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Assisting in the recovery of down regulated GABA receptors??

A

AlexxRed

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Joined
Apr 2, 2002
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melbourne, Australia
Hi all,

I'm just curious if there is anything that can be used to assist in the recovery of GABA receptors that have been down regulated? Particularly after prolonged but interspersed benzo use.

I know that there are GABA supplements but I understand that there are issues with these crossing the blood barrier membrane. Are there any that work better than others?

What about other pharms? Is there anything that can be used to assist in the recovery of GABA receptors that have been down regulated?

Cheers

Alex
 
Time works pretty well, if one can avoid benzos (but you probably knew that already).

You might want to try phenibut in reasonable doses, which could act as a sort of tapering mechanism (IF you can keep doses reasonable, and then gradually decrease/taper off eventually). It does cross the blood-brain barrier, and IME works nicely when doses are kept sane. But it has some abuse liability, like most gaba-ergics. It was available at vitamin shops & bodybuilding supplement stores, last time I checked.
 
Phenibut is just another GABA agonist ... it will actually slow recovery of receptors, but lessen withdrawl symptoms. What you need is a strict regimen of tapering benzo usage. There really isn't anything that will speed up receptor recovery, since the way your body figures out that it needs more receptors is through understimulation, which is the cause of withdrawl symptoms. A slow tapering will minimize anxiety/insomnia while allowing receptor numbers to get back to normal.
 
^^^^
Thanks for the concern, but I have no need to taper. I'm not using daily or suffering from withdrawal etc. While at one stage I was taking them for a long period of time these days I only use them occasionally.

Having said that I have noticed a tolerance and was wondering if there was anything I could do in addition to abstaining?

IE supplements or other meds that could be used the way some use 5htp or tyrosine for dealing with the after effects of MDXX or amphetamines.

Any suggestions?
 
AlexxRed said:
^^^^
Thanks for the concern, but I have no need to taper. I'm not using daily or suffering from withdrawal etc. While at one stage I was taking them for a long period of time these days I only use them occasionally.

Having said that I have noticed a tolerance and was wondering if there was anything I could do in addition to abstaining?

IE supplements or other meds that could be used the way some use 5htp or tyrosine for dealing with the after effects of MDXX or amphetamines.

Any suggestions?
Click to expand...

L-Glutamine is a precursor of GABA.
 
Dondante said:
Phenibut is just another GABA agonist ... it will actually slow recovery of receptors, but lessen withdrawl symptoms.
Click to expand...

AFAIK, Phenibut primarily hits GABA(B) receptors, so it shouldn't slow the recovery of GABA(A) receptors which have been downregulated as a result of benzodiazepine abuse.

AlexxRed, it is possible that you may have built up a long-term tolerance as a result of chronic benzodiazepine use in the past. This tolerance may come not only from changes in the number of GABA(A) receptors, but also from changes in their function (e.g., a higher proportion of benzodiazepine-insensitive receptor subunits) as well as more efficient breakdown of benzodiazepines in your body. Anyways, if your mental state is more or less normal, and you don't have significant neurological or psychiatric symptoms that could be related to downregulated GABA(A) receptors (e.g. seizures, anxiety, etc.), I'd guess that some long-term adaptive process has probably occurred, and it's not going to be easy to reverse it. A very long break from benzos might be the best way.
 
Why would you use phenibut? Even if it doesn't target the exact receptors, its still going to slow down your cognitive abilities and make you feel dumb. Its a pretty worthless drug (phenibut, but then again I think all GABA agonists are pretty worthless).

I would recommend looking into piracetam and especially searching for studies with alcoholics taking it in recovery. There is a ton of info.
 
AlexxRed said:
I'm just curious if there is anything that can be used to assist in the recovery of GABA receptors that have been down regulated? Particularly after prolonged but interspersed benzo use.

I know that there are GABA supplements but I understand that there are issues with these crossing the blood barrier membrane. Are there any that work better than others?

What about other pharms? Is there anything that can be used to assist in the recovery of GABA receptors that have been down regulated?
Click to expand...

The best thing you can do is slowly tapering your benzo dose, then stop. After a few weeks (months?) of anxiety and paranoia, you receptors should have recovered.
GABA agonists will only downregulate the receptors even more, so you should avoid Benzos, Barbituates, Carbamates, Phenibut, etc....

