Talk:Buprenorphine/Archive 1

Archive 1

Has anyone noticed the Hi Tech ( Akron ) suns have been crappy lately? Does anyone recommend a better brand?

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)

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))

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)

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)

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)

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)

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)

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)

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

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)

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)

Revamping the Rest of the Article

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

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).

Subutex vs. Suboxone

The manufacturer recommends starting with Subutex because it does not have the Naloxone component. Naloxone has side effects which could be severe enough to encourage the patient to stop taking the medication completely. Naloxone is not needed unless the patient has a propensity to inject drugs. Unfortunately, some doctors are adamant about using Suboxone. If that is the case with the patient, find a doctor that doesn't insist on Suboxone but will use Subutex instead. Even better, when the patient calls to make his first appointment, ask the nurse at the office if Subutex is prescribed. If the nurse says no, then hang up and call another doctor. Do not take more medication than you need to detox.

Also, try and move consistently down off of Sub as quickly as possible. Listen to your body. If you have been addicted for several years, it may take a longer time than if the addiction is shorter in time. It's possible to detox in a month but the patient must be highly motivated and follow a strict plan.

Some patients remain at the highest levels for extended periods of time. That is not necessary and should be avoided.

One example of a taper schedule is:

Starting at 12mg, then: 10mg-2 weeks 8mg- 3 weeks 6mg- 3 weeks 4mg- 4 weeks 3mg- 4 weeks 2mg- 4 weeks 1mg- 4 weeks .5mg-4 weeks .5mg every other day 6 weeks

Total- 35 weeks

However, keep in mind that the taper schedule will be different for everyone.

Lastly, it's often difficult to determine what the equivalence of Sub vs. the drug of choice of the patient. One tool can be found at: http://www.medcalc.com/narcotics.html. This is a good tool but it is certainly not a perfect tool. Even doctors have a hard time making this determination. For example, 10 tablets of Vicodin is about 100 mg. of hydrocodone. That translates to about 8 mgs. of Sub. Even though Sub. has a long half-life, it's also a good idea to split the Sub. dose so that the active chemical stays relatively stable throughout the day. Anyone contemplating using this med to escape narcotics, feel free to contact my Talk Page for additional help. Jtpaladin 16:34, 11 April 2007 (UTC)

OK just one comment for anyone who reads the otherwise ox comment above. Ten tablets of Vicodin would not be 100 mg of hydrocodone. It would be 50 mg. If it was Vicodin ES it would be 75 miligrams of hydrdrocodone. 10 tablets for 100 mg would be Vicodin HP (which is pretty uncommon) or another formulation of Hydrocodone/APAP.

Inpatient rehabilitation section?!

Is it just me that's deeply uncomfortable with this section in particular? A huge amount of unreferenced stuff, and frankly I've got no idea where some of it's come from or why it's in an article on subutex / suboxone / buprenorphine.

Feels to me like this could do with a lot of work, some decent and brutal editing, and a fair few more references. If there's anything I can add / reference then I'll have a peek later (particularly around detox treatments / pro-social networks in recovery) but tbh I feel there's a whole lot of stuff in here that's on the wrong page and is - frankly - largely irrelevant with a somewhat ideological hue.

A couple of the other sections strike me as a wee bit flabby / unreferenced n all, but hey. I'll have another look later, and if I can't suggest anything more constructive or make any positive additions / contributions I'll butt out completely, ha.

81.2.126.58 09:24, 13 June 2007 (UTC)Geoff

This information contained about the induction dosing is particularly necessary to an article on buprenorphine as it has a very unique initial dosing phase. The section could definitely stand to be re-written; however, I do not see most of it as irrelevant.

Perhaps if Wikipedia had an entry on "Opioid Treatment Programs" then the rest of the information contained in this section outside of the induction dosing in an inpatient setting could simply be linked to? But there is no such article.

Lucida.ann 21:14, 27 August 2007 (UTC)

Edit for Suboxone page

I just wanted to let you guys know that Suboxone isnt intended to have an orange flavor. In the actual drug form from R-B its listed as having a lemon-lime flavor. If anyone wants a picture from the brochure for proof let me know. kylewmackey@gmail.com —Preceding unsigned comment added by 67.189.252.63 (talk) 01:15, 2 October 2007 (UTC)

Being someone who takes this medication, I can say that until someone told me it was supposed to be lemon lime, I would have said it tasted like orange tang. The color of the tablet probably is enough to suggest that any citrus flavor be interpreted as orange. 66.41.0.174 (talk) 20:32, 28 November 2007 (UTC)

Updated Suboxone information under "preparations" - and comment about subsequent section lengths

11 December 2007 - London

Hello

I have added the most relevant studies around Suboxone's effects in human subjects when it is injected, as well as the best available evidence about Suboxone's potential for abuse/black market in the community (Finland only!).

In my view the following sections around buprenorphine-based detox are way too long. It would be better for Wikipedia if we instead cited external sources or guidelines around detox - these do after all vary substantially by country, as do the methods of proving opioid dependence treatment using buprenorphine-based products.

Cheers

193.130.97.35 (talk) 10:38, 11 December 2007 (UTC)

Parochial USA content makes this article confusing.

It would be useful for the reader (myself included) to seperate out the parochial USA content from the main theory and research. The USA specific information interupts the article and considerably lengthens passages. more consise information would be helpful with perhaps seperate sections for USA issues which are only specific to 1% of the global population. It would be great if someone with appropriate detailed knowledge could attempt to edit accordingly! HDTomlinson (talk) 03:38, 7 January 2008 (UTC)H.D.Tomlinson (UK)

Major changes needed

Hey Wikipedians. I just marked this article as {{cleanup-rewrite}} because, frankly, the quality of the article is terrible. This should probably be a task for WikiProject Pharmacology to take on with full force and extreme prejudice. Random bold and strike-out? Sentence fragments and run-ons? This is not how Wikipedia operates. I urge anyone who can work on this to do so, even if you can improve only one section. --Animated Cascade ^talk 06:20, 5 April 2008 (UTC)

suboxone and use during pregnancy

Suboxone is a pregnancy category C₁. Which means it should only be used with EXTREME caution during pregnancy.₂Basically this means that only if the benefits outweigh the risks on the mother and fetus. Suboxone use during pregnancy may cause the newborn to undergo withdrawal symptoms immediately after birth. The child may have to be weened off of the medication to prevent severe DT's and other side effects that come with the withdrawal symptoms. This may take weeks or months to completely rehabilitate the child.

references: 1. www.suboxone.com 2.clinical pharmacology edition 8 pg 7 dislpay 1.3 Lpn2008 (talk) —Preceding comment was added at 20:43, 16 July 2008 (UTC)

Recreational use

Buprenorphine is a popular recreational drug (typically used by opioid users) in Sweden. I would add something about this, but I'm having a hard time finding sources and articles that are not in swedish. It is also a popular recreational drug in the United States, as well, especially among users of heroin on the east coast. It is typically used in between "dry periods" when there is no heroin for sale in the area or city, so the users can stave away the withdrawals for a few days until they get their dope back. This is also a very common practice in New York, Chicago, California, and especially in Philadelphia. Philadelphia is notorious for patients who get Buprenorphine prescriptions and then proceed to sell them right afterwards for profit. 【 Mqa^Talk 】 15:24, 5 August 2008 (UTC)

That goes with any opiates. One study I recently came across showed there are half as many regular opiate users in the world as there are alcohol users. --78.86.159.199 (talk) 18:22, 16 August 2008 (UTC)

Actually, buprenorphine (typically in the form of subutex and suboxone) is very popular among opioid users in Sweden (and other scandinavian countries) - much more so than in other countries - which is why I think it would be interesting to write something about it. I will look for some research on this. 【 Mqa^Talk 】 16:08, 22 August 2008 (UTC)

May I suggest you use an electronic translators like Google and translate those articles in Swedish and then write your article. What you think? —Preceding unsigned comment added by 67.191.51.101 (talk) 15:14, 26 August 2008 (UTC)

That sounds lika a good idea, but the cited source will still have to be in swedish, and therefore hard to verify. I'll try to find something in swedish, and we'll see what I can do about it.【 Mqa^Talk 】 09:46, 27 August 2008 (UTC)

I added some information about buprenorphine abuse in Finland and Sweden.【 Mqa^Talk 】 10:56, 27 August 2008 (UTC)

Comparing the popularity of Buprenorphine over other opioids is the same as saying Vodka is more popular amongst the Russians than other alcoholic drins. Is it worth mentioning buprenorphine is used more recreationally than other opioids in Sweden? --78.86.159.199 (talk) 00:12, 1 September 2008 (UTC)

Article accuracy

Please forgive me for this unsusual approach. I am new to contributing to wikipidia and it is a whole other all gamae. I know this is not a forum. However, the reason I am addessing this issue in this way is simply this. Many of the post are accuate or have innaccurate details. I have looked at this page and hope it would conform to to feder quidlines. I ama physician no longer in practice who did early researh on the drug based upon he work of Kostin and Kleber in 1984 when at NDIA. I was certified by ASAM.For your interest, in addicitonto be being proven affective for opiod deto it was found effectivefor cocaine detox. However, he thought of placeingan opiod naive patiet on another drug wthich would habbituate him was deemed medically poor judement and was rejected by the original researcher.

NB: I AM NOT AT THIS TIME EDITING ANYTHING IN THIS ENTIR SUBJECT. The reasn is that while there is accurate writing in the entire article there are inaccurae things as well. Additionally,it is not focused and gets side tracked. Editing this would be a lot for me because I would have to return to original source, personal communications. That said I need the editor's advice on this subject. Do you want an exhaustive desciption, history, use,formulations, use in other coutnries, all indications includin detox, the history of how its use in detox was discovered, some detaiels of opiod addiction and he mechanism of thretment.

There are tons of articles on the entire subject which themselves are fairly coheren that do not cover all the topics here.

