Why Is Naloxone in Suboxone? The Truth Most People (Even Doctors) Get Wrong

[00:00:00][music] >> Why do you think there is naloxone in Suboxone with the active ingredient of buprenorphine?

[00:00:16]How does that work? Which one binds to the receptor as you take that medication under your tongue?

[00:00:23]So much confusion still this many years into it. I noticed it on my last video that discussed methadone and Suboxone.

[00:00:30]Let's get started. Dr. B here, Dr. B 360. Welcome to the channel. I just recently made a video discussing a case that a person had some problems taking Suboxone and methadone and I was trying to get to the heart of an issue which I think came across for a lot of people, but I noted in the comments that there is still significant confusion amongst many people, maybe not all, including a lot of doctors to this day that I find shocking about how the naloxone in that strip of Suboxone actually works. So, I'm going to clarify that once and for all. Okay, look. Suboxone, that's the brand name.

[00:01:16]It's a strip and now I think there's also pills of Suboxone.

[00:01:20]And the strip has naloxone in it and it has buprenorphine, which is, you know, the active ingredient that is the opioid receptor agonist antagonist partial agonist, whatever you want to call it, that takes care of cravings and withdrawals. And if you have Suboxone on board or if you have buprenorphine on board and you didn't opioid, it wouldn't bind to your receptor for the most part, depending how much there is on there and how how how long ago you took it, but basically it binds more strongly to the mu opioid receptor pound for pound than most regular opioids. Okay.

[00:02:03]In that strip, there's also naloxone.

[00:02:07]Now, naloxone binds even more strongly than buprenorphine.

[00:02:13]Okay? So, if you are taking Suboxone and it has buprenorphine and naloxone in it, and I just told you naloxone gets to the receptor faster for the most part binds more strongly than buprenorphine, then what's going on when you take that medicine? Are you getting some buprenorphine bound, some naloxone bound? Think about that. It doesn't make sense. Do you know the history of how that drug made it in there and what it does? Let me break it down.

[00:02:49]Uh about uh 26, 27, 28, 29 years ago, plus in Europe, in particular in France, they started to use buprenorphine. Call it what you want, Subutex, buprenorphine, by itself. Now, during that time, there was a lot of reports of diversion of this drug that was supposed to be medication just like methadone for opiate use disorder. The idea of buprenorphine, just like methadone, it binds and it and then takes care of cravings and withdrawal, and you could put that on.

[00:03:29]But then there was all these reports of major diversion. Here's the truth about what was happening in the diversion.

[00:03:37]There was diversion, but no one was really abusing buprenorphine or Subutex, right? It was diversion of addicts trying to treat themselves for the most part. That's what was going on in Europe, but the media and whatever was going on out there, the perception came to be addicts, bad people are abusing this stuff. No, not really for the most part. They were self-treating in the same way that there's a black market and diversion of HIV drugs in Africa, right?

[00:04:13]And that was going on in the '90s. Okay, and in 2001, you know, when it was finally introduced into the US, the company that brought in buprenorphine and introduced it to the US. And again, I'm cutting a lot of this stuff out. I want to get down to the nitty-gritty, distill this down for you, kind of make you understand. Said, "Hey, look, we can introduce buprenorphine very safely and effectively into the US. Number one, we created a strip.

[00:04:47]Why is that good? Well, it's a strip and it's harder to chop, to grind down, and uh shoot up in your veins, okay?

[00:04:57]Whatever was going on. It's a strip.

[00:04:59]People are less likely to grind it down, mix it with some sort of a solution, and shoot it up in their veins. But, we also did something else. We put naloxone on in that strip. Now, that naloxone is not active when you do it sublingually. All it does, it goes through your body and you pee it out. It can't be active in the sublingual form. It's only active when someone takes the extraordinary step of taking the Suboxone, cutting it up, uh putting it into a solution, and injecting it. When it is injected intravenously, the naloxone becomes active and gets to the mu opioid receptor faster than buprenorphine making the buprenorphine one more barrier to its abuse. And I'm not sure how much abuse you can get from injecting buprenorphine. There is some and I you know the different parts of the world it kind of happens for different reasons. We're not going to get into that. But they went to these extraordinary steps of making a strip and putting the locks on in it to divert people from injecting this medication and if they did it had the naloxone in it. Otherwise the naloxone is not active sublingually. So when you hear all these discussions about oh the naloxone is no good this that Subutex is better it's a moot point, right? It doesn't turn on sublingually, right? You don't get precipitated withdrawals for any reason other than the fact that you took the buprenorphine too early not the naloxone in the film or tablet form of Suboxone, right? So in that sense you're not going to avoid precipitated withdrawals by taking Subutex, right? I hope that's clear but you know I want to add a little something to it as we've come up over the years with this issue it just continues to be a mystery a black box and a lot of discussions around it that are irrelevant and physiologically and pharmacologically simply not true. I will add something in the case that I discussed in the last video which you can go see that individual could have been having an immunological reaction to the substance of naloxone in the Suboxone causing him sort of whatever psychological impact or withdrawal impact or side effect impact that he had. And there are those cases where a person switches from Suboxone, which has naloxone and buprenorphine in it, to Subutex and they do better better. And those are real cases and there's many of those cases, right? And then there's the issue of someone just can't take buprenorphine and I'll discuss that in another video. But what I want to make clear here is that the naloxone in the Suboxone the sublingual form whether it's paper and nowadays there's tablets with naloxone in it, when you take it orally or sublingually, it is a non-active non-contributory ingredient. It was put in there as a marketing thing to say, "Hey, we've made a strip, which is harder than a pill to dissolve, and we've also put naloxone in it so that if they go to the extent of dissolving the strip it now also has naloxone in it, which once administered intravenously, it's going to competitively get to the mu receptor before your buprenorphine and it will block whatever effect the person is looking for by trying to inject buprenorphine."

[00:09:20]I really hope that gives some clarity on this topic and I'm sure there's still going to be a whole bunch of questions, whole bunch of arguments against what I'm saying, but unfortunately this is reality what I'm describing to you. I'm not denying that some people prefer Subutex over Suboxone. Last piece I'll add to this is the FDA has indicated Suboxone for induction of opioid use disorder, but you can't supposedly do Subutex for induction of opioid use disorder. There's really no clinical physiological good reason for that. It kind of goes along this kind of diversion issue and so forth. That's it.

[00:10:10]If you have any more questions, leave them in the comments, start a debate with yourself. Do like and subscribe.

[00:10:16]I'll continue to address this issue and see you guys next time. Peace.