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Would an intranasal formulation of buprenorphine be of medical value, all concerns in mind?
Yes 80%  80%  [ 4 ]
No 20%  20%  [ 1 ]
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PostPosted: Sat Apr 28, 2012 8:09 am 
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In many countries, the patent for Reckitt's buprenorphine formulations (the household goods firm Reckitt-Benckiser, as you may know, are the inventors of buprenorphine) is due to expire soon. On an unrelated note, some patients using buprenorphine for pain find the usual dosage route (i.e., sublingual or transmucosal) to be inconvenient, as also may be the lemon-lime flavouring.

Perhaps Reckitt can hold on to their patent a bit longer by releasing a short-duration, fast-action version of buprenorphine for acute or chronic pain requiring analgesia at the opioid level only, as there may be habituation and misuse concerns. What I had in mind was a buprenorphine intranasal spray formulation, similar to allergy sprays, at the dosages of one-quarter, one-half, and one milligramme per squirt. I performed a simple, non-scientific experiment (i.e., on myself, no double blind) and concluded that the intranasal dosage form, for buprenorphine, has a shorter duration than when used sublingually, but is somewhat more potent (i.e., more bioavailable) to compensate.

Doctors in the United Kingdom do something similar for acute pain in the emergency room, mostly in paediatric (i.e., underage) patients though: a dose of morphine diacetate (i.e., Heroin®) in powder form, measured according to the weight of the patient, is mixed with normal saline or water (depending on the physician) and administered into both nostrils. This measure is used for everything from mild headaches to post-operative analgesia and rivals continuous intravenous administration (i.e., a 'drip') in speed of action, although it is less efficacious. However, the morphine must be mixed with the water by the physician or patient, making this rather inconvenient to use.

I wonder if buprenorphine/naloxone drops could be formulated by Reckitt in the same manner, but including a preservative so the mixture does not go bad, and also including some form of anti-abuse ingredient. I understand this treatment would have to be controlled because of habituation concerns, but it sure would be healthier than the usual hydrocodone with paracetamol that is so frightfully common in the U.S.A. Buprenorphine is a schedule III substance, which means physicians have a bit more breathing room to prescribe rather than being restricted in administering it like the otherwise similar but less potent drugs oxycodone, hydromorphone, and morphine.


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PostPosted: Sat Apr 28, 2012 10:05 am 
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Here in the US, RB's patent for Suboxone's tablet's expired a year or two ago, although no one has come up with a generic yet (this is when we insert our previous discussions about why RB came out with the film to protect their financial ASSets).

It sounds like you're talking about using bupe only as a pain reliever (you mentioned microgram doses) for opiate-naive persons? Is that correct? Then there would be no need for the added naloxone ingredient, as that's included in high dose bupe when used for addiction purposes to prevent the addict from hopefully relapsing.

It's true that the bio-availability is higher through nasal administration, so you're right there. Another ROA - a new option for new patients - is ALWAYS a good thing. It can bring new treatments to new patients that can't otherwise use a treatment for whatever reason.

Interesting subject; thanks for bringing it up.

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PostPosted: Sat Apr 28, 2012 3:15 pm 
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hatmaker510 wrote:
It sounds like you're talking about using bupe only as a pain reliever (you mentioned microgram doses) for opiate-naive persons? Is that correct? Then there would be no need for the added naloxone ingredient, as that's included in high dose bupe when used for addiction purposes to prevent the addict from hopefully relapsing.


I don't know about the U.S.A., but Europeans have Targin, an oxycodone product with naloxone. Naloxone has an excellent secondary use: it prevents constipation (from opiate use only). This is also a reason for the inclusion of naloxone in Suboxone, and I've also had it added (by my own request) to my morphine powders for this reason. By the way, due to its interesting binding pattern, intravenous naloxone has little to no effect on buprenorphine. Suboxone can be easily abused IV with zero preparation, and naloxone dissociates from receptors within twenty minutes.

This is why a continuous infusion of Narcan is necessary for overdose reversal: the overdose WILL come back if naloxone is not given continuously. This is also why buprenorphine overdoses are HELL, since naloxone has a lot of trouble associating to receptors and replacing part or all of the buprenorphine. And trust me, buprenorphine overdoses are very possible and very often lethal.


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PostPosted: Sun Apr 29, 2012 2:07 pm 
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hatmaker510 wrote:
It sounds like you're talking about using bupe only as a pain reliever (you mentioned microgram doses) for opiate-naive persons? Is that correct? Then there would be no need for the added naloxone ingredient, as that's included in high dose bupe when used for addiction purposes to prevent the addict from hopefully relapsing.


I don't know about the U.S.A., but Europeans have Targin, an oxycodone product with naloxone. Naloxone has an excellent secondary use: it prevents constipation (from opiate use only). This is also a reason for the inclusion of naloxone in Suboxone, and I've also had it added (by my own request) to my morphine powders for this reason. By the way, due to its interesting binding pattern, intravenous naloxone has little to no effect on buprenorphine. Suboxone can be easily abused IV with zero preparation, and naloxone dissociates from receptors within twenty minutes.

This is why a continuous infusion of Narcan is necessary for overdose reversal: the overdose WILL come back if naloxone is not given continuously. This is also why buprenorphine overdoses are HELL, since naloxone has a lot of trouble associating to receptors and replacing part or all of the buprenorphine. And trust me, buprenorphine overdoses are very possible and very often lethal.

Furthermore, OxyContin, a pill for PAIN, is often abused by injection. If Naloxone is put in the intranasal spray, people who don't know a whole lot about opiates will realise, "Hey, this has a blocker in here, I better not shoot or I'll end up in withdrawal!" even though this is not the case. If addiction can be stopped before it begins, there would be less need for treatment with Suboxone, i.e. the same thing but in pills rather than in spray.

hatmaker510 wrote:
Here in the US, RB's patent for Suboxone's tablet's expired a year or two ago, although no one has come up with a generic yet (this is when we insert our previous discussions about why RB came out with the film to protect their financial ASSets).


I'd rather have RB go into pharmaceuticals than have Merck or Bayer or Pfizer in the business. RB is a good, honest household products company first and a pain/addiction company second. I like seeing RB in the black because I think they're a damn sight better than most of Big Pharma.


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PostPosted: Mon Apr 30, 2012 7:20 am 
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You're kidding, right?

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PostPosted: Mon Apr 30, 2012 8:20 am 
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A pharmaceutical company and the words "good, honest" in the same sentence..isn't that a cop-out?

( Global consumer group Reckitt Benckiser PLC (UK:rb) on Wednesday reported a 26% rise in fourth-quarter net profit) http://articles.marketwatch.com/2012-02 ... it-markets


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PostPosted: Mon Apr 30, 2012 8:35 am 
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RB has done NOTHING to educate the medical community about suboxone - NOTHING. Yet, they've done everything they can to steer people away from their tablets towards their film, including talking insurance companies (including medicaid and medicare) into believing that the tablets are actually more DANGEROUS than the film! That's a crock of shit and it's all about them making more money. As a home products company, I'm sorry, but they don't know SHIT about producing and especially MARKETING a pharmaceutical product. They NEED to market this product right, which includes educating the medical community. But no, instead of that, we - the patients - have to explain all this to our private doctors and emergency room doctors - which is doing their job.

I could go on, but instead I'll step off my soap box now. I think everyone gets the idea.

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