A new method of developing painkillers could help curb side effects

A new method of developing painkillers could help curb side effects Orange County, CA -

March 7th 2017 - Researchers from Charité - Universitätsmedizin Berlin have developed a new method of production for pain relievers with the potential to combat the growing opioid overdose epidemic. Opioids are a powerful class of pain killer derived from the opium poppy or a synthetic equivalent. When used properly, their effects relieve chronic pain from instances of tissue damage and inflammation. However, when taken improperly and abused, can cause users to develop a dependence on the substance. Not only addictive, these medications can also produce adverse side effects like drowsiness, nausea, and if taken in high doses, respiratory arrest. Another adverse effect is the opioids impartialness in affecting healthy and inflamed tissue. Using computational simulation, researchers analyzed the interactions of opioid receptors between their new morphine-like molecules (NFEPP-prototype) and manipulated tissue by increasing proton concentration to imitate the acidic conditions found in inflamed tissues. In an animal model, the NFEPP-prototype pain reliever was able to block pain receptors and produce considerable pain relief in affected areas. This new enhanced prototype leaves healthy tissue without complications. During analysis, researchers discovered the new system of action only taking effect on the targeted inflamed tissue. "In contrast to conventional opioids, our NFEPP-prototype appears to only bind to, and activate, opioid receptors in an acidic environment. This means it produces pain relief only in injured tissues, and without causing respiratory depression, drowsiness, the risk of dependency, or constipation,” said Dr. Viola Spahn and Dr. Giovanna Del Vecchio, the first authors of the study. This could eliminate the serious side effects associated with these types of painkillers and drastically improve the quality of life for those suffering from postoperative and chronic inflammatory pain. Currently opioids are the leading cause of accidental death in the United States and this number continues to rise each year. The Centers for Disease Control and Prevention (CDC) states that the number of death from prescription opioid overdose has quadrupled since 1999, as well as the total of amount of prescription opioids sold. Despite this raise, the overall pain Americans report has not changed. In the 15 years from 2000 to 2015 more than half a million people died from drug overdoses with 91 Americans dying every day from an opioid overdose. The findings from the NFEPP-prototype study indicate that this type of development may also apply to other types of pain and even aid in receptor research. Moving forward these avenues will be explored in order to advance the production of non-dependence forming drugs. To read their study click here.