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Re: What is buprenorphine? Elizabeth

Posted by Else on July 17, 2001, at 22:28:28

In reply to Re: What is buprenorphine? Else, posted by Elizabeth on July 15, 2001, at 17:33:32

Very strange. In the U.S. people seem to have a lot more choices than here (Canada). I have never heard of an opiate being used for depression. And I don't know any adult who takes a major stimulant for ADD although schoolchildren have no trouble getting scripts. There are other drugs like Provigil and the like that are unavaillable as far as I know and I've never heard of stimulants being used as augmentation therapy for depression. Maybe because most of the research is done in the US and also there's the state run drug insurance which tends to limit choices.
> 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




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