Talk:Buprenorphine/Archive

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[edit] bupe in pregnancy

Despite what is written, buprenorphine is NOT preferable to methadone during pregnancy - see Turning Point/Royal Women's Hospital Clinical Guidelines for the use of buprenorphine in pregnancy at http://www.turningpoint.org.au/library/CTG_Bup_Pregnancy_060104.pdf --58.165.162.245 04:58, 24 February 2007 (UTC)

[edit] antidepressant use

I'm grateful to Rearden Metal for putting this section in. However, the use of buprenorphine in the U.S. off-label for depression is perfectly legal. Many doctors, including psychiatrists who have had the 8-hour training & gotten the special DEA waiver, misunderstand this. The point was correctly made by Bk0 in December ("physicians can prescribe any approved drug for off-label purposes"), but apparently there was some back-channel communication, because Bk0 immediately reverted to the erroneous sentence – which never had any source. In addition to the SAMHSA FAQ, the situation is discussed (with further links) here and here. It'd be nice to discuss why docs are reluctant to use it (see Callaway 1996 excerpts). (Hedkace 18:02, 7 February 2006 (UTC))

I reverted because it was explained to me that controlled drugs are not subject to the same governmental deference that non-controlled drugs are. Physicians can be (and apparently are) prosecuted for prescribing controlled drugs for unapproved uses (or for approved uses in arbitrarily-judged "excessive" quantities). I wasn't aware of the DEA waiver you mention above, however, so obviously the situation is more complicated. --Bk0 (Talk) 18:15, 7 February 2006 (UTC)
Hey, Bk. Thanks for replying so quickly. It is complicated and widely misunderstood. Physicians are usually prosecuted for APPROVED use of controlled substances (as you say, in "excessive" quantities). That "governmental deference" to a physician's off-label judgment applies to controlled substances EXCEPT when the doc is treating opioid addiction with an opioid (which is off-label for most opioids). (Flopzee 19:14, 7 February 2006 (UTC))
It is legal, in the strictest sense of the word, but a doctor *could* have his DEA license (and thus ability to write controlled substance scripts) yanked or could face charges from the DEA, most likely if he does it too much, just like he could for scripting it for approved uses. When it comes to controlled substance scripts, it sadly comes down to a matter (of the DEA's) opinion. Usually the dosage and number of patients treated is what would draw attention from the DEA. The only thing I know of offhand that *is* illegal is scripting narcotics off-label for opiate addiction as mentioned by Flopzee.

On another note, from personal experience and all I have heard on the grapevine, buprenorphine causes less euphoria than other opioids even with "equivalent" doses. (That part is thus an opinion.)That might be relevant in it's treatment for addiction. It does however do very unique things such as lower tolerance (in time) in people who have tolerance to opioids. - Nephalim 09:19, 11 October 2006 (UTC)

I'm also editing the phrase "dozens of other (non-opioid) medications had failed", which sounds like the patients had each used dozens of ADs. The study said, "The mean number of antidepressants previously tried was 7.6 (SD = 5.7)." (Hedkace 18:02, 7 February 2006 (UTC))

A lot more could be said about the U.S. bupe waiver system. I'm going to clarify one or two points, but more is needed. (Hedkace 18:02, 7 February 2006 (UTC))

[edit] Addiction treatment section

  • This section needs to be cleaned-up / wikified / verified. I'm going to start soon, having just done some interviews with bupe patients. --Tarnas 21:23, 31 July 2005 (UTC)

Been using Subutex sublingual tablets for three years in Australia and never heard of "lemon-lime flavour".

Subutex is unflavored; Suboxone is lemon-lime flavored. It doesn't do much to mask the bitterness of the bupe; I think it just makes it worse, personally. Porkchopmcmoose 20:21, 6 January 2006 (UTC)

The author of the article talks about the efficacy of 12 step programs and the fact that there is no research to support that efficacy. The millions using that route as a spiritual lifestyle must say something. I use methadose and have friends on suboxone. Those that are serious do well and those that are not do not. This is discussion so I'm a bit loose here. This author should not in my opinion, be bringing opinions about spiritual programs to a technical article. I don't do 12 step programs but I do respect them after doing the research. Maybe he has references showing the spiritual approach is not useful. Cite them. My source . "Appendix II AA Big Book A spiritual experience." “There is a principle which is a bar against all information, which is proof against all arguments and which cannot fail to keep a man in everlasting ignorance—that principle is contempt prior to investigation.”

