Bupe Efficiency of buprenorphine at high doses? (40mgs/day)

[Znegative]

Isnt didehydrobuprenorphine one of the most powerfull opioids on earth or something? Anyway, I know buprenorphine effects everyone differently, but I really can't see upping a daily dose of 16 mg and getting anymore of a real effect out of it. According to this half life graph, a stabilized daily dose of 16mg/day has a stacked up half life that results in a constant of 40mg in your system, which is a dose above the cieling limit if We're going with 32mg as being the maximum effects of buprenorphine.

Also, there is a reason that buprenorphine prescribed for pain is in much lower dosages. To the opiate naive, buprenorphine can be felt at something like 10micrograms. If you start a person off at dosages in the microgram quantity, you have more room to up the dose before the effects plateau. Starting someone off on even one mg of buprenorphine for pain is probably excessive, and any dose above that would really render it useless as a pain management drug in my oppinion, as tolerance developers really fast. For maintenance reasons I can understand why doctors want you to be on a high sometimes ridiculously high dosages. For one there's the theory that staying above the cieling allows the addict to dose once daily and get out of the cycle of using a pill multiple times a day to feel better. Then there's the idea that it takes high dosages of four mg or up to block other opioids ,and then I think that those doctors that really do know about buprenorphine believe high dosages are better because at lower dosages bupe acts more like a full agonist.

 

[ms4104]

Yeah in a sense...if there ever was a valid reason for a doctor to prescribe a high dose like 16mg, it would be because of it's blocking capabilities. Honestly I can take 8mg sublingually in the morning and 12 hours later get high off shooting dope. I've done it many times.. it's not as good as it would be off bupe, but I definitely get high. I do it all the time when I take a dose like 2 or 3mg bupe sublingually in the morning then at night I am getting high as fuck itchy nose nodding and all.

I know for a fact if I am on 16mg dope isn't gonna do jack SHIT...unless I am in the transitional 3-day phase where dope would take the edge off but still at 16mg you are not going to get any dopamine release. You could accomplish that with less like 10-12mg is my breaking point. Now I am not sure if that's the reason most doctors prescribe very high doses. It's likely not, because most doctors drug test. They arn't concerned with you not being able to feel high if you use lol..they are concerned with you using at all. My doctor, if you fail a drug test, you have 1 more chance, and on your second failure you rkicked out. I don't know if they taper you or not...I hope I don't ever have to find out.

But I have done that before when I am trying to stay clean. If I was having a really bad craving like I was about to cop, I would take like a lot of bupe like an extra 8mg or something so that it would be pointless to cop. Because a lot of the time I get this crazy urge, and if I can just manage to push it out of my head for even a minute it'll go away, but I usually ride with it, and once I get on that ride my head wants to stay but my body just gets in the car goes to the atm buys the drugs and you know the drill

 

[Znegative]

Yeah I mean even at 16 mg I could usually shoot a big shot of dope at night and feel 50% of the high, but it would really be a waste of money. I've read some posts on suboxforum, and the doctor there seems to think that high doses above the cieling dose prevent cravings because due to the long half life, the user feels stabil as to blood levels drop as long as they are well above the cieling dose. However it seems like that viewpoint really only takes physically cravings into concern, when its usually the psychological ones that burn you when on bupe maintenance, which is why I find being on a low dose actually helps me more because I get more of a boost out of my suboxone. Some might say that that kind of defies the whole point of maintenance, attempting to get a lift off of it at all, but I know that if I go up to eight mg a day, the bupe loses its magic, and I'll probably start shooting coke or other stimulants again since I'm not getting anything out of the suboxone and can't get high on dope and I need something to get me moving cause I can't seem to function any other way. Sad but true

 

[Captain.Heroin]

Buprenorphine isn't a full agonist and isn't that great for severe pain. I had to increase my dose approximately 10 times where I was at (4 times what I use per dosage now) just to have bare minimum pain relief. This was not the equivalent of sublingually using 40mg of buprenorphine a day but hey, I'm not going to sit here and say she shouldn't take that much. Maybe 2-3 tabs a day, or less, would work for her, but if she's in pain, she may just be getting enough pain relief to have a functional life.

and subutex is a pretty shit painkiller.

True.

3) Could she possibly get better pain relief if she cut her dose to say, 16mgs/day?

I honestly don't believe so. I mean does she take all 5 at once? If she starts at 2 and has good pain relief, she'd only redose if it was starting to wear off, not just because her instructions say to.

