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Targeted opioids with fewer side effects
A new generation of pain relievers is nearing completion. These are opioids that no longer act broadly, but instead act specifically on the sites of the injury or inflammation. According to the researchers, typical side effects of conventional opioids in the brain or intestine can be avoided.
Scientists at Charité - Universitätsmedizin Berlin have used computer simulations to develop a new generation of opioid painkillers that cause fewer side effects and have a more targeted effect. The active ingredients have already successfully completed preclinical tests. The research team recently published the study results in the renowned journal "Nature Scientific Reports".
Opioids - effective but dangerous
Opioids are known for their strong analgesic effects. Because of their strength and the sometimes violent side effects, they are administered especially for cancer, inflammation, tissue injuries and after surgery. Common side effects include drowsiness, nausea and vomiting, constipation, and in some cases even respiratory arrest. There is also a high risk of addiction.
New opioids without the typical side effects
The research team led by Professor Dr. Christoph Stein from the Clinic for Anaesthesiology with a focus on operative intensive medicine at the Charité is currently developing a new form of opioid pain reliever to eliminate the dangerous side effects. "Our innovative development method provides a solid basis for a new generation of pain medication," Stein reports in a Charité press release on the study results.
As the research team knew, there is an increased interaction between the activating agents and the docking points for pain medication in the body in injured or inflamed tissue. In computer analyzes, the scientists came to the conclusion that an increased concentration of protons in the inflamed tissue is the reason for this. As a result, the pH in the damaged tissue is lower than in the healthy one.
The pain relievers only work on the damaged area
The research team managed to design two substances so that they only lower (protonate) the increased proton concentration in an inflamed environment. Thus, the opioid receptors are activated only at the site of the tissue injury or inflammation and not in the brain or intestine. The two novel opioid substances are based on the so-called fentanyl, a synthetic opioid.
Opioids with no risks and side effects
"Such drugs could prevent the risky side effects of previous opioids and thus reduce complications," summarizes Professor Stein. In further research, the team around Stein wants to gain further knowledge on the optimization of opioids so that they can also be used for other drugs, such as for treating high blood pressure.
New pain relievers are contributing to the opioid crisis
"In addition, the new opioids contribute to coping with the opioid crisis, as is particularly noticeable in the United States," Stein explains the other benefits of the new pain medication. But the number of opioid addicts is also increasing in Germany. The locally acting opioids could remedy this. (vb)