In 1997, my team of scientists from the Southeast Louisiana Veterans Health Care System and Tulane University School of Medicine discovered a peptide, a small protein found in the brain, called endomorphin-1, that acts on the same receptor as morphine to relieve pain in the body.

Based on that finding, we looked to develop a new drug alternative to traditional opium-based painkillers like morphine, one with fewer side effects and less potential for addiction. Because our peptide has a very different structure than morphine, which comes from a plant, yet is similar to the natural peptide found in the brain, we thought it might be better at relieving pain and have fewer side effects, relative to morphine.

Our recent research study, published in the journal Neuropharmacology, tested many engineered versions of the peptide structure with three goals: to make it stable so it could serve as a drug, to provide long-lasting pain relief, and to avoid side effects.

The team conducted several tests in rats and mice, the most commonly used animal models that predict effects in humans. The first tests determined variations of the drug that produced effective pain relief, showed reduced respiratory depression (the cause of fatalities from opioids), and had less impairment of motor coordination. In other words, we selected compounds that were as efficacious as, but safer than, opium-based painkillers.

Older adults, including our elderly Veteran population, are the most in need of pain relief, while at the same time they are at the greatest risk of suffering severe injury due to a fall. Likewise, active duty military members need pain relief without the loss of motor coordination. It’s a critical safety issue.

Next, we examined longer-term effects. Drugs like morphine produce tolerance, the requirement for higher doses over time to maintain a given level of pain relief. This dose escalation can contribute to side effects. The new drug showed substantially less tolerance than morphine. This difference may be due to a nervous system inflammatory response that was seen with morphine but not with the endomorphin-based drug. The absence of an inflammatory effect may also indicate improved pain treatment for conditions like traumatic brain injury, in which inflammation in the brain can contribute to long-term cognitive impairments.

Finally, we tested several animal models for reward and addiction potential. Animals given morphine were more likely to return to the place where they were given morphine and also were more willing to work harder at pressing a bar for a morphine infusion. In other words, there was a stronger addictive tendency associated with morphine than was observed with the new endomorphin-based drug.

The development of a safer pain reliever with less likelihood of abuse is important because according to the Centers for Disease Control and Prevention, overdose deaths from opioid painkillers in the U.S. have quadrupled since 2000.

Most currently used opioid painkillers, like oxycodone and hydrocodone, are based on chemicals that were discovered around 100 years ago, or on morphine, discovered about 200 years ago. To get different results, our thinking was “why not start from scratch with a new compound.”

Because this structure could show fewer side effects, not cause a pro-inflammatory response, and be less addictive, we hope the drug will address two major issues for Veterans: better treatment for pain, and reduced opioid addiction.

There is still a lot of work to do before human clinical trials can begin, including standard FDA safety, toxicology and pharmacology tests, but our latest study and its findings could be significant in the long-term care of our Veterans.


Zadina1About the Author:Dr. Zadina is a professor of medicine at Tulane University and director of the Neuroscience Laboratory at the Southeast Louisiana Veterans Health Care System.

 

 

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12 Comments

  1. Leon Suchorski February 27, 2016 at 09:48

    As a Marine, I fight the pain all of the time, rather than take the opiods. What I take, is children’s aspirin in comparison, and am eagerly looking forward to something better, and safer. There was a time that I was on morphine, and did not like it. The pain just leaves me so exhausted. I end up sleeping up to 20 hours a day because of it. Sleep is the only thing that will mask the pain.

