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Re: Anticholinergic side effects

Posted by mtdewcmu on April 2, 2011, at 17:41:35

In reply to Re: Anticholinergic side effects, posted by desolationrower on April 2, 2011, at 14:54:22

> there is some activity of metabolites at some nicotinic receptors, but i really doubt that has something to do with 'cholinergic' side effects like dry mouth, heart rate, problems urinating, etc. cholinergic effects are usually more related to muscarinic receptors.
>

Goodman and Gillman lists the inhibition constant for bupropion at DAT as 526nM, and at muscarinic receptors as 40,000nM. So, bupropion would not appear to be a very potent antimuscarinic. But the numbers for active metabolites are curiously absent, even though the exposure is greater. The hard numbers that would settle this one way or the other are strangely hard to find.


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