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 Post subject: The Ceiling
PostPosted: Mon Mar 19, 2012 11:55 am 
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From http://suboxonetalkzone.com/ceilings/

By Dr. Jeffrey Junig:

A question was asked about the last post that warrants top billing:

“Buprenorphine acts similar to opioid agonists in lower doses, with the same addictive potential as oxycodone or heroin. In higher doses—doses above 8 mg or 8000 micrograms per day—the ‘ceiling effect’ eliminates interest and cravings for the drug.”
Buprenorphine Ceiling Effect

Ceiling Effect

I’m not sure I followed this. Can you explain more? What would you think about someone who is taking 1-2mg of Suboxone twice a day without a prescription, and says they want to stay on that dose once they find a prescriber? Are they better off on 8mg or more per day, or would it be ok for a prescriber to keep them at the lower dose? Is the answer the same if they hope to taper off the medication completely within a year (they don’t feel able to do this on their own right now, but hope to be able to when some life circumstances change). Thanks!

This gets a bit complicated, but I’ll do my best. A couple background issues; buprenorphine has a ‘ceiling’ to its effect, meaning that beyond a certain dose, increases in dose do not cause greater opioid effect. That is the mechanism for how buprenorphine blocks cravings.

If the blood level of buprenorphine is ABOVE that ceiling, the opioid receptors are maximally, 100% stimulated. If the person takes more buprenorphine, and the blood level increases, the opioid receptors don’t feel the increase, as they cannot be stimulated more than 100%. But more importantly: when the person takes less, and the blood level of buprenorphine goes DOWN, the receptors also sense nothing– as long as the level stays above the ‘ceiling’ level.

Read the above paragraph, and think on it until you grasp it– as it explains buprenorphine and Suboxone. If you understand that paragraph, you will know more about Suboxone than most doctors!

Below that ceiling level, the opioid effect from buprenorphine varies directly with dose—just as with oxycodone, hydrocodone, heroin, etc. Medications that have effects that increase with dose are called ‘agonists’. Buprenorphine is a ‘partial agonist;’ it acts like an agonist up to point, the ceiling effect, beyond which increases in blood level have no greater effect.

The level of this ‘ceiling’ varies from one person to the next, depending on efficiency of absorption (on average, only a third of a dose is absorbed from under the tongue), body size, liver function, differences in regional blood flow, and the presence of other medications that affect buprenorphine metabolism. In order for buprenorphine to have the unique, craving-blocking effects, the blood level of buprenorphine must stay above the ceiling level, for the reasons described above.

Lower levels (blood levels of buprenorphine below the ceiling level) still have SOME effects on cravings. Buprenorphine has a long half-life, an that alone reduces the desire to take more—especially if the medication is taken more than once per day– since the blood level drops very little between doses. For agonists or for buprenorphine below the ceiling level, drop in blood level equals drop in opioid effect, equals sense of things wearing off, equals cravings.

But the classic method for treating with Suboxone, as described in the certification course, is for it to be given at a high enough dose to stay above the ceiling level… and dosed only ONCE per day. If the blood level stays above the ceiling level, once-per-day dosing covers cravings completely. Yes, people still want to take more, especially initially, but that desire is not driven by chemical effects; the desire is instead based on psychological factors, like habit, or from being accustomed to feeling better after a dose, and getting a placebo ‘lift’ from taking a second dose.

A person can eliminate that second dose fairly easily, providing that the morning dose is high enough, i.e. usually 8-16 mg. To eliminate the second dose, the person should distract him/herself as soon as the thought about taking the second dose comes to mind. Immediately, do anything else—the dishes, call a friend, wrestle with the dogs… and the thought will pass. If the person does the distraction method for a few days, the need to take the second dose will go away—a psychological process called ‘extinguishment.’

Dosing every other day, and even every third day, has been studied; people cannot tell the difference, if the dose is raised enough to keep the blood level above the ‘ceiling’ (providing the person is given a placebo that tastes the same).

