Tags: narcotic antagonist

There’s No Excuse for Overdose Deaths from Opioid-Based Medications

Link: http://AddictionScience.net

Most of the adverse effects associated with overdose from opioid-based medications could easily be prevented or rectified by simply making naloxone more widely available. It seems as if the medical establish is afraid that letting people know that their overdose can be quickly and effectively reversed will give patients a green light to abuse their opioid medication. Undoubtedly it will for some, but for most it should not. And there is no doubt that it would save thousands of lives!

Naloxone hydrochloride (Narcan) is a selective narcotic antagonist that rapidly and effectively reverses the effects of opioids including those associated with overdose (e.g., respiratory depression). As long as the circulatory system has not collapsed and the naloxone is able to reach the brain, it binds preferentially to opiate receptors blocking the effects of heroin, morphine, oxycodone, methadone, hydromorphone, fentanyl, opium, L-alpha-acetylmethadol, well, you get the idea, opioids.

Naloxone has no effects in people not receiving opioids. It simply blocks the effects of licit and illicit opioids regardless of who or why the drug was administered. (Yes, I know about endogenous opioid peptides [EOPs], wrote a paper or two involving those neuromodulators myself, but the effects of disrupting the EOPs are disappointing for we neuroscientists who were hoping back in the 1980s they would hold the key to everything from overeating to some forms of mental illness.) Naloxone is virtually unnoticeable in someone who has not been receiving opioids and has a very wide margin of safety for dosing in humans.

It’s shame on the medical establishment for withholding this critical information from the public. Should the medical establish and individual physicians be held responsible for these needless deaths? Is it THEIR decision to make, who will live or die based on the availability of this life-saving drug? Why aren’t patient-advocacy groups confronting the medical establishment, lobbying more strongly and unrelentingly for take-home Narcan?

Naloxone has been around for a long time. In fact, my first research using this compound was in 1975 and my first publication with it was in 1977 when I (along with Prof. Larry D. Reid) demonstrated that naloxone hydrochloride effectively and rapidly blocked morphine’s facilitatory action on electrical brain stimulation reward. I continued using naloxone in many of my experiments for the next two decades.

There are certain precautions that must be exercised when using naloxone, and proper medical training is strongly advised. (Self-instruction cards are included in some naloxone rescue kits so that more people can be reached with this life-saving treatment, although professional training is always advisable.) Two of the most important areas for concern involve the precipitation of intense withdrawal reactions and the short half-life of naloxone.

  • Naloxone administered to a person physically dependent on an opioid can precipitate immediate and intense withdrawal reactions. What is normally an unpleasant but relatively safe experience can quickly become a medical emergency, even fatal. The usual procedure is to give the naloxone in graded amounts, increasing the dosage if the overdose victim does not respond within a few minutes. The lowest effective dose of naloxone is desired because it minimizes the adverse effects of precipitated withdrawal.
  • Naloxone’s half-life, which determines its duration of action, is much shorter than that of most opioids. Because naloxone only blocks the opioid’s occupancy of the opiate receptor and does not eliminate it from the body, when the naloxone antagonism wears off there may be sufficient amounts of opioid remaining in the system to cause the victim to relapse back into a coma and die. For this reason, hospitalization and careful monitoring even of patients that seem normal and who feel totally revived (they actually are, until the naloxone effect wears off) is essential for the well-being of the overdose victim. One of the realistic fears that healthcare workers have is that if people are revived without the aid of trained medical personnel they will simply ignore the warning to seek proper medical attention once revived. It is the responsibility of those with the overdose victim to insure that proper medical attention is sought (dial 911 immediately).

On-site resuscitation with naloxone (Narcan) is not an excuse to avoid immediate professional medical attention. For those who are concerned about getting into ‘trouble’ for their heroin overdose, consider how much trouble you or your friend will be in if you’re dead! Furthermore, naloxone is not a CSA/DEA controlled substance nor is having an illicit drug in your bloodstream an illegal act to the best of my knowledge (but then, I’m not an attorney, so I’ll “rest my case” with the first ‘argument’ :roll: – you’d be in more trouble if you’re dead).

While trying to quickly locate information online about New York State’s naloxone rescue kit program, I found a well-written, very informative article from Pain-Topics.org. Please refer to that excellent article for much more detail and discussion regarding this important topic.

New York State is to be commended for being among about a dozen U.S. states and several European and Asian countries where naloxone rescue kits are legally available. Unfortunately, while trying to 'fly-under-the-radar' of possible adverse public opinion, New York and other states make it difficult to find information about this important program. The public needs better education about the nature of drug addiction (and while we're at it, so do America's physicians!), and politicians need the proverbial fire lit beneath their butts to get them moving and starting to change attitudes about harm reduction. It's ironic perhaps to some people that the "rescue kits" are available mostly to illicit drug users, and the aging baby-boomers being increasingly prescribed opioid-based medications do not usually have access to this program. Well, at least it seems somewhat ironic to this baby-boomer (e.g., we are the least likely to "abuse" the "kits" in any sense of the word).

I have been advocating take-home naloxone for years as part of a harm-reduction strategy for illicit opioid users, but now there's a whole new group (and generation) that could benefit from this policy as well -- patients prescribed opioid-based medication who are sometimes overdose victims. This commentary is focused on this 'new' group, although my position on naloxone as part of a comprehensive harm-reduction strategy remains ever strong. Perhaps there should be a warning to politicians regarding this issue like the warnings that appear on the opioid medication bottles -- caution: prescription opioid-users vote!

Finally, I just have to state the obvious because I know that this is going to escape the attention of too many people. It's not just about accidental overdose in the person prescribed the opioid-based medication; it's also about the grandchildren who despite ones best efforts find and play with the pills and about the little puppies who quickly grab and devour anything accidentally spilled on the floor by fumbling old hands as if it were a tasty treat. THESE are the other potential victims, perhaps even more deserving of our concern!

This information is not intended as medical advice nor is it a substitute for proper medical training. It is strictly intended to bring this topic to the forefront of discussion and to argue for the widespread availability of take-home naloxone. Write your state and federal representatives in support of this program and acquire and learn to properly use naloxone rescue kits whenever practical (cost estimated under $10).

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