PLEASE BE CLEAR I AM NOT COMMENTING ON HE POST BELOW ME. I have nothing to single out about it at the moment. Just cheating on the forum aspects. I don't know why you don't have this sourcess and article need discuss.---- —Preceding unsigned comment added by Tetrasect (talk • contribs) 16:21, 3 November 2008 (UTC)

Conflicting statements about overdose reversal via naloxone

under the head Pharmacology and Pharmakinetics it says:

"Buprenorphine also has very high binding affinity for the μ receptor such that opioid receptor antagonists (e.g. naloxone) only partially reverse its effects."

and then under Adverse effects it says:

"Moreover, former doubts on the antagonisation of the respiratory effects by naloxone have been disproved: Buprenorphine effects can be antogonised with a continuous infusion of naloxone.[18]"

are these statements conflicting?Azrayl (talk) 01:04, 16 December 2008 (UTC)

Desperately needs a new intro

Specialists have rewritten this thing so many times the intro is nonsensical medicalese. We need a straightfoward, lawyman-friendly introduction. As written, this would only make sense to a specialist, and a specialist's first place to read up on it wouldn't be Wiki (I hope). —Preceding unsigned comment added by 208.226.153.24 (talk) 17:01, 3 September 2009 (UTC)

Well said. Needs new intro, but that concern, it seems to me, is secondary to wider concerns about the article as a whole. I have grave concerns about the article's content. Isn't the action and efficacy of this drug along with (for goodness sakes!) advice to readers about taking it or withdrawing from it best left to professionals at sites such as www.mayoclinic.com? It strikes me that the article and others like it are dangerous and place wikipedia in the highly inappropriate position of dispensing medical advice. 24.17.54.220 (talk) 17:54, 17 October 2009 (UTC)simonelf@hotmail.com

4 Alternate two-dimensional (2D) Buprenorphine images from one given.

Drawn differently from the wikipedia image but in the same 2D style:

a jpg • a gif • another jpg • a png (all different images, just naming them by image type even though not the same in different formats)

Someone might find these interesting. Regards, Nagelfar (talk) 13:50, 20 October 2009 (UTC)

Buprenorphine vs. Methadone

Please reduce the Buprenorphine vs. Methadone section. There is too much cross analysis and too little conclusiveness for it to be granted a paragraph under an article such as this. Either move the Buprenorphine vs. Methadone section into its own article, the article regarding opiate addiction or be prepared to leave a less analytical conclusion. --78.86.159.199 (talk) 18:22, 16 August 2008 (UTC)

With all due respect, I think the issue of Bupernorphine vs Methadone probably needs more information than it is given here. Heroin users do have a chice now on two different medications with different characteristics, assests and limitations. This is a extremly large issue for opiate users when it comes to treatment. At least it will required a special link or attention from this article. I personally do not have any problems with extensive cross analysis without conclutions. In some sciences when not enought research is available what we end up with is a lot of data and not enough conclutions until we beging to make some sense of the data.(Carlos.Franco) —Preceding unsigned comment added by 67.191.51.101 (talk) 15:22, 26 August 2008 (UTC)

You are forgetting, an encyclopedic article is not an study, essay or a place to keep comparing, analyzing different aspects of an issue or for first hand analysis. The Buprenorphine and Methadone section concludes little, but rather keeps cross comparing different issues in a rather essay styled and guide like writing. It needs cutting down heavily, with the raw facts, cited findings and conclusions only. If that writing was in the context of an study, essay, or a manual it would be totally fine, but not for an encyclopedia. It needs filtering. Also, don't forget, this is an article on Buprenorphine, not addiction or the best treatment for addiction. Mentioning that Buprenorphine, although an opioid painkiller is also used for the treatment of addictions and the reasons why it is and why it may be preferred over methadone is enough. Details on the best treatment (whether its buprenorphine, methadone, or other) for opioid addiction's are a topic of its own and have no place here. Perhaps you should open an article or add it to the article regarding opioid dependency treaments. Also remember, Wikipedia her is not a place to discuss the quality, validity of studies carried out, Wikipedia as with any other encyclopedia, needs to only mention the facts and significant findings associated with medically accepted studies, leaving any opinion based information in regards to any findings at the hand of the user. The section also drifts of to areas tottaly irrelevant to this article, such as the UK opiate prescription likelihoods, or details on detox programmes. Although I am a professional in the medical field, and most of the claimed points are arguably true, the writer, out of approximately 30 points made, only cites 5 of them with a valid source which is against Wikipedia guidelines. The section needs to be condensed with only relative information directly associated with Buprenorphine and its use for opioid addiction remaining written in a factual conclusive manner with valid sources to back the statemetns made. Rephrasings such as "in other words" or magazine/manual style explanations need to replaced with a more factual to the point phrases. Almost 1/3 of the information in the Dependence treatment section are irrelevant to the drug it self, Buprenorphine, and can find a better home in articles such as Opioid dependency, Drug addiction (treatment section) which need attention themselves. However, I personally feel the treatment of opioid addiction itself deserves a separate article, which a filtered version of the aforementioned section can find a good home.--78.86.159.199 (talk) 00:18, 1 September 2008 (UTC)

Also, most of it sounds like original research and/or totally made up bullshit. For instance, the part that states shooting up buprenorphine is easier than methadone. There isn't any reasons given besides methadone is a liquid. This actually makes it easy to shoot up methadone. They only add water when you dose methadone at the clinic. How was someone going to shoot up at the clinic anyways? Either way, that's just an example of the completely subjective rubbish that makes up this paragraph. Offense to anyone who wrote this, you are making Wikipedia rubbish. 173.24.227.245 (talk) 03:08, 10 April 2009 (UTC)

Methadone should be much more difficult to inject, for various reasons. Even though is is a concentrated liquid, a dose of even just 20 mg would be 20 ml which is quite a bit of liquid to inject. The solution itself is more a syrup. It contains dyes, flavoring and other additives that do not belong in the bodies' circulatory system. Adding water to it would make it less thick, but would result in a lot more liquid to inject as well. As for Buprenorphine versus methadone for the treatment of opioid withdrawal and addiction; this really depends on the drug(s) of abuse, severity and length of use. I have had this explained to me by a drug counselor. Buprenorphine is better suited to individuals who have perhaps been abusing prescription opioid drugs like hydrocodone (Vicodin, Lorcet, Lortab) or oxycodone at lower dosages (Percocet, Endocet, lower dosage OxyContin), perhaps even insufflation of small amounts of heroin and for a limited period of time. For instance, somebody who has been using less than or around 30 mg of oxycodone a day for less than six months and whose lifestyle has not yet been significantly disturbed (ie, they still hold a job, care for the family and have a strong support network). In scenarios such as that, outpatient treatment with buprenorphine in an office-based setting is typically sufficient at eliminating withdrawal, reducing cravings and getting the user on the road to recovery. In the case of the intravenous heroin user, who injects more than a few bags of heroin a day and has been doing so for over six months the need for treatment with methadone in an in-patient setting becomes greater. It may be more difficult for the heroin addict to abstain from using for the 24-36 hours required before buprenorphine can be administered. Methadone is also a full agonist, it is more sedating and capable of providing the addict with a greater sense of well being. For these reasons it may more sufficiently alleviate craving. Like buprenorphine it is also capable of blocking the effects of other opioids, but for methadone the blocking dose is attained more gradually. A person who is on methadone may switch to buprenorphine. In order to do this their dose of methadone must be 30 mg or less and they cannot dose for 48 hours. —Preceding unsigned comment added by 71.162.73.145 (talk) 18:12, 7 January 2010 (UTC)

Carfentanil, potency vs. binding affinity.

"Use in persons physically dependent on full-agonist opioids while not already in withdrawal will trigger an extremely intense form of opioid withdrawal, - called "precipitated withdrawal" or "precipitated withdrawal syndrome" - that cannot be reversed by high doses of any other opioid (except for the possibility carfentanil or dihydroetorphine, which are not licensed for use in humans and are active in the hundreds of nanogrammes)"

The relative potency of a chemical (by weight) has nothing to do with the binding affinity of the medication in question, and there's no reason to believe that even such potent opioids would reverse the precipitated withdrawal. Furthermore the statement isn't sourced at all. Considering it's under the label of "pharmacology" one would think the editor posting such nonsense would be aware of the fact that potency and binding affinity ARE NOT THE SAME THING.

Bupe has a notoriously high binding affinity. It binds to the opiate receptors more strongly than even naloxone, which, incidentally, is what Vets and scientists use to bring large animals out of the sedation caused by extremely potent opioids such as carfentanil. If naloxone will reverse carfentanil, yet bupe can't be displaced by naloxone, then it stands to reason that carfentanil cannot "fight through" the bupe, to put it in layman's terms.

IF potency were the only thing you needed, then a (much) larger dose of whatever opioid you're addicted to would relieve the symptoms, since full mu-agonists have no ceiling to their effects.

Having misleading, incorrect, and to be frank, possibly dangerous information in this article is shameful. If, indeed, precipitated withdrawal brought on by buprenorphine CAN be overcome with these medicines, then put it back in, and source it. Until then I suggest it be removed asap. I'll remove it myself in a few days if no one complains, or sources it. —Preceding unsigned comment added by 98.19.171.137 (talk) 17:22, 21 April 2010 (UTC)

Interesting point, let's see if I understand what you are saying. The Ligand_(biochemistry) article says: "High affinity ligand binding implies that a relatively low concentration of a ligand is adequate to maximally occupy a ligand binding site and trigger a physiological response. Low affinity binding implies that a relatively high concentration of a ligand is required before the binding site is maximally occupied and the maximum physiological response to the ligand is achieved."

Whilst Agonist says: "The potency of an agonist is inversely related to its EC₅₀ value. The EC₅₀ can be measured for a given agonist by determining the concentration of agonist needed to elicit half of the maximum biological response of the agonist. The EC₅₀ value is useful for comparing the potency of drugs with similar efficacies producing physiologically similar effects. The smaller the EC₅₀ value, the greater the potency of the agonist the lower the concentration of drug that is required to elicit the maximum biological response."

So the "biological/physiological response" and hence potency seems to be dependent on two variables - the binding affinity and the agonism of the ligand. Something like carfentanil might have a lower binding affinity than bupe but because it's a full agonist whereas bupe is a partial agonist, carfentanil would be more potent overall. Is this correct?

If you could point out a source that explains the relationship between the two, that would be useful. I might have a look in a biochem text at my uni library for an explanation and as a source. I think Wikipedia should clearly explain the relationship between binding affinity and potency because it's somewhat confusing to this lay(wo)man.

