# Downregulation of Gaba receptors



## DavidPT40 (Jun 11, 2006)

Benzodiazapenes, along with alcohol, facilitate the binding of Gaba with its appropriate receptors. I believe they act as ligands, enhancing the receptors' functions.

However, long term use (of alcohol or benzodiazapenes) does cause a loss of these Gaba receptors. Does anyone know of any studies that show how long it takes to return to previous receptor levels once either of these drugs has been stopped?


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## crayzyMed (Nov 2, 2006)

That can take pretty damn long, seems even semi permanent in many cases, however NMDA antagonists work to upregulate GABA receptors and ppl use them to aid withdrawals.


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## Recipe For Disaster (Jun 8, 2010)

crayzyMed said:


> That can take pretty damn long, seems even semi permanent in many cases, however NMDA antagonists work to upregulate GABA receptors and ppl use them to aid withdrawals.


are you sure about this? any idea how to do it? i have access to ketamine and am experiencing proctracted benzodiazepine withdrawals. are you telling me that ketamine could help?


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## bben (Oct 24, 2009)

I would go with an anticonvulsant, most can dose dependently raise GABA concentrations. I would avoid strong nmda antagonists like ketamine. 

Alcohol and benzodiazepines hit different gaba receptors with benzodiazepines being worse for permanent down regulation. 

So id go with anticonvulsant if it was me or i would wait it out.


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## Recipe For Disaster (Jun 8, 2010)

why would you avoid ketamine?


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## crayzyMed (Nov 2, 2006)

Recipe For Disaster said:


> are you sure about this? any idea how to do it? i have access to ketamine and am experiencing proctracted benzodiazepine withdrawals. are you telling me that ketamine could help?


Read my thread guys:


> Well I am down 50% on my valium now but its not comfortable - I may have to go back up or increase the memantine or add Delsym or something.
> 
> I get the distinct impression that DXM is more effective for benzos than memantine is but at the same time, I was taking 60mg of Delsym twice a day versus taking 20mg of memantine twice a day so maybe I just need to go up in the mem dose.
> 
> ...





> I tend to have any adverse reaction that is clinically possible - my body really dislikes pharmaceutical drugs so don't take my word as the final word, it was more a word of caution - but cardiac events do appear to be a problem with memantine.
> 
> I switched to DXM starting last night by taking 5mL of Delsym at midnight. I then SKIPPED my Valium dose and took another 5mL at 6AM then fell asleep about 11AM. I woke up about 3PM, which meant I missed my afternoon dose of Valium as well and then about 4:30 I finally took 5mg of Valium and that's all I've had today. I took another 5mL of Delsym when I woke up and another 5mL at 7:30 or so and will take another 5mL at midnight. Normally I'd have taken 20mg of Valium in this time period so there is definitely something to dextromethorphan versus memantine. I should also note that I have experienced no respiratory suppression or heart abnormalities since I stopped taking the memantine, even with the extreme decrease in Valium.
> 
> ...





> I took Alprazolam for 3 years, then went through accidental cold-turkey withdrawal because the local pharmacies weren't carrying any (happens where I live occasionally, sucky country/city). I experienced severe withdrawal symptoms including paranoia and transient psychosis but soon I got again on Alprazolam and thankfully didn't have a seizure. During that period I was completely tolerant to 2 mg Alprazolam's both sedative and anxiolytic effects.
> 
> Since I started taking Memantine, the tolerance was reversed somewhat and 1 mg was anxiolytic and practical enough for social anxiety disorder. 2 mg was very effective sedative. Tolerance didn't develop any further from this point on.
> 
> When I began tapering off Alprazolam for good, I was on 2 mg/day and the withdrawal was pretty negligible, only symptoms were irritability and slight sense of panicking, despite the rapid taper process.





> I'm totally getting similar results from Huperazine A. I've been taking 100 mcg twice daily for 4 days. I wonder if anyone else can relate to this w/r/t huperazine.
> 
> In case it's of interest to you, I've cut my alprazolam consumption in half. Not because I'm trying to give it up but because it's suddenly too potent. FWIW I have a 6-year daily alprazolam habit.


http://www.bluelight.ru/vb/showthread.php?t=501875

I recommend to read the whole thread for more information and to get an idea on dosing, it seems that DXM is capable of reversing tolerance while memantine rather just slows tolerance, which is probably because DXM hits the same anti addiction receptor as wellbutrin (memantine hits nicotinic receptors too but differend one's.)

