Bupe Suboxone Ceiling/Bioavailability

[biggy]

First off I’ve read this forum for years but this is my first time posting so I hope I do it correctly.

My question is regarding the ceiling dose of Suboxone and how that relates to bioavailability. For instance I’ve heard that Buprenorphine can act as a full agonist in doses 2mg and under and Bupe as a whole has a ceiling effect at 32mg.

Are those ceilings only if you are taking the drug IV and thus getting 100% bio.?

I’ve read that Suboxone sublingual is anywhere from 10-30% bioavailability. For easy math let’s say it’s 10%. Does that mean that the ceiling dose is 320mg and 20mg for the norbupe to cause full agonist effects?

What bioavailability do these ‘ceiling doses’ go off of or how does the bioavailability relate to ceiling doses?

 

[e_rep]

I don't know the math to what you're for, but I was on heroin for around a decade, with long stretches on bupe/subs and I will say this: no matter what I did or how I tried, I could not abuse it. When I first got it, it was straight bupe sold for IM or IV.

When I got scripts for subs, same thing, after being a junkie like I was, these things simply would not present any intoxication. After being clean for around 9 months and hitting kratom hard as hell for a few months, I took a sub and got the most i ever did with, and that was only a decent mood. Not a great mood, not a good mood, just not feeling like shit, basically. Why are you asking this? Oh, and yeah, it did block opiates for a good 24 to 36 hours after taking 2 mgs.

 

[smokeymcpot42088]

I do not think your equivalency is accurate. E-rep covered it well. I could always "shoot over" 2 mg of bupe if that was my current dosage. So I would say you are gunna have to go a week or so at 2mg at least (there is a bupe elimination calculator somewhere, or do the math on halflives). But at 4 mg no way, not unless it was basically straight fet that i am damn lucky the bupe blocked ENOUGH of for me to continue posting and call heroin a drug of the past. BIG FROWN. Everyone is different. Where I live *laugh now* people will take subs P.O. and still believe that bruprenorphine without naloxone is not a blocker. I.E subutex does not block opiate use or even interfere with it.

32mg ceiling hey? I think I see what you are getting at and if you need that type of dosage you are not going to get a buzz. If you need that to stay healthy, well I will be honest you are out of my depths without some research.....which I would guess you have already done somewhat desperately. (No offense, desperation comes with the territory)

30% that does suck I thought it was closer to 50 thanks for havin me look into that again greenlighter, good first post. 30% of morphine feels like alot more of a loss than 30% of bupe...if that makes any since. (if not ill just say the mg amount prescribed is usually quite high negating such a need) I guess it any different but I would feel wasteful with morphine but a fool if i did that with bupe.

as far as ceiling dose and how it relates to bioavailability you got me friend. again good first post.

 

[Juniper Bruhmomentius]

Something like 1mg is 40% or 70. 2mg iz 70% or 90. 4mg Is atleast 90% maybe More. And thats all youre realistically ever going To need.

 

[DeathIndustrial88]

I think the reason bupe feels more like a "full agonist" in lower dosages has to do with blood levels & tolerance, rather than it's full agonist metabolite having much role in any of the effects. Norbupe is incredibly less potent than bupe & will be blocked by bupe before you take enough bupe to metabolize into a worthwhile dose of norbupe, if that makes sense.

 

[kokaino]

Buprenorphine is roughly 30x more potent by weight than morphine. But if you're an experienced opioid user and looking for a high from bup, it ain't happening. For opioid virgins, it could give them a euphoric codeine- or hydrocodone-like highs at 2-4mg.

The first time I ever got a proper opioid "high", along with a wicked nod was back in 1997 as a 15 year old opioid virgin. The dose was 300mg PO (10 Codeine #3 tabs). I had played around with dosing for a couple of weeks before I took 300mg. I started with 60mg, few days later I tried 120,0mg, before deciding to do 300mg. I can honestly say that at that age and being an opioid virgin, codeine felt as amazing as heroin did years later. Heroin is a codeine prodrug, codeine has it's own intrinsic analgesic effect, though.

 

[plumbus-nine]

I think the ceiling depends on your current tolerance level to opioids. In opioid naive individuals, I read that 4mg bupe would occupy all mu receptors. But if you were using opioids and built a tolerance, there are more receptors around which need more bupe to occupy them all. But I think 32mg is a hard ceiling, above more bupe isn't more effective independent if your tolerance.

 

[Mercury'sMind]

I thought it was 24mg hard ceiling

 

[biggy]

I don't know the math to what you're for, but I was on heroin for around a decade, with long stretches on bupe/subs and I will say this: no matter what I did or how I tried, I could not abuse it. When I first got it, it was straight bupe sold for IM or IV.

When I got scripts for subs, same thing, after being a junkie like I was, these things simply would not present any intoxication. After being clean for around 9 months and hitting kratom hard as hell for a few months, I took a sub and got the most i ever did with, and that was only a decent mood. Not a great mood, not a good mood, just not feeling like shit, basically. Why are you asking this? Oh, and yeah, it did block opiates for a good 24 to 36 hours after taking 2 mgs.

