Bupe Overdosing on Opiates While on Suboxone

[daddysgone]

Ok, for anyone who does not know this, suboxone blocks the high or the sought after effects of opiates, but does not block their effect on the body. Because of this, taking any opiate while on suboxone does have an increased risk of overdose because you are combineing two different drugs that have an effect on the cns and respiratory system in larger doses. Its like alcohol and benzos, or alc and hypnotics for example. If you are just useing sub alone, overdose is not as risky compared to the average opiate because of reasons stated above. I have been on sub for over a year at one point, and I was a pharm tech and studied pharms as a hobby, and I recall when they first put me on sub in rehab two years ago, them telling me to not take any opiate, benzo, or alcohol while on it because of increased chance of overdose. You can't feel it, but you can overdose without getting high so to speak when taking an opiate on suboxone.

Ok, first off everything in this quote is incorrect. Bupe doesn't selectively block effects. It either blocks the effects of other opioids or it doesn't. However it does NOT block the euphoria yet somehow manage to not block things like respiratory depression. You have to realize that when an opioid binds to a receptor, it causes its effects (euphoria, respiratory depressions etc). If the bupe blocks the other opioid from binding, then the other opioid will obviously not exert an effect. If however the bupe does not block the other opioid, then it will exert ALL of its effects.


Now I want to try to offer an explanation which may explain how bupe could actually add to the effects when taking another opioid. Note that Im not sure that this is what happens, but it is a possible explanation.

Lets just assume you have 1000 mu receptors (I know that is a ridiculously low number but lets just assume this for now to make things easy).
Now lets imagine you take a low dose of bupe (1mg). Now lets say that at this dose, bupe does not saturate your receptors and only binds to 200 receptors.

Now lets imagine you take 80mg of oxy. Lets also assume that at this dose, oxy also doesnt saturate your receptors and will bind to 600 of them.
So, if you were to take the bupe and oxy together, you would have 600 receptors which are totally agonized from the oxy, and 200 partially agonized from the partial agonist (bupe).
Now, if you were just to have taken the oxy, you would only have agonized 600 receptors, which in theory would create less of an effect then if you took both the oxy and bupe.

Now, if you had taken a large dose of bupe that occupies almost all of your receptors, that would leave very few unoccupied receptors for oxy to bind to if you were to try to take it on top of the bupe, and thus the oxy would exert almost no effect.


So, I know that the scenario I laid out is extremely simplified, but I think it may explain how it could be possible for low doses of bupe to actually cause an additive effect when taken with a full agonist.
What do you guys think?-DG

 

[sixpartseven]

Wow.. look at all the mods.

This should be added to the OD Directory, IMO..
Lots of good information in here.. and I'm sure I'm not the only one that was also curious about this!

Directory is now updated to include this thread in the Buprenorphine section

 

[TMoney11111]

Yeah i know how receptors work, no need to show off random numbers you read on some website. I was only stating that it blocks the "high" but does not block the physical effects.

 

[Cane2theLeft]

^The high and the physical effects are caused by activation of the same receptors (mu1 and mu2). You might want to review the literature

 

[morphonorconic]

Great discussion. This has been bounced around in previous threads, but never addressed in such detail.

I like DG's explanation, because in my experience, while on a low dose of Buprenorphine, I have not only been able to get high off of a full agonist, but have in fact experienced cumulative effects from the combination of the two.

There is clearly a line somewhere regarding the (safe/unsafe) ratios of partial agonist to agonist, pertaining to compounded effects, overdose, etc. Figuring out where that line is is the challenge. Plus, it is likely different for each person due to a number of factors such as tolerance.

I think it is safe to say that it is not a good idea to use large amounts of a full agonist in the interest of getting high while on a moderate to high dose of Buprenorphine, and that one should be careful when taking any amount of full agonist on top of any amount of Buprenorphine.

Considering what we know about Bupe in addition to the various unknowns, I don't think it is safe counting on it's partial agonist nature to make an overdose impossible. Especially when combined with other CNS depressants like other Opioids or Benzodiazepines.

 

[sixpartseven]

No one is saying it makes an overdose impossible. I'm saying bupe increases the threshold, causing you to need a higher dose of the agonist to overdose.

Let's go with what DG said and assume bupe occupies 400 receptors while heroin is occupying 600. We'll also say the person normall needs 1000 receptors occupied in order to OD. Bupe won't stop the heroin from being active in this, so DG is saying the combined effects could trigger an OD. If bupe were a full agonist, this would certainly cause an OD, but it's not.

This is where we have to define what type of opiate user we are talking about. Is it a noob with no tolerance? Or, is it an experienced user that would use bupe for maintenance purposes? If it's the former, the partial agonism of bupe in this case could cause an OD. If it's the latter, you have to consider how bupe affects these people.

