On February 20, the National Agency for the Safety of Medicines and Health Products (ANSM) warned of the risks of addiction to pain medications containing opiates or morphine. Several consumer drugs such as Tramadol are targeted, in a context where we learn that in the United States there is a serious epidemic of overdoses of these narcotics. Very timely, Inserm and the CNRS announce the development of a nano-pain medication resulting from the transformation of a molecule naturally present in the body. It is as effective as morphine, but without the side effects and in particular the phenomena of dependence.
Morphine and opioids will disappear from hospitals? Researchers at the Institut Galien Paris-Sud (CNRS) and Inserm have developed a new technique that could consign these products, which are very effective in treating patients' pain but extremely addictive, to the dustbin of medical history. Their discovery consists of the modification of enkephalin, a painkiller molecule already naturally present in the human body. Their work has just been published in the journal Science Advances.
This method would be more effective than morphine. Tests on rats showed that the effects lasted twice as long. In addition, unlike morphine, which carries significant side effects, such as the risk of addiction and respiratory depression, enkephalin does not present any danger to the body.
" Like endorphins, which are well known to elite athletes, enkephalins can lower the pain threshold or fight against fatigue.describes Patrick Couvreur, the principal author of the research. That's why scientists have been interested in this molecule for a long time. "Unfortunately, enkephalin has a very short lifespan in the body, on the order of a few minutes, making it ineffective in treating pain effectively.
This is the reason why the French researchers of the "Innovative Nanomedicines for the Treatment of Serious Diseases" team led by Patrick Couvreur at the Institut Galien Paris-Sud (Université Paris-Sud/CNRS), have set out to modify the form of administration of a type of enkephalin, leu-enkephalin, by coupling it to squalene, a fat molecule naturally present in plants (found for example in olive oil), animals (especially shark liver) and humans. « In this way, we have succeeded in creating nanoparticles that have a prolonged pain-relieving effect over time, without creating an addictive effect. "says the scientist.
Unlike morphine, which acts primarily on the central nervous system, leu-encephalin-squalene nanoparticles, because of their size, are unable to cross the blood-brain barrier that protects the brain. This is why, when injected intravenously, they are limited to acting on the peripheral nervous system and more particularly in the painful inflammatory area. To put it plainly: leuencephalin is released at the right place and at the right time, without causing toxicity or side effects in the body.
This line of research could lead to an interesting alternative to morphine and opioids. But it is too early to claim victory until clinical trials are launched. The authors of the research are aware of this and also point to the need to be able to demonstrate the feasibility of producing these nanoparticles on a large scale. Again, it is a question of time and means. But doctors are optimistic because the environment of mistrust towards opiates and morphine is such that there is an urgent need to find valid alternative solutions.
Sources: Inserm, AFP
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