As for as the writer’s friend… I’m not a fan of any illicit use, but I am aware of the shortage of physicians. When the person has a physician, in my opinion the person should be prescribed a dose that allows for once per day dosing. Realize that buprenorphine wears off VERY slowly; it takes over three days for half of a dose to leave the body! So that ‘need’ to take more is almost always entirely learned or ‘conditioned.’ The medication does not wear off in that short period of time.

Even if the person has withdrawal symptoms, the sensations are almost surely imagined. How to tell? Use the distraction method, and note that a couple hours later, when the person remembers that the dose was skipped, note that the withdrawal went away. That doesn’t happen with ‘real’ withdrawal!

The sense of withdrawal that drives the second dose is simply a memory; a conditioned response that the body has that triggers the person to take more opioid. We become conditioned by drug use, just like the salivating dogs from science books! In the case of opioids, whenever we feel down, we think that an opioid will lift us up, as it has hundreds of times before. And even if what is taken is not a real opioid, the mind ‘feels’ a boost, just from expecting what has always happened in the past.

As for tapering, I look at many factors in order to recommend, or not recommend, stopping buprenorphine—things like age, presence/absence of using friends or contacts, physical health, mood, support network, personal motivation to stop buprenorphine, ability or lack thereof to dose once per day, consistently, number of relapses and personal ‘recovery’ plan, etc.

Realize that EVERYONE looks forward to a day when life circumstances will change for the better—but most of the time, life becomes more, not less challenging. Yes, it is nice to have a reliable job… but it is much more stressful being the sole breadwinner for a family with children, than working to pay for one’s self! Marriages settle down in some ways over time, but they also lose the intense infatuation that can gloss over personal differences.

As I have often written, it is VERY hard to stop opioids. It is a little easier to stop buprenorphine; I am convinced of that fact because I have seen opioid addicts taper off buprenorphine, but I know of no opioid addict who tapered off an agonist. But SOME people cannot taper of ANY opioids—including buprenorphine. I do not consider those people ‘addicted’ to buprenorphine, because they lack the constant obsession for opioids that is so destructive to the mind of an active addict. But they ARE physically dependent on buprenorphine— a fair trade, in my opinion, for a life of chaos, broken relationships, legal problems, and death.

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PostPosted: Mon Mar 19, 2012 4:50 pm 
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Very informative! Thank you for reposting!

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PostPosted: Mon Mar 19, 2012 9:27 pm 
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Quote;"on average, only a third of a dose is absorbed from under the tongue), body size, liver function, differences in regional blood flow, and the presence of other medications that affect buprenorphine metabolism. In order for buprenorphine to have the unique, craving-blocking effects, the blood level of buprenorphine must stay above the ceiling level, for the reasons described above. "

So for those "jumping" at ~ 0.1mg are actually quitting at ~0.03mg.
I can't see how tapering to that dose, and then having wd's is possilbe, let alone having paws.
But I'm gonna find out for myself anyway in the not to distant future.
All my other detoxs begun with out a taper, and paws always got the better of me, so this is new - an opiate that you can actually taper to almost zero, what an amazing Recovery Tool.
I'm at 1.4 mg over the last 3 days, no drama and shall stick to this dose for a while yet, no rushing this time!


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PostPosted: Tue Mar 20, 2012 3:44 pm 
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I'm not sure what the ceiling dose is exactly, and I know it's not an exact dosage since it depends on the person and a lot of other factors, but lets just say, for the sake of this question, that the ceiling is about 4mg. So if I take 6mg/day to stay above the ceiling, dose that really work? Because if only about a third of it absorbs, that means that I am only on 2mg/day.

I am really on 3mg/day right now because I had too many side effects above that dosage, but I figured since the sub stacks, what is actually in my body is more than 3mg.

I'm also wondering because this would also apply if I was trying to find out how my dose in mg's is comparable to other drugs, like when using the opioid dosage comparison calculator for low dosages (I know they aren't linear once you get up to a certain dosage on bup). Do I use the actual mg's I am putting in my mouth for the calculator, or the # of mg's that actually get absorbed?