The people that use bupe for maintenance typically (not 100% of the time) get no agonist effects from bupe, and most of the time, those who do experience very minimal agonism. At best, all it does is make them feel normal. There is no high, respiratory depression, CNS depression, pinned pupils, etc. In this case, taking 600 receptors worth of heroin and 400 receptors worth of bupe is not going to cause an OD because they are not experiencing any agonist effects from the bupe.

Remember that bupe is a partial agonist AND antagonist. It's not only an antagonist because it blocks other opiates, but because it doesn't stimulate the receptors nearly as much as a full agonist does (which is the mechanism behind precipitated withdrawal: less agonism than you experienced from the full agonist = a feeling similar to withdrawal (precipitated withdrawal))

Of course, this is only theoretical because looking at opiate activity in this way is not the right way to do it. It's a very basic way of explaining the way they act upon receptors.

Basically, there are too many variables to accurately predict what will happen to someone if they combine bupe with a full agonist. I know from personal experience that for me, combining the two only means I need to take WAY more than my normal dose of heroin to feel positive effects - sometimes twice as much - and I'm still far off from ODing. On the other hand, someone with a small tolerance could combine them and OD.

All I have been saying all this time is that in most cases - with tolerant, experienced users - having bupe present when taking a full agonist will most likely mean it takes more to OD than it would normally, but again, there are too many variables to say that EVERYONE requires more to OD, and it's impossible to say that it would be impossible to OD at all. It is definitely possible, it may just require a higher dose.

 

[morphonorconic]

I shouldn't have said "impossible," but rather that I think some people may have the impression that their being on Buprenorphine might make it more difficult to overdose by combining a full agonist on top of their Bupe, due to Bupe's antagonist effects. It is certainly possible that this could be true; it's possible that the opposite may be true; I don't know, but it's definitely an interesting concept, due to the unique pharmacology of partial agonist Opioids.

I think were all in agreement that it is extrememly dependant on dose, user/tolerance, timing, etc. Also, that to come up with any actual numbers and/or ratios would be a daunting task, and would likely be inapplicable anyways due to the broad variance of so many contributing factors. Basically, what (6/7) just said.

This in some ways ties in with the thread that discussed using Bupe/Suboxone/Subutex in the event of full agonist OD, an idea which seems both plausible yet potentially dangerous at the same time, due to the lack of knowledge, evidence, and experience out there. IMO, more research really needs to be done on Buprenorphine all together. Having this kind of wisdom is invaluable to anyone who uses these drugs.

 

[sixpartseven]

^ Well said. I agree completely.

 

[frogman84]

There are some great bits of work in here...

I am happy to sit back and just read, however as Six/Seven has done, could anyone else offer their own first hand experience with dosing on bupe.

Eg, you dosed low amount of bupe and felt full effects from normal dose of opiate-x, or you dosed high bupe and banged three times normal dose of opiate-x and didn't feel effects.

With more people answering with their own experiences, maybe that 600, 400 analogy could be looked at with more detail.

Keep it up!

 

[ss2brandon]

its a few months old but what the hell. i have taken three to four mgs of bupe for a few days. i took 40mg of hydro and was pretty buzzed. normatlly it would take 120 to 150 mg of oxy or 200 mg of hydro. today i took an oxy ir 30 and 80 mg of hydro and about 35-60 mg of morphine liquid. i am pretty toasted. i would say that it does synergize somewhat. not everyone is the same. maybe i'm lucky to blow through bupe so easy

 

[Oppyandme]

I have another question, I dont think this was posed yet in this thread. If someone would be able to answer this I would appreciate it.

Let's say a opiate tolerant individual takes enough bupe to fill 100% of their receptors. Then they decide to take a full agonist in whatever size dose. What happens to those opiates/opioids? Since they can not bind to any receptors due to bupe's high binding affinity, where do they go once they are flowing through your blood? Do they just get excreted out? I am very curious as to that one.

To add my 2cents to this thread, I have taken full agonists on top of very low doses of bupe and felt it synergized well. My tolerance is around 200-500mg of oxycodone or 40-120mg of oxymorphone a day ( to put it in perspective). Also, once trying to break past a high bupe dose, I actually got sick taking a lot of oxycodone. I did not get high in the least, but I got an extremely upset stomach. I am not sure what was going on, but it wasnt enjoyable.

 

[Znegative]

Bupe is weird, because it seems that sometimes it blocks, and sometimes it doesn't. People are going to say I'm full of shit, but I once dosed (I had been taking 8 mg for at least a week)24 mg and SNIFFED a bag of dope less than 24 hours later and got full effects. Then there are times where my last dose was 2 mg, and For some reason or another I cant break through with a shot of heroin, and I know it wasn't crap dope.

