New Opioid Ligands May Provide Pain Relief Without Addiction Risk

PainRelief.com Interview with:

Prof. Dr. Christoph Stein Direktor Institut für Experimentelle Anaesthesiologie Charité Campus Benjamin Franklin Freie Universität Berlin 

Prof. Stein

Prof. Dr. Christoph Stein
Direktor
Institut für Experimentelle Anaesthesiologie
Charité Campus Benjamin Franklin
Freie Universität Berlin 

PainRelief.com: What is the background for this study? What are the main findings? 

Response: Our group has studied the biology and pharmacology of opioid receptors on peripheral sensory neurons (i.e. outside the central or intestinal nervous system) for over 25 years. We have always aimed at finding mechanisms and opioid receptor ligands that can be developed into drugs inhibiting pain without eliciting typical adverse effects of conventional opioids such as apnoea, addiction, sedation or constipation.

From our previous work we knew that the selective activation of opioid receptors on peripheral sensory neurons can produce powerful pain relief in animals and human patients. Those analgesic effects are particularly strong in pain caused by tissue injury and inflammation (e.g. postoperative pain, arthritis). Together with mathematicians (Dr. Marcus Weber) at the Zuse Institute Berlin, we started out with computer simulations examining the interaction between opioid ligands and receptors in normal (noninflamed) and inflamed environments. These studies indicated a stronger binding of conventional opioid ligands (morphine, fentanyl) to opioid receptors at increased proton concentrations (i.e. low pH, as present in acidotic/inflamed tissue). We also knew that the protonation of a tertiary amine in the ligand is required for opioid receptor activation. Using those in silico simulations, we now designed a new ligand (NFEPP) that is only protonated (and capable of activating opioid receptors) at low pH, but not at normal pH (as in brain and intestinal wall). After synthesis of NFEPP (and similar derivatives) by a contractor we tested them in vitro and in vivo. NFEPP produced opioid receptor activation and analgesia selectively at low pH/tissue inflammation (as present in nerve injury/neuropathy and abdominal inflammation) without eliciting respiratory depression, addiction potential, sedation or constipation. 

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SEAL Procedure Gives Pain Relief To Some After Failed Back Surgery

MedicalResearch.com Interview with:
"Personal Injury Back Pain" by SanDiego PersonalInjuryAttorney is licensed under CC BY-SA 2.0
Michael Perloff, MD PhD

Assistant Professor of Neurology
Interventional Pain Management
Boston University School of Medicine

MedicalResearch.com: What is the background for this study? What are the main findings?

Response: Low back pain is very common. Patients with chronic low back pain that does not benefit from physical therapy, medications, or injections, often get spine surgery. If surgery fails to help (Failed back surgery syndrome-i.e. continued low back and leg pain after surgery), options for pain relief become more complex.

Typically, patients with failed low back surgery syndrome have tried complex procedures, repeat surgery or technology implants as their main options.

The SEAL procedure is a shortened, simple procedure (done in about 20 minutes) that can help as treatment for failed back surgery symptoms. In the published case series of 30 patients, some patients achieved very good, sustained, pain relief. Continue reading

FDA Approved Emgality Offers New Hope For Migraine Prevention

PainRelief.com Interview with:
Gudarz Davar, M.D., Vice President
Neuroscience Platform Leader
Eli Lilly and Company

PainRelief.com: What is the background for this announcement?  How big a problem is migraine in the US?  Who is primarily affected? 

Response: Migraine is a disabling, neurologic disease that affects more than 30 million American adults. According to the Medical Expenditures Panel Survey, the total unadjusted cost associated with migraine in the U.S. is estimated to be as high as $56 billion annually. People with migraine can miss out on significant moments in their lives—birthdays and anniversaries—and there remains an unmet need for treatment options that can help patients achieve significant reductions in the overall frequency of migraine attacks.

Emgality (galcanezumab-gnlm) was approved by the FDA on Thursday, September 27, for the preventive treatment of migraine in adults. Emgality is a humanized monoclonal antibody indicated for the preventive treatment of migraine in adults that binds to CGRP ligand and blocks its binding to the receptor, which is believed to play a role in migraine. It is offered as a self-administered, once-monthly subcutaneous injection. Emgality offers new hope to people living with migraine as one of the first medicines developed specifically for the prevention of migraine.

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Exercise Longer With Less Pain Using Virtual Reality

PainRelief.com Interview with:

This is a visual of VR exercise environment during test.