—Herbert Spencer Wolf2roger 03:00, 21 May 2006 (UTC)

[edit] Admin route

Is parenteral right? It's a bit broad, I was under the impression that the bupe formulations in question were strictly intravenous... you wouldn't want to put heroin into your muscle or skin pop it if you could avoid doing so, why would medical techs try that with bupe? —Tarnas 19:40, 21 August 2005 (UTC)

The Australian Medicines Handbook and British National Formulary list both IV and IM routes for buprenorphine analgesia, but you're right in saying that "parenteral" is too broad a term to use here. -Techelf 12:27, 22 August 2005 (UTC)

"Skin Popping" is the route used at Somerville Hospital Massachusetts USA I don't know why. That is just during the acute detox phase. Wolf2roger 03:00, 21 May 2006 (UTC)

Bupe literature in the US says it's not to be used IV (even the injectable formula, IM or SC). I don't know why. - Nephalim 06:38, 6 November 2006 (UTC)

[edit] Pharmacology

The reason μ-opioid receptor antagonists can only partially reverse the effects of buprenorphine is due to its extremely high affinity for the receptor. It's one of the most potent MOR ligands there is. Because it binds to the receptor so avidly, it blunts the activity of other opioids. This, and not its partial agonism, is why it attenuates the effects of agonists as well as antagonists. I've updated the pharmacology section to reflect this. Porkchopmcmoose 20:21, 6 January 2006 (UTC)

Do you have any references? I can find nothing in the standard drug monograph to corroborate those statements. Buprenorphine does not, from what I understand, attenuate the effects of antagonists. "...when administered intramuscularly, combinations of buprenorphine with naloxone produced opioid antagonist actions similar to naloxone." (PDR, 2006). --Bk0 (Talk) 23:41, 6 January 2006 (UTC)
The Australian Medicines Handbook 2005 says to, "Avoid use as an analgesic for the following reasons: -effect not reversed by naloxone...". -Techelf 11:22, 7 January 2006 (UTC)
The PDR also says that overdose respiratory depression is not totally reversed by naloxone, however I understood that was because of buprenorphine's kappa agonism (naloxone is exclusively a mu antagonist). Naltrexone would conceivably be more successful. --Bk0 (Talk) 11:26, 7 January 2006 (UTC)
Buprenorphine is a kappa antagonist, not a kappa agonist. At the mu receptor, it's a partial agonist, which is why it can precipitate withdrawal in patients already dependent on strong (full mu agonist) opioids. Porkchopmcmoose is correct that the difficulty of reversing buprenorphine is due to its extremely high receptor affinity, not its partial mu agonism. -User:Karn 08:41 31 January 2006 (UTC)
Karn is correct. - Nephalim 09:02, 11 October 2006 (UTC)

[edit] Buprenorphine reduction cure

I have been using buprenorphine for over three years and have recently started reducing my dosage. If anyone is curious about my progress for personal or professional reasons, make a comment and I'll gladly make regular updates.

I began the programme after a year on methadone and found bupe much more flexible - missing a dose presents negligable withdrawal symptoms in comparison; I can & do take a double dose every other day, a marked improvement over daily trips crosstown. A doctor will always tell you that the antagonist/agonist structure of buprenorphine renders the pleasurable effects of other opioids nonexistent, but this is not enitrely correct - if one is inclined to use another opiate while on the programme, it is merely a matter of injesting larger doses. Buprenorphine's familiar 'opiate effects' are somewhat different from the feel of morphine, heroin, methadone. I can decribe it best as an hour or so of drowsiness - eyes will shut if one is reading or sitting still - and a feeling of confidence, reminiscent of the overwhelming secruity & lack of self-consciousness which heroin delivers. Itchiness, pin-pointed pupils, constipation are present as usual.

Two months back I reduced my dosage from 10mg to 9mg, or a double dose of 20mg to 18mg. Last month I was on 16mg. This month I'm down to 14mg. I have noticed no significant symptoms. Bathing regularly goes a long way in keeping the skin from an irritated, sensitive state.

After withdrawing successfully from heroin and methadone, I am curious to experience the final stages when the dosage is down to 1 or 2mg, and the following days, weeks, & months. I may resort to a prescription of diazepam (Valium) and tamazepam to relax the body & mind and to take the edge off.

