New approach to fight opiate addiction

Opiate-based drugs such as morphine and heroin, produced from opium poppies, are nature’s painkillers. There are other drugs that reduce pain, but none as effectively or as universally. Unfortunately, those same drugs are also fiercely addictive. 

Most of the variants of opium also produce a euphoric high that becomes psychically and physically habituating. Sudden withdrawal of the drugs from an addicted person produces nausea, racking pain, chills and sweats, and other nightmarish symptoms that many people cannot endure.

No matter how ruinous the drug has been to their life, they can’t withstand the withdrawal process, and will do anything for one more fix.

A Long History
Morphine first saw widespread use in the United States in Civil War hospitals and surgeries. Many patients became addicted, but addiction to morphine was more socially acceptable than alcoholism.

Alcoholics became boisterous and combative before they passed out. Morphine addicts just quietly nodded off. Ironically, heroin, called diamorphine when used in a medical setting, was developed and marketed in 1895 as a non-addictive substitute for morphine by the Bayer company, the same folks who make aspirin.

Since the 1970s, the standard drug of choice for treating opiate-based overdose has been naloxone, commonly sold under the trade name Narcan.

Narcan is a staple in emergency rooms and paramedic rigs. On presentation of an unconscious or unresponsive person with the pinpoint pupils characteristic of opiate use, the medic will inject some Narcan into their IV.

The effect is dramatic. In under a minute, the person will go from completely out of it to wired and thrashing. If you don’t see that reaction, the lethargy is caused by something other than opiates.

The agitated state of the Narcan-dosed is with good reason. Naloxone has a strong affinity for the same receptors in the brain responsible for producing the euphoria. It’s the big guy that pushes the opiates off the receptor bar stool and takes their place, denying them a place to sit. The euphoria suddenly withdrawn, the subject moves into instant withdrawal.

A New Variant
A variant of naloxone, called (+)naloxone, may provide a way to administer the analgesic effects without the risk of addiction. (+)naloxone binds to a specific type of brain receptor, called Toll-like receptor 4 or TLR4. When opiates bind at TLR4 receptors, the brain produces dopamine, the body’s feel-good chemical.

People don’t get addicted to opiates as much as they do to the production of dopamine the opiates stimulate. (+)naloxone performs the same squatter function on TLR4 receptors that opiates do, but doesn’t bind to pain receptors, allowing the painkiller opiates access. The patient gets the pain relief without the addictive qualities.

(+)naloxone has an obvious function and benefit for opiate drugs administered medically, but it won’t do a thing for illicit opiates like heroin. Those are distributed through black market channels and are formulated to produce maximum euphoria and addition, ensuring the customer will come back for more.

(+)naloxone does have promise to help curb addiction to prescription drugs like oxycodone. Many communities are experiencing high rates of addiction to oxycodone (OxyContin) and hydrocodone (Vicodin), encouraged by “scrip mill” physicians who write prescriptions for the drugs without regard for legitimate medical use.

Oxycodone is so often a target of theft and robbery that many pharmacies no longer stock it, and announce this on notices posted at the door.

Research on (+)naloxone is under way at the University of Adelaide in Australia and the University of Colorado-Boulder in the U.S. Clinical trials may start within a year or so.

1.) Hutchinson, M.R., et al. Opioid Activation of Toll-Like Receptor 4 Contributes to Drug Reinforcement. The Journal of Neuroscience, 15 August 2012, 32(33): 11187-11200; doi: 10.1523/JNEUROSCI.0684-12.2012.
2.) Scientists can now block morphine, heroin addiction.

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