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PostPosted: Wed Feb 29, 2012 6:25 pm 
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I am now prescribed sublingual buprenorphine under the trade name Suboxone (only trade name available in Canada) for analgesic purposes only. I am not addicted to opioids; the simple fact is that buprenorphine is safe as well as effective in curing my pain. Furthermore, it has some beneficial psychotropic effects; in fact, my buprenorphine dose is indistinguishable from a dose of Dilaudid apart from the fact that it is longer-lasting (which is not a bad thing). I develop tolerance to Dilaudid slowly, and it is very easy for me to reverse the trend by taking the occasional vacation or using only when needed. Keep in mind that, up to this point, my subjective experience of the psychotropic effects of buprenorphine is entirely identical to a pure mu opiate agonist (the kappa antagonism may also play a part, but let us ignore it for the time being).

I hear a lot about tolerance to the characteristic euphoria of buprenorphine; in effect that, within the framework of addiction treatment, the euphoria will simply fade away and the patient will lose this benefit. However, I also know that buprenorphine has become the preferred opiate of Northern Europe, displacing heroin not for lack of availability but for its superior effects, and that such addicts continue to enjoy the intoxication of buprenorphine even after months of continued usage.

I guess the question I'm trying to ask is this: Compared to full agonists, how soon does tolerance develop to the positive psychotropic effects of buprenorphine? I say positive, because I do not simply mean the avoidance of withdrawal symptoms, but to sedation, euphoria, detachment, and other such characteristic symptoms of opiate use. Furthermore, will occasional (rather than daily) use delay the development of tolerance, as with other opiates?


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PostPosted: Wed Feb 29, 2012 6:56 pm 
If any dose of buprenorphine gives you anything remotely relatable to the word "euphoria," then you don't have a tolerance, plain and simple.

I don't know why it is becoming so popular in Scandinavia, but it's certainly not because it's more fun than dope.


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PostPosted: Wed Feb 29, 2012 7:50 pm 
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NoAlibi wrote:
If any dose of buprenorphine gives you anything remotely relatable to the word "euphoria," then you don't have a tolerance, plain and simple.

I don't know why it is becoming so popular in Scandinavia, but it's certainly not because it's more fun than dope.


Well, take a look at medical journals. It is also popular in France and in England for recreational uses . I noticed this huge divide between users of opiates in regard to doses. There are some people who manage to maintain their opiate dose, whether for medical or recreational purposes, at a stable level; for these, it seems, buprenorphine is an entirely viable option. Other people's tolerance just seems to go sky-high from square one, and, as I mentioned, due to its mixed agonist/antagonist properties, it does not cause any effect aside from the loss of withdrawal.

I have an acquaintance, Q, who was formerly addicted to heroin; buprenorphine (which she obtains legally) taken by intravenous injection actually seems to satisfy her even more than heroin.


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PostPosted: Wed Feb 29, 2012 7:51 pm 
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That's what I was thinking. Subs do nothing for me as far as getting high (with the exception of the first couple days I was on them). If this is what doing dope felt like, I never would've got hooked! I keep wondering what people are talking about every time I hear someone say they bought subs to get high when they couldn't find anything else. Maybe they were taking a ton of it to feel some kind of effect??


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 Post subject: I AGREE WITH TAURUS
PostPosted: Wed Feb 29, 2012 8:17 pm 
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I have also never felt high when taking my bup..only the first day of induction and i felt a wonderful high then that lasted a good while. ...but never again..but I hear people all the time on this forum say they can feel their dose?? I never feel anything except i don't crave opiates anymore. Of course that is why I am taking it...for addiction only..sometimes I think it might help my pain...but I'm not really sure and I am just talking about general pain from daily functions of life maybe a little arthritis at my age that is all.

I also can not imagine people who are addicted to opiates wanting it..also the more i take does nothing for me but I have heard others on here say more helps them??

