We are seeing the emergence in France of new forms of drug addiction associated with amphetamines from the cathinone family, according to our partner The Conversation.
The structure of cathinones is similar to that of dopamine, a neurotransmitter that plays a major role in the reward circuit.
The analysis of this phenomenon was carried out by Édouard Tuaillon, University professor, doctor in infectious diseases, virology and sexual health at the University of Montpellier.
In an interview published on April 18, 2021, the President of the Republic Emmanuel Macron called for “launching a major national debate on drug consumption”.
The interview mainly developed the repressive aspect of the drug control policy and the effectiveness of the measures envisaged was immediately the subject of controversy.
However, a consensus should emerge from the debate on the recognition of addictions as a major risk for public health.
The consumption of amphetamines (psychotropic stimulants), documented for more than a century, should not be excluded from this awareness.
Indeed, the emergence of new forms of drug addiction associated with amphetamines of the cathinone family is now a worrying phenomenon in France.
Brief (medical) history of synthetic amphetamines
The first chemical purification of an amphetamine (ephedrine) is attributed to Nagai Nagayoshi, a Japanese pharmacist, and would date from 1885. The synthesis of ecstasy (or MDMA, for 3,4-methylenedioxy-N-methylamphetamine) by Merck Laboratories dates back to 1912, and the first synthesis of a cathinone (β-keto-amphetamine) to 1929.
In the first half of the 20th century, the effects of these synthetic molecules captivated chemists and aroused the interest of the medical world.
Their sympathomimetic (stimulant), anorectic (appetite suppressant) and psychostimulant (doping) activities led to the marketing of the first amphetamine-based drugs: a bronchodilator with Benzedrine® in 1934 in the United States (an amphetamine sulfate ), an appetite suppressant with Obetrol® from the 1950s also in the United States (a combination of amphetamine salts), and an energizer with Pervitin® (a methamphetamine) in Germany in the late 1930s.
To increase the capacity and resistance of its soldiers, the Wehrmacht distributed Pervitin®, a methamphetamine, to them during World War II © Karolis Kavolelis / Shutterstock (via The Conversation)
Powerful methamphetamine, the latter molecule will be available in pharmacies without a prescription and widely distributed to German troops during World War II. Thanks to its long-lasting doping effect, it would have played a decisive role at the start of the conflict in the success of the blitzkrieg strategy, by allowing soldiers to march and fight without sleeping for several days.
The medical use of amphetamine derivatives continued after the war. At the end of the 20th century, psychostimulants were prescribed to fight against attention deficits such as the Ordinator® (which ceased to be marketed in 1997) or even appetite suppressants such as Isomeride® and the Mediator® (prescribed for metabolic disorders and in particular diabetes). They will be withdrawn from the market in 1997 and 2009, respectively, due to serious adverse effects resulting in several convictions from Laboratoires Servier.
Today, Zyban®, as a smoking cessation aid, and Ritalin® for attention deficit disorders in children and narcolepsy in adults, remain available but with significant prescription restrictions.
This last specialty, the actual benefit of which has been confirmed by the Haute Autorité de Santé, is probably the one that has been the most useful from a medical point of view to date.
From the natural role to the first drinks
The use of amphetamines does not date from their discovery by synthetic chemistry.
These compounds exist naturally in some plants.
They form defense molecules there against herbivores, like other plant alkaloids.
Seeds of Ephedra sinica © Omar Hoftun / Wikimedia CC BY-SA 4.0
Thus, ephedrine was purified from a plant used in the Chinese pharmacopoeia -
Ephedra sinica
.
But the most famous and socially and economically important plant is khat, from its Latin name
Catha edulis
, whose freshly harvested leaves contain β-keto-amphetamine or cathinone (which degrades quickly after harvest). .
The khat is said to originate from Ethiopia, where it grows wild in temperate zones located at an altitude of more than 1,500 meters and benefiting from good rainfall.
These cultivation requirements, close to that of Arabica coffee, allowed the cultivation of khat to spread to certain areas of the Arabian Peninsula, East Africa and Madagascar.
The consumption of khat could be before the year 1000, although it seems to have intensified from the 15th century onwards.
