buprenorphine for pain

[notredame]

How much does buprenorphine help pain, and how much would you have to take for the same amount of relief that you would get from, say, 60mg of codeine?

[DevilishOne]

Buprenorphine is sometimes used for pain control. A sublingual dose of .2 mg is loosely considered the equivalent of 100 mg of codeine. It is of course a very different type of opiate, (both agonist and antagonist) So it shouldn't be combined with or used adjacent to traditional opiates. Also, for that reason, if you need to treat pain that is typically controlled by 60mg codeine, if possible you should see a physician and get something more appropriate.

[Perromaldido]

Hi there @notredame. You should look into Temgesic (brand) 0,2 or others preparations which may be 0,3 as well. This stuff does not contain any naloxone so it's pure bupe. Actually it's not an agonist/antagonist like say pentazocine but it's partial agonist. It makes for quite a difference so if you're interested in that go google for tech. explanations. Don't want to bother with lecturing.

It's very, very different from codeine....it's a good pain killer for some kind of pain, while I found out to be totally unhelpful for others. YMMV.

I'd say a 0,2 covers 60mgs covers codeine just fine. What it's really great at is coming off
opiates and it's very effective even at these micrograms doses. Actually bupe is not like the more the better. Here 0,2s are prescribed as a pain killer even though widely used off-label for home detox. You should give it a try + I strongly suggest not to touch Subuxone tho
it's probably a lot easier to get for you if - as I believe - you're in the US.

Perromaldido

[notredame]

Hi there @notredame. You should look into Temgesic (brand) 0,2 or others preparations which may be 0,3 as well. This stuff does not contain any naloxone so it's pure bupe. Actually it's not an agonist/antagonist like say pentazocine but it's partial agonist. It makes for quite a difference so if you're interested in that go google for tech. explanations. Don't want to bother with lecturing.

It's very, very different from codeine....it's a good pain killer for some kind of pain, while I found out to be totally unhelpful for others. YMMV.

I'd say a 0,2 covers 60mgs covers codeine just fine. What it's really great at is coming off
opiates and it's very effective even at these micrograms doses. Actually bupe is not like the more the better. Here 0,2s are prescribed as a pain killer even though widely used off-label for home detox. You should give it a try + I strongly suggest not to touch Subuxone tho
it's probably a lot easier to get for you if - as I believe - you're in the US.

Perromaldido

If I may ask would "bupe" be efficient for extremely painful back / joint / muscle pain and headaches? Because a little bird tells me that "bupe" can be found much cheaper than codeine these days and the bird is low on cash. Thanks so much for the information thus far.

[Perromaldido]

@notredame, hello my dear. Tell your little bird that my Thyrannosaurus Rex found it to work just fine on any skeletal/bones related pain and relatively fine on muscles ,but would't touch a headache at all, As always, your bird mileage may vary.

Perromaldido

[Hugo]

I've been prescribed Temgesic for chronic pain for many years. It does help, especially in combination with other drugs, such as anticonvulsants and muscle relaxants. I'm currently prescribed 2mg per day (in divided doses), along with adjuvant analgesics (gabapentin, diazepam or other muscle relaxants, etc.). I've also been prescribed full agonist opioids such as dihydrocodeine and morphine for breakthrough pain on top of the Temgesic, and I've never had a problem - I feel the effect of the other opioid just fine.

I've researched buprenorphine quite a bit and discussed it with my doctors, and it is okay to mix with other opioids within the usual analgesic dose range. Problems could occur if you started taking it while already dependent on high doses of another opioid, but I don't know how common this is. I've always been on a relatively low dosage, so I've never had any problems. The one thing it seems it is not recommended for is pain that is likely to be rapidly escalating in nature, as there is a ceiling to buprenorphine's analgesic effect.