 

[Opiatemom]

What does it mean when you are on suboxone and your pupils are normal size but don't constrict in bright light?

 

[JamtasticX]

I have another question, I dont think this was posed yet in this thread. If someone would be able to answer this I would appreciate it.

Let's say a opiate tolerant individual takes enough bupe to fill 100% of their receptors. Then they decide to take a full agonist in whatever size dose. What happens to those opiates/opioids? Since they can not bind to any receptors due to bupe's high binding affinity, where do they go once they are flowing through your blood? Do they just get excreted out? I am very curious as to that one.

To add my 2cents to this thread, I have taken full agonists on top of very low doses of bupe and felt it synergized well. My tolerance is around 200-500mg of oxycodone or 40-120mg of oxymorphone a day ( to put it in perspective). Also, once trying to break past a high bupe dose, I actually got sick taking a lot of oxycodone. I did not get high in the least, but I got an extremely upset stomach. I am not sure what was going on, but it wasnt enjoyable.

This is what happens in the case of an overdose and a naltrexone injection. Lets say Naltrexone vs. Heroin.

You need 500 receptors filled to overdose, and heroin comes and fills 600 receptors for 6 hours, of which it will degrade, metabolize, and be excreted.

Naltrexone has a very short half life, for purposes say 30 minutes, and fills 600 receptors, and has a higher affinity than heroin. It will kick heroin out, and take its place, where the heroin will float around.

Once the naltrexone wears off, the heroin come backs, now it only fills 550 receptors, you will overdose again.

So I would assume based upon the scenario above, that the opiods that arn't binded to a receptor simply float around until they degrade, metabolize, are excreted, or re-bind to a receptor somewhere

 

[sixpartseven]

So I would assume based upon the scenario above, that the opiods that arn't binded to a receptor simply float around until they degrade, metabolize, are excreted, or re-bind to a receptor somewhere

Exactly.

The following paragraph isn't exactly how it would play out, but it gives you an idea of how the above quote would work. Bupe has a half life of 36 hours. So, say you dose a single dose of bupe - your first dose of bupe EVER - 34 hours ago. Lets also say that the bupe saturated all of your receptors. In 2 hours time, half of your receptors would be free. Now, lets say at the 34 hour mark, you did a shot of heroin. All your receptors are occupied, so the heroin should, in theory, not be active. In 2 hours, when half your receptors are free, the heroin that hasn't degraded/metabolized will activate.

Now, in the real world, it doesn't work like this. By the time you reach the 34 hour point, some bupe will have already left some of your receptors, allowing a little bit of heroin to bind, and as time passes, small amounts of bupe will release from the receptors, allowing smaller amounts of heroin to bind, but by the time they bind, that heroin that already binded is done doing its job. If something has a half life of 36 hours, that doesn't mean that every 36 hours, half just gets up and leaves. It's always leaving the receptors. It just means that half of it will be gone by 36 hours.

This is how bupe reduces the effects of other opiates. It prevents it from all binding at once. Instead, small amounts bind every now and then, but the bupe that is still active prevents enough from binding to get you high.

In the mean time, all that extra heroin is still present, degrading and metabolizing, and by the time all the bupe is gone, the heroin has been fully metabolized. This is why it's suggested to wait at least 36 hours before dosing another opiate. By that time, you can be sure that half of the bupe in your system will be gone. HOWEVER, depending on how often you dose bupe, 36 hours may not be long enough. If you took 32mg once, in 36 hours, half will be gone. But, if you take 32mg every 24 hours, it begins to build up. So, say you've waited 36 hours after your MOST RECENT dose of 32mg of bupe before taking heroin. There will still be residual bupe on the receptors before you even took that 32mg, so at 36 hours after your last dose, there will be more than 16mg still active. Basically, if you're taking 32mg of bupe every 24 hours, there is still 16mg active when you dose that 32mg, so really, you have 48mg the second day (32/2 + 32), 60mg the third (48/2 + 32), 66mg the fourth (60/2 + 32), 69mg the 5th (60/2 + 32), and so on and so on.

This upward trend works with any dose. Even if you dose 8mg every 24 hours, you will actually have 50% of your previous days dose still active, so you will really have 150% of your regular dose in your system.

(the numbers aren't exact, but the point is, bupe builds up in your system - that's what it's supposed to do and the whole idea behind it being used for maintenance)

So, if you are taking bupe every day and wait only 36 hours before dosing heroin and don't feel effects, this is why.

 

[JamtasticX]

Exactly.