In Yemen, where about 60% of the population consumes it (30% in Ethiopia and Somalia), its cultivation represents nearly 6% of the gross domestic product and mobilizes 14% of the working population.
Khat leaves must be consumed in large quantities and quickly because the cathinone they contain degrades quickly, which makes their use more complex.
For the consumer, access to the psychotropic effects of cathinones is not easy.
You must first obtain freshly cut twigs and then chew the bitter leaves for a long time to extract the active principle.
A bunch of 500 grams of twigs, or about 150 g of leaves, requires two hours of chewing.
Consuming khat in the traditional way therefore takes time, but also money - to the detriment of children's health or education.
From ecstasy to synthetic cathinones
Compared to khat, synthetic amphetamines offer increased psychotropic effects, while being easier to produce, transport, store and consume.
In France, amphetamines have been classified as narcotics since 1967. The development of their use as a drug from the 1990s is associated with the advent of electronic music and rave parties: ecstasy (MDMA) is then used as a drug. festive, for its doping effect and facilitator of human contact.
The turn of the 2000s was marked by the emergence of the synthetic drug market on the Internet - or new synthetic products (NPS).
There are variations of different psychotropic drugs, mainly: cannabinoids, opioid amphetamines, ketamines and, from the 2010s, synthetic cathinones - bodybuilding cousins of the khat alkaloid.
Red monkey ectasy pills © Tanjila Ahmed / Wikimedia CC BY-SA 2.0
With them, amphetamines will come out of the occasional and marginal use of few experimenters to reach a large population, socially well integrated and regular consumer.
A drug that activates the reward system
To understand the dangerous current success of cathinones, we must look at the mode of action of amphetamines on our brain.
The structure of cathinones is similar to that of dopamine, a neurotransmitter that plays a major role in the reward circuit.
The reinforcement / reward system is present in many animals (fish, birds, mammals) where it promotes behaviors essential to the perpetuation of the species: eating, learning, reproducing, having social relations.
Cathinones act directly on this system.
After ingestion, inhalation or injection, the small cathinones easily cross the blood-brain barrier which protects the brain.
They will then interact with dopamine neurons, preventing its reuptake and promoting its release.
Cathinones induce by these mechanisms a considerable increase in dopamine.
In rats, 40 minutes after the administration of a standard dose of cathinone, the increase in dopamine level is of the order of 500%.
Cathinones influence the reward system by interacting with neurons containing dopamine, a neurotransmitter involved in the sensation of pleasure © É. Tuaillon (via The Conversation)
This influx of dopamine will activate the circuits of the reward system.
It is these stimulating and entactogenic effects (altering the desire for physical contact) that consumers will seek in a use for sexual purposes in particular.
If not taken again, dopamine levels drop rapidly and return to normal after about 180 minutes.
A brief withdrawal syndrome (descent) is frequently reported by consumers 24 to 48 hours after taking, it is characterized in particular by fatigue and a general negative feeling (dysphoria).
Our "DRUGS" file
The use of amphetamines in the 20th century was thus marked not only by easier access, thanks to chemical synthesis, but also by the temptation to improve one's physiological capacities - all often in a festive context.
In our age of augmented reality and immediate satisfactions, cathinones have become the carriers of a deceptive promise to easily satisfy our desires ...
Science
Will LSD and hallucinogenic mushrooms ever be authorized drugs?
Health
Why is the dangerousness of alcohol (and other substances) so underestimated by its consumers?
This analysis was written by Édouard Tuaillon, University professor, doctor in infectious diseases, virology and sexual health at the University of Montpellier.
The original article was published on The Conversation website.
Declaration of interests
Edouard Tuaillon is a member of the French Society of Microbiology. It has received financial support, research grant grants from the following organizations: the National Agency for Research on AIDS and Viral Hepatitis (ANRS), the University and the University Hospital of Montpellier, interregional clinical research groups and innovation, the Pierre Fabre foundation, the Gilead and ViiV laboratories, the Biomérieux, Biocentric and DiaSorin companies.
Drug traffic
Addiction
Chemistry
Medication
Drug
The Conversation
Podcast
Science
0 comment
0 share
Share on Messenger
Share on Facebook
Share on twitter
Share on Flipboard
Share on Pinterest
Share on Linkedin
Send by Mail
To safeguard
A fault ?
To print