 

[Znegative]

Subutex just seems like a crazy med to prescribe someone without addiction for chronic pain. At least methadone doesn't have a cieling effect

 

[SUB SHOOTER 2010]

So do this math for me.. if methadone can give you precip withdrawals after 3 weeks according to I think it was you, and I did heroin for 4 days... why was I ok then?

by that logic methadone would have still been 'in my system' and given me precip withdrawals.

I think this was directed at me. If you had just transitioned straight to bupe from 80 mg of methadone a day you most likely would have gone through precipitated withdraws. But like you said and like I pointed out you did heroin for 4 days and 4 nights then were clean for 30 hours before you did any bupe. Heroin doesn't have nearly as long of a half life as bupe so it doesn't stay on your receptors nearly as long. And you gave your receptors time(almost 6 days if I read correctly) to get enough methadone off of it to be able to dose on bupe. That's why you were ok.

Whenever I said that I saw someone go through precipitated withdraws in rehab after dosing bupe and they had been clean from methadone for 2 weeks not 3. Their situation was different than yours. They were on 260 mg a day of methadone! A little higher dose than you. I'm not sure how long you had been on methadone but he had been on it for years. Just to give you an idea his teeth were rotting out in the back from taking liquid methadone for so long. His dentist had told him the methadone was the cause of it too.

I promise you if you take your 80 mg of methadone and the next day take some bupe you will believe that a prec withdraw is possible switching from the two drugs.

 

[Crankinit]

and subutex is a pretty shit painkiller.

Personally I find it works very well. Not quite as well as morphine/oxycodone/etc, but a hell of a lot better than any non-opioid treatment. Having had issues with back pain for years, which lead to fairly extensive oxy/morphine use, suboxone has improved my quality of life immeasurably.

I also find that it does increase in potency well above 8 - 12mg, though on a bit of a curve, the difference between 16 - 24 is less than the difference between 8 - 16, but still there.

When I was first on suboxone I worked my way up to 16mg, but after a week or two the pain relief started getting weaker, so I upped it to 24 and I'm now getting the same level of pain relief, if not more, than I was when I first hit 16mg.

That said, 32mg is the number usually quoted as the ceiling dose, but honestly, if she finds 40mg works for her, then I don't see a problem with it. Everyone has a difference metabolism and a difference brain, if it works for her, then good.

 

[ms4104]

I am not sure whre the post went but regarding subutex as a painkiller..to the person saying it works and they take 16mg doses. That magic will be fleeting very quickley if you are taking such large doses. Buprenorphine can retain it's painkilling and almost full-agonist like abilities but at small sub-milligram doses IMO. At like 4mg plus the magic is going to fade in 1-2 weeks and be totally gone in a month or so. I mean if you are having to up th dose to 24 or even 32, 40mg of bupe just to use it as a painkiller, I feel like your making a big mistake. You are putting MONSTEROUS doses's of an opiate into your body.. I can't even begin to stomach what iw oudl be like to detox from 32mg bupe!!!! I know coming from 80mg methadone 12mg bupe more than held me.. I can't imagine what 40mg bupe converts to but its astronomical. You could get the same releif with a fraction of the power using a full agonist.

I've been on bupe quite a while and I will say that for me, weither its 1 or 100mg of bupe it has zero painkilling abilities for me. It does it's job as a partial agonist and that is it. If there was anythign remotely magical about it I wouldn't have extra drugs lol. Like I never start piling up heroin adn say damn yo I have a months worth of heroin here dumdedumdedoo. Bupe just doesn't do it for me lol.

 

[ms4104]

I think this was directed at me. If you had just transitioned straight to bupe from 80 mg of methadone a day you most likely would have gone through precipitated withdraws. But like you said and like I pointed out you did heroin for 4 days and 4 nights then were clean for 30 hours before you did any bupe. Heroin doesn't have nearly as long of a half life as bupe so it doesn't stay on your receptors nearly as long. And you gave your receptors time(almost 6 days if I read correctly) to get enough methadone off of it to be able to dose on bupe. That's why you were ok.

Whenever I said that I saw someone go through precipitated withdraws in rehab after dosing bupe and they had been clean from methadone for 2 weeks not 3. Their situation was different than yours. They were on 260 mg a day of methadone! A little higher dose than you. I'm not sure how long you had been on methadone but he had been on it for years. Just to give you an idea his teeth were rotting out in the back from taking liquid methadone for so long. His dentist had told him the methadone was the cause of it too.

