Question about Subutex for someone who really really really knows :)

[Plumber101010]

Naloxone, even in minute doses can help curb OIC although Im quite positive that wasnt R&Bs reasoning. As said, its mostly garbage but it may deter the IV route of administration to some as well.

Oh yes, very true that it inhibits abuse. But of course the point is, that could've been done anytime prior to their patent running out

 

[JessFR]

I fail to see how naloxone in buprenorphine serves any deterrence factor beyond the imagined.

Either way people would fast learn the limits and the consequences fast enough. So what's the point.

 

[Kittycat5]

If you IV it with some residual full agonist still in your system youre pretty fucked.

 

[JessFR]

Yeah but how is that gonna be different with or without the naloxone. That's what I'm asking.

 

[Plumber101010]

Yeah but how is that gonna be different with or without the naloxone. That's what I'm asking.

To make it simple. The sole purpose of Naloxone is to prevent people from shooting it or abusing it. That's it. That's all. With Subutex, you can abuse it anyway you want just like any other opioid.

With Suboxone, If you just swallow it there is no difference whatsoever. The difference is minuscule. But when you inject it or even snort it really, it will PREVENT you from getting any HIGH whatsoever.

Think of Narcan which is given to people who OD. It's the exact same product. So you can't get high if you do Narcan can you? In fact the opposite happens, it puts you into immediate precipitated withdrawal. So by putting this in the Subutex, you now have Suboxone and it prevents it from being abused.

That's it that's all there is to it, it stops people from injecting it into their body, but does nothing if you swallow it. Subutex however, can absolutely be abused.

 

[Pickledlemons]

you are wrong plumber. first of all you dont swallow suboxone, you use it sublingually. second, even if you inject it, the bupe has a higher affinity for the receptors than the narcan. I know thats what the doctors say but its not true.

 

[Steady Scootin]

If someone doesn't have an opioid habit, they can totally shoot Suboxone, whether strips or tablets for recreational purposes. I don't recommend it, but it happens all the time.

 

[GiNa LyNnxx]

I am glad you asked this question, because I have always wondered from the first time I took suboxone. Why does replacing a full agonist with a partial agonist produce a worse withdrawal than having a full agonist leave the receptor completely.
First time I took subs 24 hours as asked. Next time 18 hours next time 14 and so on until I was only waiting 2 hours. And it still worked - kind of. It at least didn't make the withdrawals any worse. I was almost convinced same as you. I even thought maybe I was a special case.

Then one time I tried taking it 10 minutes after taking fentanyl. It was the worst thing I have ever experienced in my life by far, and I have withdrawn from heroin, have died and spent 3 weeks in the hospital, been hit by van, drowned in a pool, tripped on mushrooms alone in a snowstorm with no way way home, precipitated withdrawal was worse than all of them combined and quadrupled. I was in a literal pool of sweat, no part of my body could stay still, my eyes were red and sore from crying for hours, I was hallucinating people and things, I stuttered and mumbled as I forced myself to speak one sentence to my girlfriend. I KNEW opiate withdrawal couldn't kill you but I still wondered if I would be alive by morning. You have a valid question, and you are probably right that 24 hours isnt necessary. but precipitated withdrawal is real, I promise you.

As for WHY - I still wonder myself, sorry.

i remember I just got out of a detox and was taking subutex there and not realizing I came home and took naloxone,, well.. that was the worst feeling ever.. I mean it was just absolutely horrid,, my mom had to take me to the er.. I couldn't take it

 

[Plumber101010]

you are wrong plumber. first of all you dont swallow suboxone, you use it sublingually. second, even if you inject it, the bupe has a higher affinity for the receptors than the narcan. I know thats what the doctors say but its not true.

I am NOT wrong. I suggest you research it. This information is freely available everywhere. And you're trying to split hairs with the sublingual versus swallow. Sublingual goes into your mouth, for me that's swallowing!

Question was asked as to why the two were combined and my response is 100 percent accurate.

 

[Plumber101010]

If someone doesn't have an opioid habit, they can totally shoot Suboxone, whether strips or tablets for recreational purposes. I don't recommend it, but it happens all the time.

Well of course, but let's all stand focused on what my post was. The question was asked what is the PURPOSE of Naloxone in Suboxone. My response was 100 percent accurate as to "WHY" it was added.

 

[Pickledlemons]

I am NOT wrong. I suggest you research it. This information is freely available everywhere. And you're trying to split hairs with the sublingual versus swallow. Sublingual goes into your mouth, for me that's swallowing!

Question was asked as to why the two were combined and my response is 100 percent accurate.

Yes I know the information is everywhere and its wrong. The reason why bupe blocks other opiates, is the same reason it blocks naloxone.

You cant use narcan to revive somebody from a bupe overdose, why? because bupe has higher affinity... so why if you injected both would the narcan work over the bupe? doesnt make sense does it?