Slipper


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PostPosted: Wed Feb 29, 2012 8:24 pm 
Slipper, same here. I was very dopesick coming off heroin when I was inducted, and that time I felt somewhat of a high, still nothing like IV heroin or sniffed heroin or even oxycodone. I think it has more to do with being that sick. Finally getting dosed is such a relief that it kinda feels like a high.

Honeywhite: I dont wanna speak for anyone else here, but I get the message that you don't consider yourself an addict and just take Sub for pain. You don't have to keep repeating it :)


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PostPosted: Wed Feb 29, 2012 10:00 pm 
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Honeywhite -

What dose are you taking? How often are you taking it? Are you taking it regularly or PRN? You obviously are opiate-naive or it wouldn't be getting you high, it's as simple as that. And if you are taking it PRN only, then you will likely continue to feel the high until you go from opiate-naive to opiate-dependent. The way sub works is it has a "ceiling effect" that is right around 4 mg, although it varies from person to person right around that mark. Once a person hits their ceiling, they get NO MORE EFFECT - high or otherwise, from taking more. And due to the ceiling effect, there is no tolerance to be built up. Now in theory, there could be a tolerance built up when using it for pain; when I say tolerance I only mean it might take more to relieve the pain. But otherwise, there isn't even any additional respiratory depression when dosing over the ceiling.

If you keep taking sub for long enough, it's my opinion that it will stop feeling like a full agonist and it will cease getting you high. Now that said, it will continue to treat your pain, you probably will just come to a point where you just won't feel anything when you dose.

I take sub for both addiction and pain and have been on it for over 3 years. I've never felt a thing when taking my dose and I've never had to raise my dose, even to get better pain relief.

I hope this helps explain things to you. Feel free to ask any more questions you may have.

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PostPosted: Wed Feb 29, 2012 10:30 pm 
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Hey Hat, you said, "You obviously are opiate-naive or it wouldn't be getting you high, it's as simple as that.", I don't believe that's an accurate statement. In the last month, we've had 2 folks come into NA who were/are hard-core opiate addicts and their new drug of choice was Suboxone. They claim the availability of Suboxone on the streets is why they decided to switch over to it. Apparently, Suboxone is plentiful around here. These folks claim to love the high Suboxone gives them and the duration of the high. Both of them were "on" Suboxone for months and months.

I have to admit, their stories kinda made me scratch my head. I kinda got high from Suboxone, but I'd take an OC or Lorcet over Suboxone anyday.

It's pretty clear that Suboxone is being diverted to the streets and it's also pretty clear that some folks quite enjoy the "high" they get from it.

It's really infuriating to know Suboxone is being used this way, but it is.

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PostPosted: Wed Feb 29, 2012 10:41 pm 
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The people getting high I believe are opiate naive and are dosing under the ceiling, where suboxone ACTS like a full agonist. Their blood level isn't steady, they are not tolerant, and they are under the ceiling. That's the way I see it.

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PostPosted: Wed Feb 29, 2012 11:45 pm 
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Neither of these guys were opiate naive, but they may have been dosing under the ceiling, I never thought of that. I'll try to remember to ask one or both of them next time I see them.

BTW, they both got the "speech" from me about buying Suboxone off the street and abusing it and how continuing to do so could jeopardize someone who truly wants recovery. I don't know if it did any good, but I wasn't gonna sit there with my mouth shut.

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PostPosted: Thu Mar 01, 2012 12:02 am 
Romeo wrote:
BTW, they both got the "speech" from me about buying Suboxone off the street and abusing it and how continuing to do so could jeopardize someone who truly wants recovery. I don't know if it did any good, but I wasn't gonna sit there with my mouth shut.