As with any other drug, it's not going to work for everyone. It doesn't have the same feel as more traditional agonists like codeine and morphine. It makes me a little light-headed when I take a highish dose for the severe pain I have in the mornings, but it tends to make me feel more alert and energized, as opposed to sleepy and heavy, as I sometimes feel after taking morphine (immediate release tablets).

I know quite a few people who've been pleasantly surprised by how effective it is with fewer side effects than drugs they'd been on previously, such as oxycodone or morphine. Other people don't find it very helpful at all. It's probably worth trying if you have chronic pain, especially if you are concerned about long-term effects (buprenorphine doesn't effect hormone levels or the immune system in the way other opioids sometimes do, and there is a ceiling on respiratory depression, which makes it a safe alternative).

[burnout]

^That is extremely unusual. Most people on 2 mg of bupe per day would not be able to feel morphine. In my opinion, bupe is a terrible drug to be on long term. The half life is way too long, causing it to build up in your system and saturate your receptors. This leads to tolerance and not feeling much effects from the drug anymore. In other words, being on bupe will just be the new normal for you and you will still experience pain. Contrast this with morphine for instance, and if you were experiencing a great deal of pain , you could always take more morphine and get more relief. With bupe, not so much. Taking more doesnt always lead to better effects. I have also read the withdrawals last longer than those from morphine.

[Perromaldido]

Right, but that applies to anyone who abuses or has abused opiates. I once woke up during a surgery. I told them whatever opiate they'd use (if they'd use one in the process) had to be like 4x.....now I have to remove a titanium bar from my leg and 4 or 5 bolts. And after that when I wake up - even now if i'm only on some tramadol - I know their 10 mils morphine will do jack to my post surgical pain..... but do you think they'll give me a hundred because of that? No way, not here.....so I guess I'm keeping it, besides I can say next dai weather better than anyone else

[MusiciansMallet]

As mentioned, buprenorphine is used for pain & is an effective synthetic opioid (not an opiate) in some respects- particularly in individuals with low tolerances to opiates (to the OPer, your tolerance is NOT high). However, its a longer acting opiate & more appropriate for chronic pain rather than "break through" pain. Its partial agonist activity makes its pain relief less effective at higher doses and higher tolerances.

It is of course a very different type of opiate, (both agonist and antagonist) So it shouldn't be combined with or used adjacent to traditional opiates.

@DevilishOne
Just a slight correction; buprenorphine is absolutely not an "agonist and an antagonist" -- this is functionally impossible. buprenorphine is highly selective and has higher binding affinity for mu-opioid receptors than most all other opiates & opioids. This high "binding affinity" is completely independent of agonist or antagonist activity (A drug can have high affinity for a receptor and be an antagonist, agonist, inverse agonist, etc); this merely means buprenorphine will "kick off" other opiates with less binding affinity & replace it with itself.

Buprenorphine happens to be a partial agonist at opioid receptors. So while it kicks off other opiates from receptors (because of its higher binding affinity), it has its own opioidergic activity. But, being a partial agonist, it doesn't fully "plug into" the mu-opioid receptors. This is irrelevant for people w/ no tolerances or small tolerances to opiates/opioids & at normal dose-ranges. But it gives the illusion of being an antagonist if say, one has a high tolerance & is dependent upon morphine, oxycodone, heroin, hydrocodone (all opiate/opioids with LESS BINDING AFFINITY). If the user takes buprenorphine, this "kicks off" the morphine (or hydrocodone, heroin, oxycodone, etc) from mu-opioid receptors & the bupe replaces itself at these same receptor sites. But since it is a *partial agonist*, the level of mu-opioid activation is not high enough & may precipitate withdrawal symptoms in people who are dependent upon higher levels of opiates or opioids.

[Perromaldido]

@MusiciansMallet you are absolutely right in defining bupe a 'partial agonist' and explaining its effects at the major receptors. Pure bupe at least, Subuxone comes with full antagonist naloxone in a ratio 1:4, hust -they say- to prevent use diversion.

