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Re: What is it about Zyprexa that makes it so sedating

Posted by Caleb462 on June 16, 2003, at 18:04:12

In reply to What is it about Zyprexa that makes it so sedating, posted by kotsunega on June 16, 2003, at 16:01:37

> Zyprexa has sedating properties that the other atypical antipsychotics don't share to any real degree. What makes Zyprexa so sedating? I found an Aripiprizole receptor binding chart (http://sl.schofield3.home.att.net/medicine/aripiprazole_binding.pdf) that compares the receptor binding properties of Abilify to other atypical antipsychotics, but I don't see a relationship between the degree of binding for any receptor with Zyprexa, unless it's the 5HT1A receptor for which Zyprexa has a very strong affinity. Could this be what causes it's sedating action?


You're looking at the chart wrong, the HIGHER the number, the LOWER the affinity. Small numbers signify high affinity.

So, looking at it now you'll see... Zyprexa is a fairly strong ANTAGONIST at EVERY dopamine receptor. Where as the other atypicals display strong affinity for a couple of dopamine receptors, and somewhat lesser affinity for the others.. I think this plays a part.

You'll also see that zyprexa is the strongest anti-histamine, other than clozaril, out of the bunch. It's also tied for with clozaril for most anti-chollinergic, and it's anti-adrenergic effects are pretty strong too. Overall, it works out on paper as the most sedating atypical.


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