New Painkiller May be Addiction-Proof

New Painkiller May be Addiction-Proof

Many of the best, most effective, and most often prescribed painkillers are a class of drugs called opioids. The only downside to these potent medications is the fact that they are addictive. Not everyone who uses opioids becomes addicted, but many do and it is a rising problem in the U.S. According to the National Institute on Drug Abuse, 5.1 million Americans abuse prescription pain relievers. Abusing means that these people are either taking the medications without a prescription, or they are taking them in a manner that is contrary to their doctor’s directions.

Opioid painkillers include morphine, codeine, thebaine, fentanyl, methadone, oxycodone, and others. They act on receptors in the brain and peripheral nervous system called opioid receptors. These receptors become desensitized over time, which means that the user must take more and more of the drug to get any effect. This can very quickly lead to tolerance, withdrawal, and addiction. When used as directed by a doctor, opioid painkillers are mostly safe, but there is always a risk that the patient will use them incorrectly and addiction may result. Recovering from that addiction is an uphill battle.

Because of the risk of addiction, any new advances in painkillers that can take that risk away are greatly anticipated. The latest development is a new drug that would be taken with an opioid painkiller. It boosts the effectiveness of the opioid, while simultaneously reducing the risk of addiction. The results come from animal trials only, but give great hope that in humans the new drug will have the same effects.

A study on the new findings was published recently in the Journal of Neuroscience. Researchers gave rats a drug called (+)-naloxone. This is a mirror image of a drug already in use, most often just called naloxone, but compared to the new compound is called (-)-naloxone. The plus and minus signs indicate that the two compounds are mirror images of each other. (-)-naloxone is an antidote given to those who have overdosed on an opioid. When the rats were given the mirror image compound along with an opioid, they did not display the addictive tendencies that they would if they had been given the opioid alone. The rats would show addiction by hanging around the place where they received the opioid or administering the opioid for themselves.

The mirror-image naloxone not only blocked the rats’ tendencies to show addictive behaviors, it also seemed to enhance the painkilling properties of the opioid. That the naloxone blocks the high, or pleasant feeling, from the opioid while also making it better at reducing pain is a brand new result, not seen in research before. It changes the way researchers now look at the effects of opioids on the brain.

The new findings suggest that the tolerance, withdrawal, and the addictive properties of opioids do not originate in the pleasure pathways of neurons in the brain as previously thought. Researchers are now suggesting that these negative effects are caused by immune cells in the brain, called glia. These immune cells may play a role in increasing activity in the neurons that leads to a sensation of pleasure and the new drug, (+)-naloxone, may be reducing the activity of the glia.

The new medication has yet to be tested in humans and represents the very early stages of a new breakthrough in pain medication. The potential for using this new drug as a non-addictive addition to opioids is very promising, but there are concerns as well. Some believe that taking away the high from an opioid could actually reduce its ability to counteract pain. Although the new naloxone seems to increase pain relief in the rat studies, some experts think that the high that a human gets from an opioid is essential to its painkilling properties. The high gives the user relief not just from pain, but also from anxiety. It separates the person from the pain and causes relaxation. Previous attempts to take the high out of opioids have not been effective.

Attempts throughout the history of medicine have failed to reduce the addictiveness of painkillers. Heroin was at one time supposed to replace morphine, but turned out to be even more addictive. OxyContin was also expected to be a less addictive opioid, but it was not. Nevertheless, the new research is very promising. By exploring the role that immune cells play in pain, pain relief, and addiction, researchers may be able to find the magic drug.

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