New ‘safer opioid’ delivers pain relief without addiction risk in early tests
“At preclinical therapeutic doses, DFNZ produced a moderate and sustained increase in brain oxygen rather than depressing respiration,” the authors wrote.
“Repeated doses of the drug did not result in tolerance, drug dependency or meaningful withdrawal effects.”
The only classic opioid withdrawal symptoms observed with DFNZ was irritability, they noted.
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DFNZ could potentially be used as a safer treatment for opioid use disorder, the researchers suggested, as well as for patients undergoing surgery and experiencing cancer-related or chronic pain.
“There’s a lesson here – that even a dangerous chemical can lead to a potential treatment,” Siegel noted. “This needs to be tested in humans, but I think there is potential for a much safer pain drug that is not only not addictive, but may also be a potential treatment for addiction.”
In the study, the team created a drug called DFNZ, a metabolite (derivative) of nitazene, which provided at least two hours of pain relief in mice after just five or 10 minutes in the brain. (iStock)
Among DNFZ’s benefits is that it was found to increase oxygen flow to the brain rather than decrease it, and that it binds tightly to the opioid receptor but doesn’t cause the feared side effects of breathing suppression or addiction, according to Siegel. “It releases dopamine more gradually, which is safer.”
The findings were published in the journal Nature.
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“DFNZ has an unprecedented pharmacology for an opioid,” Michaelides said. “It is a potent and high-efficacy analgesic, but in certain contexts it resembles partial agonists, drugs that activate the receptor with low efficacy, which is what scientists think is needed for safety.”
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“Its capacity to be administered at therapeutic doses without producing respiratory depression is very important.”
The study did have some limitations, primarily that it was conducted with animal (rat) models. The effectiveness and safety of human use is unknown.
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It also did not explore long-term impacts or rare adverse effects, the researchers acknowledged.
Clinical studies will be needed to fully understand the drug’s addictive potential.
The research team plans to conduct more preclinical studies before seeking regulatory approval to conduct human clinical trials.
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Dr. Hooman Melamed, a board-certified orthopedic spine surgeon and sports medicine expert in Beverly Hills, California, said the new research looks “promising,” but urged caution with the early findings.
“Many opioids are known to slow down intestinal mobility, leading to issues like constipation and impaired digestion,” a doctor said. (iStock)
“This new drug claims to release a lower-dose opioid alternative that might be able to offer pain relief without the addictive properties,” Melamed, who was not involved in the study, told Fox News Digital.
“It’s also important to note that this has not been tested on humans, and we don’t know how this will impact people in the long run.”
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Melamed also noted that there is often a “very narrow therapeutic threshold” with this class of drugs.
“In other words, a small increase in the dosage could become addictive for people, and without solid human data, we just can’t know the dependency risk,” he said.
“It’s important to note that this has not been tested on humans and we don’t know how this will impact people in the long run.”
Article source: https://www.foxnews.com/health/new-safer-opioid-delivers-pain-relief-without-addiction-risk-early-tests