Posted by Elizabeth on July 15, 2001, at 17:33:32
In reply to What is buprenorphine?, posted by Else on July 14, 2001, at 14:18:43
> For a long time I assumed it was Stadol but that's buterphanol. What is buphrenorphine? I've never heard of it.
OK, so, there are 3 different subtypes of opioid receptors: mu, kappa, and delta. (sigma turned out not to be an opioid receptor) Stadol is a kappa agonist (meaning it selectively activates kappa-type opioid receptors) and partial mu antagonist (meaning there's a ceiling on its intrinsic effect at these receptors).
Buprenorphine is a partial mu agonist and kappa antagonist. In the US, it's sold in an injectible solution under the brand name Buprenex (there's also at least one generic available, but it's still expensive). In some other countries it's available in a sublingual tablet called Temgesic or Subutex.
A sublingual formulation which would contain both buprenorphine and naloxone (the latter is to prevent people from melting & injecting it) is under investigation in the US as a treatment for opioid dependence.
There used to be a similar sort of drug, dezocine (Dalgan), but that got taken off the market.
-elizabeth
poster:Elizabeth
thread:70125
URL: http://www.dr-bob.org/babble/20010714/msgs/70225.html