Additionally, it might be a useful statistic to include the binding affinity for the target protein in descriptions of various ligands. Factomancer (talk) 03:35, 22 April 2010 (UTC)

Ok, I found a useful source on Google Books that explains the relationship between drug potency, ligand efficacy and binding affinity -- [1]:

There are two main differences between binding and functional experiments. The tirst is that functional responses are usually highly amplified translations of receptor stimulus (see Chapter 2). Therefore, while binding signals emanate from complete receptor populations functional readouts often utilize only a small fraction of the receptor population in the preparation. This can lead to a greatly increased sensitivity to drugs that possess efficacy. No differences should be seen for antagonists. This amplification can be especially important for the detection of agonism since potency may be more a function of ligand efficacy than affinity. Thus, a highly efficacious agonist may produce detectable responses at 100 to l,000 times lower concentrations than those that produce measurable amounts of displacement of a tracer in binding studies. The complex interplay between affinity and eflicacy can be misleading in structure activity studies for agonists. For example. Figure 5.1 shows the lack of correlation of relative agonist potency for two dopamine receptor subtypes and the binding affinity on those receptor subtypes for a series of dopamine agonists. This data show, that for these molecules changes in chemical structure lead to changes in relative efficacy not reflected in the affinity measurement. The relevant activity is relative agonist potency. Therefore, the affinity data is misleading. In this case, a functional assay is the correct approach for optimization of these molecules.

<ref name="AffinityVsEfficacy">{{cite book |title=A pharmacology primer: theory, applications, and methods |first=Terrance P. |last=Kenakin |page=79 |pages=318 |publisher=[[Academic Press]] |year=2006 |month=November |isbn=978-0123705990 |language=English |url=http://books.google.com/books?id=d0phlW5cCmQC&lpg=PA79&dq=potency%20binding%20affinity%20agonist&lr&pg=PA79#v=onepage&q&f=false}}</ref>. Factomancer (talk) 06:34, 22 April 2010 (UTC)

Bioavailability: 31% (sublingual, from ethanolic solution)?

from what research I've done on Buprenorphine and bio availability this statement is infact wrong and i have seen this on the page for a long time now.I would like to see where this information came from. Im not a pharmacologist but my research says that buprenorphine sublingual ethanol solution actually increases the bio availability to 50-70%. where did the information about the low bio availability of ethanol mixed with buprenorphine come from? and same thing goes for the sublingual high dose tablet, I do not believe that the bio availability is 50-60%. infact a high dose tablet without ethanol is about 30-40%. I cant believe you would put this information out there without any facts or data. I was using those statistics for my own suboxone use and im sure other people are to. Do you realize how much buprenorphine is wasted without adding ethanol to the buprenorphine. Thanks for throwing my money down the toilet. I dont know how to remove bad and stupid data but the whole bio availability part should be removed until a source is show. I would love to help with the bio avail part myself. —Preceding unsigned comment added by Paulination (talk • contribs) 23:34, 2 June 2010 (UTC)

Translation?

I've just done a light copy edit. Does anyone understand this and, if so, could you please make it clearer?

Typically, the first day dosage is no more than 8 mg or it may precipitate withdrawals as antagonistic effects overwhelm agonistic effects, after which initial daily dose totals around 8–16 mg of either Suboxone or Subutex.

Does it mean daily dose after the first is around 8–16? Anthony (talk) 05:40, 13 August 2010 (UTC)

The article is so redundant that I'm not sure where that sentence is, or even if it is still in the article. My rough translation would be: On the first day of treating an opioid addict, the dose of buprenorphine is generally kept to at most 8 mg, due to the possibility that it will displace the last few molecules of the previous opioid used and thus precipitate withdrawal. In the next few days the usual dose is 8 mg-16 mg, but it may be increased or reduced over the next days or weeks as required.Rose bartram (talk) 16:35, 15 December 2010 (UTC)

"Withdrawal Danger ?"

To me this sounds like cases where doctors have overprescribed buprenorphine, and some one is taking upwards of 16mg a day, which is insane. I went from a huge heroin habit, to several hundred milligrams of oxycodone, and started on 4mg of subutex a day. Very few doctors even remotely understand this drug, yet somehow went through all the work to become licensed to prescribe it.

After Working with lots of folks who have taken or are still taking buprenorphine, and being an addict myself who takes buprenorphine. "extreme acute withdrawal" is not something I have EVER witnessed or felt-first hand with buprenorphine. www.heroin-detox.com is not a reference/citation. Unless there is a real source for this date, this should be removed. Azrayl (talk) 18:13, 1 July 2008 (UTC)

I think you make a great point, my hat goes off to you. I am both an addict and a professional in the field. Like you, although I have never had a huge habit of over seven bags (shity Miami dope before the Columbians came in the mid 90s), I have seen plenty of addicts both active (I tried doing an underground needless exchange while I was on methonde) and in recovery. I think there is a huge amount of data missing regarding buprenorphine.

I have "heard"(pretty reliable source,someone like me :), but not me) of one case of an extremely bad and long withdrawal from an IM bupernorphine (not Suboxen)addiction. I understood the guy got it from Spain a few decades ago. He was, intermuscular shoot huge (way over 16mg in the 100s) amount of bupernorphine per day and the doctor in USA who apparently knew very little about buprenorphine at that time attempted to withdraw the guy quicker than "prescribed". The same source told me that eventually this gentleman tried to IV the buprenorphine and suffere a stroke (I do not know if this is rare or a comman situation... I understand this gentleman still around but not doing well. But from what I understood from my source is that his withdrawl at that time was very bad.

Again, my hat goes off to you, for requesting and demanding data. I do not know whether we should be requesting that information should be removed... I suggest that a note should be placed, at the source and the location of your complain indicating your givance and to see the discussion. That way we should indicate the need for data and demand for research in that category. As "addicts" and consumers of this services, we should be "demanding"<for a lack of a better word" more relevant data and creationg of best practice protocols. Whose treatment is it any way? Good point yours.

Stroke caused by IV is pretty common amongst many IV users of all types of drugs. It's generally due to improper injection, needles, adulterants and other factors which in turn form a clot leading to stroke. Buprenorphine does not cause a stroke is used properly. --78.86.159.199 (talk) 00:04, 1 September 2008 (UTC)

Had exactly the same situation described on top of the section,no one needs 16 mg. a day or even 8,but that is what usualy prescribed. After 2 years of about 3-4 mg. a day of subutex I decided to stop taking it at once,was amazed to have almost no withdrawal,could function normaly and sleep. —Preceding unsigned comment added by 84.108.77.177 (talk) 09:52, 17 March 2011 (UTC)

Commercial preparations

It says no human studies have been done on the effectiveness of intravenous buprenorphine/naloxone preparations but in the manufacturer's prescribing information it talks about studies done with IM injections of buprenorphine/naloxone? I'll double check the insert, but I'm pretty sure it's all there.

Effect of Naloxone: "...whereas administered intramuscularly, combinations of buprenorphine with naloxone produced opioid antagonist actions similar to naloxone."

to print these results in an insert they would have to have observed these effects in humans, correct? Azrayl 02:09, 18 September 2007 (UTC)

I'm not sure I understand. Intravenous is not the same as intramuscular. --Galaxiaad 03:15, 18 September 2007 (UTC)

Oh I am sorry, I was reading intravenous as intramuscular, so the article is correct that there has not been (official) human studies observing intravenous bupe/naloxone preparations. Azrayl 17:25, 18 September 2007 (UTC)

There are several generics of the buprenorphine hydrochloride 0.3 mg/mL solution (Buprenex); I suggest mentioning these in this section. Off the top of my head I can think of generics marketed by Bedford Laboratories (in 1 mL vials) and Hospira (in cartridges for use with their Carpuject system, http://www.hospira.com/Products/carpujectsyringesystem.aspx). (Buprenex comes in 1 mL ampoules.) 174.111.242.35 (talk) 16:43, 21 March 2011 (UTC)

New to Suboxone

I have been struggling with Hydrocodone addiction for 20 years, spent 2 and 1/2 of those years in prison as a result of my addiction, and suffered most of the consequences other addicts experience...yet I still found myself wrapped up in the vicious cycle again after over 2 years of clean time. Just last week I finally got the nerve to confide in my doctor, parole officer, and family that I was back on the pills. I stopped the Hydrocodone at 2am last Sunday morning, saw my doctor on Monday morning and took my first dose of Suboxone right away. The 1/2 of the sublingual strip did little or nothing to help my withdrawls and I was given the other 1/2 45min. later. I felt immediate relief, even felt that familiar euphoric feeling...maybe stronger than hydro had given me in years. I told my doctor of this feeling and he was not concerned. I had to see him the following day for my second dose and again reminded him of the 'high' feeling I was experiencing. He was still not concerned and sent me home with a week's worth of Suboxone (1 8mg-2mg strip/day). I remember very little of those first 4 days and barely was able to function, even slurred my words and was clumsy. I decided yesterday to not take any at all and did just fine...no withdrawls, no cravings. My doctor is now insisting I take at least 1/2 strip per day until I see him next week, but I really have no desire to continue. Why take something that makes me feel 'higher' than the drug I am attempting to stay away from? It seems ludicrious!!!! —Preceding unsigned comment added by 97.87.179.5 (talk) 10:49, 23 April 2011 (UTC)

Street Reports

I've got a street report that the president was kidnapped by aliens. Should we include that in Wikipedia too? Please remove this. Not only is it completely without source, a "street report" wouldn't be a reliable source anyways. Thanks.12.207.120.160 (talk) 09:50, 18 August 2008 (UTC)

I don't know if or how recently this was added, but there are citations given to publications in professional journals. Probably the researchers interviewed street users and this is the source of the "street reports." 174.111.242.35 (talk) 11:20, 18 June 2011 (UTC)

something's wacky here, needs to be fixed

from the "dependence treatment" section:

"In the United States, a special federal waiver is required to prescribe Subutex and Suboxone for opioid addiction treatment on an outpatient basis. However, if the doctor meets none of the other clarifications, an 8-hour course is all that is required)."

"clarifications?" huh?

This is poorly stated - Subutex and Suboxone are both ONLY prescribed for opioid addiction, for which a dr. must have a DATA2000 waiver this would also allow them to prescribe methadone. However, unlike methadone, an additional 8-hour course is required before being approved to prescribe Suboxone/Subutex.

TIP-40 is a publication detailing Suboxone/Subutex use, clinical guidelines, and legal specifics. A copy should be linked to. I'll see about adding that.

