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For serious 5ht2C-antagonism, LOW doses are needed

Posted by Brainbeard on April 6, 2011, at 2:26:19

In reply to Re: It seems Ago + Prozac is the perfect match BUT..., posted by desolationrower on April 5, 2011, at 21:28:16

> not sure which of the two drugs. But you need a highish dose of prozac/fluoxetine for the 5ht2c to be significant.

The very opposite is true in this case! You need a low dose of Prozac for the 5ht2C-antagonism to be significant.

This is why: serotonin receptors have to be (nearly) saturated by a reuptake blocking molecule for SRI to reach clinical significance. 5HT2C receptors, on the other hand, only need a little antagonism to result in significant effects (boosted dopamine and noradrenaline, basically). On top of that, 5ht2C-antagonism and SRI are opposing mechanisms. At normal and higher doses of Prozac, the 5ht2C-antagonism is lost since it is flushed away by all the serotonin that begins to agonize 5ht2c-receptors (as well as all other serotonin subtype receptors). This is borne out by the fact that Prozac, in high doses, can be used as an agent against bulimia since it suppresses - which is an effect of 5ht2C-agonism.

For reference/evidence, see I've written about this before in this post:

Current meds: clomipramine 225mg, fluvoxamine (Luvox) 50mg, dexamphetamine 5-10mg, bethanechol 20-60mg. As needed/wanted: oxazepam 5-20mg.




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