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Re: What is buprenorphine like? » Elizabeth

Posted by MB on January 31, 2002, at 2:12:54

In reply to Re: What is buprenorphine like? » MB, posted by Elizabeth on January 30, 2002, at 16:36:21

> > One time in detox (heroin) I was given buprenorphin sublingually to ease the withdrawal. I wasn't too impressed with it.
>
> How much were they giving you? The sublingual dose needs to be rather high, I think, especially for addicts and especially if you're using the injectable solution marketed in the U.S. Some addicts say it really helps them to detox and others don't, so you're not alone.

They gave me an ampule and a straw and said suck the whole thing under your tongue and hold it there for as long as possible (of course, detoxing, I was salivating badly, and the buprenorphine was pretty quickly diluted...seemed like a waste). I don't know how much was in the ampule: glass bottle with a scored, breakable neck.

> > It didn't seem to help much, but then again, there was no way of telling how bad I would have felt if I *hadn't* been givin that accepably palatable liquid to suck on.
>
> It's in a 5% dextrose solution (a type of sugar), hence the funky-sweet taste. How long did they tell you to keep it in your mouth?
>
> > For all I know, it was a godsend, but my intuition tells me that I wouldn't have been much worse off without it.
>
> Have you ever experienced heroin withdrawal without buprenorphine?


Yeah, but I had tons of Xanax and clonidine. I prefere benzos and clonidine when it comes to easing opiate detox (clonidine stopped the chills and the Xanax let me sleep--for a little while at least).

> I'd expect buprenorphine to do more for you if you took it outside the context of opioid dependence (i.e., when you hadn't taken heroin for a while and so did not have any tolerance).
>
> BTW, when the doctor in the hospital gave you the IM injection, do you know what the dose was?


No I don't. Probably the same amount that was in the ampules they gave me to use sublingually. I'm looking in the PDR and the .3 mg ampules look like the ones they gave me.


> > My limited and extremely adulterated experience with buprenorphine compels me to ask this question: what is the medication like under normal circumstances--i.e., circumstamnce where the patient is neither habituated to opoid agonists nor in a state of withdrawal from such agonists.
>
> (Right, that's what I meant. You expressed it a lot better.)
>
> > Is is sedating?
>
> For some people. It seems that there are people who experience paradoxical stimulation on opioids (like myself), though. My experience is that every opioid I've tried has been activating, not just buprenorphine. I think sedation is more common. I don't know if the paradoxical response is predictive of antidepressant response.


I get activated on opiates, but they also give me narcoleptic type nods. One time I was doing fine, standing in the check out line in the supermarket, and I fell asleep (standing up!!) right when the checker was reading my total. I feel like getting out and "living life" on opiates, but I do tend to nod in weird situations.

> > Is it nauseating?
>
> Yeah, you have to be cautious about the dose.
>
> > Dysphoria, euphoria, etc.
>
> Neither, but a feeling of calm and "wellness." (Again, there's a subset of people who get dysphoric on opioids; these people will probably feel dysphoric on buprenorphine too, but this is a general reaction to mu agonists, not a specific reaction to buprenorphine.) I also find that it clears up "brain fog."


I get dysphoric on opiates only if the dose isn't high enough. I wonder if it has to do with the way different receptors are hit at different doses. Or, more honestly, it may just be because I'm a junky at heart...a low dose is just an annoying tease.

> > Is there a waiting period before antidepressant effects are noticed, or is relief immediate as with the pure agonists?
>
> It takes about an hour when administered intranasally, IME. Presumable it's faster when given IM.
>
> > I've taken butorphanol before. That was weird. A lot of kappa agonism I think. Is buprenorphine anything like butorphanol?
>
> Its pharmacological profile is opposite that of Stadol (butorphanol) -- buprenorphine is a kappa antagonist, partial mu agonist. I've never taken Stadol so I can't really say anything about how they compare.

I kind of liked Stadol...I think kappa agonism is pretty strange.

I've never understood how a drug could be a "partial" agonist at a receptor. It seems counterintuitive to my relatively pharmacologically naive view on things that something could agonize and antagonize a receptor at the same time. How does that work?

MB



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