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PostPosted: Tue Mar 20, 2012 11:43 pm 
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Taurus - whatever measurement they use to calculate the ceiling is for sublingual dosing, so bioavailability is taken into account. ie ceiling of IV buprenorphine would be a lot lower. Once we take into account variability of absorbtion, things get incredibly complicated.

Also, it seems there's been a revision of opinions, namely of Dr. Junig and that of Suboxforum. The isn't as static and absolute as it was once thought. For a while it's been said that the ceiling for everyone is 4mg, and there is no effect of taking more than 4mg. Now Dr. J is of the opinion the ceiling is 8-12mg, and wherever a person's ceiling lies in that is dependent on factors unique to that person.

Given how much is yet to be discovered in the field of neuroscience, it's fair to assume there will be more revision of ideas about buprenorphine in the future as more research is done.

Quote:
Below that ceiling level, the opioid effect from buprenorphine varies directly with dose—just as with oxycodone, hydrocodone, heroin, etc. Medications that have effects that increase with dose are called ‘agonists’. Buprenorphine is a ‘partial agonist;’ it acts like an agonist up to point, the ceiling effect, beyond which increases in blood level have no greater effect.


When Dr. J says that doses below the ceiling act more like a full agonist, is this what he is referring to?


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PostPosted: Wed Mar 21, 2012 6:30 am 
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tearj3rker wrote:
Quote:
Below that ceiling level, the opioid effect from buprenorphine varies directly with dose—just as with oxycodone, hydrocodone, heroin, etc. Medications that have effects that increase with dose are called ‘agonists’. Buprenorphine is a ‘partial agonist;’ it acts like an agonist up to point, the ceiling effect, beyond which increases in blood level have no greater effect.


When Dr. J says that doses below the ceiling act more like a full agonist, is this what he is referring to?


Yes, that's always been my understanding. And it's what we've/I've always said. This is why at low doses many people can "feel" their dose - because of how he describes it above.

I don't think it's been a revision, per se, but we've always said ~ 4 mg is the ceiling (and often we add "but it's not written in stone"), we're just lately getting more and more specific the more we as a group understand suboxone more. I think that's a GOOD thing, not a bad thing. Our knowledge is growing.

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PostPosted: Wed Mar 21, 2012 8:29 am 
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I'm just trying to figure out where in Dr. J's post it says that people can feel their dose more at doses under 4mg?

I thought what he meant was people get more reward from boosting their dose when it's under the ceiling, which is pretty obvious. ie a person on 2mg would get much more effect from doubling their dose than a person on 12mg.

The idea that people get more opioid effect from 2mg than 12mg just doesn't make sense.


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PostPosted: Wed Mar 21, 2012 8:47 am 
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He didn't say it in this post, I did. What he has said in many places is that the opioid effects can (not will) be felt along with dose increases when a person is below the ceiling. That goes for ALL the opiate effects, from respiratory depression to "feeling" the effects.

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PostPosted: Wed Mar 21, 2012 9:26 am 
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I have bounced around a lot since my induction, trying to find the right dose for me. I think I've finally found it after 3.5 weeks on sub. I started at 8mg and got migraines and nausea, so I lowered it to 6mm for about 5 days. I still got a mild headache every day and mild nausea. Around the 4th or 5th day on 6mg, I started feeling irritable and tweekerish. So I lowered to anywhere between 2-4mg. I found at 2mg I would get tired after a couple days, and I started having cravings. At 4mg I couldn't sleep well and would itch like crazy and get mild headaches. So I have been at 3mg for about 5 days and I think that is the right dose for me. I haven't felt high from any of these doses, even though they are below the ceiling. But I do feel something for a couple hours after taking it. It's weird...I either feel really energized and clean the house, run errands, etc., or if I take it and then lay down, I am really relaxed like I took a muscle relaxer and could lay there for hours. This is not normal for me because I have always had neck pain that keeps me from laying still for more than a couple minutes at a time, making it very difficult to get to sleep. Anyway, my point is...I do feel something, though it is not a high. I don't know if you guys feel this too, or if you feel nothing at all? And I don't know if it's because I am still in the beginning of treatment, and maybe it will go away after I've been on sub for a while. Maybe it won't since I am below the ceiling? Or am I? If I'm taking 3mg/day and subs have a stacking effect, I might really be above the ceiling after a couple weeks.