I promise you if you take your 80 mg of methadone and the next day take some bupe you will believe that a prec withdraw is possible switching from the two drugs.

I don't doubt that if I took methadone, then bupe the day after I would get precipitated wtihdrawals..duh. I never said that wouldn't happen..i mean it's a full agonist adn your switching to a partial agonist. I just didn't want people reading your comment about not being able to switch to bupe from meth...that you could get precipitated withdrawals even if you wait 3 weeks from your last dose of methadone. It's just not realistic. Maybe for that one case or something...but I still don't believe it. Also, the majority of people on here are not on 250mg+ methadone daily. So I don't want the misinformation to spread. It is possible to switch from methadone to bupe. Plenty of people on here have done it without tapering to 30mg if you are on a reasonable dose in the low 100s or less daily. You need to give it atleast 4-5 days and if you have a really long history like over a few years maybe give it a little more. The transition won't be a walk in the park..

But surely you don't have to worry about going into PW's from left over methadone in your body after detoxing/not dosing methadone for 21 days. Whether or not you are using dope during that time won't effect the rate of methadone eliminating from your body, so that information is not important to us.

And I am sorry but what does the dentist know about your friends transition from meth to bupe? Thats worse than taking advice from your sub doctor regarding how big od a dose you should take daily lol.

I ain't trying to fight but I would feel bad if someone methadone was like DAMN any attempt I will make at getting on sub is futile..how am i supposed to go without done for over 3 weeks!!!???!!

 

[Znegative]

I am not sure whre the post went but regarding subutex as a painkiller..to the person saying it works and they take 16mg doses. That magic will be fleeting very quickley if you are taking such large doses. Buprenorphine can retain it's painkilling and almost full-agonist like abilities but at small sub-milligram doses IMO. At like 4mg plus the magic is going to fade in 1-2 weeks and be totally gone in a month or so. I mean if you are having to up th dose to 24 or even 32, 40mg of bupe just to use it as a painkiller, I feel like your making a big mistake. You are putting MONSTEROUS doses's of an opiate into your body.. I can't even begin to stomach what iw oudl be like to detox from 32mg bupe!!!! I know coming from 80mg methadone 12mg bupe more than held me.. I can't imagine what 40mg bupe converts to but its astronomical. You could get the same releif with a fraction of the power using a full agonist.

I've been on bupe quite a while and I will say that for me, weither its 1 or 100mg of bupe it has zero painkilling abilities for me. It does it's job as a partial agonist and that is it. If there was anythign remotely magical about it I wouldn't have extra drugs lol. Like I never start piling up heroin adn say damn yo I have a months worth of heroin here dumdedumdedoo. Bupe just doesn't do it for me lol.

Bupe will work as a painkiller. I was in the hospital a few months ago and i was in tremendous pain. I had to stop taking my buprenorphine so they could give me dilauidid, when I got back on the buprenorphine,I was still in a lot of pain,and sometimes I couldn't move half of my body, but the suboxone worked decently enough. I was taking two mg two times a day, but it was being metabolized rather quickly because I was on iv rifampin. It definitely wasn't ideal, but the doctors would only give me dilaudid prn every four hours and once the infection that caused the pain started to clear they wanted me to stop taking the dilaudid, but at the same time didn't want me to go back on buprenorphine until I got this procedure done where they were going to use fentanyl to anesthetize me. So I had to go about thirty six hours without bupe or dilaudid, for a procedure where I ended up being conscience the whole fucking time because they didn't listen to me when I said I would probably need more fentanyl than the average joe... Anyway, I got back on the bupe and it provided as a decent pain med once the pain lowered a bit, but yeah it's no dilaudid.

 

[SUB SHOOTER 2010]

I don't doubt that if I took methadone, then bupe the day after I would get precipitated wtihdrawals..duh. I never said that wouldn't happen..i mean it's a full agonist adn your switching to a partial agonist. I just didn't want people reading your comment about not being able to switch to bupe from meth...that you could get precipitated withdrawals even if you wait 3 weeks from your last dose of methadone. It's just not realistic. Maybe for that one case or something...but I still don't believe it. Also, the majority of people on here are not on 250mg+ methadone daily. So I don't want the misinformation to spread. It is possible to switch from methadone to bupe. Plenty of people on here have done it without tapering to 30mg if you are on a reasonable dose in the low 100s or less daily. You need to give it atleast 4-5 days and if you have a really long history like over a few years maybe give it a little more. The transition won't be a walk in the park..

