Painkillers are one of the most effective medicines for those who are suffering from severe pain and tissue damage. Painkiller abuse or addiction is a serious issue, most painkillers today have side effects, which is said to kill millions of people worldwide. Analgesic or Painkillers are said to be very bad because they always come with various side effects such as Nausea, Vomiting, Dizziness, Addiction, Unconsciousness, Respiratory depression, Constipation, etc. Those types of drug or analgesic must always be taken under limited quantities/doses, and only when required.

Painkillers impact the opioid receptors in the brain, which prevent the release of neurotransmitters such dopamine, which is the neurones released chemical, that send signals to other nerve cells. When this happens, the neurotransmitters flood the brain, creating the high and causing side effects.

Now we have some good information for people about a new form of painkillers. Researchers in Germany have discovered a new way of developing painkillers that are more effective and without dangerous side effects. The team of researchers from Charite Universitatsmedizin Berlin used computational simulation to analyse interactions at opioid receptors (the cell’s docking sites for painkillers) to create a morphine-like molecule that only targets the inflamed tissues and interacts with opioid receptors without affecting the healthy ones. This research has been published in the current issue of the journal Science.

Based on their findings researchers created a prototype of a morphine-like molecule and when tested in an animal model. Researchers were able to show that this molecule was able to produce substantial pain relief in inflamed tissues in an animal model without affecting surrounding healthy tissue. However, healthy tissues remained unaffected, suggesting that the severe side effects currently associated with these types of painkillers might be avoided. The findings suggest the prototype of these molecules could be used to eliminate or reduce pain without severe side effects like those linked to opioid medications.

There are painkillers being used that are strong. These are called opioids and are a class of strong pain-relieving medications. Opioids are commonly used by people to treat pain linked to tissue damage and inflammation, such as that caused by surgery, nerve damage, arthritis or cancer. Common side effects from opioid medications associated with their use can include drowsiness, nausea, constipation and, in some cases, dependency and, in some cases, respiratory arrest. Opioid addiction has grown to epidemic proportions in America in recent years, as well as in other countries.

“By analysing drug-opioid receptor interactions in damaged tissues, as opposed to healthy tissues, we were hoping to provide useful information for the design of new painkillers without harmful side effects,” explains Prof. Dr. Christoph Stein, Head of the Department of Anaesthesiology and Surgical Critical Care Medicine on Campus Benjamin Franklin.

Treating postoperative and chronic inflammatory pain should now be possible without causing side effects. Doing so would substantially improve patient quality of life. Photo Credit:- The Irish Times

Professor Dr. Christopher Stein has made the research to develop new painkillers together with Professor Dr. Marcus Weber from the Zuse Institute Berlin. With the help of innovative computer simulations, the scientists were able to analyse morphine-like molecules interact with opioid receptors in the brain. They were able to pinpoint a new mechanism of action, which is capable of relieving pain solely in the desired target tissues affected by inflammation. This then spares healthy tissues from any effects.

With the new painkiller, treating chronic and postoperative (after a surgical operation) inflammatory pain should now be possible without causing side effects. Doing so would substantially improve the quality of life for many patients.

The authors of the study are Dr. Viola Spahn and Dr. Giovanna Del Vecchio, explain: “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.”

After devising and synthesising the drug prototype, the scientists subjected it to experimental testing. Using computerised model, the scientists simulated an increased concentration of protons, thereby mimicking the acidic conditions found in inflamed tissues.

“We were able to show that the protonation of drugs is a key requirement for the activation of opioid receptors,” conclude the authors of the study.

According to Science Daily reports, their findings could also apply to other types of pain and may even find application in other areas of receptor research. Thereby, the benefits of improved drug efficacy and tolerability are not limited to painkillers, but may include other drugs as well.


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