This is actually incorrect. As a patient of back surgery I have been put on Subutex for back pain. It works incredibly well. Aftre being on the pure agonists I find Subutex to be an excellent pain killer. My pain mgmt. doctor uses his regular DEA # to prescribe this for me. He said that his DEA # begins with a Z, may be an X but i think a Z, when he prescribes for opiate dependency. He uses his normal DEA # for regular pain mgmt. when scripting for subutex. —Preceding unsigned comment added by 68.84.119.213 (talk) 18:16, 15 May 2008 (UTC) 66.41.0.174 (talk) 20:30, 28 November 2007 (UTC)

I can also confirm that this is incorrect, while I receive subutex for opioid addiction, my doctor prescribes it off-label to some of her patients for pain. Temgesic is available for pain in Canada and other places in the world but not here in the USA for some reason. Because Suboxone and Subutex are the only available buprenorphine medications available in the USA, we now have doctors prescribing high-dose buprenorphine treatment for pain rather than low-dose treatment which is more effective. My own personal opinion is that low-dose buprenorphine works better in general whether it be for opioid addiction maintenance or pain management.Azrayl (talk) 23:56, 15 December 2008 (UTC)

Suboxone and subutex are not the only available buprenorphine medications in the USA. For one, there is the IM/IV solution (Buprenex and several generics). More recently, the transdermal patch, Butrans, has been approved (for pain, so it comes in appropriate doses). Also, as I noted somewhere else on the talk page, a compounding pharmacist can make a customized dose form that would basically be the same thing as Temgesic. Veterinarians frequently use bupe, particularly for cats which are apparently sensitive to other opioids but tolerate bupe; because their patients require doses (usually) lower than the human dose, they often employ compounding pharmacists.

174.111.242.35 (talk) 20:04, 18 June 2011 (UTC)

 I also receive Subutex for the treatment of pain. My dr did have to go for special certification to be able to prescribe this. I take 2 (2mg) sublingual tabs 4 times a day. I see him once a month but he has given me 1 refill at times if he was not able to see me before my month's supply would run out. He does also use it for opoid addiction but that is not the only thing he uses it for.  —Preceding unsigned comment added by SettleDownKim (talk • contribs) 16:53, 31 March 2009 (UTC) 

Source of Buprenorphine

The introduction to the article states "Buprenorphine is a synthetic Bentley compound derived from an alkaloid of the plant Papaver somniferum (the opium poppy), known as thebaine." The linked article, Thebaine, says that while it is "[a] minor constituent of opium" thebaine is extracted for commercial use from Papaver bracteatum (the Iranian poppy).

Johhtfd (talk) 15:37, 20 July 2011 (UTC)

New Generic Formulation of Subutex?

Recently returned from pharmacy, only to find that my generic buprenorphine (Subutex) pills had shrunk! They are the 8mg version, produced by a company I'm not familiar with, "HI-TECH." I am about to look into the company, since I've NEVER heard of them...and I've heard of lots of pharm manufacturers before. I had never heard about a version made by them either. Is it possible they removed the binders completely? Because they are SMALL. I'm trying to think of a good comparison...maybe the size of a generic Klonopin? The pink, slightly rounded ones. Possibly a bit smaller. It seems that whatever the case, either less binders or whatever else it could be, that it assists in letting more of the medication get absorbed through the prescribed sublingual method. This seems experientially to be because less pill causes less saliva buildup, making it less likely more of the medication gets swallowed (where even less of it gets absorbed). Just wanted to put this out these and see if anyone has any experience with them, or has seen them (or the manufacturer) before. 70.44.100.103 (talk) 22:38, 27 August 2011 (UTC)

Removed section

I have removed the following text from the article because it doesn't have enough context for the reader to understand it (suboxone films are not even defined, for example), and it is vague, poorly written and not well supported by the reference. If anyone wants to fix it up and put it back, please feel free. -- Ed (Edgar181) 14:40, 9 March 2011 (UTC)

Starting in January 2011, Many Vermonters (on Suboxone) have been forced to switch to Suboxone Films (so Suboxone users can't crush up the pills and snort them). Medicaid stated that they will be no longer paying for the Suboxone pills. Drug treatment clinics have claimed that the Suboxone Films are more potent and take less time to work, but users of the Suboxone Films have mixed opinions http://subotex.com/suboxone_film-v-s-suboxone-tablets/. In many cases, anyone prescribed more than 16 MG (more than 28 mg pills) was brought down to 16 mg of the Suboxone Films.

Yeah, when I read that excerpt, I thought the entire population of Vermont was doped up and forced to watch pro-Suboxone propaganda movies. I wondered if Vermont had turned into 1984 and Brave New World simultaneously. 76.115.63.153 (talk) 01:52, 18 February 2012 (UTC)

Suboxone Flavor

clip::

SUBOXONE is an uncoated hexagonal orange tablet intended for sublingual administration. It is available in two dosage strengths, 2mg buprenorphine with 0.5mg naloxone, and 8mg buprenorphine with 2mg naloxone free bases. Each tablet also contains lactose, mannitol, cornstarch, povidone K30, citric acid, sodium citrate, FD&C Yellow No.6 color, magnesium stearate, and the tablets also contain Acesulfame K sweetener and a lemon / lime flavor.

From
http://www.rxlist.com/cgi/generic/suboxone.htm67.189.252.63 18:06, 2 October 2007 (UTC)Kyle Mackey

it's the most god awful lemon lime i've ever tasted. the taste of it makes me want to puke more than the opiate content. 65.210.123.70 (talk) 21:08, 6 June 2008 (UTC)

HAHAHHAH... ok im not laughing at you, im laughing with you, im got some in my mouth right now.

• • • Kyle that "god awful" taste making you want to "puke" is the naloxone, it is orally active and there is a population that react to it strongly. you may only have a slight response enough to mean that you cave in to the pressure to force people to take suboxone when subutex would give them a far superior control and stability of neg opioid symptoms.

my experience, is that use of opioids shut down your endogenous endorphine production and people who still retain endorphin production (not considering up/down regulation of receptors) ((not most by any means) individuals (perhaps over 10%)) have a strong aversive reaction to the naloxone orally or otherwise!! this is the truth no matter how many times 'addiction experts' and the shillitary assert that it doesnot cause any problems orally ! bs. to these i say, ive been given the chance to trial suboxone in a formulation that was designed to appear to be bupe, as part of the original trials showing it was equivalent. here in australia i have participated in two such trials years apart with suboxone designed to look like subutex and with the newer strips which are suboxone only!, both times i observed that the conductors of the study completely unethically used discretion to invalidate people that had a bad reaction to subOXONE due to the nalOXONE, which only a cruel and sadistic or completely ignorant bastard would give to people with opioid dependancy. I had severely disrupted sleep for a month which did not stabilise (on one occasion i was sick with pneumonia in hospital and could not be given any analgesic because of the buprenorphine blockade yet the naloxone made my pain and suffering significantly worse, i took it completely correctly and did not misuse anything anywhere around the duration (not within months), i also transitioned from real pure bupe to the sadistic shite suboxone which is purely about power and control, it does not stop diversion anyway. this may seem contradictory but what i am saying, but read carefully; it causes a mild to strong aversive reaction in me and others no matter how it is taken, people can belt it up and it is so-so, aleviates serious withdrawal but replaces it with a naloxone sickness. i know because ive spoken to many people that would still use suboxone iv if that was all they could access and they were withdrawing badly, it doesnot cause precipitated withdrawal (in years ive only seen that once, although it looked quite unpleasant the person has to literally still have heroin in their system, ie has taken the two within hours to get precipitated withdrawal and this one case happened with just buprenorphine too, so in that case it was not due to naloxone anyway because it was not present!!!!ffs).

(the pituitary gland where beta-endorphine is produced always together with ACTH as a cleavage product of POMC, requires cysteine and excess glutamate (which the "opioid inactive" enantomer affects, which is why methadone has a worse withdrawal than just about any other opioid because it is half a glutamatergic drug (in germany they use only the single therapeutic enantomer but everywhere else is no regulation and methadone could easily be adulterated with a higher than 50% amount of the inactive enantomer which would account for experience that some formulations, or dispensations, of methadone have widely different potency and quality).

causes cysteine depletion and strongly contributes to the endogenous endorphine shutdown) This page is full of inaccurate information and unfortunately there is no consensus with many incorrect and biased claims pushed even by the so called authorities including manufacturers and other bodies with an interest in the Freshly Patented suboxone which justifies $10+ a day dosing here in australia for something that costs cents. of course the patents on buprenorphine have elapsed but there is just too much money to be made for the truth to stand up to.

the strategy is to transition to only dispensing the strips using automated retinal scanning machines, this way it will not be possible to get subutex prescribed and their long term income will be guaranteed. of course if you are PREGENANT subOXONE cannot be taken which pretty much blows the claim that the naloxone is not orally obsorbed out of the water. in fact around 10% absorbs so on 32mg of bupe a day that means 8mg of naloxone and so approx 0.8mg of naloxone into the brain, which explains the experience of naloxone effects YES EVEN WHEN TAKEN ORALLY! — Preceding unsigned comment added by 220.101.100.14 (talk) 14:13, 26 April 2012 (UTC)

In the UK Suboxone has the flavour of oranges, and is more unpleasant than the 'neutral' though bitter taste of Subutex. — Preceding unsigned comment added by 86.181.36.210 (talk) 09:29, 22 April 2012 (UTC)

Lots and lots of changes made

Hello everyone....

Came across this page tonight and found it riddled with errors of all sorts, including that NA hadn't made a statement regarding maintenance therapy and that buprenorphine is PREFERABLE over methadone during pregnancy!!! (Which I'm going to guess anyone reading this knows is totally not true.)

I added and changed A LOT, and I will be adding in the remaining associated links, etc., for the information I changed/added.

--Lisamarie (talk) 07:35, 26 January 2008 (UTC)

Are you sure you dont mean simply that there is more experience with methadone during pregnancy, i personally disagree, i think methadone is wreaking havok on the unborn childs neural development, buprenorphine may well be safer in this regard, but lets do a literature survey. thx — Preceding unsigned comment added by 220.101.100.14 (talk) 14:33, 26 April 2012 (UTC)

Use for pain relief?

