominantly on dopamine, the mood-lifting effect occurs more quickly than with many other antidepressants. Because the drug 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 withdrawing the active ingredient from the market in Portugal and France. In 2005, production of amineptine was discontinued worldwide.
Pharmacologic action
The active ingredient amineptine acts primarily on brain metabolism. Thus, the drug triggers a strong reuptake inhibition for 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 in both the brain and the peripheral nervous system. Also slightly attenuated is the effect of histamine, which plays an important role in the human immune system. Amineptine has the greatest effect on the happiness hormone dopamine. Nerve cells that have high levels of dopamine are located primarily in the human midbrain. The hormone controls a variety of functions within the human organism; for example, dopamine also controls blood flow to the internal organs. Norepinephrine, 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 both as a hormone and as a neurotransmitter. It performs 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 norepinephrine in the human brain.
Medical application and use
Originally, amineptine was developed to treat major depression. This is a mental disorder with various symptomatic manifestations. In diagnosis, the leading symptom is mental dejection, which afflicts almost all patients affected by depression. Other typical symptoms of depression are drive inhibition, inner restlessness and sleep disturbances, the cause of which lies in an intact 24-hour rhythm. There are some gender-specific differences: Dejection is typical for female patients, while men tend to show aggressive behavior and increased irritability. According to estimates by the German Federal Ministry of Health, around four million people in Germany are acutely affected by depression, and a further ten million have suffered from depression at some time in their lives. This makes depression by far the most common mental disorder, although it is difficult to diagnose because of the relatively diffuse symptoms. Amineptine has also been used to treat Parkinson’s disease and attention deficit hyperactivity disorder. This is a mental disorder that begins in childhood and continues into adulthood in a large proportion of affected patients.
Risks and side effects
Because amineptine has liver-toxic properties, liver inflammation may be an unwanted side effect when the drug is administered. Common side effects also include adverse skin reactions such as acne. Because amineptine is used as a doping agent in professional sports, the preparation is considered a marketable but non-prescribable narcotic in Germany. In addition, the preparation harbors a high potential for addiction. In combination with the drug cocaine, amineptine can even develop cross-tolerance. In Germany, where the drug has not been marketed in any case, possession is punishable unless the owner has the express permission of the Federal Opium Agency. The drug amineptine was developed in the late 1970s as a treatment for severe depression. Later, it was also used to treat conditions such as Parkinson’s disease and ADHD.Because the drug is highly addictive and has been used as a doping agent in sports, amineptine has been discontinued since 2005.