 

[Plumber101010]

Yes I know the information is everywhere and its wrong. The reason why bupe blocks other opiates, is the same reason it blocks naloxone.

You cant use narcan to revive somebody from a bupe overdose, why? because bupe has higher affinity... so why if you injected both would the narcan work over the bupe? doesnt make sense does it?

I disagree. As I say, there is a wealth of information out there explaining this. And I have a tendency to want to believe all of my research, all of the many times this question has been answered, all the experts and all of the doctors, more so than I would a rogue poster.

When a thousand people say this is correct, and a couple say not, who do you believe? In fact somebody JUST posted after your original post and said they were on Subutex with no problem but took Suboxone by mistake and went into precipitated withdrawl! What does that tell you?? How do you explain that with your theory that it's not powerful enough to make a big difference on the receptor?

So I just don't really understand what you're trying to say? Narcan is the exact chemical used to reverse overdoses, so commonsense would tell you that if you add that to any product, it's going to prevent you from getting high since it's purpose is to REVERSE that high!

Still doesn't matter anyway, and that's not important. What's important is the question that was asked was what is the difference and what was the reason behind it. My answer is still 100% correct as to WHY they SAID they added it. As previously discussed we think it's just to keep their patent going but that doesn't change my answer from being correct.

And honestly I can't understand why you think Narcan, which is used by millions of professionals every day to reverse overdose, suddenly and without explanation, will not do anything when it's combined with Subutex?

There are far too many documented cases of people taking Subutex with no issues and Suboxone with major issues so the proof is in the pudding so to say

 

[Plumber101010]

so why if you injected both would the narcan work over the bupe? doesnt make sense does it?

Because the Narcan doesn't have to work over the Bupe, it only has to work over the opiate.

 

[Jekyl Anhydride]

Sublingual goes into your mouth, for me that's swallowing!

They are right about the sublingual part and the fact that people shoot Suboxone regularly to get more mileage out of what they have.

"It is a lipophilic molecule with poor oral bioavailability (approximately 10% ), but good sublingual bioavailability (approximately 50% ) potency is high and serum concentrations are linearly related to dose from 1–32 mg."

http://www.mascc.org/assets/documents/pain_Rational_Use_sublingual.pdf

Naloxone injection may not reverse the effects of certain opiates such as buprenorphine (Buprenex, Butrans) and pentazocine (Talwin). Naloxone injection is in a class of medications called opiate antagonists.

https://medlineplus.gov/druginfo/meds/a612022.html

I disagree. As I say, there is a wealth of information out there explaining this. In fact somebody JUST posted after your original post and said they were on Subutex with no problem but took Suboxone by mistake and went into precipitated withdrawl!

I think you were mistaken as she took Naloxone. I think the response is dose dependent, a heavy dose of naloxone might overpower the bupe but not the amounts in Suboxone for most people, IMO.

i remember I just got out of a detox and was taking subutex there and not realizing I came home and took naloxone,, well.. that was the worst feeling ever..

 

[Plumber101010]

You are correct I misread that and they "said" they took Naloxone direct.. of course it could be that they misspoke also, because I'm not sure you can take that direct without it being in the form of Narcan??? I hear tell of stories for doctors prescribing it as a pill, but I can't really imagine why? I don't know I've never looked into that before.

I think the point of sublingual versus the terminology I used of swallowing is being WAY overworked here and again I say it's splitting hairs.

The point is, is that when it is taken orally, the Naloxone has no affect, or a very minuscule one and as such, it doesn't do anything negative.

How you consider oral, whether it's swallow, putting it under your tongue or sucking on it, I think everyone understands the point that there's a difference between putting it in your mouth and shooting it in your veins!

But once again I just don't think that anyone is following here. Everyone is too busy trying discuss the merits of it, trying to discuss whether or not it actually works. This discussion is NOT about whether or not it works. This particular discussion of this part of the thread was that the gentleman implied that I was wrong, and I was NOT wrong and I answered the posters question perfectly!

The purpose of adding it to the pill was under the guise that it will prevent people from using it in the form of IV use. Everyone is trying to discuss whether or not that actually works or not!

The poster didn't ask whether it works! He simply said he didn't understand what was the difference between the two and purpose of adding it.

The explanation I gave as to WHY it was added and WHAT the difference was is 100 percent correct. I am perplexed why no one seems to understand this?

If anyone wants to discuss the attributes of it, whether or not its successful, fine, that's great, but that has nothing to do with answering the question that was asked.

 

[JessFR]

I am NOT wrong. I suggest you research it. This information is freely available everywhere. And you're trying to split hairs with the sublingual versus swallow. Sublingual goes into your mouth, for me that's swallowing!

Question was asked as to why the two were combined and my response is 100 percent accurate.

You probably are wrong and you've given no evidence to the contrary.

Even if you don't have an opioid habit the naloxone still shouldn't do anything.