This article doesn't mention much about the use of this drug for pain relief, even though as it says it is much more potent by weight than morphine. I found some discussion of this here [2] and it does sound like there is some use of the drug. I am perplexed, because given the level of prescription drug addiction, I would think that it would make sense to use an anti-addictive medication as the first-line opiate for relief of moderate pain. What is the problem with it? Wnt (talk) 01:36, 27 October 2008 (UTC)

Good question! Subutex (Suboxone is inappropriate in this case) is being used off-label for pain management. It's hard to say exactly why it is not FDA approved for pain management in the USA but I will explain some of the drawbacks to buprenorphine treatment for chronic pain. They should really have a low-dose formulation like Temgesic on the market here in the states. However do not confuse yourself. While buprenorphine is used for opioid addiction treatment, it is not non-addictive and dependence and (to a lesser degree) tolerance is to be expected if put on a daily dose of it. An argument could be made that it is less addictive and habit-forming than full agonists, when used to treat pain. There are a few hurdles with that however which include the dosage ceiling (32mg) and the fact that at a certain point it starts to become more of an antagonist than an agonist so you can't simply take more if you are already at a high dose (I've been told the metabolite norbuprenorphine is a full agonist below 2mg and higher than that it starts to become an antagonist, but I have no source for this). The other problem is the blockade effect it creates so you cannot have a fast-acting medication to take for break-through pain. In my experience with drug it works much better in doses below 2mg, yet I cannot find any studies that indicate this besides my own personal experience.Azrayl (talk) 01:16, 16 December 2008 (UTC)

SL or IM/IV buprenorphine can be used for management breakthrough pain. It is fairly fast-acting. One problem with using this drug long term is that if you have a medical emergency requiring a stronger analgesic (e.g., severe burns), it takes a very high dose to "break through" the antagonist effect of the buprenorphine. An illustrative case: a patient who had been on buprenorphine discontinued it 36 hours before scheduled surgery. During the surgery, she was given fentanyl to prevent postop pain. When she awoke, it was apparent that the fentanyl had not been adequate, as the first thing she did was scream bloody murder. After three more doses of fentanyl, the pain finally began to recede.

My experience in treating pain with buprenorphine has been that surprisingly little tolerance develops even with long-term use. I should note that it is not a suitable treatment for severe pain, whether chronic or acute. For outpatients, a compounding pharmacist can produce custom dosage forms similar to Temgesic so that patients are not limited by the lack of a lower-dose commercial product.

Azrayl: when you say "In my experience with drug it works much better in doses below 2mg," which formulation are you talking about, and do you mean 2mg/day or 2mg in each dose?

174.111.242.35 (talk) 11:17, 18 June 2011 (UTC)

I seem to recall reading somewhere that the equivalent IM dose is supposedly 1/2 the SL dose, so (assuming this is correct) 0.3 mg (= 1 mL) of IM soln (Buprenex) would be equivalent to 0.6 mg SL tablet (Temgesic). Don't think I've ever seen any dosing recommendations for IV use.

BTW, Buprenex (R) is FDA-approved for pain in the US, as are several generics. Probably the reason Temgesic isn't available in the States is simply because no pharmaceutical company feels it would be sufficiently profitable to be worth jumping through all the hoops required to get it approved. Mia229 (talk) 15:13, 8 March 2012 (UTC)

Update...I'm getting contradictory information from different sources. I asked a hospital pharmacist about it, and after looking into it (presumably consulting *his* sources :) ) he told me that the equivalent SL dose of buprenorphine should be 3x the IM dose. On the other hand, my old pharmacology textbook (Goodman & Gilman, 9th ed. - the 12th ed. (2010) is current, so this is definitely outdated, but still usually accurate, when the information is there: while newer drugs and more recent findings and that sort of thing are of course not going to be in there, I've never found anything in there that actually turned out to be *wrong*...until, possibly, now) says that 0.4mg buprenorphine IM or 0.8mg SL is equianalgesic with 10mg of IM morphine (this must be the "somewhere" I mentioned in my previous comment, where I vaguely recalled reading that the SL dose should be 2x the IM). (Note that all this applies only to single doses, not necessarily total daily dose.) Does anybody know which of these is right — or if they're both wrong, does anyone know what the correct data are? (Or am I perhaps misinterpreting the data, somehow? It's true that it's been a while, but I can't think of any reason this wouldn't be perfectly straightforward; still, I'm not willing to rule out the possibility.) Mia229 (talk) 06:33, 27 June 2012 (UTC)

Metabolism

I think we need to have section about Buprenorphine's metabolism, both in-vivo and in-vitro. It is not sufficient to say that buprenorphine's metabolite is nor-bupe, although the pharmaco-dynamics of OH-bupe and OH-nor-bupe haven't been elucidated. Here is a study on the in-vitro metabolism: http://dmd.aspetjournals.org/cgi/content/full/33/5/689

If someone wants to get this started, I'll collect the references for you. A lot of the data I find is very contradicting with other data from trials. There are studies indicating in-vitro buprenorphine and nor-buprenorphine are both also CYP 3A4 and 2D6 (??) inhibitors. Aj1976 (talk) 02:24, 1 December 2008 (UTC)

I don't remember what the second isoenzyme is, but it's not 2D6, I'm pretty sure of that. Mia229 (talk) 06:50, 27 June 2012 (UTC)

Patent status

Does anyone have a source pointing to the patent status of this drug? —Preceding unsigned comment added by 24.206.182.80 (talk) 02:06, 21 July 2009 (UTC)

This sort of thing is regulated differently in different countries, but in the US, at least, new formulations of a drug are patented separately. The patents have expired on the IM/IV solution (Buprenex), and, more recently, the SL tablets (Subutex). I'm not sure about Suboxone. I'm pretty sure that the patents for all the other formulations have not expired. Mia229 (talk) 07:18, 27 June 2012 (UTC)

buprenorphine as antidepressant - legality [section 2.3.1]

Use of buprenorphine or other opioids to treat depression is not a legal "grey area." At least in the US, off-label prescription is legal. Quite simple, no "grey area" whatsoever. Now, whether physicians are willing to do it is another matter, but there is nothing illegal about it. 174.111.242.35 (talk) 08:48, 19 June 2011 (UTC)

This is correct. I don't have any information about what the law is in other countries, but in the States there is no legal "grey area" regarding the prescribing of a drug off-label (that is, for a purpose other than the one for which the drug is marketed, for which it was officially approved by the FDA). American physicians, however, often tend to be fearful of the DEA, which has been known to use its powers to go after them for doing things, based upon their own professional judgment, that are technically legal but may "look suspicious" (or whatever) — e.g., prescribing "too much" pain medication. (I'm not sure how justified such fears really are, but it certainly is true that getting one's DEA license revoked is a career disaster for a physician in the States.)

Suboxone, but not Subutex, is an exception: while Subutex can be and frequently is prescribed off-label for pain (and less frequently, for mood disorders), US law permits Suboxone to be prescribed only for substance dependence. Mia229 (talk) 17:49, 26 June 2012 (UTC)

I went ahead and got rid of the "legal grey zone" claim; it was at best misleading, if not downright false, and the references given had nothing to do with the claim (they're about overly-aggressive drug enforcement agents going after doctors for prescribing opioids). I didn't want to try removing the references themselves (40 and 41) from the list, as I've never tried mucking about with a Wikipedia reference list and don't want to end up creating new problems with the page. (You know — first, do no harm. :) )

On an unrelated note...what does the bit about morphine for OST have to do with buprenorphine as an antidepressant??? Shouldn't that be under "off-label uses?" Or is it actually approved for that under whatever systems the countries in question use? Mia229 (talk) 11:17, 30 June 2012 (UTC)

Added more in-depth history....WITH REFERENCES!

I added a more in-depth explanation of how buprenorphine came to be. It's the first paragraph in the history section. It looks horribly juxtaposed once the second paragraph comes in with its lack of references and incorrect information. I'd do more to fix it myself but I just don't have the time. My two references contain an amazingly detailed account of the history of buprenorphine. If somebody wants to pickup the history after 1982 and how it came to be in the US, these two links will help: http://onlinelibrary.wiley.com/doi/10.1111/j.1749-6632.2011.06352.x/full#ss4 http://rzbl04.biblio.etc.tu-bs.de:8080/docportal/servlets/MCRFileNodeServlet/DocPortal_derivate_00001868/NIDA179.pdf (around page 17, John Lewis' In Search of the Holy Grail)

Tunafizzle (talk) 20:37, 5 August 2012 (UTC)

Opioid dependence section

This section needs a lot of work and sources. It is written from a mainly U.S POV and includes information that is best covered in other articles. It's also long winded and I'm sure it could be largely edited while retaining the core information. I've done some work but it needs more. Coinmanj (talk) 01:06, 21 August 2012 (UTC)

The thriving black market for suboxone speaks volumes about how hard life can be for addicts in this country

• Doctors and dealers battle for addicts salon.com Aug 22, 2012. Nemissimo (talk) 17:33, 22 August 2012 (UTC)

Contraindications

The only reference for this section is a dead link. There are also some claims which seen dubious to me, particularly the equivalence of 2 mg buprenorphine with 80 mg morphine. That doesn't sound right. The whole paragraph needs a reference and some of it may have to be removed.Rose bartram (talk) 16:35, 15 December 2010 (UTC)

It doesn't mention what route of administration it's referring to. Comparing IM/IV, SL, or transdermal buprenorphine to oral morphine would be sort of like comparing apples and oranges. I have read that 0.3 mg buprenorphine is approximately equivalent to 15 mg morphine (IV or IM). I'll see if I can find a source; I'm sure Goodman & Gilman has something to say about this.

On a related note, I would like to see a an equivalence chart for the various formulations of bupe, comparing total daily dose of the solution, the SL tablets, and the patch.

174.111.242.35 (talk) 18:01, 18 June 2011 (UTC)

Wow, this link's been dead since 2010? There's no question 2mg of Suboxone is on a whole different level than 80mg of morphine. And if it's buprenorphine without naloxone a naive person could easily use this wrong information to overdose. I just marked it dead, I think I'll just delete this sentence and link to Opioid_comparison. I think that's the more responsible thing to do, especially considering how long this link's been dead -- I can't believe it's stayed up for so long. Pfoot (talk) 19:58, 6 September 2012 (UTC)

sigh Created the link -- the unsourced info there (Opioid comparison) supports this same equivalency previously posted here... I'll search for more reliable data Pfoot (talk) 20:13, 6 September 2012 (UTC)

2xsigh Okay after some searching it seems that some sites have similar equivelencies set; I've also read it's practically impossible to make a reliable comparison between Suboxone and other opiates/opioids because of its particular method of operation. To my mind it surely depends if the person is using buprenorphine for opiate withdrawal maintenance, or using it to get high, otherwise not having a tolerance to opiates.

