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Re: 5H-T 2A blockers and sleepiness

Posted by john Henry on August 1, 2003, at 21:50:44

In reply to Re: 5H-T 2A blockers and sleepiness » jemma, posted by zeugma on August 1, 2003, at 19:44:49

Actually most of the heavy sedation from these drugs comes from their blockade of the histamine-1 receptor.But yeah 5ht2a does cause sleep improvement.Sedation or sleepiness is mostly caused by:
1-blockade of histamine-1
2-blockade of 5ht2a
3-blockade of Alpha-1 NE receptor

Remeron,Elavil,Seroquel,Zyprexa etc. are all VERY sedating because of their most potent site is the Histamine receptor.

The difference between Serzone and Trazodone,which is it's parent drug,is Serzone doesnt have the effect on the Histamine-1 receptor.It is not nearly as sedating.But like Trazodone,it has to be taken 2-3x day which can make some sleepy throuout the day.It is also known for having much dizziness.If you want something that blocks 5ht2a....Remeron and Zyprexa are 2 drugs that have a most potent effect on 5ht2a.Your best bet would be to try Remeron.

Remeron:
-Only taken once at bedtime
-dosent have the side effects of the TCA's
-In vitro studies show it's a little better at getting the 5ht2a than serzone.
-It is very sedating but,you can get used to it in time with little to no drowsiness the next day.
-Has less drug interactions


Here is the difference:

Serzone:
-blocks 5ht2a
-blocks Alpha-1 NE
-weak 5ht uptake inhibition

Remeron:
-Blocks-histamine-1
-blocks-5ht2a
-blocks-5ht2c
-blocks-5ht3
-blocks-Alpha-2 NE

The only major difference is Serzone has Serotonin inhibition.It is very weak though because even at 300 mgs of serzone,it doesnt appear to even have the effects of an SSRI at its lowest dose.
The TCA's seem to have to many sides to try first. Take care


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poster:john Henry thread:245623
URL: http://www.dr-bob.org/babble/20030728/msgs/247491.html