Nonetheless agonist/antagonist are a class of Pk's (Think about Pentazocine -Talwin - or Butorphanol - Turbogesic) It's like they agonize Sigma and Kappa (and a bunch of the minor ones) but it is a full antagonist at Mu. For example, administering P'zocine to a Methadone patient - as well as a road junky or a pillhead- will invariably result into precipitating wds with nothing you can do to reverse for at least 24 hours. Again if one patient does not have a tolerance to opiates he couldn't care less how they work.

[waterlogged]

I was prescribed the butrans patch while on 3- 7.5 mg hydro's a day and found it did nothing for me. In fact the adheasive caused much discomfort and the area where the med was would cause skin rash. Used the paches for 3 months before dr discontinued it. went to 4- 10mg hydros after that. Had high hopes for it because of the time release but just didn't work for me.

[Perromaldido]

I didn't even know those patches existed . IMO 7,5 hydro -although 3x day-is quite weak, besides this combo may be not so well thought out because of tha presence of bupe......

[DevilishOne]

As mentioned, buprenorphine is used for pain & is an effective synthetic opioid (not an opiate) in some respects- particularly in individuals with low tolerances to opiates (to the OPer, your tolerance is NOT high). However, its a longer acting opiate & more appropriate for chronic pain rather than "break through" pain. Its partial agonist activity makes its pain relief less effective at higher doses and higher tolerances.



@DevilishOne
Just a slight correction; buprenorphine is absolutely not an "agonist and an antagonist" -- this is functionally impossible. buprenorphine is highly selective and has higher binding affinity for mu-opioid receptors than most all other opiates & opioids. This high "binding affinity" is completely independent of agonist or antagonist activity (A drug can have high affinity for a receptor and be an antagonist, agonist, inverse agonist, etc); this merely means buprenorphine will "kick off" other opiates with less binding affinity & replace it with itself.

Buprenorphine happens to be a partial agonist at opioid receptors. So while it kicks off other opiates from receptors (because of its higher binding affinity), it has its own opioidergic activity. But, being a partial agonist, it doesn't fully "plug into" the mu-opioid receptors. This is irrelevant for people w/ no tolerances or small tolerances to opiates/opioids & at normal dose-ranges. But it gives the illusion of being an antagonist if say, one has a high tolerance & is dependent upon morphine, oxycodone, heroin, hydrocodone (all opiate/opioids with LESS BINDING AFFINITY). If the user takes buprenorphine, this "kicks off" the morphine (or hydrocodone, heroin, oxycodone, etc) from mu-opioid receptors & the bupe replaces itself at these same receptor sites. But since it is a *partial agonist*, the level of mu-opioid activation is not high enough & may precipitate withdrawal symptoms in people who are dependent upon higher levels of opiates or opioids.

Yup, I omitted the word "partial". I was just trying to express my humble opinion that because "buprenorphine will "kick off" other opiates with less binding affinity & replace it with itself", it might not be a good choice to use as replacement or in conjunction with codeine. Thanks for the clarification.

[dsteury]

@nortedame the best thing to come out recently is produced by Prudue Pharma it's called the Butrans Patch 5,10,20 mcg/hour 7 Day patch?. The initial reports have been so favorable that Purdue is actively pushing Bustran Patches rather than Oxycontin. I ask my pain management guy and he said cancel what you get now and I'll give you Bustran Patches any day he thinks this is breakthrough stuff when used with the right combination of breakthrough pain killers and, may be some Benzos. Check it out it's interesting and the seven day thing is probably a little bit of a stretch I never seen any patch that would stay on for seven days.

[Hugo]

There is an interesting experiment that showed how much of available mu opioid receptors are occupied by certain doses of buprenorphine. A single 2mg dose binds about 40% of mu opioid receptors, while a single 16mg dose takes up approximately 80%. I generally take between 1.2mg and 1.8mg a day (but sometimes up to 2mg, which is what I'm prescribed per day).