Early in this article it's written that buprenorphine is used to "control moderate acute pain in non-opioid-tolerant individuals in lower dosages (~200 µg)". Perhaps direct conversions should be avoided when it comes to buprenorphine -- replaced maybe by these general types of dosages for Suboxone's respective uses -- legal or otherwise. Far better than to have some naive person use this info to get high and possibly overdose -- just my take. Pfoot (talk) 20:45, 6 September 2012 (UTC)

ASAM

ASAM -American Society of Addiction Medicine does NOT have a low status. These physicians are in need and they pay them extremely well, given their rarity and need. That was clearly a personal opinion considering ASAM specialists to be in low regard. — Preceding unsigned comment added by 152.130.6.194 (talk) 08:12, 25 December 2012 (UTC)

Suboxone Withdrawal

I agree with everyone about suboxone withdrawal, although perhaps more vehemently - I personally went through it. There isn't a lot of substantiation on this from traditional sources -- most of what's on the Web comes from message boards. although there is an entry on Livestrong. (I'm naturally suspicious, but the manufacturer may have something to do with this.) The withdrawal varies in severity, but it exists, and for this article to be complete, it needs to address it. JSFarman (talk) 23:52, 11 March 2013 (UTC)

After reading the article, I thought it would be helpful if there were more information about withdrawal from Suboxone. There is currecntly a lot of discussion by users in various online communities regarding the claims that withdrawal from Suboxone is milder as reported by both the manufacturer and literature (that is, milder than the opioid one was dependent on before Suboxone treatment. While withdrawal symptoms are subjective, some users' experiences of Suboxone withdrawal are not consistent with the word "milder" and it would be nice to see some new research here or at least a mention of the problem. —The preceding unsigned comment was added by 72.200.68.198 (talk) 09:52, 18 March 2007 (UTC).

I fully agree. The subjective reports vary so wildly for buprenorphine withdrawal. I think the word "milder" is not the right word to use. It might be mild for a percentage of people coming off, but a lot of the cases I've seen indicate that the withdrawals can be really bad. Aj1976 (talk) 02:28, 1 December 2008 (UTC)

Without question there is a lot of misinformation about this subject floating around and perhaps that should be a focus within this subtopic here. Having experienced Suboxone withdrawals personally on a few occasions, I can tell you it is an opiate/opioid withdrawal, the severity of which depends mostly on how much the user has been taking and for how long. One thing prescribers and manufacturers like to avoid is the length of the withdrawal period. This drug has an extremely long half-life which results in a long, drawn out withdrawal period (e.g. three weeks as opposed to the 36 - 72 hours for dilaudid, on average). As any addict will tell you, withdrawal is withdrawal and it is terrible no matter how "mild" so the duration of a full-on, get it on, suboxone DT is beyond what almost anyone can withstand. Which fully explains the recidivism rate for long term maintenance patients who have had their regimens discontinued.

I think what people mean when they say it's "milder" is that the symptoms are somewhat less intense. I've had the special privilege of experiencing withdrawal from many different opioids, and while it's hard to say that any one is "worse" than another, I do have to say that I found some more intolerable than others, if that concept makes any sense. It's universally hellish, but some of it gets to you a lot faster than others. For example, I find withdrawal from high-dose oxycodone much less scary than withdrawal from high-dose morphine, because in my experience, at least, the symptoms get nasty MUCH faster with morphine. If I am currently taking oxycodone and I oversleep my dose time by two or three hours, let's say, I usually wake up with akathisia, yawning, watery eyes, and the like. I will be very uncomfortable, but I will also know that I have time to ingest my medicine and feel better before things get REALLY bad. However, with morphine, my first sign that something is wrong may well be nausea and vomiting. I can go from feeling perfectly fine one moment to full-blown puking, heat waves, and all the worst parts of withdrawal the next. And once it gets that bad it's nearly impossible to get medicine into my system to make it stop. Also, oxycodone withdrawal is definitely torturous, but I managed to make it through four days of it once relatively sane and self-controlled, if miserable, whereas I can't take 24 hours of morphine withdrawal without totally losing my mind and becoming psychotic. Granted a lot of this is because of personal pathology, but the point is that something is chemically different between the two drugs to a significant enough degree to cause radically different withdrawal profiles in an individual. So in my personal experience, I could reasonably say that high-dose oxycodone withdrawal is "milder" than high-dose morphine withdrawal. Again, both are miserable, hellish experiences, but I can definitely identify things about one that are more tolerable than the other. I hope this helps elucidate what people likely mean when they describe any sort of opiate withdrawal as being "milder" than another sort. It likely means in terms of what that individual can tolerate without feeling as if they're going insane. It's one thing to be suffering, but to be in yourself and to know the suffering won't last forever. It's another thing to completely lose it and think you're dying of radiation poisoning and hearing mechanical spiders crawling on the ceiling. 75.18.179.81 (talk) 14:28, 31 August 2012 (UTC)

shortage of parenteral buprenorphine 0.3mg/mL soln followed by massive cost increase

Recently a lengthy shortage of buprenorphine injectable, during which it was impossible to get it (at least for retail pharmacists – if any was available, hospitals got first dibs), ended after lasting a very long time. I had been getting it from a compounding pharmacist. Although the patent has been expired for some time, and prior to the shortage, there were several generics available in the US, now the only brand you can get at a retail pharmacy is Reckitt Benckiser's Buprenex, the original brand-name product. Before the patent expired, the retail price of Buprenex was about $300-400/month; now, it's about $1000 for the same quantity. Can anyone tell me:

- What is the cause of this "shortage" in the first place? (The closest thing to an answer that I've been able to get, even from people who should have at least some idea what's going on, is that in "many" cases, it had to do with problems getting the raw matter. This, of course, cannot be the cause in this case, since Subutex/Suboxone and other formulations were available, and of course my pharmacist had no problem getting the raw materials to compound it.)

- Why have there been so many drug shortages in the US lately (and, AFAIK, no more shortages than usual in other countries)?

- Why is only Buprenex available now, and how can they get away with charging so much for it? (This is a lot more even than it costs to get it compounded.) I mean, inflation (and greed) is always a problem, but it hasn't been *that* bad, has it?

TIA to anyone who can help answer my questions. Mia229 (talk) 20:48, 4 January 2013 (UTC)

At the top of this page, it should say, "This is not a forum for general discussion of the article's subject." But since it doesn't, I'm telling you now. Wikipedia is not a forum. This is not a place for getting your questions answered. This is a place to talk about the article. While I'm sure there are plenty of nice people here that will gladly answer your question (I would have if I knew the answer), if it has no direct relevance to editing the article, I'm afraid this is technically against policy. Charles35 (talk) 02:50, 5 January 2013 (UTC)

You are right of course; my apologies. I did not intend solely to use this page as a forum, although looking back I realise that any reasonable person would probably see it that way. I thought that the shortage (and its causes) might be something that would be appropriate to cover either in this article or in some other Wikipedia article. Of course, I was motivated in part by my own interest in the subject, but also by the knowledge that I am far from the only person affected by this. Given how long the drug shortage (which has been a major problem in the USA; I don't know about the rest of the world) has been going on, that this information is something we ought to try to include in the appropriate article, whichever that turns out to be (which may depend on the cause of the shortage). Mia229 (talk) 11:11, 8 October 2013 (UTC)

Buprenorphine page should be separate from Suboxone page

I know that things like hydrocodone and vicodin are not generally given separate pages, being that they differ in one active ingredient. But they both server the same purpose - pain relief.

Also, Suboxone is buprenorphine and naloxone at a ratio of 4:1. Suboxone is actually two drugs in one. — Preceding unsigned comment added by 108.176.105.38 (talk) 09:00, 15 October 2013 (UTC)

In the case of Suboxone, its use is different than the use of either of its components alone. It is used for opioid addiction treatment, not pain relief. I think separate articles would go a long way in making this information more accessible. Especially given the general dislike the 12-step proponents seem to have of this drug, and lack of neutrality the article tends to display. (on and off as differing camps edit the article back and forth.)

66.41.0.174 (talk) 20:38, 28 November 2007 (UTC)

                    QUESTION=HOW LONG IS BUPRENORPHINE IN YOUR SYSTEM?  —Preceding unsigned comment added by 71.234.226.18 

(talk) 05:18, 27 January 2008 (UTC)

Look at the article, it has a mean half-life of 37 hours, so expect it to be in your system for at least 72 hours.

Suboxone does not need a seperate article. Subutex, Suboxone, Temgesic and any other brand seeking to use Buprenorphine as its active ingredient seeks right to be listed under this article. This article focuses on Buprenorphine which entails any drug using Buprenorphine as an ingredient, now and in the future. There are 100's of different morphine preparations, it would be stupid to open an article for each one. However, I do agree this article needs pay less emphasis on the different brands such as Subutex and Subuxone. --78.86.159.199 (talk) 18:14, 16 August 2008 (UTC)

If anything, Suboxone would have its own article, I would think. Being the "unique" formulation including buprenorphine on the market, it seems the most likely to warrant "special attention" 70.44.100.103 (talk) 22:38, 27 August 2011 (UTC)

Speaking of differing camps editing the page, the segment before last, "Ending treatment of Suboxone/Subutex," is incredibly biased and makes reference to the fact that addiction is comprised of "especially spiritual" aspects of one's personality. This is ridiculous, subjective, and should be removed. The entire section about ending treatment is worded as though from a single person's perspective and is all conjecture and totally subjective. Should be removed. 72.188.184.3 (talk) 19:26, 12 December 2010 (UTC)

when can a talk page be cleaned up

the article has been tidied up a good bit, how about this talk page? — Preceding unsigned comment added by Tunafizzle (talk • contribs) 04:27, 3 July 2014 (UTC)

Miszabot is the way to go, it will archive old discussions. I'll take a crack at installing it. Anastrophe (talk) 05:38, 3 July 2014 (UTC)

Meh, it didn't work, at least not fully, because a manual archiving was done once previously. Investigating. Anastrophe (talk) 05:50, 3 July 2014 (UTC)

Close enough I think. Hopefully miszabot will figure it out when it runs, and I can delete the link to the very old archives. Anastrophe (talk) 06:05, 3 July 2014 (UTC)

Looks much much better, thanks.Tunafizzle (talk) 01:20, 24 July 2014 (UTC)

Biased argument on binding affinity and marking

This section seems to be written in a hostile tone and seems to try to force an opinion on the topic rather than just presenting facts. It should be rewritten or deleted. — Preceding unsigned comment added by 130.132.173.197 (talk) 20:15, 30 September 2014 (UTC)

MOR agonist with DOR antagonism

How common is this among opioids? Even Bupe's active metabolite Nor-bupe doesn't have this (straight across full agonism). For example thiobromadol is a mu-agonist that is equally potent as a delta-antagonist. Is buprenorphine notable as being in a similarly exclusive category with that drug as an unusual case worth mentioning? Nagelfar (talk) 22:25, 30 September 2015 (UTC)

Conflicting affinity information?