  2. paul lesassier February 27, 2016 at 09:34

    Certian politicians and lobbyists for the pharmaceutical companies use thier power and money block the passage of any favorable medical break throughs. Especially where new cancer prevention drugs are involved. Drug companies won coverage for prescription drugs under Medicare in 2003 while blocking the government from negotiating prices downward. They have so far kept out imports of cheaper medicines from Canada and other countries. I don’t think there is a patient-advocacy group in America that does not receive some level of funding from a pharmaceutical company, Since 1998, drug companies have spent $758 million on lobbying — more than any other industry, according to government records analyzed by the Center for Public Integrity, a watchdog group. In Washington, the industry has 1,274 lobbyists — more than two for every member of Congress. The industry’s deep inroads into the government are rooted in its dependence on federal decisions. The government determines which products drug companies can market and how they’re labeled. The government buys massive quantities of drugs through Medicaid, the Veterans Administration and other programs. Billy Tauzin, a former Republican congressman from Louisiana who now heads the Pharmaceutical Research and Manufacturers of America (PhRMA), serves as testament to the industry’s power. Tauzin says the lobbying presence is needed to protect the U.S. marketing system for prescription drugs. The United States “is probably the last place on Earth which encourages innovation and discovery, In other countries, he says, government-controlled pricing has robbed drug manufacturers of the profits that finance new drug development. Drug companies and their officials contributed more than $17 million to federal candidates already this year. Google pharmaceutical lobby spending in washington to see who and how much is spent. I am not optimistic that something this good will be allowed to come to the aid of our veterans because of corporate greed.

  3. David Felten February 26, 2016 at 22:10

    Are there any vets out there who have the SAH grant and are getting “screwed” by the miserable way it’s implemented????????

  4. Dorothy Littrell February 26, 2016 at 18:06

    I have been receiving my health care through the V.A. for almost forty years. The V.A. Health Care has changed in remarkable ways. I couldn’t be happier with the facilities or care that I now receive through my primary care and the several specialty clinics that I visit. Another plus is the fact that any V.A. Medical Facility has immediate access everything concerning my health care. I do not believe that I could get better care anywhere.

  5. Whitney Philbrick February 26, 2016 at 16:02

    I’m a USMC Vet with chronic pain since 1989, where do I sign up for trials!!

    Whit

  6. Johnny Sullivan February 26, 2016 at 15:09

    I’ll tell you what if a team of lawyers and legal experts would ban together and draft up laws pentalizing and making it a treasionist crime . For polticians and lobbyists to lobby for the pharmicutical companies in helping them block the passage of any favorble medical breakthroughs. They should be put on public trial for treasonist crimes against their fellow Americans. I just thank that its a crying shame when the greedy ass companies and politicians have to stupe so dann low to make a buck. And also I think if we had more watch dog groups out there watching out for stuff like this and putting the names of these culprits out there to be exposed for such acts. Then maybe they wouldn’t be so gun hole to sponsor such a bill.

    P.S look forward to any other good ideals to be posted.☺☺

    • Keith Schoonmaker February 28, 2016 at 17:54

      I think you’ve got a great idea there!!! Someone PLEASE find a way to make this happen!!!

      I’ve suffered with pain in my back & legs since before I was medically discharged in 87. I’ve been on morphine since 89 and I’ve had a Neurostimulator implant to help with that pain since 99. I’d sign up for trials tomorrow if it were possible. I’ve also got COPD/emphysema so I just hope I’m still alive to see it. Stranger things have happened though so you never know! Especially with this presidential race going on right now.

  7. William R. Pomeroy February 26, 2016 at 13:01

    I’ve been taking various opioids since 2000 and this new treatment sounds like a very attractive alternative. How can I volunteer for any Clinical Trials (I am 1 hour from New Orleans)? I am willing, able, and very interested. Thx.

  8. Walter J. Petts February 26, 2016 at 12:32

    Sounds “GREAT”. The plant based drugs (that GOD put here to help people) do not have the side effects that chemical drugs do but are not allowed on the market if the BIG drug companies can not find a way to charge BIG bucks in selling them and with their POWER and BIG BUCKS they can make sure that it is not approved for use. If it is working well in your tests, I believe that there are probably MANY people that would be willing to be used to try it. I pray that somebody would be able to get something like this into the marketplace to help Veterans AND OTHERS without BIG drug companies being able to stop it.

  9. Natalie Neckermann February 26, 2016 at 12:23

    As someone who did serious damage to her joints as a Marine MP, I am very excited about this news! I now have RA and would love to participate in the trials for this!

  10. Robert Hebert February 26, 2016 at 10:47

    Excellent. I’m very happy to hear that someone is working on this. And the VA? Who knew? Thanks for your efforts. I hope this is a turning point.

    • HM-RT February 27, 2016 at 16:42

      Many VA facilities work in conjunction with Universities that get grants for research like this one. It’s really a win win scenario as this article has demonstrated. Best of luck to this team of researchers and may the Lord guide you all with your work.

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