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Question for chemist on benzos (experts) + MORE.

Posted by jlbl2l on April 22, 2004, at 3:21:24


you seem quite knowledgable on many medicines, (and I am trying to become a qualified expert myself) so I thought I'd ask some questions or re-affirm some things that I may be wrong at. I may append more to this post later and I would like to continue discussion of other things if I find this helpful.

First, Klonopin and Xanax (in general) have both roughly the same equivalency at dosage of 0.5mg, however xanax has a much earlier onset of action and hit's a slightly different subset of gaba-a receptors creating the quicker and more "high" feeling in most people. It also seems to be more of a relaxant probably hitting what, i think c subtype of the gaba-a - is for muscle relaxant properaties? Anyways, Xanax metabolies into oxazepam , like almost every benzodiapine, correct? So when I take Ativan, or Xanax, or (another common benzo (not klonopin though) it is actually just oxazepam that i would be taking, correct? In most drug tests, they usually only test for oxazepam (unless special tests are ordered) since almost all benzos metabolize into it. Anyways, My comparison here is Klonopin vs Xanax and the tolerance vs the 2 and effectiveness vs the two and the metabolites vs the two. I am aware Klonopin converts uniquely (amoung only a few others benzos) to its specific form of 7-amino-clonazepam rather than most benzos which convert to oxazepam. Question -> Does this effect the feeling of the benzo in any way? I know this would effect a drug test, but would it convert AFTER or BEFORE the binding, do you understand what I am saying? Second thing, is that Klonopin seems to also have an antidepressant effect like xanax, but it wears off after you gain tolerance. It seems this has been established through interactions through 5HTP/SEROTONIN interactions. Can you explain how benzos are helping in this (speicfically), and why klonopin eventually stop's working, while xanax, doesn't seem to from what i have heard. Could it be the half life factor; in that its harder to gain tolerance to xanax? Also, For Klonopin, What Gaba-A subtype receptors does it hit the most. Obviously, we know it hits the anxiolytic subset and the (hypnotic areas-as most benzos do) but it doesnt do much for muscles (for me at least). I guess this is why it is an ideal agent for social phobia, esp the long half life and anti-d effects. Can you just "babble" for me a bit (feel free to go into very,VERY much chemical and technical detail such as ion channel, calicum influx, potassium blockage etc.. and such as I understand most of this, I study neuropharmcology and neurochemistry but from your posts it seems you could aid in my knowledge. Also I am HIGHLY interested in pregablin and neurontin ( I know how they generally work, but I would like to know a lot more on why they aren't scheled subtances LOL (in your opinion). I mean, they work through calcium influx mechinisms correct? but they work throughout the entire body, not just the brain , so they work at all levels , hence the benefit to neurpathic pain and fibro patients etc.., those substances interest me the most actually because of the possibily of no downregulation or upregulation, though, i know thats probably impossible. Thoughts on topamax would be nice as well, especially its glutamate blocking properaties (and where it blocks it to IE NMDA ?), and its whole "brain" level of raising gaba and how it does this and what does it do with NP-Y and the other factors - I know theres 2 other hormone like factors it effects that are related to sleep, eating and behavior. Anyways. Thanks again


neuropsychopharmacology researcher




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