Let’s clear up some of the confusion around the role of naloxone in buprenorphine treatment.
Have you ever wondered the purpose of that other ingredient in your Suboxone or other buprenorphine-containing medicine? If you are prescribed buprenorphine for addiction treatment in the United States and you're not pregnant, then you're probably getting Suboxone, Zubsolv, or another buprenorphine formulation that comes paired with a second ingredient—naloxone. If you're wondering what that other chemical is or what it's doing in your bupe, you're not alone. There's actually quite a lot of confusion surrounding the role of naloxone in buprenorphine among opioid addicted populations. I remember that when I was buying my bupe on the street to use as a harm reduction method, before I enrolled in treatment, I heard a lot of different, confusing, and often conflicting assumptions from other people who used illicit opioids. Today, I'm here to clear up some of the confusion around the role of naloxone in buprenorphine treatment.
What Is Naloxone?
First off, let's start by talking about what exactly naloxone is. You might have heard of it before under the brand name Narcan. Narcan, and other naloxone-only formulations, is a life-saving medication that can reverse an opioid overdose almost instantly. It comes as an auto-injector or a nasal spray. It works by knocking opiates out of the receptors to which they bind. This means that if someone has too much of an opiate in their system, naloxone will bind more strongly to those receptors, knocking them free and reversing a potentially-fatal overdose. It is an amazing chemical that some people have ventured to even call miraculous.
Why Is It In My Bupe?
So if naloxone is a drug intended to reverse opioid overdoses, and buprenorphine is a partial-opioid agonist, why is naloxone paired with buprenorphine? Buprenorphine/naloxone formulations, when used as directed, are taken sublingually, which means it's placed under the tongue and allowed to dissolve. This is because buprenorphine has a high sublingual bioavailability. Basically, it is absorbed really well under the tongue. Naloxone, however, does not. So if you're taking your bupe as prescribed, then that naloxone is essentially doing nothing. So you don’t have to worry that it will reverse the effects of your buprenorphine.
Huh? It does nothing? Why is a chemical included in medicine if it does nothing? Because if it's snorted or injected, it no longer does nothing. Remember how naloxone for overdose reversal is available for injection or nasal use? That's because while it doesn't work sublingually, it does work when injected or used nasally. If used that way, it will kick out other opioids—putting someone with an opiate dependency into precipitated withdrawal. Precipitated withdrawal is a nasty, rapid-onset storm of withdrawal symptoms that occur when someone is put through withdrawal suddenly, rather that going into withdrawal naturally by abstaining from opioids. It's really awful, and nobody in their right mind will put themselves through it for no reason. All of this is to say: naloxone is included in buprenorphine to stop users from injecting or snorting the drug.
Some people become addicted to the ritual of injection. It's called needle fixation; though it's not widely recognized in the United States, it is recognized other countries, like Australia and the UK. I experienced it. It's pretty nasty, and it can lead people to inject drugs simply for the purpose of injecting them. Buprenorphine patients—especially new ones—who also experience needle fixation might have a desire to crush and inject their medication. Which is absolutely not how it should be used. That is a continuation of addictive behaviors. Naloxone is meant to deter that.
Does Buprenorphine Block Out Other Opioids?
One of the biggest confusions I encountered among other people who were using heroin was around whether or not buprenorphine could block the effects of other opiates without naloxone present. Many people believed that buprenorphine-only formulations would stave off withdrawal, but would not cause precipitated withdrawal if taken too closely after using a short-acting opioid. That is simply not true. Buprenorphine is a powerful partial opioid agonist, which means it binds to the opiate receptors enough to block the effects of other opiates, but doesn't cause euphoria. It will also knock out a less powerful opioid (like heroin or oxycodone) if taken too soon after the last dose, resulting in—yes—precipitated withdrawal. Naloxone has nothing to do with this function, so yes, your buprenorphine-only formulation will do the same thing, when used as prescribed, as your buprenorphine/naloxone combination medicine.
But don't just take it from me. Here's what Jana Burson, an addiction treatment physician who specializes in opioid agonist therapy, has to say: "The pharmacologic properties of buprenorphine cause withdrawal if taken too soon after full opioids, with or without naloxone. Buprenorphine has a high affinity for receptors, meaning it sticks to them like glue, blocking other opioids – with the possible exception of fentanyl."
Can You Use Suboxone to Reverse An Overdose?
If naloxone is in Suboxone and other buprenorphine formulations, and naloxone is the drug that can reverse an overdose, then it makes sense that you could potentially use Suboxone to reverse an overdose, right? Well, there actually haven't been many studies done on this, but the Harm Reduction Coalition says that if it were to work, it probably wouldn't be from the small amount of naloxone. Instead it would be due to the buprenorphine, which can also knock other opiates out of the receptors.
Burson says, "I don’t know of any studies, but I’ve heard stories from the street where people give buprenorphine, either monoproduct or combo product, to reverse overdoses and it’s worked," but adds, "Of course, we don’t want to tell patients to think they can rely on this unless/until there are studies done. Much better to make naloxone available." Naloxone overdose reversal doses are also basically good to go right out of the package. If you wanted to inject someone with buprenorphine to reverse their overdose, you would have to crush or melt it down, get it into a syringe, and then get that syringe into the overdose victim's vein—which might not be super easy if this person is a habitual IV drug user. It might be better than nothing in a true emergency, but it's definitely not a solution anyone should count on.
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Elizabeth Brico is a freelance writer with an MFA in Writing & Poetics from Naropa University. Her blog, Betty's Battleground, was recently ranked by Feedspot as one of the top 75 PTSD blogs. She is also a regular contributing writer for HealthyPlace's trauma blog. Her work has appeared on Vice, Vox, Stat News, The Fix, and others. When she isn't working, she can usually be found reading, writing, or watching speculative fiction.