The following paragraph isn't exactly how it would play out, but it gives you an idea of how the above quote would work. Bupe has a half life of 36 hours. So, say you dose a single dose of bupe - your first dose of bupe EVER - 34 hours ago. Lets also say that the bupe saturated all of your receptors. In 2 hours time, half of your receptors would be free. Now, lets say at the 34 hour mark, you did a shot of heroin. All your receptors are occupied, so the heroin should, in theory, not be active. In 2 hours, when half your receptors are free, the heroin that hasn't degraded/metabolized will activate.

Now, in the real world, it doesn't work like this. By the time you reach the 34 hour point, some bupe will have already left some of your receptors, allowing a little bit of heroin to bind, and as time passes, small amounts of bupe will release from the receptors, allowing smaller amounts of heroin to bind, but by the time they bind, that heroin that already binded is done doing its job. If something has a half life of 36 hours, that doesn't mean that every 36 hours, half just gets up and leaves. It's always leaving the receptors. It just means that half of it will be gone by 36 hours.

This is how bupe reduces the effects of other opiates. It prevents it from all binding at once. Instead, small amounts bind every now and then, but the bupe that is still active prevents enough from binding to get you high.

In the mean time, all that extra heroin is still present, degrading and metabolizing, and by the time all the bupe is gone, the heroin has been fully metabolized. This is why it's suggested to wait at least 36 hours before dosing another opiate. By that time, you can be sure that half of the bupe in your system will be gone. HOWEVER, depending on how often you dose bupe, 36 hours may not be long enough. If you took 32mg once, in 36 hours, half will be gone. But, if you take 32mg every 24 hours, it begins to build up. So, say you've waited 36 hours after your MOST RECENT dose of 32mg of bupe before taking heroin. There will still be residual bupe on the receptors before you even took that 32mg, so at 36 hours after your last dose, there will be more than 16mg still active. Basically, if you're taking 32mg of bupe every 24 hours, there is still 16mg active when you dose that 32mg, so really, you have 48mg the second day (32/2 + 32), 60mg the third (48/2 + 32), 66mg the fourth (60/2 + 32), 69mg the 5th (60/2 + 32), and so on and so on.

This upward trend works with any dose. Even if you dose 8mg every 24 hours, you will actually have 50% of your previous days dose still active, so you will really have 150% of your regular dose in your system.

(the numbers aren't exact, but the point is, bupe builds up in your system - that's what it's supposed to do and the whole idea behind it being used for maintenance)

So, if you are taking bupe every day and wait only 36 hours before dosing heroin and don't feel effects, this is why.

Only thing about halflife, is by following the definition, one time you'll have all of the dose out by the halflife, and another time you could have none of it. Halflife is really just a best guess measure, since by law it's impossible to guess what molecules will decide to degrade, and which won't.

 

[sixpartseven]

^ Right. That's why I said the numbers weren't exact, but it gives you an idea of how, in general, half-life works. If it worked exactly the way it should, the numbers I listed for dosing every 24 hours would be higher than what I said. After 36 hours, half is eliminated, but the other half isn't eliminated in another 36 hours - half of the remaining half, then half the remaining half, then half the remaining half, and so on and so on - so with continual, 24 hour doses, you will have a massive build of bupe in your system. Even without half life being exact, you're still going to have a large build up, which is why some people have shit luck when trying to get high even DAYS after their lost dose of bupe.

 

[JahRed24x]

Oxycodone and Hydrocodone and other opiates like that (Dilly D, Opana) never seem to work while on subs, even when on small doses.. especially oxy, i always thought maybe this is cause both Bupe and Oxy are derived from the same alkaloid thebaine. But when it comes to stuff like Diacetylmorphine, then you can easily "break-thru" the bupe (at small doses 1mg) and get pinned eyes and a lil opiate high.

 

[sixpartseven]

^ That probably has a lot to do with each opiates affinity for the receptors. Heroin has a higher affinity than things like Oxycodone or Hydrocodone, so is more likely to break through. I'm not 100% sure, but I would think that heroin, immediately after administration, would easily knock off bupe molecules that have been present for a while and are almost ready to unbind on their own. I have no idea if that's actually how it works (I'm not a biology expert by any means), but from what I do know, I would guess that that is the case, or at least close to it.

Personally, I haven't used Oxy or Hydro in years, so never had the chance to see how it affected me while using Suboxone. With heroin, it was easy to get high (I did need a larger dose, though), but the duration was much shorter. For me, bupe only blocked it in doses higher than 3 or 4mg, but with doses below that, it just shortened the duration. I would guess, that in that instance, heroin is breaking through, but the bupe eventually knocks the heroin off and rebinds. I don't know for sure though.

 

[JahRed24x]

^ Yeah i know what you mean, and thats an interesting insight into how the bupe and other opiates work in regard to their binding affinities. What you said made sense but i dunno for sure how it works either when it comes to the specifics of how it effects your brains opiate receptors