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Etizolam is strongly Inhibited by both CYP2C19 and CYP3A4 according to this Study?

Thomas29

Bluelighter
Joined
Oct 25, 2010
Messages
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There are not much studies done on Etizolam but the main ones I read which these were just the top picks from Google is that CYP2C19 which I was told by a Moderator it is useless for anything besides Valium for Inhibition which doesn't seem to be the case... It feels like I am getting recycle from recycle answering sources lol.


I MAY have read the Study wrong as I simply don't have time to be reading about Etizolam Inhibition it is not on my Agenda for the last 2 Hour I got left in my day I mean 45 Minutes now.
 
Biotransformation of etizolam is extensive and involves hydroxylation and conjugation 9. The main metabolite formed via 1'-hydroxylation is α-hydroxyetizolam which retains pharmacological activity comparable to that of the parent drug, indicating that the action of metabolites may contribute to the clinical effects of etizolam. CYP3A4 is predicted to be the main CYP enzyme responsible for mediating etizolam metabolism. CYP2C18 and CYP2C19 are also involved in the metabolic pathways.

From this it seems to imply that CYP3A4 does most of the 'heavy lifting' but that inhibition probably wouldn't do much as the metabolite that is created is active as a benzo, i.e. metabolism by CYP3A4 does not 'deactivate' etizolam.

The other CYP enzymes probably play minor roles in metabolism and are therefore less worth worrying about.

you said:
I simply don't have time to be reading about Etizolam Inhibition it is not on my Agenda

And yet here you are posting a study you went out of your way to find.
 
No i am posting a study I came across when googling something totally irrelevant to etizolam and yet you continue to assume things... This feels kind of personal dude. I even specifically posted in the OP that this Studies are just from Me googling it and copy and pasting them from the "top of the google search page" how is that going out of my way to research it lol I came across it remembered it and thought I'd ask about it?


Did you simply read the studies I copied and pasted since that is not exactly the most thorough studies not that I would know which ones are the most thorough hence I came to ask about it?
 
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For the record what I was looking at wasn't the link above it was this:

(I think it's been 2 years lol)

I stumbled upon this. I found it interesting... including the info regarding etizolam.

revised review benzodiaz CDM - Zenodo

https://zenodo.org › record › files › article

PDF
A study has found that rectal administration of bromazepam increases the drug. AUC by 70% and its Cmax by 60% with respect to oral administration [34].

(The Authors suppose that this effect is due to a lack of degradation of bromazepam by this route. The drug metabolism presumably involves cytochrome P450, since it is inhibited by fluvoxamine [35], however the specific subtype has not been clearly identified. In fact, fluvoxamine is a potent inhibitor of CYP1A2, a less potent CYP3A4, 2C9 and 2C19 inhibitor, and a negligible inhibitor of CYP2D6. However, CYP3A4 probably is not the responsible enzyme, since itraconazole does not affect)


Thank you for the reply btw.
 
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