Drug revolution Local opioids almost ready for action

Targeted opioids with fewer side effects

A new generation of painkillers is nearing completion. These are opioids, which no longer have a broad-surface effect, but specifically at the sites of injury or inflammation. Thus, according to the researchers typical side effects of conventional opioids in the brain or intestine can be avoided.

Scientists at the Charité - Universitätsmedizin Berlin have used computer simulations to develop a new generation of opioid pain medications that cause fewer side effects and are more targeted. The active ingredients have successfully completed preclinical tests. The research team recently published the study results in the renowned journal "Nature Scientific Reports".

A newly developed opioid works only on the damaged area and does not trigger the typical side effects such as addiction, drowsiness, nausea, constipation or respiratory arrest. (Image: Rido / fotolia.com)

Opioids - effective but dangerous

Opioids are known for their strong analgesic effect. Due to their strength and sometimes severe side effects, they are especially used for cancer, inflammation, tissue injury 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 headed by Professor Christoph Stein from the Department of Anesthesiology with a focus on surgical intensive care of the Charité is currently developing a new form of opioid analgesics to eliminate the dangerous side effects. "Our innovative development method provides a solid foundation for a new generation of pain medication," says Stein in a press release from the Charité on the study findings.

About the research

As the research team knew, there is increased interaction between the activating agents and the pain medication docking points in injured or inflamed tissue in the body. In computer analyzes, the scientists came to the conclusion that an increased concentration of protons in the inflamed tissue is the cause of this. As a result, the pH in the damaged tissue is lower than in the healthy one.

The painkillers only work on the damaged area

The research team succeeded in designing two substances in such a way that they lower (protonate) the increased proton concentration only in an inflamed environment. Thus, the opioid receptors are activated solely at the site of 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 without risks and side effects

"Such drugs could prevent the risky side effects of previous opioids and thus reduce complications," sums up Professor Stein. In further research, the Stein team wants to gain further insights into the optimization of opioids in order to make them usable for other medicines, for example for the treatment of hypertension.

New painkillers contribute to the opioid crisis

"In addition, the new opioids make a contribution to coping with the opioid crisis, which is particularly noticeable in the USA," says Stein, explaining the further advantages of the new painkillers. But in Germany, too, the number of opioid addicts is increasing. Here, the locally acting opioids could help. (Vb)