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PostPosted: Wed Mar 21, 2012 9:35 am 
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Taurus, I think you're getting too deep and/or literal into the numbers. Does it matter? Or maybe what I should say is what is more important, you feeling fine where you're at or determining exactly what number you're at? There are so many variables that you (or anyone) will probably never know exactly the amount of sub in your system. For all you know, the dosage you are at is at your ceiling, although it does sound like you ARE feeling your dose. Which may pass.

Dosing is like walking a fine line. We have to find the lowest possible dose that will accomplish the highest benefits - extinguish cravings and withdrawals with the least amount of side effects. Does the number of the dosage really matter? We as individuals are the ones who determine what dose we feel best at anyway and it's not by the number, it's based on HOW WE FEEL. If I were you, Taurus, I wouldn't be too concerned about the mg of your dose, only that you feel you're at the right dose for you.

That's just my opinion though. :)

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PostPosted: Wed Mar 21, 2012 5:06 pm 
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hatmaker510 wrote:
This is why at low doses many people can "feel" their dose - because of how he describes it above.


Are we saying that a person on 2mg can "feel" their dose more than a person on 12mg?

I still don't understand how?


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PostPosted: Wed Mar 21, 2012 5:39 pm 
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Yes, sometimes people can feel it when they dose at levels under the ceiling. For example, when people are tapering and get to low levels, they sometimes begin to feel it when they dose whereas they didn't used to feel it. Many people on the forum have attested to this with their tapers. (We used to talk about this some time ago more frequently than we have of late.) Even just recently a member who is right around and possibly under the ceiling is experiencing something that MIGHT be called feeling their dose.

I always say "can" feel their dose because it's so very subjective by nature. The opiate effects are there and will go up and down like a full agonist (just like respiratory depression is an opiate effect) right along with the dosing until they reach that person's ceiling.

I hope I'm explaining it to you satisfaction. Forgive me if I'm doing a lousy job.

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PostPosted: Wed Mar 21, 2012 10:56 pm 
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Ahkay it kinda makes sense now. Whenever I heard people say "bupe acts like an agonist at low doses", I always thought they meant that bupe acted like a full agonist on individual mu receptors. Now I'm thinking it has more to do with changing bupe plasma levels throughout the day.

I guess because their dose is so far below the ceiling, they would notice their buprenorphine blood levels rising and falling a lot more. Whereas those of us who dose over the ceiling such that our blood levels never fall below it, we don't notice the wearing off effects at all. And noticing a dose kick-in and wear-off is reminiscent of addiction to agonists with shorter half lives.

Especially given that the people that dose so low they may be getting mild withdrawals in the morning - they would easily be able to feel the effects of their daily dose as it would provide relief from the withdrawals. Buprenorphine could then be associated relief, which could lend to an addictive mindset.

But that would be more because of the lower tolerance people have at the end of their taper than buprenorphine molecules magically transforming into agonists.

If you or I took 2mg tomorrow, we definitely would not feel it more than our current doses.


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PostPosted: Thu Mar 22, 2012 12:09 am 
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By George, I think he's got it!

Yes, that's pretty much what I've been trying to get across.

BTW, check out an intro or induction thread called, "Hello all, my first post and a few questions". The subject of a short term detox using sub came up and the question of "am I dependent on sub or X opiate?" came up. Check it out. I'm re-wording/forming/thinking/organizing my thoughts and knowledge with regard to our previous discussions.

