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Re: imipramine ) Inhibition of 5-HT Uptake Pump (%)

Posted by sowhysosad on September 15, 2009, at 22:00:46

In reply to Re: imipramine ) Inhibition of 5-HT Uptake Pump (%), posted by Brainbeard on August 18, 2009, at 4:31:06

> I can't find it right now, but Dr. Ken Gillman had a table suggesting that imipramine was in between citalopram (Celexa, less strong) and fluvoxamine (Luvox, stronger!) as for SRI potency.

According to Preskorn it has less affinity for the serotonin uptake pump than all of the SSRI's but is equal to venlafaxine.

> I have been wondering myself how much imipramine would be necessary to reach the usual 80% 5HT receptor occupation. I don't know how 5HT receptor affinity relates to drug concentration, but if 50mg of citalopram is enough to reach about 80% 5HT occupancy, and 150mg of fluvoxamine is enough, and imipramine ranks in between, might it be that about 75mg of imipramine might be enough for some serious SRI? Or am I being an irresponsible amateur dumb *ss here?

It has stronger affinity for the noradrenaline uptake pump than for serotonin. Presumably you'd need to achieve almost 100% occupancy of the noradrenaline pump before the serotonin kicked in.

Certainly when I took 150mg I felt the agitated panicky noradrenaline effects but couldn't discern any serotonin.

It's active metabolite, desipramine, is also an NRI not an SSRI/SNRI, so I wonder if that would also affect things?


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poster:sowhysosad thread:909605
URL: http://www.dr-bob.org/babble/neuro/20090701/msgs/917310.html