A study on cancer patients who were switched between buprenorphine and morphine, and then given the buprenorphine patch with oral morphine as rescue for breakthrough pain, concluded that 'buprenorphine is as efficacious as morphine in the treatment of severe chronic pain and is completely compatible with the use of morphine as rescue medication.' Another study used buprenorphine as extended-release medication with other opioids as rescue for breakthrough, and concluded: 'These results support the view that there are no limitations to combining buprenorphine with pure mu-agonists in the analgesic dose range'. (from 'Buprenorphine - the Unique Opioid Analgesic: Pharmacology and Clinical Application', edited by Budd & Raffa, 2005). The Palliative Care Formulary also states that it is safe, and describes alternating between therapeutic doses of buprenorphine and morphine.

The information that comes with my Temgesic prescriptions states that the full effect of other mu agonists such as morphine and oxycodone can be achieved within the standard analgesic dose range.

As I mentioned, I'm prescribed up to 2mg a day, and some days I can get by with as little as 1.2mg - on average, I'd say around 1.4 - 1.8mg. Sometimes the buprenorphine is not enough to keep my pain levels down to a bearable level, so the doctor gives me immediate-release morphine or tramadol to take in addition to the Temgesic. I've found this does help, although having said that, nothing keeps the pain levels down as far as I would like, and if I don't rest when I'm having a flare-up, it seems nothing I take is up to the task of dealing with the combination of deep grinding musculoskeletal pain and the burning, stabbing neuropathic pain that I get. I'm also prescribed non-opioid medicines, and use other pain relief techniques, such as TENS/TSE and exercise.

My own experience, as well as the information given to me by my pain management doctors going back many years and other sources I've researched in my time as a chronic pain patient, bears this out. I sometimes take morphine 30mg (IR), and I feel the effect just as well as I did prior to being prescribed Temgesic. The same goes for dihydrocodeine, codeine, tramadol and oxycodone. I have taken all of these along with buprenorphine, and have never felt a diminished effect. I had been on these analgesics before I ever started being treated with buprenorphine, so I know their effects on my pain.

I can only speak for myself, obviously, and I can't compare my own experiences to those of people who've been on buprenorphine for non-analgesic purposes (these tend to be higher doses than those typically used for pain relief). The comments I've seen from other chronic pain patients who are taking buprenorphine after having tried other strong opioids have generally been favourable.

[MusiciansMallet]

@MusiciansMallet you are absolutely right in defining bupe a 'partial agonist' and explaining its effects at the major receptors. Pure bupe at least, Subuxone comes with full antagonist naloxone in a ratio 1:4, hust -they say- to prevent use diversion.

Nonetheless agonist/antagonist are a class of Pk's (Think about Pentazocine -Talwin - or Butorphanol - Turbogesic) It's like they agonize Sigma and Kappa (and a bunch of the minor ones) but it is a full antagonist at Mu. For example, administering P'zocine to a Methadone patient - as well as a road junky or a pillhead- will invariably result into precipitating wds with nothing you can do to reverse for at least 24 hours. Again if one patient does not have a tolerance to opiates he couldn't care less how they work.

Yes, these drugs are agonists & antagonists, but at different receptor sites; a drug cannot concurrently be both an agonist and an antagonist at the SAME receptor (the mu-opioid receptor in this case), at least at the neurological level, end-result effects may cause a sort of "antagonist" effect, but this doesn't mean its an antagonist at the receptor site (neither pentazocine nor butorphanol are full antagonists at mu-opioidergic receptors, see below). & Kappa opioid receptor agonists have little to do w/ pain (Salvia is a kappa-opioid agonist, & it produces effects no where NEAR opiates & opioids. Same w/ the sigma i know you weren't necessarily saying this, just further explaining for anyone reading this, though). Same w/ sigma; its a poorly understood receptor, it has more in common with PCP & cocaine its effects than typical opioidergic drugs.

