New Approach to an Overgrown Problem: ‘Non-addictive’ Painkillers Tested to Replace Opioids

We have pretty dutifully, and thoroughly, covered the historic spike in prescription drug and opioid abuse on this blog.

We have also, along with others in the media, health policy, and addictions treatment field, reflected on its costly, truly heartbreaking fallout – a massive increase in the numbers of overdose deaths, hospitalizations, and shattered lives and families in the last several years as our country tries to find its way out of an overreliance on opiate-based prescription medications and street drugs.  Rightly so. This is a huge issue for individuals and our public health as a nation.

But importantly, we have always tried to advance the conversation by asking, “What is being done about it (if anything concrete), and to what effect?” Thankfully, there has been more than just presidential dialogue on the subject, though we noted that even that was welcome earlier this year.  Since that time, we have seen legislation passed allocating nearly half a billion dollars to expand efforts to prevent, and treat, opiate addiction. And, even as the Comprehensive Addiction and Recovery Act (CARA) was being debated and revised in Congress, we began to see new prescription drug monitoring programs take hold, additional guidance and education efforts about how best to treat pain gain steam, and even programs launched to explore how treatment might be made more widely available. Progress to be sure…

A perhaps more interesting and exciting development, however, has been the recent fire that the opioid problem has lit in the realm of research and innovation. Just this week, a government-funded study was published showing promise for a new compound that would have the analgesic pain-relieving effects of opioid products like OxyContin or Percocet, but (at least as research now seems to suggest) without the high potential for addiction or wealth of negative effects.  The medication, known as BU08028, is able to both relieve pain and minimize addictive reactions in those who take it because it was designed to interact with two different kinds of brain receptors – those that interfere with pain sensations and those that make us want to experience that reward and pleasant feeling over and over again, often prompting the addictive pursuit of a substance.

It is estimated that more than 100 million Americans suffer from chronic or debilitating pain. And for hundreds of years, opioids have been a drug of choice to provide relief. They work by reducing the intensity of pain signals reaching the brain, primarily by interfering with neuroreceptors known as opioid receptors. The main target for opioid drugs is a particular receptor called the mu-opioid peptide receptor (MOP) which helps to regulate the feeling of pain. However, opioid medications tend to be so addictive because these same opioid receptors that respond to pain signals are also involved in regulating emotional impulses such as the desire for reward, euphoria, and cravings.

Previous research has found that drugs that work on another neuroreceptor called the nociceptin-orphanin FQ peptide receptor (NOP) can block the addictive effects of opioids. So, Stephen Husbands, a professor of medical chemistry at the University of Bath in England, created a dual-receptor-binding drug that simultaneously targets both the MOP and NOP brain receptors to produce opioid-like pain relief while reducing the risk of addiction.

“There is a clear need for more effective pain medications, which hopefully should relieve pain without central side effects due to an action on the brain — such as sleepiness, confusion or double vision — and without constipation or the potential for addiction,” said Dr. Stephen Waxman, a professor of neurology at the Yale University School of Medicine in New Haven.

Scientists tested the new medication on rhesus monkeys and are optimistic about observing similar results in humans because monkeys’ brains and physiological responses to stimulation are so similar to our own. In the tests performed on monkeys, they found that BU08028 doesn’t seem to slow breathing, disrupt the cardiovascular system, or cause addiction – side effects common to opiates. What’s more, BU08028 did not cause such effects even at 10- to 30 times the dose needed to relieve pain. And, lead researchers say, it appears to be better at reducing pain than over-the-counter painkillers.

The exploration of new compounds to replace opiates seems to be trending, as the medical, treatment, and consumer populations all come to terms with the dangerous explosion in opioid addiction rates and deaths. In fact, in many ways, we seem to be looking to fill a medication void once solidly occupied by drugs like Vicodin, morphine, codeine, and OxyContin. Earlier this spring, Tulane University scholars tested a similar peptide-based drug in rats that also showed promise in relieving high levels of pain without triggering addictive responses or cardiac depression.

In both cases, testing on humans and a pill form of these drugs in the marketplace will not happen for at least a couple of years. And some are skeptical that human trials will be as successful as those conducted on animal subjects.

Still, the work to find a fundamentally different way to address pain through brain science is a boon. We just hope that the efforts to replace one drug for another do not eclipse the wealth of other alternatives, holistic approaches to mitigating and managing pain like mindfulness meditation, acupuncture therapy, and even cupping – which gained unexpected new attention and cache` based on the positive experiences of Rio Olympic athletes. While these age-old methods of addressing pain and promoting healing and relaxation may not be singularly effective at addressing more severe cases, they should be considered as a natural and healthy way to deal with the pain that does not involve trading one pill for another. And that’s always a good thing from our perspective.

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