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PostPosted: Mon Mar 29, 2010 12:17 pm 
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I found the following at Dr J Blog which I found very informative and at odds with what most subs patients know and believe about their dose and the effects they receive taken on a daily basis. It's always interesting to learn truth vs myth/rumor with regards to suboxone :

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I will talk about buprenorphine, the active medication in Suboxone, just to simplify things a bit– although Suboxone will have the same effects. First, when talking about the dose, it is important that the method one takes it is identified– as that is what determines how much active drug ends up in the bloodstream. I will assume that the person is taking steps to get maximal absorption of Suboxone; for example keeping it exposed to mucous membranes for a long-enough time, and not rinsing the mouth with liquid for at least 15 minutes after dosing, to avoid rinsing away drug that is attached to the lining of the mouth but not yet absorbed. As an aside, there is a post somewhere on this blog entitled ‘maximizing absorption of Suboxone’ for those who want more info.


When a person takes Suboxone, he is taking a ’supra-maximal’ dose of buprenorphine. Buprenorphine is used to treat pain in microgram doses; the BuTrans patch is used in the UK to treat pain, and it releases buprenorphine at a rate of 5-20 MICROGRAMS per hour! One 8mg tablet of Suboxone containes 8000 micrograms! So whether a person is taking one, two, three, or more tabs of Suboxone per day, he is taking a very large dose of buprenorphine— a dose large enough to ascertain that he is up on the ‘ceiling’ of the dose/response curve. It is important to be on the ceiling, as this is the flat part of the curve (I know– a silly statement) so that as the level of buprenorphine in the bloodstream drops, the opiate potency remains constant, avoiding the sensation of a decreasing effect which would cause cravings.

I have read and heard differing opinions on the dose that gets one to the ‘ceiling’ but from everything I have seen the maximal opiate effect occurs at about 2-4 mg (or 2000-4000 micrograms), assuming good absorption of buprenorphine. I base this on watching many people initiate Suboxone; if a person with a low tolerance to opiates takes 2 mg of buprenorphine, he will have a very severe opiate effect; if he takes that dose for a few days and gets used to it, and then takes a larger dose, there is no significant increase in opiate intoxication– showing that once he is used to 2 mg, he is used to 16 mg— and is ‘on the ceiling’ by definition. I see the same thing in reverse; there is very little withdrawal as a person decreases the dose from 32-24-16-12-8 mg, but once the person gets below 4 mg per day, the real withdrawal starts. This again shows that the response is ‘flat’ at those high doses, and only comes down below about 4 mg of buprenorphine.


The flip side of all of this is that tolerance reaches a maximum at about 4 mg of buprenorphine, and further increase in dose of buprenorphine does not cause substantial increase in tolerance. Tolerance and withdrawal are two sides of the same coin; the lack of withdrawal going from 32 to 8 mg of buprenorphine is consistent with no significant change in tolerance across that range.

So in my opinion, being on 32 vs 4 mg of Suboxone doesn’t raise your tolerance. But in regard to upcoming surgery, there is an additional concern. One issue with surgery on buprenorphine is the high tolerance, but the second issue is blockade of opiate agonists by buprenorphine– and this effect is directly related to the dose of buprenorphine. A person on 32 mg of Suboxone will need much, much higher doses of agonist to get pain relief than will a person on 4 mg of Suboxone– not because of tolerance but because of the blocking effect, which is competitive in nature at the receptor. When people are approaching surgery I recommend that they lower their dose of Suboxone as much as possible– to 4-8 mg if possible. Because of the very long half-life (72 hours), this should be done at least a week before the surgery. Then I have them stop the Suboxone three days before the surgery; it usually takes 2-3 days for significant withdrawal to develop. I say all of this to give a general sense of the issues involved; people should discuss the issue with their physician rather than act on what I am describing here.
=========================


I think this is important information with regards to the amount of Bupe we take each day. This explains to me why I felt essentially no withdrawls when I tapered from 12 mg to 2 mg and very little when dropping from 2mg to .5mg. Based on the above article a dose of .5mg is 500mcg and still a relatively high amount when compared to what is prescribed for pain.... which would be 120-480mcg per day... via the patch.

This may cause some to re-think taking a high dose of 12mg+ and whether or not they are getting a good absorption. I found the half life duration of 72 hrs different then what I thought. I had believed this was 37 hrs.


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 Post subject: What's the point?
PostPosted: Mon Mar 29, 2010 3:57 pm 
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suboxfreedom,

I would have to agree with the conclusions you have come up with based on my observations as well and because of this
I always have sympathy for those patients who's doctors have them on 24 or even 32 mg per day. It seems like a waste of money to me. I guess I'm missing something. How can someone possibly benefit from these high doses when you take into consideration the long half-life and the low ceiling of buprenorphine?