Again, buprenorphine has a higher binding affinity than naloxone. The same chemical process that causes precipitated withdrawal should also prevent naloxone from working.

In other words if someone is somehow overdosing on buprenorphine, naloxone shouldn't work effectively to reverse it like it would just about anything else.

That's the whole point of my question. I'm well aware there is plenty of ignorance on this subject on the internet including by people who should know better, so just telling me to research it is pointless.


Buprenorphine causes precipitated withdrawal by displacing other Opioids in the system because it has a higher binding affinity. Naloxone may not be an opioid but it's close enough that it should get replaced too.

Normally naloxone works by having a higher binding affinity it replaces the Opioids in your system, but buprenorphines is even higher than naloxone. So naloxone should be at the least ineffective and at worse totally pointless.

Until I see real evidence of a real purpose naloxone a inclusion in the pill serves. I'm gonna go with the likely truth being what others said which is that it is for marketing purposes and at most psychological deterrence. Seems like the most likely answer.

Way I see it, the only other explanation is that the effect naloxone would normally have is only diminished but not entirely prevented by the buprenorphines higher binding affinity.

Seems just as likely though that it's added to satisfy regulators who already understand the concept that naloxone = less abuse and that they are very unlikely to understand the pharmacology well enough to know better.

 

[Pickledlemons]

Not only are you wrong plumber, but its pretty common knowledge around here. Hence the question in the first place.

I dont blame you for thinking the naloxone is there to prevent IV use... if you asked 100 doctors 90 of them would probably give you that answer. But reason that narcan cannot revive a bupe overdose is the same as for why it does not have an effect in the suboxone ( regardless of Roa). The bupe binding affinity is higher.

You are a smart guy... you are knowledgeable on suboxone... its not that hard to understand. Bupe forces other opiates out of receptors and stops them from re-entering... Same with naloxone. That simple.

 

[JessFR]

People don't realize what doctors do and don't know. When it comes to the pharmacology of the drugs they use they are often shockingly ignorant.

In their defense it's because most of the time such knowledge is not something they need to know compared with an enormous amount of more important information. That doesn't really excuse it for the times they do need to know, but that's why.

Even if they had been taught this stuff at one time since it's not something they need to know most of the time it gets forgotten.

It's a very common mistake to think that doctors are particularly knowledgeable about the pharmacology of the drugs they prescribe. They're knowledgeable in what they do not how they do it.

Its the pharmacists that really should know that stuff.

Another even worse mistake is assuming doctors are always intelligent. There are plenty of retarded doctors because it's a field that is a lot more about rote learning than abstract problem solving.

 

[Plumber101010]

I give up. For one reason or another, nobody seems to understand something that's sooooooo simple. Just Google it and the first 500 million replies you receive will be it was added to prevent IV use. I don't have to give evidence to the contrary when the evidence is anywhere and everywhere to be found. I don't have to give evidence that the sun does set everyday...

Everyone is STILL trying to discuss whether it works or not. Discussion is why it was added. Not whether it works. And why I cannot get that simple point across to anybody it's beyond my imagination.

And "why" it was added has NOTHING to do with whether it works, if it does, if it's fake, if it's a ploy, if it's real or not real as to the reason. But the reason behind the "why" was to prevent ABUSE.

Y'all can discuss all day and all night about whether that's works, whether it's crap, whether it's to extend the patent, that's not the point. The point is that's the reason it was added has nothing do with any of the points everyone is bringing up!

There are far too many intelligent people on this site not to grasp that simple concept. The reason it was done was to prevent abuse. This is so documented it's not even worth a discussion! This isn't Doctors saying so. It's everyone everywhere saying so.

Everyone is trying to take it step 2,3 and 4 and there is no other steps when it comes to the "REASON" that something was done. Whether or not it was reasonable? Can be discussed later but my response was 100 percent accurate, as is the same response that the individual would get by googling this information.

If I tell you the reason I put a nail in a board was to hold up the side of the house, nothing that you say will ever change the fact that that's the reason I put the nail in the board. You can discuss all you want whether that works, whether it was stupid, whether it was dumb, or anything else you want to debate about, but you cannot ever change the fact that that was the reason I chose to do it!

 

[Jekyl Anhydride]

Whether it was Keif's suggestion of evergreening, to smooth out the FDA approval process or to prevent abuse, it's unnecessary to put one reason in first place, they all apply. I think everyone agrees that allowing a generic manufacturer to submit an Abbreviated New Drug Application (ANDA) would have been more helpful allowing users access. Not everything done by drug companies is for the greater good, hence the new cancer drugs just released at a hefty price or Martin Shkreli, prisoner #87850-053.

Oxycontin was developed because MS Contin's patent had run it's course, not as a novel new way to alleviate pain. Even with hundreds of millions of dollars in fines they still made a pretty penny. In closing, it might behoove you Plumer to approach others with some humility when dealing with subjects like this one, hopefully this thread can slide down the front page now. Merry Christmas everyone..