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 Post subject: Well written!
PostPosted: Sun Nov 04, 2012 11:07 pm 
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Hat maker,
That was incredibly well written and I really appreciate it. Even though I disagree about the dosing part (we have already debated that). Maybe med students need to read this in their pain management class.


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PostPosted: Sun Nov 11, 2012 5:29 pm 
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Hi old friends!!! Long time no read! Please point me in the direction of a post about the best generic subutex. I just switched from sub to bupe and I want the best generic. I have the ones with the arrow now(hi-Tec) and I heard Di not get the Roxanne brand and have read that a lot. If the teva is better than hi-tech is what I'm trying to find out.

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PostPosted: Wed Mar 20, 2013 11:08 am 
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How was the switch from subs to subutex? Any problems? I was going to switch but my idiot doctor is not a fan of subutex. He says its an overdose potential because theres no anti analgest whatever. He just a bichazz, I have no history of iverdosing on anything or any thoughts of taking all my meds in one day like an idiot. He just doesnt want me having any fun. The suboxone films are absolutely no fun and I need to find a new doc thats into subutex. Might have to go into a russian neighborhood, they scribe anything lol. My doc also confurmed they not producing the sub tablets anymore, just the laim films. Too many kids eating the tablets and oding supposedly. I said if you chew the tablets and swallow doesnt that kill the bup effect? He was like uhh yaa, so how are kids oding? I think this is all bs.


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PostPosted: Wed Mar 27, 2013 9:54 am 
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A few years back, I switched from Subs to Subutex due to insurance issues. My insurance stopped paying for my medication so I wanted to go the cheaper route with Subutex generic. I could not tell a difference when I switched over.

I think your doctor is probably worried that you could:
1/ take Subutex with other opiates to intense the high
2/ not take it subligually and inject or snort it.

I personally got off of Subutex later and then I got put on Suboxone films when they were available. But I couldn't tell a difference between the 2.


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 Post subject: Re:
PostPosted: Sat Jan 11, 2014 2:35 pm 
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hatmaker510 wrote:
Dosing is like walking a fine line. We have to find the lowest possible dose that will accomplish the highest benefits - extinguish cravings and withdrawals with the least amount of side effects. Does the number of the dosage really matter? We as individuals are the ones who determine what dose we feel best at anyway and it's not by the number, it's based on HOW WE FEEL. If I were you, Taurus, I wouldn't be too concerned about the mg of your dose, only that you feel you're at the right dose for you.


Agree with this, and I want to mention that it sounds like those who are benefiting from the pain control properties of buprenorphine might find relief at lower doses. Taurus, I am similar to you; 4 MG is now entirely too much for my needs. I am on 3 MG currently and dropping to 2 MG. When my pain is controlled, I neither feel a "high" nor think about taking painkillers. The obsession is 100% eliminated. While this flies in the face of current, conventional wisdom dictating that the ceiling effect is reached at a minimum of 4-8 MG, I think we need to take into account that everyone is different, we each got started on painkillers for different reasons, and we are on bupe for different reasons.

Some doctors consider opiate-seeking behavior in a pain patient to be a marker of pseudo-addiction, and for those who agree with this theory, it is demonstrated by the patient when s/he stops thinking about pain meds after a proper painkilling dose is achieved. Remember, bupe is a POWERFUL drug, and if you experience pain relief from it at a lower dose, you are not alone by any stretch. It is no coincidence that painkilling doses of bupe are MUCH lower than addiction recovery doses – often, measured in micrograms. When on bupe for pain control, the goal is not to reach the ceiling so that the patient stops thinking about scoring dope or pills, so much as it is to reach a dose where the patient stops thinking about pain.


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 Post subject: Re: The Ceiling
PostPosted: Sat Oct 22, 2016 1:57 pm 
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Question for hatmaker510. Read this whole post and I'm trying to find the post you were referring to called hello my first post intro or introduction thread where you say you explain and organize your thoughts better. I am new to this forum and perhaps I'm not using the search feature properly. If you could give me any advice in finding this post I would really like to read it thank you


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