• Neuroscience & Pharmacology Discussion Welcome Guest
    Posting Rules Bluelight Rules
    Recent Journal Articles Chemistry Mega-Thread
    FREE Chemistry Databases! Self-Education Guide

  • N&PD Moderators: Skorpio

Flumazenil for anxiety

Charles Ferdinand

Charles Ferdinand

Bluelighter
Joined
Apr 29, 2009
Messages
323
Location
Rocky Point, México
Hi! I've always suffered from Genaralized & social anxiety disorders, with the ocassional obsessions and panic attacks. That's why I started to use alcohol, which to led to me being prescribed klonopin by some stupid psychiatrist.
I was addicted to benzos for 5 years and suffered through the classical dangerous symptoms: depersonalization, seizures, insomnia, etc. for at least 2 months, but am clean now.
My anxiety disorder was originally quite severe: had to get drunk to go to high school and then had to drop out of two different universities (before any drugs or psychiatrists). Was secluded in my home for the last couple of years doing things as turning the lights off after sunset for fear of someone coming by and seeing me.
Anyway, I'm much better, finished school, got a job but I'm still not ok from the benzo wd, so my question is, now that I'm clearly off the brutal GABAergic wd's, you think I could us some flumazenil IV to, maybe "reset", my receptors? Could it even work somewhat for anxiety?
Perhaps some ketamine (NMDA) and topiramate (AMPA/Kainate) would be in order, too?
Any other meds, wouldn't work: back in the day I tried olanzapine, risperidone, paroxetine, escitalopram, levomepromazine, venlafaxine, bupropion, fluoxetine, moclobemide, amitryptiline, alprazolam, bromazepam, clonazepam, propranolol, phenobarbital, ziprasidone, amisulpride & sulpiride (both low dose for social anxiety), memantine, amantadine, pregabalin, gabapentin, kava, and many others I don't remember from 5 psychiatrist, plus 7 different therapists, and amphetamines or opiates are out of question and have never tried them. (To be fair, pregabalin, barbs and benzos worked incredibly well, until they just didn't...) Pregabalin works amazingly again when combined with an nmda antagonist and gabapentin, but I also need benzos for this to work, and they just don't nothing to me anymore.

And btw, I (AMAZINGLY, I must say) got better by forcing myself to get an easy job and then socializing (though the first couple weeks I did had to use a low dose of tramadol).
I also have a friend of mine who's a doctor and is able to get the flumazenil, topiramate and ketamine, could administer those to me, if I tell him to, but he admits he doesn't know shit about psychopharmacology.

Thanks in advance.
Charles.
 
We're really not big on psychiatry threads in ADD, however if you can find some journal articles relating to the topic I'll leave it it open.

EA
 
not looking for a cure to my diseases, just asking if flumazenil and glutamate antagonists might be a good possibility to somewhat "reverse" my benzo tolerance and PAWS, everything was just kind of background information.
 
I've read some supposedly experimental reports suggesting that some doctors utilize flumazenil with a ketamine iv drip for patients that have a protracted benzodiazepine withdrawal syndrome (the epitome of hell if you ask me). I imagine that such a procedure is anything short of absolutely fucking horrifying, especially for someone with down-regulated gaba-alpha receptors. I have also read of a couple reports of people that have undergone the procedure... whose veracity is questionable, but some of which stated that they have received some positive results. I would avoid this procedure at all costs, because as ebola? says, such a procedure is very likely to cause excitoxicity, which can cause relatively widespread nerve cell death, since both NMDA antagonists and gaba-a antagonists are excitoxins.

I have a few friends that have experienced a protracted benzoidazepine withdrawal syndrome (mine wasn't too protracted, fortunately)... some of them found kratom helpful to ease suffering in some way (it can paradoxically help with insomnia, depression, low energy, anxiety, etc)... though they did wait until they could tolerate light stimulants. From personal experience I suggest you avoid NMDA antagonists until you have fully recovered, as they are EXTREMELY unpleasant during benzodiazepine withdrawal, not to mention dangerous due to your already greatly reduced seizure threshold.
 
Yeah...flumazenil therapy could be conducted more safely under medical supervision, as interventions may be made if seizures occur.

ebola
 
I was under the impression that ketamine was an anesthetic and neuroprotective agent by virtue of its NMDA antagonism, but I'm also aware that you just can't put someone out with ketamine IV, mechanical ventilation and all AT HOME. Hence the low dose, or it could be any other NMDA antagonist such as memantine, plus the topiramate. I do get why flumazenil would cause excitotoxicity, but again I wasn't thinking of a big dose.
Regards,
Charles.
 
Ketamine only selectively suppresses glutaminergic transmission, and we can't assume it to completely counteract glutaminergic overexcitation via GABA-A antagonism (or in this case, an antagonistic allosteric modulator). GABA-antagonists tend to be nasty, horrifically unpleasant, physically dangerous drugs (think of them as inducing high-level benzo withdrawal, including seizures).

An onsite clinician will be necessary to ensure proper, dynamic calibration of the dose of flumazenil and the adjunct agents which temper its effects.

ebola
 
ebola? said:
Ketamine only selectively suppresses glutaminergic transmission, and we can't assume it to completely counteract glutaminergic overexcitation via GABA-A antagonism (or in this case, an antagonistic allosteric modulator). GABA-antagonists tend to be nasty, horrifically unpleasant, physically dangerous drugs (think of them as inducing high-level benzo withdrawal, including seizures).

An onsite clinician will be necessary to ensure proper, dynamic calibration of the dose of flumazenil and the adjunct agents which temper its effects.

ebola
Click to expand...

Would using flumazenil in the case of a benzodiazepine overdose still cause excitotoxicity? I'm assuming it might be dose-dependent?
 
It would be highly dose-dependent and somewhat unpredictable, but something that would be doable in a clinical setting.

ebola
 
As in absinthe? They chose flumazenil specifically to somehow "reset" the bzd allosteric sites.
For other purposes thujone might work but Tramadol would be milder, and nicer too (GABAa antagonist also).
 
What about imidazenil (http://www.ncbi.nlm.nih.gov/pubmed/8394902)? Come on, its structure is so similar to benzodiazepine agonists that it can't take ages to evaluate its toxicity. I would be fearful now to take a partial agonist as there's no way to assess the measure of the mess in my GABA system. But I know how hard tapering down is and how much time it took me to get off. 9 years on benzodiazepines and half of that was thinking how to quit.
 
It might be related to tramadol's penchant for seizures at higher doses.

The GABA antagonistic effects might only be significant at 400mg or higher.
 
From what I have read about flumazenil, it only has an effect when an individual has benzos in their system. My impression of things was that flumazenil doesn't act like a typical GABA antagonist (such as a β-carboline) at all, and this is what makes it particularly useful. Isn't the idea that patients suffering PAWS long after the actual active BZD ligand is out of their system can receive great benefit from flumazenil therapy, with the theory being that it can somehow reset the receptor to its normal functional state? Forgive me if I've gotten this totally wrong, as I have less knowledge regarding the nuances of GABAergics than I do in other areas of neuropharmacology. That being said, please correct me if I totally bungled things up here.
 
You must log in or register to reply here.
Top