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Re: HELP - BUSPAR, part 2: total confusion! Tony P

Posted by SLS on December 4, 2003, at 6:54:10

In reply to Re: HELP - BUSPAR, part 2: total confusion!, posted by Tony P on December 4, 2003, at 3:48:03

> Scott: [much good info clipped] I believe people attribute buspirone's antidepressant activity to its metabolite, 1-PP, which is a NE alpha2 antagonist (i.e. yohimbine), which are presynaptic and increase the release of norepinephrine. ...

Thank you! I completely forgot about that!

Unfortunately Remeron and idazoxan worsen my depression, otherwise I probably would have tried Buspar by now. The 1-PP thing happens with gepirone too. For me, that sucks, but for you, perhaps it is a cleaner drug. Gepirone was close to getting approved last I heard. The 5-HT1a agonist that I would like to have seen developed is flesinoxan. It isn't metabilized into 1-PP.

> This metabolite is actually found in much greater concentrations in the blood after buspirone than the unchanged drug itself. That probably explains why I always get the activating effect about 2 hours _after_ taking Buspar, when the slightly dopey feeling wears off.

Do you think the dopey feeling is due to DA D2 blockade? Gepirone is supposed to be free of that.

> BTW, I have always had an immediate activating and stress-reducing response to Buspar, although it's a moot point now since I take it regularly (20-30mg/day).

Hmmm. Maybe I should give it a try at some point - maybe with Effexor.

> It used to _prevent_ me from sleeping, so I always took it morning & noon, but lately it has made me sleepy if I am lying down in a quiet place. Our bodies just keep on adapting....

I wish my body wasn't so adaptive. When once I responded robustly to a combination of Parnate + desipramine, now it is of little help. I have had numerous 3-day responses to antidepressants, only to have my system adapt to them and allow me to relapse.

Thanks for posting.

- Scott




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