A course of DXM certainly wont hurt to try, and then well have some more experiences too.

Regarding the cardiovascular stuff with memantine, it appears to slow down heartrate in some very rare cases, however some caution when combining it with depressants like opiates can be a good idea (get a heartrate monitor or something) and it also appears to potentiate the heartrate increase caused by serotogenic drugs like MDMA in some people.


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## 49erJT (Oct 18, 2010)

0


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## DavidPT40 (Jun 11, 2006)

My doctor still prescribes me Klonopin. However, since I began taking 2mg/day of klonopin, if I go 24 hours without taking any, I have difficulty breathing. Its the main symptom of the panic attacks I was having (which is why I began taking klonopin in the first place).


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## Recipe For Disaster (Jun 8, 2010)

crayzyMed said:


> Read my thread guys:
> 
> http://www.bluelight.ru/vb/showthread.php?t=501875
> 
> ...


i read the entire thread at bluelight and i made a post over there. can you recommend a dose to start with?


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## crayzyMed (Nov 2, 2006)

Recipe For Disaster said:


> i read the entire thread at bluelight and i made a post over there. can you recommend a dose to start with?


30-60mg 2 or 3 times a day.


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## Recipe For Disaster (Jun 8, 2010)

how long should it take for results to become apparent?


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## crayzyMed (Nov 2, 2006)

Recipe For Disaster said:


> how long should it take for results to become apparent?


After a few days allready, keep us updated!


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## MBL (Oct 5, 2010)

re: DXM & NMDA drugs

I was considering low low doses of that maybe.
My problem is I wonder if it interacts with other drugs.

Such as anti-psychotics & Lyrica... anybody have any info on this?

thanks..


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## crayzyMed (Nov 2, 2006)

MBL said:


> re: DXM & NMDA drugs
> 
> I was considering low low doses of that maybe.
> My problem is I wonder if it interacts with other drugs.
> ...


DXM will only interact with other serogenics.


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## crayzyMed (Nov 2, 2006)

For those that try it consider updating my thread on bluelight, some more reports would be great.


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## crayzyMed (Nov 2, 2006)

> Originally Posted by RigaCrypto
> Do you think methoxetamine would lend itself to use as an anti-depressant in repeated low doses in the manner possible with ketamine?
> I can't compare it with ketamine but can say MXE does work in this way. When I first got it I only used it only like this for almost a week. 2-5mg doses every few hours seemed to work quite well as a mood stabilizer/antidepressant.


Same guy explaining:


> The reason I had tried the small, regular doses was to try to manage a hyperactive glutamate system due to gabaergic dysfunction caused by past benzodiazepine use and withdrawal. It did help with some of my symptoms and I eventually realized that it worked better for me when used less often and in larger doses. I thought that maybe the less often dosing worked better because I am sensitive to things, but maybe its not me and just the nature of the substance.
> 
> I have noticed antidepressant benefits lasting for days after a single dose and so far I think this works best with doses >10mg. I don't get the antidepressant effect until after it wears off. YMMV though.


It appears that Methoxetamine works against protracted withdrawals for this person, i would expect low doses of ketamine and possibly memantine and DXM to do the same, while memantine and DXM do work very well against tolerance, the acute antidepressant effects of ketamine and MXE appear to be stronger.


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## metamorphosis (Dec 18, 2008)

Lyrica can mask withdrawal symptoms but will definitely not stop the physiological withdrawal taking place in the body. Alcohol does have the same affinity towards GABAa as benzos and will help more physiologically. But it does not act as strong in the bonding of GABA receptors but is definitely a strong, short term detox help along with the others mentioned above. Cannot express how it is important to use everything at your disposal. difeerent meds/drugs, supplements(l theanine,valerian,l glutamine) along with diet and exercise and sleep. also take a strong multi and load up on the b-vits and magnesium. Which is easily cooked out of foods and is a huge central nervous/muscle relaxant. Plenty of sleep and when in need tit-rate slowly down. It should be an integrative approach. Not a ,"take this" period!!!

