Can Painkillers Provide Relief Without Dangerous Side Effects?

Highlights

• Painkillers provide relief by interfering with the nerve signals that perceive pain.
• Opioid drugs are often used as painkillers for treating tissue damage and inflammation.
• A recent study finds a new way of developing painkillers without any dangerous side effects.

Painkillers are powerful drugs which are capable of interfering with the transmission of nerve signals that perceive pain. A research team from the University of Charite-Universitatsmedizin Berlin has found a new way of developing painkillers which could provide relief and reduce the severe side effects of the drug. The research team used computational simulation for analyzing the interactions at opioid receptors which are the docking sites for painkillers.

The research study was published in the journal Science.

Professor.Dr. Christop Stein, Head of the Department of Anesthesiology and Surgical Critical Care Medicine on Campus Benjamin Franklin, said, "By analyzing 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."

The research team together with PD Dr. Marcus Weber from the Zuse Institute Berlin, and the help of computational simulations, were able to analyze the morphine-like molecules and interactions with opioid receptors.

They were able to identify a mechanism of action, that is capable of producing pain relief in the desired target tissues which is affected by inflammation.

Dr. Viola Spahn and Dr. Giovanna Del Vecchio, explained that, "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."

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The synthesized drug prototype was further subjected to experimental testing. The research team mimicked the acidic conditions of the inflamed tissues by increasing the concentration of the protons.

The authors concluded that, "We were able to show that the protonation of drugs is a key requirement for the activation of opioid receptors."

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The study findings may also apply to other types of pain; this may extend to other areas of receptor research.

Opioid Drugs
Opioids belong to a group of strong painkillers. Hydrocodone, morphine, methadone are some of the drugs used as painkillers.These drugs are used for treating pain associated with tissue damage and inflammation, that can be caused by nerve damage, cancer or arthritis.

Side Effects of Opioid Drugs

• Drowsiness
• Nausea
• Constipation
• Dependency
• Respiratory arrest

Facts on Prescription Opioid Use

• One out of five patients with non-cancer pain is prescribed with opioids.
• Older adults are more likely to use opioid drugs for pain relief.
• When compared to men, women use more prescription opioids.
• Non-Hispanic Whites may use more prescription opioids when compared to Hispanics.

References

1. V. Spahn, G. Del Vecchio, D. Labuz, A. Rodriguez-Gaztelumendi, N. Massaly, J. Temp, V. Durmaz, P. Sabri, M. Reidelbach, H. Machelska, M. Weber, C. Stein. A nontoxic pain killer designed by modeling of pathological receptor conformations. Science, (2017);DOI: 355 (6328): 966 DOI: 10.1126/science.aai8636
2. Injury Prevention & Control: Opioid Overdose - (https://www.cdc.gov/drugoverdose/data/prescribing.html)

Source-Medindia