But surely you don't have to worry about going into PW's from left over methadone in your body after detoxing/not dosing methadone for 21 days. Whether or not you are using dope during that time won't effect the rate of methadone eliminating from your body, so that information is not important to us.

And I am sorry but what does the dentist know about your friends transition from meth to bupe? Thats worse than taking advice from your sub doctor regarding how big od a dose you should take daily lol.

I ain't trying to fight but I would feel bad if someone methadone was like DAMN any attempt I will make at getting on sub is futile..how am i supposed to go without done for over 3 weeks!!!???!!

I'm not trying to fight either but you are sorely misreading my posts.

The reason I even commented in the first place was because you were downplaying how easy the transition from methadone to bupe was. You words exactly were that you didn't go through any detoxing or any taper during your transition and no withdraws. And you thought it was a "bunk" information that you had to do so. I simply brought up the fact that you didn't take any methadone for more than 5 days before you switched to bupe that's why it was easy for you. Not to mention you said you were doing heroin right after you stopped taking methadone for 4 days and 4 nights. That should give you a pretty good idea of why you didn't go through any methadone withdraws. The people that the transition is hard for are the ones that switch quickly from one to the other. I imagine it would be pretty easy if you go on a heroin binge for a few days while the methadone is leaving your receptors.

And for the second time I NEVER said he went into prec withdraw after 3 weeks. I said TWO weeks and the only reason I said this had happened was because his dose was soooo high. If you read any of my posts I NEVER said you couldn't transition from methadone to bupe ever. And I said just to give you an idea of how much methadone this guy was taking it was rotting his teeth out and his dentist told him it was from the methadone. I NEVER said anything about the dentist giving advice on the methadone to bupe transition or dosing. The dentist said something about the guy's teeth. Which that is what a dentist specializes in so I think hes entitled to give his opinion there.

I NEVER said anything about the transition being impossible at all. You just have to take the proper steps and respect the power of bupe. I didn't even mention the story about someone going through prec withdraws after 2 WEEKS transitioning from meth to bupe in this thread. In that thread I was just giving an example of a difficult case of transitioning for someone that I had witnessed myself.

 

[adder]

How did you get your hands on didehydrobuprenorphine?

Laboratory. When you actually know how Bentley compounds are synthesized, you know a didehydro compound is the one you get at first, then you have to hydrogenate it.

Didehydrobuprenorphine is simply buprenorphine with a double bond instead of a single bond between 18C and 19C. It's ~2 times as potent as buprenorphine on a weight basis, it's not any powerful opioid like etorphine.

Bupe is a novel compound. Less is definitely more.

Maybe it is when you're stable on a higher dose and then you taper it down. It definitely works wonders for withdrawal but I've only experienced it at very high doses and I could manage to taper it down. I really started getting chills and sweats at 8mg diminishing the dose gradually when I stabilized on 16mg. I can't imagine starting at an ultra low dose after ceasing any full agonist and staying off it for a long enough period for withdrawal to kick in.

 

[Znegative]

Does that mean that didehydrobuprenorphine is still a partial agonist, and would be the same as regular buprenorphine, you would just take half as much?

I can see starting at a low dose of bupe for something like a minor Vicodin habit, but yeah I agree with you adder, when transitioning from a full agonist I've always stayed at doses of eight for the first day or two, though I think four mg would probably be enough to get by.

 

[adder]

Yes, 18,19-didehydrobuprenorphine has a similar pharmacodynamics profile to buprenorphine (although it has a higher MOR affinity and lower KOR and DOR affinity compared to bupe, and it's totally different in that it doesn't induce CPP). The bridge created in the annelation reaction in this one is "endoetheno" as opposed to buprenorphine's being "endoethano", cyprenorphine has a similar structure but the side chain at C7 is different.

Anyway, I don't see it coming as an alternative for buprenorphine as you see more differences when you look in-depth.

 

[Missykins]

Good Lord, 40 mg of buprenorphine? That's above and beyond the ceiling effect and her opiate receptors are probably so down-regulated that she has very few left. God bless her if she ever needed a root canal for a tooth root abscess or was hospitalized for a painful procedure. Bupe is only a partial agonist: think of the mu opiate receptor as a door, bupe only opens the door halfway.