The proper restoration of any psychological disability take all the proper and progressive movement. Plus, rest, rebuilding time and patience as it should really be always on the mind with all daily activities, eat and sleep!!

There's not one magical pill!!


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## crayzyMed (Nov 2, 2006)

> Lyrica can mask withdrawal symptoms but will definitely not stop the physiological withdrawal taking place in the body.


It however most likely inhibits the neurotoxiticy involved in withdrawals, wich is mediated by glutamate hyperactivity.


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## metamorphosis (Dec 18, 2008)

How can that be proven at this point,Wes???


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## crayzyMed (Nov 2, 2006)

metamorphosis said:


> How can that be proven at this point,Wes???


It protects against excitoxiticy, wich is what causes neurotoxiticy involved in benzo withdrawal.


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## metamorphosis (Dec 18, 2008)

By the random blockage of the release of certain neurotransmitters through thousands of neurons??


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## metamorphosis (Dec 18, 2008)

Fact is,is that Lexapro is a cross labeled drug. Whose only known use in the brain is as a strong voltage calcium blocker. Anything else is strong hypothesis!!


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## crayzyMed (Nov 2, 2006)

^^ Its not a hypothesis, we can be quite certain of this, NMDA antagonists protect against excitoxiticy too.


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## metamorphosis (Dec 18, 2008)

We can also be quite certain that wanton claims of how a drug works without peer reviewed studies is open to liability. 
Lexapro blocks certain neurotransmitters from release from one neuron to another.
Give me the hard statistics you claim about it's role in glutamate. Not, a hypothetical theory that some scientist are thinking, yo!!


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## Positive (Jun 29, 2009)

metamorphosis said:


> Lyrica can mask withdrawal symptoms but will definitely not stop the physiological withdrawal taking place in the body. Alcohol does have the same affinity towards GABAa as benzos and will help more physiologically. But it does not act as strong in the bonding of GABA receptors but is definitely a strong, short term detox help along with the others mentioned above. Cannot express how it is important to use everything at your disposal. difeerent meds/drugs, supplements(l theanine,valerian,l glutamine) along with diet and exercise and sleep. also take a strong multi and load up on the b-vits and magnesium. Which is easily cooked out of foods and is a huge central nervous/muscle relaxant. Plenty of sleep and when in need tit-rate slowly down. It should be an integrative approach. Not a ,"take this" period!!!
> 
> The proper restoration of any psychological disability take all the proper and progressive movement. Plus, rest, rebuilding time and patience as it should really be always on the mind with all daily activities, eat and sleep!!
> 
> There's not one magical pill!!


I like this post and hope it works. What brand for magnesium?


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## metamorphosis (Dec 18, 2008)

Most believe in magnesium glycinate pwd. I believe in any chelated magnesium pwd added to water(citrate, Kata-glutamate). Add it to your water 2-3 used throughout the day is really incredible.
No joke!!


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## gabaaid (Oct 10, 2012)

*magnesium supplement*

I'm curious to know what this forum thinks about the use of Epsom salts as a magnesium supplement. How does this compare to other forms of magnesium. I've had sucess with it in treating withdrawal from gabapentin.

I'm not a doctor just a curious observer and love internet data min:teething.


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## istayhome (Apr 4, 2012)

gabaaid said:


> I'm curious to know what this forum thinks about the use of Epsom salts as a magnesium supplement. How does this compare to other forms of magnesium. I've had sucess with it in treating withdrawal from gabapentin.
> 
> I'm not a doctor just a curious observer and love internet data min:teething.


Epsom Salt (Magnesium Sulphate) Is a very poor magensium supplement, ingesting it will mainly produce laxative affects.

There are far better forms of magnesium which are actually bio-available.I personally recommend Magnesium Taurate, Magnesium Glycinate is equally bio available. But I think supplementing with Taurine along with the Magnesium makes Magnesium Taurate the superior option.


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## Charles Ferdinand (May 4, 2012)

Well, it can take up to a year, and even after that year you might never get the same effects again. 
Carbamazepine upregulates GABA Alpha receptors, Memantine and NMDA antagonists lower tolerance to almost any drug and to specifically reverse benzo tolerance you are gonna need a specific antagonist: Flumazenil. 
Other than that a GABA antagonist would be in order: tramadol would be the easier to come by. 
Dr. Ferdinand


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