Pain Relief Without Opioids?

pain relief

There are many non-opioid pain-relief products in the works, but scientists think this one could be a game changer

By Jason Langendorf

Researchers have identified a new substance that offers pain-relieving effects similar to those of opioids but without the risk of dependence or overdose. It’s a potentially game-changing development in managing pain and tackling the opioid crisis.

Published in the journal Science earlier this month, the work of researchers at Friedrich-Alexander-Universität Erlangen-Nürnberg in Germany revealed a new chemical compound that activates adrenal receptors instead of opioids receptors, allowing for the relief of pain without the usual (and significant) risks of respiratory depression and addiction accompanied by opioid-based medications.

Peter Gmeiner, a professor and the chair of Pharmaceutical Chemistry at FAU and a member of the team of researchers on the project, said in a statement that while some other non-opioid receptors are involved in pain processing, only a small number of them have been fully developed into pain-relief therapies.

As promising as the researchers’ results may be, patients and clinicians shouldn’t hold their breath waiting for an adrenaline-based analgesic to hit the market.

“Various tests confirmed that docking on the receptor was responsible for the analgesic effect,” explains Gmeiner. “We are particularly pleased about the fact that none of the new compounds caused sedation, even at considerably higher doses than those that would be required for pain relief.”

FAU describes the separation of analgesic (pain-relieving) properties and sedation as “a milestone in the development of non-opioid pain medication.” And if the consortium of researchers are able to continue building on their work, that characterization may prove to be spot-on.

The Legitimate Need for Pain Relief

The ongoing crackdown on opioid-based medications in the management of pain may be understandable, in light of the rate of overdose deaths—which, although having slowed somewhat in recent months, remains at more than 100,000 per 12-month period. Yet that offers no relief to the countless number of chronic pain sufferers, including burn victims, cancer patients and people in hospice care.

Other currently approved therapeutics may have some effect, but medication such as acetaminophen, anti-inflammatories and more direct applications (injections and anesthesia, for instance) lack the potency of prescription opioids like codeine, morphine, oxycodone and hydrocodone.

Increasingly, opioid addiction and overdose prevention have become all-agencies-on-deck affairs.

But the nation is in the grips of an epidemic precisely because opioids’ potency doesn’t end there. In the latest information covering opioid medications on its website, the U.S. Food and Drug Administration (FDA) writes that “[r]educing the number of Americans who are addicted to opioids and cutting the rate of new addiction is one of the FDA’s highest priorities.” The agency reasserted this stance in September, with the release of its most recent Overdose Prevention Framework: “Supporting primary prevention by eliminating unnecessary initial prescription drug exposure and inappropriate prolonged prescribing” appears first on the new framework’s list of priorities.

Increasingly, opioid addiction and overdose prevention have become all-agencies-on-deck affairs: A $350 million-plus program called HEALing Communities, for instance, is overseen in partnership by the National Institute on Drug Abuse (NIDA) and Substance Abuse and Mental Health Services Administration (SAMHSA). Among the initiative’s cited priorities is supporting “new clinical trial programs and the expansion of existing programs to evaluate innovative therapies for pain management.”

The Gmeiner Project

Peter Gmeiner

It was Gmeiner who, in 2016, discovered an active substance that bonds known opioid receptors, offering the same level of pain relief as morphine. He and his fellow researchers are now focused on the receptor responsible for binding adrenaline, which has been targeted by other analgesics, though none of those also produce a strong sedative effect. The group’s work narrowed down a virtual library of 300 million molecules to just two that “fulfilled the desired criteria.”

As promising as the researchers’ results may be, patients and clinicians shouldn’t hold their breath waiting for an adrenaline-based analgesic to hit the market. The hope is that these findings eventually will lead to therapies and prescribing practices that can help reduce the number of opioid prescriptions (and, thus, the incidence of diversion and misuse). But as all things are in pharmaceutical development, it’s a process.

“We are currently still talking about basic research,” says Gmeiner. “The development of medication is subject to strict controls, and in addition to significant amounts of funding, it takes a long time. However, these results still make us very optimistic.”

Top photo: Thought Catalog