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I came across this article from the Journal of Neuroscience and found it interesting, so I'm sharing it here for others.
Drug allows morphine to relieve pain without addiction
22:00 14 August 2012 by Catherine de Lange
A potential new treatment to prevent morphine addiction is at hand. Researchers have identified an immune receptor involved in addiction to the drug, and found a way to block this receptor without affecting pain relief. The discovery offers hope that morphine can be used to relieve pain without running the risk of addiction.
Opioid drugs such as morphine are known to target opioid receptors in the central nervous system, which block pain signals to the brain and flood it with the "feel-good" chemical dopamine. This reward response is what makes opioids so addictive.
Morphine is a widely used pain killer, but its addictiveness means it has to be administered with caution, and often cannot be used for protracted periods of chronic pain.
Mark Hutchinson from the University of Adelaide, Australia, and colleagues have now discovered that as well as working through the central nervous system, opioid drugs like heroin and morphine trigger an immune response, which seems to boost their addictive effects. Blocking this immune response in animals inhibits their addiction.
Hutchinson's team previously observed that opioids bind to TLR-4 immune system receptors in the cell membrane which are responsible for identifying foreign bodies. However, the team did not know how this binding affected the body.
Immunity receptor block
In their latest study, the team found that the receptor acts as an amplifier of reward when opioids are bound to it. The team did a series of experiments looking at addictive behaviour in rats and mice that had been given either morphine alone, or a drug called plus-naloxone which blocks the TLR-4 receptor followed by morphine.
Rats given plus-naloxone before receiving morphine did not exhibit behaviour linked to addiction. Their brains also showed a significantly lower release of dopamine than in rats that only received morphine. Using a heat sensitivity test, the team also showed that the rodents given plus-naloxone still experienced pain relief from the morphine, despite lacking signs of addiction.
To make sure that the TLR-4 receptor really was controlling these differences, the team also bred rats that lacked the receptor. Under the same tests, these rats behaved like those that had been given plus-naloxone.
The idea that the rewarding effect of opioid drugs is potentially mediated by this receptor "flies in the face of current opinion," says Chris Bailey, a pharmacologist from the University of Bath in the UK. "People for hundreds of years have been trying to come up with an opioid analgesic which isn't rewarding," he says.
These findings are particularly interesting, he says, because it's the first time a mechanism has been identified that separates the pain relief and reward responses to opioid drugs. "It has always been seen that the analgesia and the rewarding aspects go hand in hand," he says.
The next step will be to find out exactly how the receptor helps to control the reward behaviours linked to addiction, he adds. Clinical trials to test the effectiveness of combining morphine with a drug like plus-naloxone could begin as soon as 18 months from now.
Journal reference: Journal of Neuroscience, DOI: 10.1523/jneurosci.0684-12.2012
Drug allows morphine to relieve pain without addiction
22:00 14 August 2012 by Catherine de Lange
A potential new treatment to prevent morphine addiction is at hand. Researchers have identified an immune receptor involved in addiction to the drug, and found a way to block this receptor without affecting pain relief. The discovery offers hope that morphine can be used to relieve pain without running the risk of addiction.
Opioid drugs such as morphine are known to target opioid receptors in the central nervous system, which block pain signals to the brain and flood it with the "feel-good" chemical dopamine. This reward response is what makes opioids so addictive.
Morphine is a widely used pain killer, but its addictiveness means it has to be administered with caution, and often cannot be used for protracted periods of chronic pain.
Mark Hutchinson from the University of Adelaide, Australia, and colleagues have now discovered that as well as working through the central nervous system, opioid drugs like heroin and morphine trigger an immune response, which seems to boost their addictive effects. Blocking this immune response in animals inhibits their addiction.
Hutchinson's team previously observed that opioids bind to TLR-4 immune system receptors in the cell membrane which are responsible for identifying foreign bodies. However, the team did not know how this binding affected the body.
Immunity receptor block
In their latest study, the team found that the receptor acts as an amplifier of reward when opioids are bound to it. The team did a series of experiments looking at addictive behaviour in rats and mice that had been given either morphine alone, or a drug called plus-naloxone which blocks the TLR-4 receptor followed by morphine.
Rats given plus-naloxone before receiving morphine did not exhibit behaviour linked to addiction. Their brains also showed a significantly lower release of dopamine than in rats that only received morphine. Using a heat sensitivity test, the team also showed that the rodents given plus-naloxone still experienced pain relief from the morphine, despite lacking signs of addiction.
To make sure that the TLR-4 receptor really was controlling these differences, the team also bred rats that lacked the receptor. Under the same tests, these rats behaved like those that had been given plus-naloxone.
The idea that the rewarding effect of opioid drugs is potentially mediated by this receptor "flies in the face of current opinion," says Chris Bailey, a pharmacologist from the University of Bath in the UK. "People for hundreds of years have been trying to come up with an opioid analgesic which isn't rewarding," he says.
These findings are particularly interesting, he says, because it's the first time a mechanism has been identified that separates the pain relief and reward responses to opioid drugs. "It has always been seen that the analgesia and the rewarding aspects go hand in hand," he says.
The next step will be to find out exactly how the receptor helps to control the reward behaviours linked to addiction, he adds. Clinical trials to test the effectiveness of combining morphine with a drug like plus-naloxone could begin as soon as 18 months from now.
Journal reference: Journal of Neuroscience, DOI: 10.1523/jneurosci.0684-12.2012
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What would be good is having pain management where your body doesn't build up a resistance to the dose. That would be better pain management. Sounds like they may be making some steps towards that.
Thank you for posting this.
I'll watch for updates on this drug. Thanks for sharing.
Also, I think it's just good to know that there continues to be at least some research done into better medications for treating chronic pain.
I've been investigating micro-dose naltrxone with opiates ( it doesn't apply only to morphine specificly in its potential for being beneficial to those on long-term..or permanent..opiate use.
It also has the potential to increase the pain-killing effects of opiates with lower doses.
..the great hope behind this, is that..those of us getting opiates for pain....when we take this option..will eliminate the drug stigma!
( for the record..this is NOT the same as low-dose naltrexone for autoimmune disorders)
Informative post, G...thanks
Hugs. jc
I wonder if all of us (humans) have the TLR-4 receptor, or if it's just in those folks who have addictive personalities. If so, isolating this would help determine if a person was more likely to abuse a narcotic. I'm not saying that if you did have this receptor, and others didn't, that you couldn't be allowed to take narcotics- it would just raise the awareness of the potential for abuse.
Interesting article, I'm also glad that someone is doing more research on pain management. It can only help!
Sandy
I'm not a scientist..
But..I'm pretty sure the TLR4 receptor is a human..and other mamals..thing..not an addict thing.
It plays a part in immunology, as well..that's why it's hoped to also be effective low-dose ( as opposed to micro-dose).. for certain auttoimmune disorders.)
For this of y'all who remember when the pharmacy screwed up and landed me in the emergency room..
This is what it was about.
I was supposed to get the micro-dose of naltrexone..which can be taken with opiates..
I got the low-dose amount...which cannot be taken with opiates.
I think, eventually, they'll include this ( sort of).. in all legal opiates..as it will eliminate the reason for abuse.
If they can isolate that factor..maybe they'll be able to eliminate other problems with opiates..like digestive issues, in the future, as well.
I think this will ultimately be really good for chronic pain sufferrers.