From: "Steve Harris" <sbharris@ix.RETICULATEDOBJECTcom.com>
Subject: Re: Buprenorphine (Buprenex) for chronic pain
Date: Thu, 27 Feb 2003 15:26:37 -0800
"Emma Chase VanCott" <email@example.com> wrote in
> Daniel Prince <firstname.lastname@example.org> wrote:
> : I have read that Buprenorphine (Buprenex) is 30 to 40 times more
> : potent than morphine as an analgesic but it is not abusable. Is this
> : true? If it is true, why isn't it used to treat chronic pain that is
> : not relieved by over the counter analgesics? Thank you in advance for
> : all replies.
> I believe it is what they call a mixed agonist/antagonist, eh?
> (Morphine is an agonist.)
> What also matters is which opiate receptor subtype(s) is/are stimulated by
> a drug. Stimulating some of them cause euphoria) whereas some of them
> cause dysphoria (kappa? or delta?).
> Alternately, sometimes methadone is used. Or the duragesic (fentanyl)
Apples and oranges. Buprenorphine is in theory abusable, but
you can't get into the high mu-receptor range with it,
because it starts becoming its own antagonist at doses much
over those used in non-tolerant "opiod virgins" who have
moderate pain. You can't get more than the pain control of
the standard dose of morphine (10 mg), and even then, only
in non-tolerant people. Using Buprenex in a opiod abuser or
even a heavily narcotic tolerant chronic pain patient would
be pretty cruel, almost like giving naloxone.
Buprenex is at present schedule V, and would indeed be a
good candidate for the first OTC narcotic. But first
somebody will have to market an oral form (approved not long
ago, but not yet on the market, so far as I can tell-- it's
always been injectable only) and after that, the DEA would
still have to get over its narcotic paranoia. Buprenex is a
respiratory depressant, and if it was OTC there's no doubt
more doofuses would OD with it in combo with a lot of other
downers (alcohol etc) and manage to kill themselves. So it's
not as though there was no downside to the government in
making it as available as Tylenol.
It will be very interesting to see if the oral form comes
out C(V), and if it is denatured with APAP or ASA, which is
a typical DEA trick (unnecessary here, but habit is habit).
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