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Misc GABA antagonists

elgrego

Greenlighter
Joined
Jul 4, 2016
Messages
8
Hallo
I've been on zolpidem for about a year and although it's the least sedative during daytimefrom the rest of the drugs I've used for sleep,it's still having a calming effect that hinders my well being.
That is ,for the most of the next day I feel drowsy and kinda drunk and not 100% conscious and awake.

Is there a drug or supplement (even better as I could get it myself) that can act to reverse zolpidem's effects in the morning ?
As zolpidem works on the GABA receptor,perhaps a GABA antagonist or blocker ?

Any help appreciated
 
Flumazenil, basically "Narcan for benzos," is for use in medically controlled settings to reverse benzodiazepine overdose, or otherwise when a reversal of benzodiazepines is desired, e.g., in anaesthesia reversal; in psychiatric patients on benzodiazepines receiving ECT, standard practice is to give a bolus of flumazenil to reverse the anti-seizure effects of the BZDs; the flumazenil is short-lived enough that by the end of the postictal phase and once the patient is reverting to baseline the anxiolytic effect of the BZDs is kicking back in. We also use flumazenil among other things (formerly intravenous caffeine, which apparently is no longer available; theophylline is another possibility) to reduce the seizure threshhold period to get better effects of ECT a lower dose of electricity.

This aside, flumazenil outside of these contexts is not a good idea. It might well kickstart you from out of your sedation, but it's quite short acting. Still, theoretically, short T½ aside, it might be enough to get you out of bed, reverse the grogginess until you can get to your morning cup of coffee and the z-drug wears off, but it's still ill-advised, starting from baseline, it's primary effects would be extreme anxiety with a side of possible seizures, i.e., it's pretty much guaranteed to be a bad time and possibly worse if you overshoot your dosage even mildly. Apparently it has been explored to treat sleep disorders, but this is not a currently accepted indication. Besides, it's only available in intravenous formulation. It's not scheduled but I doubt it's easy to source.

Dose your z-drugs at a better time, practice better sleep hygiene, and take your morning coffee. If you need something stronger to combat daytime sleepiness secondary to sleeping pills (or sedating psychiatric medications, as we occasionally use,) I'd suggest modafinil (C-IV and expensive without insurance and prior authorization) or one of it's analogues (quite readily sourced and a bit cheaper), they are quite mild, it has a longer onset than most stimulants, but it will do the job. Due to it's slow onset, it won't help you much initially getting out of bed in the morning—perhaps set an alarm, take your modafinil, sleep an hour, wake up when it kicks in? Something that I've done with some success with other stimulants.


This post is not medical or clinical advice. I make no claim to any professional credentials nor to dispense professional information online. Even if I do possess credentials personally, to which I make no claim, as I have not evaluated you in person, or performed any other clinical assessment, review of your records, overall life situation and the larger context of your illness, psychiatric and medical history, medication history, and many other factors that may impact your situation as described, nothing that I post here can or should be taken as professional advice and furthermore there is no professional relationship established or implied. Anything that I post here is my personal opinion and strictly for informational purposes only and before undertaking any treatments, interventions, or changes to your current treatment, it is essential that you contact your physician or other provider(s), including providing absolute and full disclosure of substance abuse and/or other sensitive issues.
 
Still would suggest modafinil (see my [edited] post above) instead of rooting around for z-drug-reversers.
 
Fasoracetam - GABA B antagonist.

^Adrafinil - modafanil's prodrug - will be easier to get your hand's on as it is not a controlled substance or a prescription and is easily/legally available as a dietary supplement.
 
fasoracetam sounds interesting; wonder if it would defer some of the side effects of OP's complaint, or some side effects I experience with gabapentin. I kind of doubt they would be very pleasant drugs to take though
 
It would definitely work for gabapentin100%. Fasoracetam has a lot of good user reports (negative ones notwithstanding) and is a very popular nootropic. I have some but have yet to try it. My 1 gram tub is still as of yet unused - as my scale is still broken, as I decided to rip it apart while nodding on phenibut for some reason...? :/
 
next ti-me I pick up some random nootropics I might grab some and see. I also currently don't have a functional scale currently; not taking anything currently although I'm considering starting adrafinil on a daily basis, think I might go aheand and take it toright about now actually (I leave for work in an hour or so ...)
 
It's a prodrug so take 300mg and stagger dosages every half hour like you do with gabapentin for optimal absorption/effect. It works best this way I have found. And don't do more that 900/1200, as modafinil is a partial agonist at the D2 receptor (like abilify) so it has antagonistic effect on dopamine in the mesolimbic reward pathway at higher dosages and will block euphoria so there is a ceiling effect! :)
 
I sure would like to try fasoracetam and see how it goes.
How about dosing and mode of use ? (empty/full stomach,etc)

I've tried modafinil through the same doctor that prescribed me zolpidem,but somehow it doesn't feel like it's reversng zolpidem's effects.Jut creates some hyperactivity on my body (increased heart rate,sweat,nervousness,butterflies in stomach) but no hyperactivity on the brain which is what I need mostly.It somehow makes me feel winded and after some time even tired while still leaves me half-awake.I only use modafinil when falling asleep is not an option (night driving).
 
Sublingual is the only way to do it cost effectively as the stuff as really fucking expensive. My one gram was 20 I think. they say to take 10 - 20mg sub three times a day.

I get that two from modafinil. That is due to it's D2 parial agonist activity, which cuts dopamine activity off, via presynaptic autoreceptors.
 
I need the gaba antagonist to help me kickstart my day,will a need to take it throughout the day ? I'm worried it might not let zolpidem work at the end of the day.
 
Adrafinil is easyier and way cheaper to get than Modafinil but metabolises into Modafinil anyway hence it being a pro drug but if you look hard enough you can source Modafinil pretty easily and that's what I would suggest taking.
 
It would definitely work for gabapentin100%. Fasoracetam has a lot of good user reports (negative ones notwithstanding) and is a very popular nootropic. I have some but have yet to try it. My 1 gram tub is still as of yet unused - as my scale is still broken, as I decided to rip it apart while nodding on phenibut for some reason...? :/

Hey just off topic for a sec. I really like your post's and am curious to know what dose of phenibut you take especially one that makes you nod cause i can't say I've ever nodded from phenibut?
 
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