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  1. Beenthere2Hippie
    While the opioid epidemic continues kill more than 40 Americans every day, researchers and health experts are frantically searching for ways to curtail use of the highly addictive, pain-quenching drugs. In March, the Centers for Disease Control and Prevention even released new guidelines directing doctors to simply refrain from prescribing opioids. But if a new study holds up, the health agency may be able to reverse course.

    According to a report in the Proceedings of the National Academy of Sciences, an opioid drug referred to as BU08028 was able to alleviate pain in a dozen monkeys just as well as other opioid painkillers, such as morphine. Yet, unlike every other opioid drug, BU08028 showed no signs of being addictive. Even at high dose—at which other opioid drugs inhibit the respiratory and cardiovascular system, which can be fatal—BU08028 was harmless.

    "Based on our research, this compound has almost zero abuse potential and provides safe and effective pain relief," Mei-Chuan Ko, a professor of physiology and pharmacology at Wake Forest Baptist Medical Center and lead author of the study, said in a statement. "This is a breakthrough for opioid medicinal chemistry that we hope in the future will translate into new and safer, non-addictive pain medications."

    In pain experiments, which involved dipping monkeys' tails into hot water, BU08028 was a potent pain-killer. A single dose relieved pain for up to 30 hours. Next, in experiments in which the monkeys were trained to self-medicate, BU08028 proved no more habit-forming than a control dose of saline. Scientists forced one group of monkeys to take BU08028, while another group was forced to take morphine. When the drugs were taken away, the monkeys who had taken BU08028 showed no withdrawal symptoms, unlike the monkeys who had blazed on morphine.

    BU08028's lack of nasty side-effects may hinge on its dual-action biochemistry. Like other opioids, it controls pain by targeting the nervous system's classic μ-opioid peptide receptors, called MOP receptors. But BU08028 also targets “nonclassical” opioid receptors, called NOP receptors for nociceptin receptors, in the nervous system. These receptor proteins generally don’t interact with opioid drugs, yet they share similarities with the receptors that do. NOP receptors regulate pain, like their MOP counterparts, but they are also involved in a host of other brain functions, such as memory, cardiovascular functions, and anxiety.

    “To our knowledge, the present study provides the first functional evidence in nonhuman primates that BU08028 with mixed MOP/NOP agonist activities is an effective and safe analgesic without apparent abuse liability or other opioid-associated side effects,” the authors conclude.

    Next, the researchers hope to test BU08028 at treating chronic pain without risks of addiction or overdoses. Regardless of BU08028's fate in subsequent trials, the researchers are hopeful that the strategy of co-activating NOP and MOP receptors will eventually lead to a safer painkiller.

    Proceedings of the National Academy of Sciences, 2016. DOI: 10.1073/pnas.1605295113 (About DOIs).


    By Beth Mole - Ars Technica/Sept. 5, 2016
    http://arstechnica.co.uk/science/20...ithout-being-addictive-or-deadly-in-primates/
    Photo: John Moore, getty
    Newshawk Crew

    About Author

    Beenthere2Hippie
    BT2H is a retired news editor and writer from the NYC area who, for health reasons, retired to a southern US state early, and where BT2H continues to write and to post drug-related news to DF.

Comments

  1. Beenthere2Hippie
    Other than my always feeling terribly sorry for the plight of test monkeys, I'm thrilled to think there just might actually be a medication that will take away my chronic pain and replace the addictive version of opioid and opiate I've been living on for years now: oxycodone and morphine.

    Of course, I'm having a difficult time believing such a wonder drug's development - free of side effects - is even close to an actuality, but it is it would be amazing for many of the world's millions of pain patients. Can you begin to imagine the world of good such a drug would do to enhance average people's lives?

    That's if, like so many other Big Pharma products, BU08028 is not priced out of reach...like epipens and high quality cancer drugs...
  2. aemetha
    If it becomes the world's only non-addictive non-euphoric opioid painkiller you can guarantee it will be price gouged beyond all imagining by big pharma. Doctors will immediately stop prescribing any other opioid.

    I can believe the part about no opioid side effects, I'm a little dubious about no side effects at all though, especially if it's targeting receptors involved in memory, anxiety, and cardiovascular function. The human trials when they happen will be interesting to see, I hope it doesn't turn out to be one of those cases where the true extent of the side effects isn't known until several years after it's introduction.
  3. nomud
    Dipping monkeys' tails in hot water!

    I'd like to see those A-holes fed to a
    wood chipper feet first ;) Not the monkeys
    the ones dipping their tails in hot water>
  4. RoboCodeine7610
    Classical opiates will always be around. Some people may be allergic to these compounds or simply tend to suffer from some specific side-effect.

    I actually think the wide availability of pharmaceutical-grade opiates is a great way to prevent a great deal of overdoses from black blobs or white powders of unknown concentration and composition. Anyone using illicitly produced opiates who simply does not wish, or more likely, cannot quit, has the right to be treated like a human being and be given sterile, properly synthesized diacetylmorphine as replacement therapy.

    Think about it: Giving them methadone or buprenorphine indefinitely is considered a proper way of maintaining an addict, even if it severely impairs them. I've seen countless addicts constantly nod out from methadone, administered at the prescribed maintenance dosage. So what's the difference? I'll tell you what: Heroin is actually enjoyable. But I really can't grasp is why heroin addicts actually enjoying their replacement medication for as long as they think they need it is such a terrible thing. If they choose to try to get clean after some voluntary counselling or by their own initiative then you can consider things like a buprenorphine taper.

    So yeah, I just don't get what the problem is with addicts feeling good at no extra cost to anyone else...

    Robo
  5. malsat
    The replacement of standard opiods with this drug would see a great increase in overdoses and other harms as people switched over to heroin en masse. I doubt it would curtail new addiction much either. People would just end up with different crutches. Booze, benzos, stims, RCs, whatever, and even those who would have never seen themselves on heroin would still have a path to its use.

    Having said that I am skeptical that this medication will be able to be used chronically without the development of tolerance and withdrawal symptoms and, as mentioned by aemetha, nonclassical opiod side effects. That is just how neuro-active medications work, the brain adapts, while altering its function creates side effects.
  6. Weltmeister
    https://www.researchgate.net/figure...effect-of-BU08028-A-and-buprenorphine-B-alone
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