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Research Breakthrough

A Way to Produce Non-Addictive Opiates

posted 09:42 PM EST, Sun August 19, 2012
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By adding a medication called +Naloxone to opiates, researchers managed to "remove" intoxication and addiction while retaining their pain relieving properties. 

Opiates work amazingly well for pain relief, but that effectiveness comes with an inseparable cost: they produce such pleasure that a substantial percentage of those that use them succumb to addiction.

Now, a team of Australian and American researchers think they've come up with something huge - a way for people to use opiates and get full pain relief without getting any of the intoxicating side effects and without any risk of developing an addiction.

Adding the Drug +Naloxone Makes Opiates "Non-Addictive"

Naloxone is an opiate antagonist which instantly reverses the effects of substances like morphine and heroin and it can be a lifesaving medication when administered in time to a person overdosing on any kind of opiate.

By tweaking Naloxone a bit, the researchers developed a new medication called +Naloxone, which targets TLR-4 immune system receptors on cell membranes. TLR-4 receptors work to identify substances such as bacteria, viruses or psychoactive substances like opiates, as they bump against cell walls. When +Naloxone is administered with an opiate, it binds to the TLR-4 receptor and blocks its influence.

The research team had previously demonstrated that opiates bind to TLR-4 receptors in the brain, and though they suspected that TLR-4 receptors played a role in addiction, they weren't sure what that role was.

The Experiment

  • For the experimental period, one of group of rats received doses of morphine only and another group of rats received +Naloxone followed by morphine.

The Results

  • Rats given morphine only displayed behaviors of animal addiction.
  • Rats given +Naloxone and morphine displayed no behaviors of addiction
  • Pain tests showed that both groups of rats received equal analgesia
  • When looking at brain activity, the researchers observed that the rats given +Naloxone and morphine showed no extra dopamine release


Commenting on the significance of the results, lead study author Mark Hutchinson Ph.D. wrote, “Our studies have shown conclusively that we can block addiction via the immune system of the brain, without targeting the brain’s wiring. Both the central nervous system and the immune system play important roles in creating addiction, but our studies have shown we only need to block the immune response in the brain to prevent cravings for opioid drugs.”

The full results are published in the Journal of Neuroscience.

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Story Highlights
  • Non Addictive Opiates: Adding +Naloxone to opiate drugs may render them non addictive but still useful for analgesia
  • Role of the Imune System: +Naloxone blocks TLR-4 immune system receptors, which seem to play a substantial but still poorly understood role in the development of addictions
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