Posted by Elizabeth on June 6, 2001, at 21:55:06
In reply to Buprenorphine- check this great article out !!, posted by Pacha on June 6, 2001, at 9:22:29
> Buprenorphine was developed in the UK in 1972 and has approval there as a primary treatment for pain relief and opiate detoxification. France recently (1996) added Buprenorphine under the trade name Subutex as its primary therapeutic tool for opiate detoxification.
It seems to work very well for a lot of people. Because of a ceiling effect (above a particular dose it becomes ineffective), however, it's not adequate for a lot of people who have heavy heroin habits.
> This moves treatment of opiate abuse from the stigma of the methadone clinic into the office of the primary care physician. The US is
> looking into this option themselves as the French model has been incredibly successful.Weird that the US would look into something that actually works, huh? < g > MMT as it's done in the US is hard to implement and, as a result, isn't available to most of the people who need it. Letting primary care doctors prescribe buprenorphine for maintenance treatment of addiction would make help available to many more people.
> Recently, Drug Czar McCafferty has stated publicly his advocacy of this action.
That was Clinton's drug czar (that sounds like a Russian variant on the Latin American _narcotrafficante_, not a government position!).
> As an analgesic, Buprenorphine is currently accepted for use in the US, ...
But it is only available
> Highly effective (35 times as powerful as Morphine by volume)
By mass, not volume. Volume depends on the medium (morphine is available in many forms in the U.S.; buprenorphine is in an injectible 5% dextrose solution that contains 0.3 mg buprenorphine per mL solution). 0.3 mg of IV buprenorphine is supposed to be equivalent to about 10 mg of IV morphine.
> With significantly lower abuse potential than the status quo (Schedule V on the controlled substance list as opposed to Methadone -a Schedule II)
> we are experiencing a paradigm shift in the opiate abuse treatment armamentarium as well as a major discovery and treatment potential for refractory depression and other panic and anxiety psychiatric disorders.
I hope so. (Some people find opioids helpful in panic disorder, OCD, and social phobia as well as depression.)
Another possibility is tramadol, an opioid with low intrinsic activity and mild monoamine reuptake inhibiting properties.
> Pharmacological studies have defined three classes of Opiod receptors where these endogenous opiods bind; delta, kappa, and mu.
A promising possibility exists that the addition of a delta antagonist could prevent tolerance to mu agonists. I hope that research continues in this direction.
> The kappa receptor is most commonly associated with sedation ( nodding often seen in Heroin addicts).
That's not so clear. Buprenorphine, a kappa *antagonist*, can cause nodding (but without euphoria) and is commonly sedating.
> Underproduction or over-removal (severe re-uptake)
Or metabolism -- there was some work in the early '80s or so on "enkephalinase inhibitors" (unfortunately it turned out that "enkephalinase" was a general polypeptidease, not specific to enkephalins, making these drugs non-viable for use in people).
> Buprenorphine's superior efficacy when dealing with these disorders is due to the aforementioned unique pharmacological profile as a PARTIAL MU RECEPTOR AGONIST combined with a FULL KAPPA RECEPTOR ANTAGONIST.
I'm not convinced that it works better than full agonists. Obviously there have been no head-to-head comparisons. Stadol, a kappa agonist/mu antagonist, is often experienced as dysphoric by depressives, but it's hard to conclude much from that.
> The kappa antagonism of Buprenorphine also offers a new approach in the treatment of depressive disorders. Clinical studies have shown that the overproduction or under-removal of the endogenous kappa agonist dynorphin can have a direct causal relationship with various depressive disorders.
Really? I haven't heard of clinical studies in this area.
> Buprenorphine's unique pharmacological profile referenced earlier make it the only medication that offers this concurrent treatment alternative.
Yes -- Dalgan (dezocine) is similar, but it was taken off the market recently.
> Conventional antidepressants and antipsychotics work gradually over a period of weeks or months, whereas maximal benefit is apparent with Buprenorphine in a matter of days and in some cases hours.
Intranasal buprenorphine works in about 1 hour. Intramuscular administration might produce more rapid effects. The effect I refer to is a complete reversal of all symptoms of depression (complete compared with MAOIs). Opioids have been found to work in a wide variety of subtypes of depression, too, which I find interesting.
> A recent clinical study at Johns Hopkins University Dept of Psychiatry of Buprenorphine and its efficacy in psychiatric disorders, a number of patients received a complete remission of the symptoms of depression based on the universally used Hamilton Rating Scale for Depression. (See reference 2 below)
? Reference 2 wasn't a clinical study in humans. Did you mean #1?
-elizabeth
poster:Elizabeth
thread:65538
URL: http://www.dr-bob.org/babble/20010605/msgs/65601.html