This is a visual of VR exercise environment during test.
Credit Maria Matsangidou

Maria Matsangidou, PhD
School of Engineering and Digital Arts
University of Kent

PainRelief.com: What is the background for this study? What are the main findings?

Response: The results show that Virtual Reality (VR) technology can influence the perception of task difficulty, endurance performance and pain experienced during exercise. Most importantly, exercising through the use of VR technology revealed a significant decrease in Pain Intensity and Perceived Exertion reports, and a significant increase in Time to Exhaustion. This was contrary to conventional non-VR exercise which was found to have a significantly higher Pain Intensity and Perceived Exertion reports, and a significantly lower Time to Exhaustion.

In addition the results show that personal characteristics of internal body awareness, such as Private Body Consciousness, does not influence the efficiency VR has on the time to and the perceived pain and exhaustion. This means that the effectiveness of VR technology on time and the perception of pain and exhaustion could not be influenced by personal characteristics of internal body awareness.

A possible explanation could be that the attention of the participants is shifted from the observation of internal functions onto the virtual room and exercise.

PainRelief.com: What should readers take away from your report?

Response: That VR provides a new form of reality, where the individual’s is able to exercise for longer with less pain and effort, and by extension this can increase physical activity. One can imagine how beneficial it would be for specific populations, such as athletes or individuals who are reluctant to engage in physical activity, as well as clinical populations where their recovery can be enhanced through physical physiotherapy.

PainRelief.com: What recommendations do you have for future research as a result of this work?

Response: Future research may investigate the conditions under which Private Body Consciousness may influence immersion and potentially the effectiveness of VR. For example, more research is needed to determine whether the virtual environments representing natural and photorealistic environments are more or less effective than ones presented in cartoonish form.  Furthermore, it would be worthwhile adopting a mixed-methods approach (questionnaire and interview) in order to address user preferences for the design of VR environments.  Finally,  this  study utilized participants who  were  both  active  and  inactive,  therefore  future  work  should  seek  to replicate  this  study  with  a  group  of  sedentary  participants,  as  this  is  where  the  greatest potential for positive impact on behavior may be. 

No disclosures 

Citation:

Maria Matsangidou, Chee Siang Ang, Alexis R. Mauger, Jittrapol Intarasirisawat, Boris Otkhmezuri, Marios N. Avraamides. Is your virtual self as sensational as your real? Virtual Reality: The effect of body consciousness on the experience of exercise sensations. Psychology of Sport and Exercise, 2018; DOI: 10.1016/j.psychsport.2018.07.004

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Fixed-Dose Combination Acetaminophen/Ibuprofen for Postoperative Dental Pain

PainRelief.com Interview with:

Prof Chris Frampton PhD Department of Medicine University of Otago Christchurch, New Zealand

Prof. Frampton

Prof Chris Frampton PhD
Department of Medicine
University of Otago
Christchurch, New Zealand

PainRelief.com: What is the background for this study?

Response: Acute pain is a significant burden to the individual and to society. In light of the ongoing opioid crisis, there is a need for effective nonopioid pain medications that provide improved analgesia over common analgesics, without compromising tolerability. Multimodal analgesia combines multiple drugs with different mechanisms of action to improve pain relief while limiting side effects. Fixed-dose combination tablets containing acetaminophen and ibuprofen are already available in many countries; however, the therapeutic advantages of such products are not available to patients in the United States. The US Food and Drug Administration (FDA) has restricted the dose of acetaminophen in prescription drugs to 325 mg per tablet, therefore an existing product containing acetaminophen 500 mg + ibuprofen 150 mg per tablet (two tablets per dose) has been downscaled to comply with FDA restrictions (acetaminophen 325 mg + ibuprofen 97.5 mg, three tablets per dose). The goal of this study was to determine the efficacy of the new fixed-dose combination of acetaminophen 975 mg and ibuprofen 292.5 mg (FDC 975/292.5) relative to acetaminophen or ibuprofen monotherapy, or placebo following the surgical removal of at least two impacted third molars.

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Performance Health and Drew Brees Launch “Safer Pain Relief”

“To help inform Americans about existing, non-prescription solutions for pain relief, Performance Health, makers of Biofreeze Pain Reliever and TheraBand exercise and recovery tools, will partern with NFL pro and current New Orleans Saints quarterback, Drew Brees to launch a national “Safer Pain Relief” campaign.

The “Safer Pain Relief” initiative will address the dangers of misusing opioid pain relievers and the opportunity, in many cases, to use alternatives.

http://www.prweb.com/releases/2017/07/prweb14503305.htm