Can anyone shed some light on this subject for me? Thanks!


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PostPosted: Mon Mar 29, 2010 5:49 pm 
I had read that information from Dr. Junig as well some time ago. In part, that is why I reduced from my initial Suboxone as quickly as I did. When you're paying for the meds out of pocket and/or do not desire to be on any higher of a dose of medication than is necessary for whatever reason, it makes sense to research and know this type of information. As so many of us have, I readily discovered that getting down to 8mg/day was not a big deal and in fact, I found that I felt better with the lower dose.
I choose not believe that most doctors start us out on higher doses for any gain to themselves. I think it is more likely that they don't fully understand, as Dr. Junig does, the way this medication really works. The other factor I think is in play is that the higher doses ensure a total blockade effect to full-agonist opiates. I think it's important especially when therapy is initiated that those opiate receptors are sufficiently and totally loaded. In that way, a 'slip' with the former DOC will give the user no positive reinforcement to repeat the behavior. The other thing is, it's necessary to be certain that the ceiling is reached to stave off cravings and prevent withdrawal symptoms. To me, that explains at least to some degree the rationale behind starting off on doses that are really higher than what may be necessary.
I do think there is a need, however, to get the word out to the prescribing doctors as well as all bupe patients that it is probably best practice to lower the dose once the patient has been stabilized. I believe that prescribing doctors have been notified that 'best practice' is to not have patients on doses higher than 16mg/day to begin with. Why some continue to prescribe doses higher than that I do not know. I really like my doctor but he is among those who do prescribe doses over 16mg/day. I'm glad I took the initiative and found this forum and began educating myself so that I would not continue on that high a dose. From what I can see, there is just no need to be on that much Suboxone, unless you're a chronic pain patient or there is some other reason for it.
Anyway, that's the little bit I know on the subject. Thanks for bringing that information forward Suboxfreedom. Good stuff!


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PostPosted: Mon Mar 29, 2010 7:18 pm 
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Thanks setmefree for adding that qualifier at the end of your post about chronic pain patients. I'm one of those patients. When I'm constantly being questioned, judged, or receiving "sympathy" I don't need, because of it, well, it can become quite tiresome.

So thanks for making sure to mention those of us whose only option left to treat chronic pain is with bupe.

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PostPosted: Mon Mar 29, 2010 7:45 pm 
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Thankyou for posting this i found it really interesting to read. so say somebody on a very high dose goes in for emergency surgery what would they be given for pain?


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PostPosted: Tue Mar 30, 2010 12:08 pm 
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Bboy42287 wrote:
Thankyou for posting this i found it really interesting to read. so say somebody on a very high dose goes in for emergency surgery what would they be given for pain?


Thats a good question... I think the surgery itself would be no problem since the anestheseologist can still put you under. However, as dr J. indicates in the above articles last paragraph, the healing period and tolerance level could create problems. Hopefully, the high dose of bupe would control the post-op pain. I must admit I was concerned about this myself and it was a major motivating factor for tapering.

The real problem could be an ER dr not taking the time to research the right protocol for a subs patient or else an unconscious subs patient who took a high dose within a 1/2-1hr of getting to the hosp.... As i understand it, the naloxone would still be very active on the brain receptors and if given an opiate, precipitated wd would happen.

here is a reference for you:

http://www.suboxonehelpline.com/anesthesia/


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PostPosted: Tue Mar 30, 2010 10:08 pm 
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suboxfreedom wrote:
Bboy42287 wrote:
Thankyou for posting this i found it really interesting to read. so say somebody on a very high dose goes in for emergency surgery what would they be given for pain?


Thats a good question... I think the surgery itself would be no problem since the anestheseologist can still put you under. However, as dr J. indicates in the above articles last paragraph, the healing period and tolerance level could create problems. Hopefully, the high dose of bupe would control the post-op pain. I must admit I was concerned about this myself and it was a major motivating factor for tapering.

The real problem could be an ER dr not taking the time to research the right protocol for a subs patient or else an unconscious subs patient who took a high dose within a 1/2-1hr of getting to the hosp.... As i understand it, the naloxone would still be very active on the brain receptors and if given an opiate, precipitated wd would happen.here is a reference for you:

http://www.suboxonehelpline.com/anesthesia/


The naloxone in Suboxone is inactive unless someone disolves the pill and injects it. When taken orally or sublingually, the naloxone is eliminated by the liver. There would be no "active naloxone" at the opiate receptors regardless of how recently a Sub patient had taken his/her medication.