Romeo, I definitely understood why you felt the need to chastise them. People abusing Subz create unnecessary roadblocks for those of us who use them legitimately. However, I feel that we must not judge, for if we judge, when does it end?? There are so many grey areas with this..like, say you are selling your Subz (at cost, no profit) to someone who uses them legitimately (not just between scoring their DOC), because that person has no insurance and cannot afford a doctors visit every two weeks plus $8-10 a pill. This is something TJ (or anyone not in the US, sorry for pickin on ya TJ :) may not really understand like we do, him being from Aussieland where sick people get treatment even if they can't cough up the dough. At that point, well, you are technically breaking the law already by diverting your meds. The cops won't see that you are morally in the right, they'll just slap you with a felony. Okay, so lets say you think its (morally) acceptable to divert meds as long as you aren't making a profit. How far of a jump is it to giving your Sub (again, at cost) to someone who can't find opiates and is dopesick. If you give em Sub, they won't need to prostitute or rob someone or break into a car to get their next fix. That sounds like harm reduction to me, and I'm all for that.

I'm just trying to point out that the matter of diverting meds isn't black and white. I think my opinion is what it is because I had a friend like that. He really wanted recovery and he stayed on his program with only one slip up in 8 months..but then he lost his job and couldn't keep paying the clinic $99 every two weeks plus $9 a pill! So I helped him out, at very little profit (he insisted I take some $$ for the trouble). I'd do it again, too, as long as I knew my friend was serious about recovery. I'd probably help a dopesick friend in need too, but I don't hang with dopefiends anymore, and I'm sure I would quickly tire of them taking advantage of my Subutex script


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PostPosted: Thu Mar 01, 2012 1:23 am 
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Hey NoAlibi,

I definitely felt a little hypocritical while chastising them. I know all the pain pills that I bought off the street could have eventually lead to some area doctors not being so willing to prescribe pain pills to those in need. That still bothers me to this day. Here I was basically doing the same thing these two guys were doing, I was just doing it with a different med. But the fact remains, what I was doing and what they were doing was wrong, we were all buying meds with the sole intention of getting stoned off our rocking chairs, and I spoke up.

I understand the gray areas, I try not to be judgemental, but in this case, I had to say something.....even though I felt somewhat silly as I was doing it.

BTW, I think selling to your friend was an act of compassion and I support that 100%.

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PostPosted: Thu Mar 01, 2012 8:33 am 
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Hey Honeywhite! Interesting questions about onset of tolerance. It's really hard to say. Any of the evidence would be anecdotal. It would only be suitable to compare buprenorphine with methadone, as half-life likely is an important factor in development of tolerance. ie the ultra short half life opioids (like fentanyl) are known to cause very rapid onset of tolerance.

For me, I get the feeling that buprenorphine has a similar tolerance onset to methadone. I remember because for both drugs it would take me around ... 3-5 days to adjust to a dose increase?

Regarding the ceiling effect. The 4mg ceiling applies to respiratory depression only. The ceiling does not apply to analgesic effect. There is still increasing analgesia at higher doses. That's why buprenorphine is prescribed at doses over 4mg.

Quote:
Analgesic ceiling effect – A presumed ceiling effect (increasing doses have
progressively smaller incremental effect) for buprenorphine has limited its
clinical use. This assumption based on animal studies has never been shown
in clinical practice. In a recent study in cancer patients who were no longer
responsive to the highest dose Transtec achieved adequate analgesia at an increased dose of 3.2 mg/day.
Buprenorphine is expected to exert full analgesic efficacy in doses up to at least 7 mg.


http://www.grunenthal.com/cms/cda/_common/inc/display_file.jsp?fileID=85500392

The analgesia from suboxone comes from its affinity to the mu receptors, the same place its euphoria comes from. With opioid narcotics, it seems the analgesia is inseperable from the euphoria.

Occasional use would no doubt delay the onset of tolerance. I don't believe buprenorphine is any different in this regard.

