Use of self-formulated intranasal buprenorphine @ 1mg/puff

[honeywhite]

I've finally found a pretty stable pain cocktail that also fixes some psychiatric issues I have had; out of the over 10 drugs I've been prescribed, I take only three, one of which is psychoactive. These drugs are propranolol, testosterone, and buprenorphine. I had problems with the buprenorphine as initially prescribed, but I changed my doses first, asked questions later, and am now satisfied. Instead of taking the 16mg/diem I was prescribed at once, I take 8mg/diem, in divided doses of 2mg qid. Instead of the tablets I was given, I'm using a self-formulated nasal spray that can reliably deliver 1mg of buprenorphine per puff.

So, here's my question. At this (relatively) high dose (usual buprenorphine doses are 400 *micro*grammes per dose), I feel a pronounced euphoria, akin to that of morphine. Unlike morphine, though, buprenorphine is stimulating, not depressing. I never used high doses of opiates, but for half my 20-year lifespan, I've been on opiates every day (5-10mg of oxycodone, 2-4 mg of dilaudid, 15-30 mg of prescription heroin/diamorphine). Is the euphoria a normal feeling when buprenorphine is taken in the doses I take it, and the way I take it (by nose)?

 

[dais]

burenorphine has around twice as high bioavailability when taken nasal in comparison to the sublingual route; so you're essentially doubling the rate of absorption with your method.

as bupe is not a full mu agonist and has antagonistic properties, once past a cartain dose range - usually around 8mg iirc - it starts to become dysphoric and more negative effects start to become present.

i feel the same way about bupe. it gives me a sense of motivation and stimulation with low doses as well as slight euphoria, though, nothing in comparison to morphine. it satiates my needs and wants for using.

 

[nAON]

Fairly normal, it's quite a high dose of bupe after all, compared to your previous opi usage. Don't expect it to last, though, chances are the euphoria will go away after you've used it daily for more than a couple weeks.

 

[honeywhite]

I've been using for months. Still feels good. If anything, now that I figured out that it needs to be used in moderation to kill pain and to feel good, it works even better. The 8mg dose doesn't do the job half as well as a couple 2mg doses spread apart. I never really liked the opiate nod—I liked the mood lift. 30 mg of morphine gives me roughly the same mood lift as just 2 mg of buprenorphine, but with a bit of a sedative character. It even gives a mood lift when taken orally. I can say with confidence, however, that the little 2 mg lemon candies are far, far better than the big 8 mg whoppers. It doesn't even kill pain properly at a high dose. It's a paradox; I have the feeling that dose response for this drug is a quadratic equation (you know, one of those U-shaped lines, where you try to hit the sweet spot at the bottom of the "U").

Also, when I said buprenorphine has a stimulant effect, I failed to mention that it will NOT keep you awake if your body needs sleep, like amphetamine will.

 

[nAON]

Yeah, bupe has quite a strange dose/response, after a certain amount taking more just won't do anything.

 

[honeywhite]

Yeah, bupe has quite a strange dose/response, after a certain amount taking more just won't do anything.

That's actually the weird part. What you're saying is true of methylmorphine/codeine, but *not* true of buprenorphine (B.). If I, say, take 300 mg of codeine by mouth (it can not be taken by injection), it will do no more than 200 mg of codeine by mouth, because only 200 mg can be metabolised into morphine by the liver at any one time. The other 100 mg may lengthen the effects slightly, but probably will not, because it is also being metabolised but not into morphine. If I plotted the dose-response, it would be a diagonal line with a horizontal line (plateau) from about 200 mg onward.

Buprenorphine is different. If I take 16 mg of B. by injection, it will actually do *worse* than 2 or 4 mg.

Assuming that I'm correct about the pharmacodynamics of B., I think I may know why this happens. B. latches onto opiate receptors in the body, but does not activate them to their full potential. The body produces opiates as well---these also latch onto opiate receptors, but activate them fully. However, B. has a stronger preference for opiate receptors---if there is a free receptor around, B. will hook up to that one, but if there is even an occupied one, B. will kick whatever was occupying it off and latch on instead. If only 2 mg. is given, there is not enough B. for all the opiate receptors and it hooks up to the free ones (i.e. behaves like a full agonist). The body's own opiates don't get disturbed. If 16 mg. is given, there is way too much B. for the free receptors to handle, and it starts kicking off whatever it can to make space for itself. I believe that because endorphin etc. is stronger than B., the body senses the imbalance and goes into mild withdrawal.

 

[dhopeless]

Sorry to bump an old thread, but damn that makes so much sense! That seems to explain why sometimes, and only once in a while, bupe gets me really high. Like tonight. I had waited longer than I usually do, dosed, and then had sex and I was wondering if the natural endorphin release was responsible for this killer high I am experiencing right now. Great post.

That's actually the weird part. What you're saying is true of methylmorphine/codeine, but *not* true of buprenorphine (B.). If I, say, take 300 mg of codeine by mouth (it can not be taken by injection), it will do no more than 200 mg of codeine by mouth, because only 200 mg can be metabolised into morphine by the liver at any one time. The other 100 mg may lengthen the effects slightly, but probably will not, because it is also being metabolised but not into morphine. If I plotted the dose-response, it would be a diagonal line with a horizontal line (plateau) from about 200 mg onward.

Buprenorphine is different. If I take 16 mg of B. by injection, it will actually do *worse* than 2 or 4 mg.

Assuming that I'm correct about the pharmacodynamics of B., I think I may know why this happens. B. latches onto opiate receptors in the body, but does not activate them to their full potential. The body produces opiates as well---these also latch onto opiate receptors, but activate them fully. However, B. has a stronger preference for opiate receptors---if there is a free receptor around, B. will hook up to that one, but if there is even an occupied one, B. will kick whatever was occupying it off and latch on instead. If only 2 mg. is given, there is not enough B. for all the opiate receptors and it hooks up to the free ones (i.e. behaves like a full agonist). The body's own opiates don't get disturbed. If 16 mg. is given, there is way too much B. for the free receptors to handle, and it starts kicking off whatever it can to make space for itself. I believe that because endorphin etc. is stronger than B., the body senses the imbalance and goes into mild withdrawal.

 

[hatrix]

why are you doing this? just use as prescribed

This is an old thread, OP probably won't even notice more replies and the reply was simply understanding another post in the thread regarding the pharmacodynamics of buprenorphine.

 

[Swimmingdancer]

This is an old thread, OP probably won't even notice more replies and the reply was simply understanding another post in the thread regarding the pharmacodynamics of buprenorphine.

^This. I'm going to close it so that people don't see it on the front page and assume it is new. BDD is a fast-moving forum and we prefer that people don't bump old threads unless they have something very important to add. Please PM me if you have any questions.