I honestly stopped checking this post after a few days and forgot about it. Know it’s quite a while later but I still find this interesting so I’ll answer your question and give my experience.

I first got on subs a few years ago after a very bad habit. Over about 18-22 months I got all the way down to about .2-.5mg of a suboxone strip and that would hold me for 24 hours. It was at that point I read about norbupe and how under 2mg of suboxone would act as a full agonist. I had plenty of subs and I tried doing 1.5mg of a strip. It felt amazing. Up to that point I had never felt anything good from suboxone and in the past had tried upping my dose from 4 mg to 10mg hoping for a high but never got anything. This made me believe that the information about norbupe was true and acted as a full agonist.

When I made this post I had just got back on suboxone as I regretted ever getting off. I was curious as I was hoping to once again get my tolerance down and then have days where I could raise the dose and feel great. I didn’t want to get all the way down to .2-.5mg though so was hoping for more information to know exactly how norbupe/suboxone as a full agonist worked in low doses. I’d read many places of the 2mg ceiling on norbupe but never saw anyone say how that relates to dosing method/bioavailibity.

Sorry for the late reply but hope that answered your question and would still love to know more how this all works

 

[biggy]

I think the reason bupe feels more like a "full agonist" in lower dosages has to do with blood levels & tolerance, rather than it's full agonist metabolite having much role in any of the effects. Norbupe is incredibly less potent than bupe & will be blocked by bupe before you take enough bupe to metabolize into a worthwhile dose of norbupe, if that makes sense.

I think I understand what you’re saying and I agree. When I was doing 12mg of suboxone I couldn’t just drop right down to 2mg and get high. I had to lower my tolerance to .2-.5mg and then when I did 1-2mg I’d feel amazing. It felt like a real full agonist opiate. I’d tried upping my dose many other times when my dosage was higher and it never helped. Going from 8mg and then doing 16 or going from 4 to 8 didn’t get me any kind of good feeling. However going from .5mg to 1.5mg and I felt a real high

 

[biggy]

I think the ceiling depends on your current tolerance level to opioids. In opioid naive individuals, I read that 4mg bupe would occupy all mu receptors. But if you were using opioids and built a tolerance, there are more receptors around which need more bupe to occupy them all. But I think 32mg is a hard ceiling, above more bupe isn't more effective independent if your tolerance.

Do you know how that relates to bioavailability though? Is that 32mg at 100% bio meaning IV? If that’s the case the sublingual ceiling could be 3-5 times higher. That’s what I’d really like to understand. I’m much more interested in the ceiling for norbupe though and how that relates to bioavailibity but the answer to one question is probably the same as the other

 

[thurston]

Buprenorphine is roughly 30x more potent by weight than morphine. But if you're an experienced opioid user and looking for a high from bup, it ain't happening. For opioid virgins, it could give them a euphoric codeine- or hydrocodone-like highs at 2-4mg.

The first time I ever got a proper opioid "high", along with a wicked nod was back in 1997 as a 15 year old opioid virgin. The dose was 300mg PO (10 Codeine #3 tabs). I had played around with dosing for a couple of weeks before I took 300mg. I started with 60mg, few days later I tried 120,0mg, before deciding to do 300mg. I can honestly say that at that age and being an opioid virgin, codeine felt as amazing as heroin did years later. Heroin is a codeine prodrug, codeine has it's own intrinsic analgesic effect, though.

4mg would have an opiate virgin puking for 24 hrs.

 

[Eligiu]

I've heard the ceiling is pretty low, 16mg. I try very hard to make sure I do not go on a higher maintenance dose than equivalent 8mg a day, and that high dose (for me) was because to go on the buvidal monthly injection that is the minimum dose (64mg month).

It's not a very good drug to abuse, honestly. And it's better not to as well because it's genuinely a medicine and the abuse of it leads to it being restricted more from people who need it. I went on the injection so I wouldn't be chained to a pharmacy all the time. Yeah, I love maintenance therapy and it saved my life. But I fucking love being able to fly anywhere on a holiday without needing a permission prescription so long as I'm back for my shot.

Buprenorphine is an extremely strong blocking agent for full opiate agonise drugs. I had a laporascopic hysterectomy to finish off medically transitioning and I was full on freaking about pain relief.

Turns out, to even get past the blocking mechanism for a *laporascopic surgery* pre surgery I got spinal fentanyl, and spinal morphine. Upon waking up I was given a PIC machine (those ones you press the button every 5 minutes and it administers more of the drug) of IV fentanyl again (I was told max dose too), IV morphine, IV ketamine and oral oxycodone.

I STILL was in pain, while I was in the hospital. Curiously upon discharge, not at all. And the oxycodone was utterly useless anyway.

I have NEVER dosed over 8mg for maintenance therapy (except once when this dumb doctor put me on 24mg and I felt the exact same so I dropped to 8mg in a week then 6mg the next week then stabilised myself happily at 4mg). The benefits of this have been that when tapering off, I have often experienced nil withdrawal at all when following a schedule for dose reduction I've devised.

Tl;Dr. Don't dose suboxone too high. There is no point.