Sub patients will not go into precipitated withdrawal in the ER if a doctor gives them a full-agonist opiate. That is not how precipitated withdrawal works. Precipitated withdrawal happens when you have a lot of full-agonist opiates in your system and then you take buprenorphine. The buprenorphine will out-compete the full-agonist at the receptor, blocking the full-agonists but not fully stimulating the receptor, causing symptoms of withdrawal. Precipitated withdrawal has nothing to do with naloxone. You can not get precipitated withdrawal by taking a full agonist AFTER you're already on suboxone.

What might happen in an ER situation is that the ER doctors wouldn't give you enough full-agonist medication to break through the buprenorphine and you'd have inadequate pain control. This is a problem, but there are some ways to work around it. Non-opiate painkillers could work, or a nerve block, and sometimes high doses of full-agonist medication will work if the Sub dose is not too high.

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 Post subject: Thanks
PostPosted: Wed Mar 31, 2010 1:49 pm 
Thanks you so much for posting this - I didn't see it on the blog. Way back when I first went on Sub I tried to figure out how it compared to other opiates, and I think I read that 0.3mg of bupe (IV) = 10mg morhine. I was stunned. But then I guess I just thougt that bupe isn't absorbed very efficiently sublingually, so that is why we are on such high doses. But now I am starting to question that. I feel like I really am taking too much, and that taking a higher dose doesn't give an increased benefit. I was corresponding with someone who used what I used in roughly the same amounts, and she was on 2mg/day at most. I, on the other hand, have been taking 12 mg/day. I know everyone is different, but seeing the facts in that article really is making me question matters. My dr. is not helpful on this subject. He would give me 32mg/day forever if i wanted,
Thanks again - I'm really learning a lot from this forum
Lilly


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PostPosted: Thu Apr 01, 2010 10:33 am 
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Lilly wrote:
Thanks you so much for posting this - I didn't see it on the blog. Way back when I first went on Sub I tried to figure out how it compared to other opiates, and I think I read that 0.3mg of bupe (IV) = 10mg morhine. I was stunned. But then I guess I just thougt that bupe isn't absorbed very efficiently sublingually, so that is why we are on such high doses. But now I am starting to question that. I feel like I really am taking too much, and that taking a higher dose doesn't give an increased benefit. I was corresponding with someone who used what I used in roughly the same amounts, and she was on 2mg/day at most. I, on the other hand, have been taking 12 mg/day. I know everyone is different, but seeing the facts in that article really is making me question matters. My dr. is not helpful on this subject. He would give me 32mg/day forever if i wanted,
Thanks again - I'm really learning a lot from this forum
Lilly


According to the article... most people are taking more bupe than they need. Even if used for pain.

12 mg is 12,000 mcg and in europe dr's prescribe 120 mcg- 480 mcg per day for pain. I think you're pretty close regarding morphine as I have a reference which indicates bupe is 15-25 times more potent than morphine.

I have retained shell fragments in both legs, chest, and lung which is how I got to pain mgt. I've personally found I get the same relief with .50mg as I do with higher dosees. The problem with pain though is that most of us need to take the right dose every 4-6 hrs [at least for me] to be pain free. Which means I need to take about 1.5mg a day for total pain relief.... which i don't do. Instead I take the .50mg once a day and remain inactive or take over the counter in the PM.


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PostPosted: Sat Apr 03, 2010 9:05 pm 
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The article doesn't mention anything about taking suboxone for pain or the required dosage levels or frequency at which you would need to take sub for pain. It doesn't say people are taking too high of a dose "even" for pain. I just wanted to clarify that.

Cherie


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PostPosted: Tue Jun 26, 2012 7:15 am 
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I wanted to resurrect this thread because of the discussion of the ceiling and that fact that it includes statements made by Dr. Junig that I just reviewed. There's been talk lately about the ceiling level no longer being considered as ~4 mg, even though it's been said to be that for the past 3+ years.

So consider it resurrected!

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 Post subject: How I feel
PostPosted: Fri Aug 17, 2012 4:01 pm 
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I think my ceiling must be higher, or something, b/c even after over 2 years I can tell a contrast in my mood between 16 mg and 24 mg. And I know it's not just absorption level, either.

Bunny


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PostPosted: Sat Aug 18, 2012 12:00 am 
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Yeah Dr. J said ceiling level depends on different factors incl metabolism, bioavailability etc. I wouldn't be surprised if it could be even high in some people, esp those with fast metabolism. The idea is to have your levels over the ceiling level for a full 24 hours, so if you burn through your sub really fast you need a higher dose to keep it over the ceiling all day.


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Fond Du Lac Psychiatry
Dr. Jeffrey Junig, M.D., Ph.D.

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