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Re: Can serotonin reuptake inhibition be countered?

Posted by Brainbeard on July 2, 2009, at 8:13:31

In reply to Re: Can serotonin reuptake inhibition be countered? » Brainbeard, posted by garnet71 on July 1, 2009, at 8:48:20

> Hey thanks for the information...Are there any articles you can point me to that discuss this further?
> ________________________________
>
> Low dose Prozac raises noradrenaline and dopamine levels in certain parts of the brain more than inhibiting serotonin reuptake. Even a 2.5mg dose would be enough. Some people got good results with even less. Buspar, perhaps unexpectedly, when taken in combination with Prozac, helps to raise DA and NA levels even more. So your doc might be right. The thing is that this stimulation is not very likely to help with anxiety in the long run.
> I was on such a low dose of Prozac + Buspar myself for a while. I gained weight on it very fast though.
>

Yeah: 'Low dose Prozac raises noradrenaline and dopamine levels in certain parts of the brain more than inhibiting serotonin reuptake': first of all, check this link: http://www.lef.org/protocols/prtcl-165a.htm and scroll down to the 'Listening to Prozac'. There you'll find some evidence for even very low doses of Prozac to have an antidepressant effect. Stahl's Essential Pharmacology Online briefly summarizes the probable cause for this in the following link http://stahlonline.cambridge.org/prescribers_drug.jsf?page=0521683505c32_p183-188.html.therapeutics&name=Fluoxetine&title=Therapeutics as follows: 'Fluoxetine also has antagonist properties at 5HT2C receptors, which could increase norepinephrine and dopamine neurotransmission'. Elsewhere he expresses himself more strongly, but that was a presentation I gained acces to yesterday but thah I couldn't bookmark since it appears to be a subscription page. This is the link: http://cme.medscape.com/viewarticle/484929 Anyway, on low doses, Prozac doesn't do much SRI yet, but it's a strong 5HT2C-antagonist. 5HT2C-receptors inhibit dopamine and noradrenaline release, so blocking them 'disinhibits' DA and NA.
STahl in mentioned presentation (I could gain access through google): 'Have you ever given a dose of fluoxetine (Prozac) to a patient and had them have an activation? Fluoxetine is the only other drug that has powerful 5HT2C antagonist properties [not true; Zyprexa is a stronger 5HT2C-antagonist; sertindole is even stronger; and the newer AD agomelatine is also a (strong?) 5HT2C-antagonist - but that's a very recent drug (BB)] in fact, fluoxetine has more powerful antagonist properties than reuptake blocking properties.'

'Buspar, perhaps unexpectedly, when taken in combination with Prozac, helps to raise DA and NA levels even more': http://cat.inist.fr/?aModele=afficheN&cpsidt=2585906

The reason I gained weight rapidly on a low dose of Prozac must precisely be because it's a potent 5HT2C-antagonist: http://jop.sagepub.com/cgi/content/abstract/20/4_suppl/15. I hadn't expected this, since I didn't know about the 5HT2C-antagonism (only that Prozac raised DA and NA) and thought that without significant SRI, it wouldn't make me gain weight.


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poster:Brainbeard thread:901465
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