I don't understand these things that well so maybe I just don't get it but in the section Suboxone and naloxone theres a phrase "Published data clearly shows the Ki or binding affinity of buprenorphine is higher (0.2157 nM) than naloxones (1.1518 nM)." Cited source seems to deal with MOR affinities. Later in the articles Pharmacodynamics section the Ki value for MOR is 1.5 nM. Is there a conflict or am I missing something.--Custoo (talk) 12:42, 15 October 2014 (UTC)

I added Contradiction-inline templates to draw more attention to this question.--Custoo (talk) 00:31, 4 November 2014 (UTC)

i'm confused by this, too. on the page, it states that the Ki (affinity for receptor) rating for the mu receptor to be ~1.5, but in this section it states ~0.2. further confusing is when the naloxone page is brought up, the Ki rating for naloxone doesn't match any of these values. — Preceding unsigned comment added by 198.49.6.225 (talk) 05:14, 27 May 2016 (UTC)

Carfent.. again ... and again

Hello friend, you didn't sign the preceding comment. It's cool to be a stickler for sourcing, just remember, when you point a finger, there are always three fingers pointed back at you, and there is a long tradition on the Internet of being harder on others than we are on ourselves. Be of clean hands before making demands.

I'm not 100% sure what you're saying here, but it appears that you're stating that PWDs cannot be overcome with a bolus of one's drug-of-choice. This is not entirely accurate. Fentanyl and even "lowly" hydrocodone can certainly overcome a bupe block, but it's entirely dependent on how much bupe was taken vs. how much hydrocodone is taken. Bupe patients need emergency pain relief in the ER from time to time, and ER doctors can and do overcome the bupe block by using relatively massive doses of another opiate. This also, obviously, would relieve any PWDs the patient might be experiencing.

The following link is probably not sufficient basis for a encyclopedic source, but it does address real-world, actual situations in which bupe blocks are overcome by very high doses of other opiates.

http://suboxonetalkzone.com/emergency-pain-relief-while-on-suboxone/

With regards to binding affinity, the reason bupe causes PWDs is because it has a higher binding affinity than the drug(s) that it displaces. This being the case, it stands to reason that bupe would be similarly be displaced by any drug with a higher binding affinity than itself ... given in sufficient quantity. Given in a quantity much higher than bupe itself, bupe PWDs could also be overcome by taking an opiate with lower binding affinity. Binding affinity and ED is only comparable in 1:1 ratios. A (usually much) higher quantity of a drug with a lower binding affinity can and does displace drugs with a higher binding affinity, which succumbs to a constant barrage of the "weaker" drug attempting to displace it. 10x the dose of a drug with a Ki of 2, can overcome the antagonism of a drug with a Ki of 1. It all depends and there are many other factors at play besides Ki. Yuno Aye Feltersnatch (talk) 18:40, 10 June 2016 (UTC)

Causes physical addiction/withdrawl

This fact is probably something that readers of the article would want to know. A recent edit deleted the fact https://en.wikipedia.org/w/index.php?title=Buprenorphine&diff=prev&oldid=723869251, (it was not cited), and maybe it should be obvious that this is a physically addictive drug with physical withdrawal effects, so I added a bit in adverse effects and I think that the obvious needs to be stated at least somewhere in this article.TeeVeeed (talk) 15:38, 25 June 2016 (UTC)

OK-so I went back and added a ref to the drug's page that states that it directly CAUSES a physical dependence. The history section implied that it does not after the old deletion, and actually implied that what researchers were originally looking-for, (a non-addictive opiate)- is what this is when that is false and not even supported by the warning labels currently on the drug. The fact that this drug is physically addictive--(produces withdrawal symptoms upon discontinuation) WAS part of this article, and that fact has been removed at least two times now.

 "SUBOXONE Film contains buprenorphine, an opioid that can cause physical dependence with chronic use. Physical dependence is not the same as addiction. Your doctor can tell you more about the difference between physical dependence and drug addiction. Do not stop taking SUBOXONE Film suddenly without talking to your doctor. You could become sick with uncomfortable withdrawal symptoms because yo..."--from the manufacturer's website

I don't want to get into an argument about physical dependence vs addiction. Feel free to change my words in article, but physical dependence and discontinuation syndrome--whatever you want to call it, needs to be included, and especially following a statement that implies that this is not "addictive"--when many people consider a physical dependence to be a physical addiction, we don't want to mislead by semantics here.

This could be really confusing because Suboxone can cause precipitated withdrawal upon initial use from an opiate-user's regular narcotic, so "withdrawal"-is a known adverse event but it also causes physical dependence and withdrawal if used without other drugs-when used as prescribed,(as-in a long-term maintenance program on Suboxone), and we don't want to imply or say that it doesn't.TeeVeeed (talk) 21:39, 25 June 2016 (UTC)

Research section especially refractive depression and cocaine dependence clinical trails

The clinical trials referenced in relation to depression and cocaine dependence should be concluding soon and there will need to be an update to reflect those results. I note that some sources in the scholarly literature indicate dissapointing or mixed results for the ALKS 5461 compounds. Similarly the results for the same compounds trialled for cocaine dependence (undertaken by the same pharma co) due to be released sometime in 2016 are still pending. However there appears to be recently published literature that is sufficient for a review and update of the research sections. This is something that I will not be doing but would suit another editor.

Alternatively the sections for research on treatment resistant depression and coccaine dependence could be deleted because they are experimental clinical applications in smaller psychiatric populations. This maybe the more appropriate course for an encyclopaedic article. Dr.khatmando (talk) 01:19, 23 February 2017 (UTC)

Carfent.. again.

While I appreciate your attempt at understanding the pharmacology behind affinity vs. potency, the fact remains the statement IS NOT SOURCED. Therefore it has no place in the article and if it isn't sourced by tomorrow, I'm going to remove it. It's dangerous and misleading. ( i can see some poor addict trying to break into a vet's office to get ahold of these potent analogues and leading to SERIOUS consequences...) It's simply a failure of encyclopedic integrity (sp?).

As far as the pharmacology is concerned, there are dozens of opioids more potent by weight than buprenorphine, including nearly *all* (several dozens or so..) fentanyls. Fentanyl itself is approx. 2-3 times as potent as bupe by weight, yet it can't offset precipitated withdrawal either. To repeat myself, if potency were the only issue, then simply MORE of the individual's drug-of-choice would work (provided it was a full agonist) simply because full agonists don't have ceiling effects. More heroin = more potency. By that standard, even lowly hydrocodone would stop precipitated WDs *if* you took enough of it. However, that just isn't the case.

Binding affinity and potency aren't the only pharmacological reasons for this. The fact that Bupe is a partial ANTagonist plays a large part as well. When the statement is sourced, then I'll be fine with it, until then, it should be removed. I'm surprised someone with no understanding of pharmacology in the first place put it in the article, and then didn't source it. I'm sure you'd be hardpressed to FIND a source for it in the first place. One must understand the mechanisms behind PWDs before one can understand the reason "more potency" won't cure the problem.

Source it, or remove it. — Preceding unsigned comment added by 128.163.103.30 (talk • contribs) 21:06, 5 November 2014 (UTC)

Research section especially refractive depression and cocaine dependence clinical trails

The clinical trials referenced in relation to depression and cocaine dependence should be concluding soon and there will need to be an update to reflect those results. I note that some sources in the scholarly literature indicate dissapointing or mixed results for the ALKS 5461 compounds. Similarly the results for the same compounds trialled for cocaine dependence (undertaken by the same pharma co) due to be released sometime in 2016 are still pending. However there appears to be recently published literature that is sufficient for a review and update of the research sections. This is something that I will not be doing but would suit another editor.

Alternatively the sections for research on treatment resistant depression and coccaine dependence could be deleted because they are experimental clinical applications in smaller psychiatric populations. This maybe the more appropriate course for an encyclopaedic article. Dr.khatmando (talk) 01:19, 23 February 2017 (UTC)

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New changes editor wanted help

Please discuss your edits here. Thank youTeeVeeed (talk) 16:57, 24 May 2018 (UTC)

Hi TeeVeeed,

New to this and was wondering how i can provide sources to someone and they can add footnotes etc to distinguish the various types of buprenorphine available. Critical to mention long acting and their place in the treatment spectrum. Just a well meaning physician who lacks editing prowess and may need to cite more sources. Any help would be appreciated. — Preceding unsigned comment added by DrXMD (talk • contribs) 19:06, 24 May 2018 (UTC)

The long acting formulation has nearly nothing published about it. Strange.[3]

We already contain a statement from the FDA " A once a month injection has been approved in the United States and it should be available in 2018."

DrXMD do you have high quality secondary sources on the long acting formulation?

Doc James (talk · contribs · email) 05:05, 25 May 2018 (UTC)

Yeah I was able to find very little about it so far and I wonder if it is actually available everywhere? The funny thing is I know of someone who recently suffered a relapse and getting a shot /(not getting it) was what set them off and then there was a strangely brief detox and then some red-tape about getting this "shot" again (having to order it and rules about getting it) and I assumed it was vivatrol but maybe it was this? I would like to know more about it. TeeVeeed (talk) 20:55, 25 May 2018 (UTC)

Okay so I have found some info. Not suitable as references but some things are becoming clear about this. One that insurance is not covering it because it is alleged "not proven scientifically" see quote further on. Two--that there has been a little forum-spamming/trolling to promote. Three-the pharma reps gossip forum calls it worst product launch ever.http://www.cafepharma.com/boards/threads/could-sublocade-grab-record-for-worst-launch-in-history.620687/page-4 Four--additional paperwork, a month wait to be approved to use the drug-drug is ordered and shipped to dr from drug company. Also medical staff may not be comfortable with this invasive procedure. And remember the doctors authorized to administer these injections must have the special DEA waiver and up til now, no skill in depot-style painfull injections was needed for a buprenorphine waiver physician. Five. (a forum/review site quote) "declined my prior-auth for reasons of “medication lacking scientific data”. This isn’t surprising. Remember, this medication was rushed (to me, two 24-week trials with less than 900 patients is rushed) to market and those trials will turn in to real world studies." end quote Also info. (again not verified) has been posted saying that %15 of the test subjects had trouble with the injection itself.

