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New Painkiller Is More Powerful Than Morphine Without The Side Effects

Discussion in 'Pharmacology' started by Hadeel Abdelkariem, Oct 18, 2018.

  1. Hadeel Abdelkariem

    Hadeel Abdelkariem Golden Member

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    A new chemical compound might pave the way for a new option in the fight against the opioid crisis.

    Researchers developed an experimental painkiller option that’s as powerful than morphine at a dose that’s 100 times smaller. Published Wednesday in Science Translational Medicine, the study found that the compound, called AT-121, doesn’t have the same side effects as more dangerous painkillers.

    "In our study, we found AT-121 to be safe and non-addictive, as well as an effective pain medication," Mei-Chuan Ko, a professor at Wake Forest Baptist Medical Centre, explained in a statement. "In addition, this compound also was effective at blocking abuse potential of prescription opioids, much like buprenorphine does for heroin, so we hope it could be used to treat pain and opioid abuse."

    More than 115 people die from opioid overdoses every day in the United States, according to the Department of Health and Human Services. Between 21 and 29 percent of patients who are prescribed opioids for chronic pain misuse the drugs—and between eight and 12 percent end up developing an opioid use disorder. From July 2016 and September 2017, opioid overdoses increased 30 percent in 52 areas in 42 states.

    Current opioid drugs focus on the mu opioid receptor, which is a part of the brain that helps a person not to feel pain. The team aimed to create a drug that would activate that receptor, but would also activate the nociception receptor, which can block the side effects of opioids, like addiction, respiratory depression, and increased sensitivity to pain.

    "We developed AT-121 that combines both activities in an appropriate balance in one single molecule, which we think is a better pharmaceutical strategy than to have two drugs to be used in combination," Ko said.

    The researchers tested AT-121 on non-human primates and it acted the way they hoped—it provided pain relief without the side effects. When the monkeys were allowed to self-administer the drug by pressing a button, they chose not to. The scientists believe this shows that the drug doesn’t make someone feel like getting AT-121 is a reward or that it’s addictive. However, researchers still need to look into any other potential side effects on other parts of the brain.

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    A pharmacist holds prescription painkiller OxyContin. Between 21 and 29 percent of patients who are prescribed opioids for chronic pain misuse the drugs.GEORGE FREY/REUTERS

    "The results are really clear-cut, but there are a few things that still need to be done before it can ultimately go forward," Bryan Roth, a professor at the University of North Carolina at Chapel Hill and wasn’t involved with the study, told Live Science. “It's very important to find out—does [AT-121] interact with any other receptors or ion channels or transporters in the body?"

    Next, the scientists hope to go through the safety and toxicology studies that the U.S. Food and Drug Administration requires, and then continue on to human trials.

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