Dose related SERT inhibition

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Vercingétorix
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Dose related SERT inhibition

Unread post by Vercingétorix »

Hi I've found this article :
https://thelastpsychiatrist.com/2007/07 ... st_im.html

I f you don't want to read it, you can just look the chart that shows striatal 5htt occupancy related to the dosage of citalopram (celexa). So we can see that if you go from 1 mg to 20 mg of citalopram the difference is huge, you go from 20% to 80% of 5htt occupancy. But if you increase the dose from 20 to 40 or even 60 mg, the difference is very small. In fact the decrease or decrease of the dose of citalopram has the bigest impact if you make changes when you are in the 0 - 10 mg range, and from what I've understood, it is the reason why it is advised, when you make a tapper off, to go more slowy when you reach small doses.

Well, that is what this article says... Do you think this article is true, and the chart correct ?
In my case, I saw a big change when I went from 60mg to 20 mg citalopram, so I don't know what to think.
sovietxrobot
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Re: Dose related SERT inhibition

Unread post by sovietxrobot »

Makes sense to me. Drug effects are often nonlinear.
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succubus76
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Re: Dose related SERT inhibition

Unread post by succubus76 »

Yes once you get % of blockade more of the drug will only give you more side effects.
Regarding sert inhibition paroxetine is the strongest of all and has the most sexual side effects complains.
Effexor is more weak at sert and might not cause as much sexual dysfunction and even his NET blockade might increse orgasms potency
Vercingétorix
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Re: Dose related SERT inhibition

Unread post by Vercingétorix »

Thanks, that's interting. So the antidepressant effect starts when 80% of SERT occupancy is reached.
Tree
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Re: Dose related SERT inhibition

Unread post by Tree »

We need a study that shows ssri's can permanently inhibit sert. My guess would be if they researched pssd that's what they would find.
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succubus76
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Re: Dose related SERT inhibition

Unread post by succubus76 »

Tree wrote: Sat May 01, 2021 5:56 am We need a study that shows ssri's can permanently inhibit sert. My guess would be if they researched pssd that's what they would find.
It doesnt, even if they irreversible antagonist sert, the body Will make new receptors as in the case of some irreversible antagonist drugs there.
Tree
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Re: Dose related SERT inhibition

Unread post by Tree »

succubus76 wrote: Sat May 01, 2021 4:27 pm
Tree wrote: Sat May 01, 2021 5:56 am We need a study that shows ssri's can permanently inhibit sert. My guess would be if they researched pssd that's what they would find.
It doesnt, even if they irreversible antagonist sert, the body Will make new receptors as in the case of some irreversible antagonist drugs there.
All of my experiences align with sert/5ht1a desensitization theory. I can trust my experiences because their consistent and extreme. If there are epigenetic alterations at the serotonin transporter by ssri's that could explain permeant down regulation. There could also be another mechanism not yet discovered. Researchers have only just discovered central binding sites where Citalopram attach.

I read that sert inhibition is time dependent too.

https://als.lbl.gov/antidepressants-blo ... transport/
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