Six--this was approved in late 2017 and six month reports are just coming in now especially considering the one month lag time to get the drug (it is a six month treatment plan??). I do not agree with those statements just noting that I had to go deep to find info about this and it is NOT VERIFIED. I was also able to see where the pharm. company has invested pretty heavy in this market including a lawsuit/patent to try and make a Buprenorphine generic film. I have questions about the dosing (inclu. How many shots? How many pellets?)-----the drug is very very weird anyhow, and this dosing schedule seems a bit arbitrary but there do seem to be some good reasons for utilizing it. I am going to have a hard time reconciling, "prevents diversion" as a strategy since from the very beginning diversion was actually PROMOTED haha as a buprenorphine benefit (pretty sure there are reliable cites for that). Drug addicts running out early--(using the daily self-dosing), abusing-- and being robbed of meds or feeling like they must sell it for cash Okay, this will be an obstacle there/prevent that. They already test people in the Buprenorphine program to make sure that they ARE using it not selling it so this injection is more like pre-insurance against that. How MUCH of the drug is being released approximately daily is a question and they are going from"300" to"100" to ?????? nothing? when it wears off? I thought that no more than a 20% drop at a time in opiates was the best way to go but no cite for that sorry this weird drug may have special powers. Or do they go back to daily dosing or proceed to vivitrol/or naloxone/something else??? Since it has barely been on the market for the six months recommended for treatment, "after-reports" are not out there. So at some point, everything wears off---(do they get the pellet removed?)-we would want to answer that, they install more pellets during the six month treatment? what happens to the old ones do they remove them-how is the pain with something like that? And going from "100" to nothing that slowly eeeeks out of your system might be bad after about five to ten days or so after the stuff is completely depleted. And I DO have good sources that say that medical professionals are "not sure" about the best way to ween someone off buprenorphine anyhow but that seems like a pretty steep cliff to drop someone off of so there must be some follow-up drug unless they want a slow-onset cold-turkey situation. I do think that there may be interest in this drug having a page on our project but I'd like to see some questions answered by reliable sources.23:29, 25 May 2018 (UTC)

Per "observation" recommendation

The source says "Buprenorphine alone is preferred for the initial (i.e., induction) phase of treatment, administered under the supervision of the prescribing physician in the office setting.202203 Following induction, buprenorphine in fixed combination with naloxone is preferred for maintenance treatment when use includes unsupervised administration.202 214Administration of buprenorphine without naloxone in an unsupervised setting should be limited to patients who cannot tolerate naloxone"

For unsupervised use the combination with naloxone is recommended. Doc James (talk · contribs · email) 21:24, 24 May 2018 (UTC)

Right but the way we have in article is confusing and a misrepresentation. The thing is that what they are talking about is the 1st time that the drug is used it is under observation (induction). The way that we have it makes it look like all use is supervised? I'll try to reword and keep the monitored use for induction.TeeVeeed (talk) 00:19, 25 May 2018 (UTC)

Okay so I reworded so it does not look like we are saying that all buprenorphine without naloxone use is supervised. Also added precipitated withdrawal to next paragraph. The induction period/supervised is for two reasons, one to avoid precipitated withdrawal by looking for physical signs of withdrawal and surveying about last opiate use, AND to determine that the drug is effective in relieving physical withdrawal symptoms. There could prob. be a rewrite or section added for induction practices since readers may be interested in that.TeeVeeed (talk) 00:39, 25 May 2018 (UTC)

The induction phase is a number of days not the first dose. When the person is switched to unsupervised dosing it is recommended they be given buprenorphine/naloxone not buprenorphine.

That is why there is this sentence "Administration of buprenorphine without naloxone in an unsupervised setting should be limited to patients who cannot tolerate naloxone"

Doc James (talk · contribs · email) 04:49, 25 May 2018 (UTC)

The source defines induction as "Induction Sublingual Initially, buprenorphine 8 mg on day 1 and 16 mg on day 2. From day 3 onward, administer buprenorphine in fixed combination with naloxone at the same buprenorphine dose as on day 2." Doc James (talk · contribs · email) 04:57, 25 May 2018 (UTC)

How about "For opioid addiction it is typically only recommended for the first to days of treatment under direct observation of a health care provider. For longer term treatment of addiction a combination formulation of buprenorphine/naloxone is recommended to prevent misuse by injection." Doc James (talk · contribs · email) 04:59, 25 May 2018 (UTC)

sorry about removing this thread in this diff. didn't mean to Jytdog (talk) 06:00, 25 May 2018 (UTC)

Basically what they do is try to perscribe the naloxone version for patients that are taking the drug unsupervised. That part about "a few days" for the induction phase observation is not acurate in almost all cases. Also, the drugs.com does say something about precipited withdrawl. "To avoid precipitating withdrawal, give the first dose when objective and clear signs of opiate withdrawal are evident.202 214" I would like to add something about that but I'd like to use another source besides the drugs.com one to replace what you say is not a valid source ( A patient is assed prior to first drug administration to avoid precipitated withdrawal.https://www.naabt.org/faq_answers.cfm?ID=70.) I can probably find prescribing info. about the office visit observation induction phase that verifies that only ONE office visit is the norm so I'd like to do that using a different source. I'll post that source here before changing because I'm not sure what would be acceptable.TeeVeeed (talk) 12:30, 25 May 2018 (UTC)

So I would propose that we avoid using terms that mention 3 days, one day,... and use "medically supervised office visit"? I like this source https://www.samhsa.gov/medication-assisted-treatment/treatment/buprenorphine Is this acceptable? Here is what they say about "induction" and I would like to use simalar words. "The Induction Phase is the medically monitored startup of buprenorphine treatment performed in a qualified physician’s office or certified OTP using approved buprenorphine products. The medication is administered when a person with an opioid dependency has abstained from using opioids for 12 to 24 hours and is in the early stages of opioid withdrawal. It is important to note that buprenorphine can bring on acute withdrawal for patents who are not in the early stages of withdrawal and who have other opioids in their bloodstream.". Maybe a link to COWS score? https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2774236/ . Also it should be mentioned about the physician waiver needed to prescribe this drug for opiate dependence. I would like to use the SAMHSA site as a source for that also if it is an acceptable source? TeeVeeed (talk) 13:32, 25 May 2018 (UTC)

Some of this only applies to the US such as the physician waiver. That could go in the body but would need to state that it is US specific.

In some places a pharmacist observing the person taking the treatment is perfectly suitable (what is done most of the time in Canada). This bit "qualified physician’s office or certified OTP" is US specific.

Agree that a person should have not used opioids for some time / be in early withdrawal before starting. Added this.

The problem with that source is it does not clearly separate when it is talking about buprenorphine versus when it is talking about buprenorphine/naloxone. Doc James (talk · contribs · email) 18:32, 29 May 2018 (UTC)

Opioids

Opioids include agonist, partial agonist, and antagonist Buprenorphine can be all three.

Source says "Exhibits analgesic1 2 71 112 129 and opiate antagonist activities.1 2 4 8 71 74 86 111 112 148 Acts as a partial agonist at μ-opiate receptors8 10 112 147 160 173 175 178 189 194 202 213 214 in the CNS8 160 and peripheral tissues,8an antagonist at κ-opiate receptors, and an agonist at δ-opiate receptors.202 213 214"[4]

We discuss this in the second paragraph. Doc James (talk · contribs · email) 23:34, 22 September 2018 (UTC)

Moderate addiction liability

Which ref supports that? Doc James (talk · contribs · email) 23:00, 10 February 2020 (UTC)

Subutex

The first paragraph states, "It is available in a variety of formulations: Subutex, Suboxone, Zubsolv (buprenorphine HCl and naloxone HCl; typically used for opioid addiction)"

...however, Subutex does not contain naloxone, and I feel that this should be pointed out. Thus, I think Subutex deserves its own sentence; something like "Suboxone, Zubsolv (buprenorphine HCl and naloxone HCl; typically used for opioid addiction), Subutex (sublingual tablets for opioid addiction), Temgesic (sublingual tablets for moderate to severe pain), etc.". Thoughts? Psychonaut25 - 13375p34k / C0n7r1b5 04:32 AM EST, 15 October 2013 (UTC)

need some where to buy online or get a script

Dustin699185 (talk) 13:13, 14 February 2020 (UTC)

Depression

In the depression research section of this article, for: "Buprenorphine/samidorphan, a combination product of buprenorphine and samidorphan (a preferential μ-opioid receptor antagonist), appears useful for treatment-resistant depression.[76]"

Would Opioid Modulation With Buprenorphine/Samidorphan as Adjunctive Treatment for Inadequate Response to Antidepressants: A Randomized Double-Blind Placebo-Controlled Trial be a better source than Pharmacodynamic and pharmacokinetic evaluation of buprenorphine + samidorphan for the treatment of major depressive disorder, since RCTs are higher quality than Expert Opinions?

Justinmumma (talk) 03:14, 17 February 2020 (UTC)

less severe Opioid withdrawal from Buprenorphine

The article says: > Opioid withdrawal following stopping Buprenorphine is generally less severe than with other opioids

I'd like to see at least one additional sentence to help quantify how much less severe. Nei1 (talk) 16:49, 6 October 2020 (UTC)

Buprenorphine

May contribute to severe dental disease including tooth loss with oral dissolving delivery. 2600:1011:B109:C875:49B1:4CC4:C4F2:3DD2 (talk) 22:44, 13 January 2022 (UTC)

"Simplified terms"

In the Pharmacology section under Pharmacodynamics and Opioid Receptor Modulator is the sentence:

In simplified terms, buprenorphine can essentially be thought of as a nonselective, mixed agonist–antagonist opioid receptor modulator, acting as an unusually high affinity weak partial agonist of the MOR, a high affinity antagonist of the KOR and DOR, and a relatively low affinity, very weak partial agonist of the ORL-1/NOP.

This is just a complete restatement of the bullet points listed above it. Also, I doubt anyone would consider these "Simplified terms".

I would suggest removal of that sentence completely, but really some actual simplified terms would be nice. Reradical (talk) 01:07, 29 September 2022 (UTC)