If there is this "huge divide" between buprenorphine users tolerances like you're saying, it could be related to a person's addiction potential just as much as tolerability. Say 2 people are given 1mg buprenorphine for pain. They feel a nice buzz for a few days before they become tolerant and the analgesia diminishes somewhat. One of them is a bit disappointed the effect has subsided, but is still content that their pain is less than it was beforehand. The other one goes "FUCK that feeling was great! Where have you been all my life?" and takes more and more buprenorphine, so increasing their tolerance further. For them, it was more about wanting to chase a high than anything physiological.

Re people abusing buprenorphine. I knew some people that preferred to abuse buprenorphine instead of agonists, including a heroin dealer who was happy to take Subutex as payment. Their reasoning behind it was pretty similar to the reasons we use it here - it let them function better. It lasted 24 hours instead of 5. It was cheaper. It was cleaner. Maybe Scandinavian addicts care more about being functional than everyone else? :o

take care.


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PostPosted: Thu Mar 01, 2012 9:46 am 
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Quote:
The analgesia from suboxone comes from its affinity to the mu receptors, the same place its euphoria comes from. With opioid narcotics, it seems the analgesia is inseperable (SIC) from the euphoria.


I'm not quite sure what you mean by "inseparable". It almost sounds like when you get one you automatically get the other, too, but for some reason I doubt that's what you mean, because for people like me on HDB (high dose bupe), we get analgesia from taking sub, but no euphoria to go along with it. So maybe you can clarify what you mean by "inseparable" so I can get a clue or get over this brain fart I'm having.

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PostPosted: Thu Mar 01, 2012 11:50 pm 
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There has been a claim for a long time, not just here but everywhere, that buprenorphine has a ceiling on euphoric effect at 4mg. But there hasn't been one piece of research to back it up. The only research has gone into respiratory depression. Whether or not it applies to euphoria is as yet unknown. But given it doesn't apply to analgesia, indications are the magical 4mg figure doesn't apply to euphoria.

Quote:
Conclusions. While buprenorphine’s analgesic effect increased significantly, respiratory depression was similar in magnitude and timing for the two doses tested. We conclude that over the
dose range tested buprenorphine displays ceiling in respiratory effect but none in analgesic effect.


http://bja.oxfordjournals.org/content/96/5/627.full.pdf

This is what I gather from what I'm reading at the moment, but it seems there is still a LOT of speculation in medicine about the actions of drugs in the brain. Even though both the euphoria and analgesia come about from the mu-receptors being activated, the resulting mechanisms appear to be different. The euphoria comes from mu-activation enhancing the release of dopamine (also implicated in analgesia). There are a few possible mechanisms for the analgesia but the medical world is apparently still uncertain.

It appears to be a lot more complicated than this, and there are other minor brands of opioid receptor involved. But they play only a minor role compared to the mu receptors.

http://pharmacology.ucsd.edu/graduate/courseinfo/2.%20PHARM%20255%20Opiate%20Analgesics.pdf

The only reason I can see why a person can have a degree of analgesia from an opioid with diminished euphoria would be because tolerance may develop faster to the euphoria than it does to the analgesia. Ie after a person grows tolerant to the euphoria, the analgesia may be diminished, but is still present.

This does make some sense for me, as I've had some pain-killing effect from every opioid I've been on even after I'd become tolerant to the buzz, whether it be methadone or buprenorphine. It seems that taking a narcotic we're tolerant of has more painkilling effect than being on no narcotic at all.

The idea that people get no effect from buprenorphine over 4mg never made sense to me. If there was no reason to go over 4mg other than analgesia, 4mg would be the maximum dose for addiction treatment. I always felt a euphoric buzz whenever I've increased my dose of buprenorphine over 4mg. ie I am on 8mg now. I guarantee if I took 12mg tomorrow, I'd be fuzzy through the day. This has been my experience any time I increase my dose, whether I'm on 16mg or 6mg.


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PostPosted: Sat Mar 03, 2012 4:26 am 
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I found something that may be interesting:

Quote:
At low doses buprenorphine in humans produces morphine like subjective, physiological and behavioural
effects. These include analgesia, sedation, pupillary constriction and euphoria. When the dose of
buprenorphine is increased, the intensity of its actions does not seem to exceed that achieved with 30-60 mg
morphine. When given sublingually, morphine like subjective effects (euphoria) reached a ceiling at about 8-
16 mg.


