Microdosing Flumazenil

[TheLightBringer]

Has anyone tried microdosing the selective GABA A receptor antagonist flumazenil? Im curious if the long term microdosing of flumazenil and eventually increasing the dosage would upregulate GABA receptors to the point of a noticeable difference in well-being ie less stress and anxiety.

From wikipedia:
”In vitro studies of tissue cultured cell lines have shown that chronic treatment with flumazenil enhanced the benzodiazepine binding site where such receptors have become more numerous and uncoupling/down-regulation of GABAA has been reversed.[19][20][21] After long-term exposure to benzodiazepines, GABAA receptors become down-regulated and uncoupled. Growth of new receptors and recoupling after prolonged flumazenil exposure has also been observed. It is thought this may be due to increased synthesis of receptor proteins.[22]”

Im unsure if dosing flumazenil long term would lead to any significantly increased effect from endogenous gaba and similar neurotransmitters and neurosteroids affecting gaba or if the extent of it is just more of a ”reset” to receptors that have been damaged by GABA agonist abuse.

Anyone with more experience or knowledge who knows if microdosing flumazenil would have desirable benefits?

 

[negrogesic]

For the purpose of benzo withdrawal, the protocol is a short period of treatment via infusion: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4014019/

Note that flumazenil has a short half-life and must be administered as an injection (usually as an infusion due to short half-life).

Additionally, having some weak partial agonist action on GABAA, daily microdosing is probably a bad idea since it could, in theory, downregulate GABAA with daily use.

But even if were to be microdosed, it would have to be done via injection, and a single dose wouldn't make much sense due to the extremely short half-life.

So microdosing flumazenil doesn't make a whole lot of sense. Nor has anyone here tried it here because it is hard to come by and again must be administered by injection. It is also tricky to dose.

I would be interested myself in getting a course of flumazenil infusions for benzo withdrawal PAWS. But not much chance of finding a doctor in the US who would do that. Need to travel to Europe for that.

 

[TheLightBringer]

Finding flumazenil online is not super difficult if you know where to look, and 4 subq injections per day should be manageable I was pinning 4 - 6 subq peptide shots per day at one point. (Edit, just looked up again how truly short flumazenils DOA is IV seems to be up to 1h so idk if 4 subq shots would be enough per day hmm) Its definetly possible if you wanna go through the trouble but Im unsure if it would yield any worthwile benefits in the long term. Hoping that someone with experience will answer. I have found a few using it daily on reddit however for other purposes.

Additionally, having some weak partial agonist action on GABAA, daily microdosing is probably a bad idea since it could, in theory, downregulate GABAA with daily use.

Im not sure I follow are you saying that using only flumazenil daily in theory could downregulate GABAA or just the partial agonist?