Naloxone: The Antidote (aka The Cruel Awakening)

This drug is the OPPOSITE OF FUN.  For real.  You do NOT want naloxone (Narcan) unless you absolutely, positively need it.  Naloxone is an opioid receptor antagonist.  Think about it.  Owwwwww.

The most important thing to know about naloxone is that it is the best way to rescue someone that has either overdosed on or had a bad reaction to morphine/heroin/any opioid.  The reason it is NOT a fun drug is that it actually kicks morphine (and other opioid agonists) off the mu receptors, essentially reversing the peaceful, pain-free, near-death experience and throwing it into the complete opposite.

It’s certainly a nice thing to have around, and an absolute necessity when you are giving an opioid analgesic, but please, use it with care!

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5 thoughts on “Naloxone: The Antidote (aka The Cruel Awakening)

  1. I’m new to this site, so please forgive me if I’m putting this in the wrong place or if it’s entirely inappropriate. BUT…what have you heard about ZoHydro? Apparently it was recently approved by the FDA and has the SUD community up in arms because it’s orders of magnitude more potent than OxyContin and comes as a crushable tablet.

    1. Hi Mary!
      This is the big problem. On one hand, we have patients (like those with pancreatic cancer) who are in constant severe pain. Having a tablet that can be taken once per day and still have a more potent, long-term analgesic effect is quite attractive. Unfortunately, these patients will likely already have some opiate analgesics on board, and I am assuming you *could* use this (though I haven’t yet thoroughly researched it) along with short-term adjuncts like morphine.

      On the other hand, we have seen from the OxyContin abuse epidemic that these drugs can be seriously dangerous, especially in rural areas. The need for tighter control is imminent, though I can’t help but think that in this world, susceptible people will always find a way to obtain these drugs. I don’t blame people for being super concerned about this drug!

      I do wonder if they yet have a formulation, like that in Suboxone, that includes a parenteral antagonist or intranasal burning agent…so you could only take it orally instead of IV or insufflated. One of my patients told me that snorting Oxy with the burning agent was worse than detoxing! I believe he was exaggerating a LOT, but it still sounded pretty torturous!

      On the other other hand, this is a REALLY cool drug. Genius. Except for that little (HUMONGOUS) snag.

      Thanks for bringing that up!

  2. Author: Naloxone is an antagonist for all opioid receptors, not just the Mu receptor, or pleasure-seeking receptor associated with opiate addiction. Better to use it IV than hold the drug and hope for the best. The pt is losing brain cells as you wait for an order to inject the naloxone slow IV push. It’s quite an experience to inject a opiate addict near death with Narcan just to watch him sit up straight and mumble a few slurry words to you.

    1. Hello again, Chris, and thank you for your comments. Yes, as I said above, Naloxone is an opioid antagonist, which includes multiple receptors. The cruelty in the awakening that I am referring to is the sudden loss of the “euphoria” associated with kappa receptors. You will find, again, that this blog is not for clinical recommendations, but a fun way to give an overview of what is out there.

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