On this note, I recommend to any heroin addicts reading this to forego methadone altogether and segue straight into an appropriate dosage of bupe. The last time I kicked methadone, I experienced constant mild withdrawal symptoms and regular nightmares for a period of roughly three months. It is the cruelest of the opioids. -Jones


wondering how your coping with coming off bup? I am currently writing a gap year project on buprenorphine and naltrexone. would you say buprenorphine is in general a more popular alternative to methadone? or does its decreased 'high' effect make it less popular? just out of interest, please do not feel obliged to answer if you don't wish to. Student glasgow 12:07, 1 February 2007 (UTC)

[edit] Nephalim's Buprenorphine FAQ

My wife added it to the links, I hope that isn't inappropriate. It is definitely not garbage, and it is thorough and touches all bases (for use for opioid addiction, at least.) I know that short of Wikipedia's article it's really one of a kind. It does have a few errors that need to be corrected, although nothing serious, and needs more sourcing done. Please feel free to give your opinions as to if it's a legit (including morally) thing to do and any and all comments regarding it, including corrections and constructive criticism. Nephalim 09:10, 11 October 2006 (UTC)

Since Beetstra took it out without explaination (other than a link to Wikipedia's external linking standards), I will provide a link here.
a Comprehensive Buprenorphine FAQ
Nephalim 09:27, 11 October 2006 (UTC)

(copy section from user talk:beetstra):

It appears you took one look and removed it. I read the external linking and it does appear appropriate. Please tell me why you removed it.—Preceding unsigned comment added by Nephalim (talk • contribs)
Having a look, brb. --Dirk Beetstra T C 09:38, 11 October 2006 (UTC)
OK, I had a look. The reason why I removed it at first, was that the edit looked a bit vandalous, not only the link was included, also a stray 'A', and the edit was performed by an anonymous editor (on an anonymous IP this could be a link to an own website, which would not comply with wp:el, moreover, there is a vandal-warning on the talk-page of the ip, already). I did have a glance at the page, and the tone of the page looked like 'personal research' (though it is not included in the page, but have a look at wp:or). I think the way you have chosen now (adding it to the talk page) is at least an appropriate one, maybe others can help in the decision. By the way, I am not fond of this type of links, imagine everybody linking to a personal page with their own experiences with ethanol (though I understand that with medicine the group will be way smaller, still it might amount to hundreds of such links). Could you write a request for the link being added to the talk-page? I guess that after a couple of (positive) answers, and/or a couple of weeks, you are free to add the link (point to the discussion on the talk page in your edit summary). Hope to see you around, happy editing. --Dirk Beetstra T C 09:58, 11 October 2006 (UTC)
Dirk Beetstra T C 10:02, 11 October 2006 (UTC)
Well, consider it that request then (a request for my FAQ to be added to the external links of this page.) Thanks for the thorough reply. The IP is a dynamic one, or at least a carryover. If there is a vandal warning, it's highly likely dynamic. It's ADSL.
I am very modest, but am quite proud of my FAQ, and many people write to me having read it. -Nephalim 10:52, 11 October 2006 (UTC)
I do not have strong objections, though (as I said), I am not fond of these EL's. --Dirk Beetstra T C 11:27, 11 October 2006 (UTC)
Just a reminder of my request. Please voice any opposition if you have any. I am currently updating it so that it is fully sourced as it should be, it's a small part of a book I am writing, and when it's finished despite my general modesty I will be very proud of it and myself, and think it will be a relevant and useful link. My wife stands behind me and is the one who added it as I mentioned but that point is moot, as I clearly want it here and won't hide behind my wife. I have also made the edit summary clear so no one misses it. Thank you. --Nephalim 09:03, 30 October 2006 (UTC)

[edit] Article on Buprenorphine for Refractory Depression

Within a decade or two, Buprenorphine will be commonly accepted by medical orthodoxy as a legitimate antidepressant. In parallel, the neurotransmitter re-uptake inhibitors will inevitably fall out of fashion (much like bloodletting, mercury salves, and eugenics).

I'm not sure if I should try slipping my website into the 'Links' section on the main page. For those who are interested in learning more, my essay connects all the dots, and cites the few existing scientific papers which form the basis for my opinion:

www.ProhibitionKills.com Rearden Metal 05:10, 14 October 2006 (UTC)

You have my vote of approval, but my opinion is perhaps tainted due to my own desire to have my FAQ on buprenoprhine for opioid addiction linked. It's the type of thing that's not OK in heavy doses, but IMHO in this situation there isn't a ton of stuff out there to link to that truly is relevant and warranted.Nephalim 10:31, 16 October 2006 (UTC)

