Buprenorphine intranasal formulation

Author: honeywhite

Posted: Sun Apr 29, 2012 1:07 pm

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.