Pentazocine is only an "antagonist" if the formula w/ naloxone is used and is injected in someone dependent upon opioids, it is a partial-agonist by itself however. It will precipitate withdrawal, but this mode isn't really understood; & its definitely not due to antagonism, most likely binding affinity (see article below). If you have sources otherwise, please correct me if i'm wrong (i'm always open to construction criticism as long as i'm learning something in the process! but i have not read otherwise). Talwin is just a formulation containing pentazocine; & butorphanol's mode of action is less understood (surprise surprise! the patent has run out so no further double-blind studies exploring its pharmacology! no big-bucks to be made!)- it displays mixed antagonist/agnoist properties, most likely due to a mode similar to that of buprenorphine.
Precipitated withdrawal by pentazocine ... [J Pharmacol Exp Ther. 1993] - PubMed - NCBI
Butorphanol-precipitated withdrawal in ... [J Pharmacol Exp Ther. 1988] - PubMed - NCBI (although this says butorphanol is a mixed agonist/antagonist at the beginning of the abstract; the end/conclusion clearly states the antagonist effects are different than normal antagonists like naloxone & are likely due to a different mechanism)


And in regards to Suboxone; heh, yea.. "so they say" for sure! (i'm on 4 mg suboxone/day, full disclosure!) ...back to binding affinity- buprenorphine has MUCH higher binding affinity than naloxone; and it will not-fully reverse buprenorphine's effects, even if injected. (recent studies have been done on this). There is no medically available agonist if overdose occurs w/ buprenorphine use b/c of its superior binding affinity (and LONG acting nature of course; where as IV naloxone is only 1-2 hours). There are some opioid antagonists in research stages that have extremely high binding affinity, but whether its higher than that of buprenorphine is not yet known..



.......Anyway, don't mean to derail this thread into a debate on pharmacology! Sorry guys!

[Perromaldido]

I don't want to debate strict pharmacology matters either, anyhow I guess we've given a rather enuogh complete picture on this subject, And what you says about salvia on sigma is right, in fact p'zocine at 150mg feeks like a mix o k, salvia and opies, way too edgy to be my cup of cofee, yet signifactly maintaining its pking profile, and nice talking to you btw, mate.

Oh btw you may old enoug to remenber T's and blues, full agonists users had o problem with inj that, I guess those blues -an anthystaminic AFAIK -reeversedtalwin propertie somehow....

[Laugh]

I can't say with certainty that is treats pain with the same force as a prescription painkiller of any sort...But my gerbil was prescribed Bupe in an effort to reduce withdrawal symptoms, and boy did that work. After two weeks of use, the gerbil kicked the dope habit for weeks and started running in his wheel again.

[waterlogged]

I was on the 10 mcg Butrans patches for three months and they never took away or made the hydro any less effective. In fact they did nothing and yea I believe they are being pushed. my doc sure seemed to be pushing them but Im now on the 10 mg hydros along with 20 mg oc (new formula) and I find this much more effective than the patches. will probably step up to 30 mg oc and reduce the ammt of hydros to 60 or so and I will be fine with that I believe. The patches can be expensive but they do come with a coupon if ins wont cover it.

[DeepSouth]

Bupe is definately useful for pain! It is one of the Strongest pain killers on the market, many people would not know this, I think it may be 2ng under Fentanyl. But I do take a high dose (4-6mg daily). I am actaully trying to get to the lowest dose of this med as possible, I was originally put on this medication for opiate addiction , but it has worked wonders for pain. In 3 years of being on this medication, I have never really hurt except maybe a few days (I have 2 bulging discs and a ruptured 1 in my back). I see they make a 0.2 version in other countries so a 2mg and 8mg that they make definately shows this is a strong med. I think they are actually pre scribing it now off label for pain, I dont know how docs would do this without being certified to prescribe (here in the US doctors have to take a class to prescribe Bupe and can only prescribe to so many patients). I thnk they should let every doctor use this med at low doses for pain.