[edit] Risk of Overdose

The risk of overdose in people using the medication properly - esp. that aren't opioid niave (have a tolerance) - is minimal at best, that ceiling works oftly well. I will assume that benzodiazepines don't increase this risk unless the drug is injected or used by opioid niave individuals. Unfortunately that is at this point an opinion but one I am 99% sure of. I personally use it in long-term maintenance, *have* used heroin on top of it (the key word there is 'have'), and have since I began treatment used benzodiazepines including, if not mostly, in high and very high doses. I have also mixed it with TWO *other* serious depressants (amitriptaline and Tegretol) without any problems. That's all my experience, but I am including the evidence I know of (that when combined with benzodiazepines causing death it was misused - possibly with those whom are opioid niave or have been clean for a while) and common sense (it's ceiling effect) together with it to formulate my opinion. Can anyone provide evidence otherwise? That the risk of overdose is high when injected (without benzodiazepines) or combined with benzodiazepines, both cases in persons with opioid tolerances (i.e. those in treatment with the medication)?Nephalim 10:43, 16 October 2006 (UTC)Nephalim

[edit] Revamp of Methadone vs. Buprenorphine by Nephalim

It was filled with weasel words and a non-NPOV. The suggestion for instance that buprenorphine (flat out!) isn't used indefintely or life-long is bogus, and I for one am living proof of that. Off the top of my head, another thing was the incorrect statement that a patient getting long-term (i.e. month) scripts for Subutex/Suboxone MUST get other treatment. This is incorrect, as described in the article. An unfortunate (depending on your POV) fact that while naloxone doesn't block other opioids buprenorphine itself does must be addressed and I hope I did it well. Perhaps I should have added the medical implications (i.e. when you need pain relief.) Methadone does it too, block other opioids, and I made that clear. Also, I added the pregnancy benefits of buprenorphine, and the down/up sides of switching between meds. Let me know what you think. I would do more through referencing, but I simply don't have the time, and its not like it was referenced before. If challenged I will prove myself at least with time, but I urge you to find the answer yourself. That's not to say I am infallible. -Nephalim 10:36, 3 November 2006 (UTC)

I like the work you've done here recently, Nephalim.
Listing all of the many points we agree on would be boring- Instead, I'll just mention the one point where we may have a difference of opinion: Methadone is clearly inferior to bupe in most cases, IMO- and not just because of the strict nanny-state restriction on 'done.

How many long time (two years+) methadone users do you know of, who are happy with this medication? Is it zero, or is it zero? Methadone turns on the patient after a while, making his/her life miserable. That's why bupe is so much better. Rearden Metal 06:40, 4 November 2006 (UTC)

Thanks. We don't necessarily disagree. I think buprenorphine is superior to Methadone - but I can't prove it so it doesn't belong in the article (actually, in treating opioid addiction, it is superior to methadone up to 90mg of methadone - it's been proven, and I should drag that study in here, don't know it offhand, requires a google search). It causes changes in the brain that lower tolerance (again, need to find the study), and it doesn't cause the massive problems i.e. getting off that methadone does. However, being on buprenorphine 6 years now I can tell you that both of these meds can "turn" on you after a while. - Nephalim 05:03, 5 November 2006 (UTC)
Minor refinement - added that buprenorphine is harder to get on than methadone from a heroin/potent opioid addiction vs methadone, and that a woman can take the difference between methadone and buprenorphine during pregnancy into account before becoming pregnant, an obvious conclusion that I missed. It looks like more was changed than it is because I cut a paragraph into two. - Nephalim 11:04, 3 November 2006 (UTC)
Addendum: I need to add Wikipedia page links that I forgot but I won't do it now. - Nephalim 11:10, 3 November 2006 (UTC)

[edit] Huang Study re: Norbupe

It's not accurate. For one bupe is not an agonist, full or partial, at the kappa receptors. It's an extremely potent antagonist. If norbupe is it's irrelevant as its actions are completely antagonized by bupe. I am nearly certain that buprenorphine has no effect at delta, agonist or antagonist, and also nearly but not as certain that norbupe doesn't either. I'll look into it further eventually. - Nephalim 02:09, 4 November 2006 (UTC)

[edit] Revamping the Rest of the Article

Talk here. I hope it's as NPOV as possible. - Nephalim 09:29, 6 November 2006 (UTC)

[edit] Anelgesia and Buprenorphine

Can anyone comment on the analgesic properties of Buprenorphine?

I have been on MS for 5 years and will not increase my dose past 100mg for analgesia. When I reach my max dose I'll use clonodine as an aid to decrease my dose 20 or 30 mg over 4 to 6 weeks. This isn't an easy process and anything that can help would be welcome, but in my condition I can't function without the pain relief.

Thanks, AR —The preceding unsigned comment was added by Al Renner (talk • contribs) 06:35, 17 March 2007 (UTC).