So according to this study the ceiling effect for subjective euphoria is around 8-16mg - likely meaning dose response begins to curve and plateaus in the 8-16mg range.

The only reason I can think people may be prescribed over 16mg would be to facilitate once daily dosing, so trough serum levels are high enough to hold each individual, esp those with faster metabolisms.


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PostPosted: Mon Mar 05, 2012 12:00 pm 
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Seriously, I will never understand these people who say bupe makes them high. It just seems so crazy to me! It has never made me high, just made me....feel normal. I was on 100 MG of methadone for about 3 years, and other opiates for years before.

I might be wrong on this, but it seems to me if someone takes Suboxone and they are getting high off of it (especially in the extreme), they are opiate naive enough to never have needed it to get clean.

I could be convinced otherwise, but that is my initial thought.


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PostPosted: Tue Mar 06, 2012 2:46 am 
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Yeah I agree. To get a buzz off Sub a person's gotta have a tolerance somewhat below the ceiling. I don't know if they gotta be completely opioid naive though. If I reduced my dose down to 4mg and stabilised at that level, then took 12mg ... I'd feel a bit high. I know this because I did this a bit years ago on Subutex. ie saved up my subutex 4mg for 1-2 days to drop my tolerance, then I'd have 8-12mg and get an effect. It's not responsible sub use I know. But we all come from somewhere.


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PostPosted: Tue Mar 06, 2012 8:34 am 
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I take between 16-24 mg per day. Sometimes I'll be at 16 for weeks and one day I'll have severe pain and have to take that extra third tablet. NO HIGH. NEVER ANY HIGH from upping my dose. NEVER. From the time I first stabilized on sub, I've never felt a thing from taking my sub. And when I say stabilized I mean after the first month or two.

As for the ceiling, Diary once posted a beautiful explanation, but I can't find it. Basically she posted a graph of the ceiling effect, which when one looks at it, it clearly appears that the ceiling is at 4 mg. But when one looks closely at it, the line is like a think marker in that the ceiling area actually covers an area wider than just 4 mg, or a wider range. So technically, the ceiling has a wider variation among different people. For some their ceiling might be 2-3 mg and others it might be closer to 6 mg or even higher. I wish I could explain it as well as she was able to.

I think people are looking at that 4 mg ceiling as it being carved it stone when it really isn't.

And when I had a procedure last year I had to take full agonists. I still had plenty of sub in my system and i felt no euphoria from them, but I did get some pain relief. No I don't know if that fits into your info/theory, TJ, but I thought I'd mention it. It's a bit too early for me to make sense out of what you posted, but I get the gist of it, I think.

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PostPosted: Sat Mar 10, 2012 9:02 am 
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I haven't started Sub yet, so I have no personal experience yet. But, I get my DOC off the street. I have never optained a script for it. Didn't need to. Anyway, its not very popular in my area. Every addict I know and a few that I have spoke with...after I have told them about me quitting pills etc...and I tell them about my future Sub treatment...this is what I hear "Oh!Suboxone is good shit, it will fuck you up" ::SMH:: Anyway so I'm guessing when they run out of their DOC they take subs....its costly, so they aren't getting 'much' of it. They aren't building a tolerance to it. They haven't reached or gotten to the ceiling effect. As hard as it is to believe, I think even the heavest of users do get a long lasting high from it. Until they find OCs, percs whatever...EVERYONE I've spoke to just on this forum ALL say the first 2 days gave them a high. I'm just babbling/thinking out loud here (its early lol) But am I right in saying IF you stay on a low dose...will you always be high???? Because, I want to start and stay on a low dose (if it works for me at a low dose) for a short term. ::slaps forhead:::groans::: this med is so complicating LOL

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