Sunday, October 15, 2017

Naloxone; The Physiology Behind It

The opioid epidemic affects over 64,000 (Fleishman, 2017) people within the United States and of those heroin accounts for 14,000 with an increase each year (Opioid Overdose…, 2016). The documentary Heroin(e) focuses on this deadly endemic and while watching it I was fascinated with the immediate affects Naloxone, also known as Narcan, had on the overdosees (Colegrove, 2017). After injection, some of the patients would snap out of the overdose and start talking as if nothing happened. This sparked my interest regarding what physiologically was happening within the brain to create such immediate and substantial results.

After heroin is introduced into the body and crosses the blood-brain barrier, an enzyme converts it back to morphine. Morphine then binds to specific opioid receptors thus sending a cascade effect down a signal transduction pathway and in the end producing substantial amounts of dopamine. This binding action triggers sensations of pain relief and euphoria because it depresses functionality in the CNS. This then leads to the decrease in the ability to breathe and in a lot of cases causing death.

Naloxone is an opioid antagonist, meaning it is a highly competitive inhibitor of the opiate receptor (Pijl et al., 2017). It has a higher affinity for the receptor versus heroin, thus essentially kicking the heroin off the receptor and because it does not activate the signal transduction pathway the opiates do, it immediately stops the side effects. This almost instantly reverses the biological side effects, i.e. restoring respiration function (Pijl et al.,2017). It also does not promote dependency because there is no “high” that occurs after taking it therefore,  having no addictive traits. Naloxone’s ability to combat an overdoes without the dependency is what makes it an amazing drug but, there is controversy whether it encourages injection of extreme amounts of heroin just to get a “good high” (Coker & Mackson, 2017).



References
Coker, P., Mackson, I.(Directors). (2017). Heroin(e) [Documentary]. United States. TryBoro Productions.
Fleishman, J. (2017). Documentary looks at the bravery and despair on the front lines of America’s deadly drug epidemic. LA Times. Retrieved from http://www.latimes.com/entertainment/movies/la-ca-heroin-documentary-opiods-20170920-story.html
Opioid Overdose Reversal with Naloxone (Narcan, Evzio). (2016). National Institute on Drug Abuse. Retrieved from https://www.drugabuse.gov/related-topics/opioid-overdose-reversal-naloxone-narcan-evzio
Pijl, E. M., Bourque, S., Martns, M., & Cherniwchan, A. (2017). Take-Home Naloxone Kit Distribution: A Pilot Project Involving People Who Use Drugs and Who Are Newly Released from a Correctional Facility. Canadian Journal of Criminology & Criminal Justice, 59(4), 559-571. Doi: 10.3138/cjccj.2017.0001.R2


5 comments:

  1. I also watched the documentary you reference and found this phenomenon to be fascinating! Naloxone is responsible for saving the lives of so many who have overdosed and has surprisingly few side effects, none of which are long lasting or serious. Because Naloxone knocks opioids off their receptors, it also has no side effect on people who are not overdosing, because there is nothing to "knock off" of the receptor. This drug is also non-addictive and is no less effective for individuals who have had it in the past, which is huge because so many people relapse in their drug use and overdose multiple times over the course of their life and even during their recovery process. There is a really interesting site that talks about Naloxone addresses questions, I attached the link below!

    http://naloxoneinfo.org/sites/default/files/Frequently%20Asked%20Questions-Naloxone_EN.pdf

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  2. Naloxone seems like a miracle for drug users and has the potential of saving a number of lives. I am curious about how it is distributed and how it is reaching those most in need? Those who are overdosing aren't always nearby a medical professionally and may require time to get them to an area with Naloxone. What is the timeframe in which Naloxone works?

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  3. This topic is very interesting to me. I have had addiction present within my extended family and I have grown up watching documentary shows such as "Intervention" or "Cops." These programs have shown Naloxone being given when it comes to overdosing.
    However, I think you have a good point about the controversy when it comes to getting an "amazing high" and being able to use Naloxone afterward. I read that Naloxone is injectable by professionals, however it is also available as Evzio or Narcan Nasal Spray.
    Evzio is a pre-filled auto injection devise. It injects Naloxone into the outer thigh, and similar to automated defibrillators, will provide verbal instructions on how to deliver medication.
    Narcan Nasal Spray is pretty self explanatory. It's a nasal spray that is injected into the nasal cavity while a patient lays on their back.
    These two treatments of Naloxone are readily available as a prescriptions just like prescription drugs. They can be used by family members or friends that are near the drug abuser. Sometimes an insurance company will even have a co-pay for these drugs. Some pharmacies even offer Naloxone without a patient bringing in a prescription from a physician.
    While I think it is a great idea to make Naloxone readily available to prevent a drug abuser from dying from an overdose, it is also enabling the drug abuser. If the drug abuser is able to get Naloxone and have it around while they use drugs, it will enable them to continue to use drugs and think they are invincible with a drug that has no side effects and will immediately stop an overdose from happening.
    I think Naloxone should be harder to attain because it wouldn't enable to drug abuser to reach such an "amazing high" and risk their life just because this drug is readily available to them.

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    Replies
    1. https://www.drugabuse.gov/related-topics/opioid-overdose-reversal-naloxone-narcan-evzio

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  4. Narcan is a sort of miracle drug for the heath care industry. I think it is important to point out that while there are no contra-indications to this drug, it is not ideal to use it in large quantities. The drug user that requires Narcan is generally a repeat user and will wake up very angry that you just "killed their high". These patients are very combative and unwilling to allow medical treatment. Further, the half-life of Narcan is much sorter than heroine or other respiratory repressing drugs, so if the person administering Narcan doesn't know this, it is easy for them to drop back in respiratory arrest and get high again.

    So the bottom line is that if you administer Narcan, the person NEEDS to go to the hospital, no matter who is administering it and since it is distributed to the greater public in many places (including Colorado, over the counter) a great amount of public education needs to to in place for those who have access to it. If this in not happening, people will continue to decline into overdose, in spite of Narcan administration.

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