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Re: Best Opioids for social fear? - Experiences jerrympls

Posted by Chairman_MAO on May 6, 2005, at 9:53:57

In reply to Re: Best Opioids for social fear? - Experiences, posted by jerrympls on May 3, 2005, at 22:40:08

I would definitely go with buprenorphine for depression first. You see, buprenorphine is a kappa antagonist; dynorphin stimulation of the kappa receptor can induce depression and dysphoria via inhibition of DA release in the VTA (the picture I'm sure is more complicated than my understanding of it). That is the opposite effect of the mu-1 receptor, stimulation of which releases more DA in the VTA (sounds like a rap lyric, doesn't it?)

I'm not positive, but hydrocodone I think has kappa agonist activity. Buprenorphine is also a mu partial agonist, which means that it can stimulate the mu (euphoriant/mood boosting/analgesic) receptor to a point past which it does little more, and then in higher doses still, acts as an antagonist. Thus, it has virtually no abuse potential except in opioid-naive users, who will build a tolerance to the "nod", etc. within 3-5 days and will not be able to escalate the dose any higher as they could with traditional opioids (although the "ceiling" dose is equivalent to 30mg IV morphine, so it's not as if it is THAT weak, heh). Buprenorphine's mechanism of action is extraordinarily complex and a full account is somewhat beyond my understanding of the subject and way beyond the scope of psychobabble.

I tend to think of buprenorphine as an "opioid system stabilizer" first and an analgesic second. That is, it does have activity that's like traditional opiates/opioids, but it also has a pharmacological profile that allows it to provide a limited yet sustainable mood boost while minimizing the risks, such as dependence and respiratory depression. It's really phenomenal stuff for psychiatric problems.

You can always switch to something "stronger", but I'll bet you'd find buprenorphine more effective in the long run. You'd probably also experience fewer side effects. After being at the ceiling dose for 2 weeks (been on it for about 5 weeks now), I barely even have any constipation or any S/E from it at all.

I believe it also is devoid of the endocrinological side effects common with many other opioid drugs, such as methadone, but you'll hvae to double check on that one.

> I'm on hydrocodone for depression. yes, I have a pdoc who finally prescribed it for me. However, I'm wondering if buprenorphine would work better???? Any literature anyone can point me to?
> Thanks
> Jerry




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