What could work is Tiagabine. It is a GABA reuptake inhibitor.
As it is not a direct agonist, maybe it doesn't downregulate the receptors.

Another thing that could work is Vigabatrin. It inhibits the enzyme that breaks GABA down.
Again, no downregulation....

These 2 medications (Tiagabine and Vigabatrin) are very easy to get.
They're prescribed for epilepsy I think, but you can easily convince your doc to prescribe them to you for anxiety, or maybe as mood stabilizers...
Tiagabine brand name = Gabitril
Vigabatrin brand name = Sabril

-

Another thing is that Tiagabine and Vigabatrin are both AMAZING for benzo or opiate potentiation.
And taken alone, they provide great stress/anxiety relief. Maybe just as much as benzos.
 
^^^^^
Thanks for the info jasoncrest. As I have said eariler I am (fortunatly) not dealing with benzo addiction/withdrawal or anxiety issues. In the past I used them alot and now only very occationally; but I have a tolerance.

I was just interested if there was anything I could use in conjunction with total abstainance to assist in the recovery of down regulated GABA receptors.
 
^^ Indirect agonists like GAT and GABA-T inhibitors should still increase downregulation, as they still enhance GABA-A receptor activation.

And this is assuming that benzo tolerance even comes from receptor downregulation, which it probably doesn't, at least in the conventional sense of loss of surface neurotransmitter binding sites, see alpha5 downregulation and diazepam.
 
jasoncrest said:
The best thing you can do is slowly tapering your benzo dose, then stop. After a few weeks (months?) of anxiety and paranoia, you receptors should have recovered.
GABA agonists will only downregulate the receptors even more, so you should avoid Benzos, Barbituates, Carbamates, Phenibut, etc....

What could work is Tiagabine. It is a GABA reuptake inhibitor.
As it is not a direct agonist, maybe it doesn't downregulate the receptors.

Another thing that could work is Vigabatrin. It inhibits the enzyme that breaks GABA down.
Again, no downregulation....

These 2 medications (Tiagabine and Vigabatrin) are very easy to get.
They're prescribed for epilepsy I think, but you can easily convince your doc to prescribe them to you for anxiety, or maybe as mood stabilizers...
Tiagabine brand name = Gabitril
Vigabatrin brand name = Sabril

-

Another thing is that Tiagabine and Vigabatrin are both AMAZING for benzo or opiate potentiation.
And taken alone, they provide great stress/anxiety relief. Maybe just as much as benzos.
Click to expand...

Is taking pure GABA supplement (the one that don't crosses the BBB, but helps me preety well) will also downregulate the receptors even more? I take recommended doses...
 
GABA isn't gonna help much, if at all.

In my experience, benzo tolerance never ever comes back down, and it takes very little to get it way.
 
i take GABA supplement & i feel normal the first time since i quit benzos!
i smile, talk, enjoy social events, walk proudly on the street... any AD never ever helped me (social phobia) like GABA does.

but my question is would GABA downregulate the receptors even more?
 
Really? I've never heard anyone get any effect from oral GABA supplementation.

Since it's not crosing the bbb, and assuming the effect isn't placebo, I think the first step to answering that question would be to figure out how it's doing what it's doing.

is it increasing the gaba available in your brain by filling up the rest of your body, or something more complex?
 
i really don't know, but yes it took away my anxiety.
again, i don't feel any sedation (& of course no euphoria) from it, but i just feel naturally great, all the anxiety & negative thoughts\feelings\metal shit goes away...

my guess is maybe i have a natural lack of GABA after withdrawling a year recreational benzo habit cold turkey in february (i did felt like i do have a lack of GABA without a doubt judging by my normal mental state after i w\d'd).
so maybe this GABA supplement is just inuff to fill the needs...

i pray that it won't stop working...
 
L:yrica and Gabapentin help with benzo w/d. I don't think they do anything to help the receptors recover directly, however they work through a different mechanism and can provide a sedating high in high doses. Especially Lyrica. I'm talking at least 600mg Lyrica though. Right now I'm finding 300mg Lyrica, 1200mg Gabapentin and 50mg amitriptyline is helping me sleep through opiate w/d (for the most part anyway...I have my bad days) mixed with some weed.

You need to leave them alone (GABA receptors) so they can recover. That can take a long time if you've been on them long enough. Especially if you have developed a physical addiction. I've been using them on and off since the 70's including a 5-6 year stretch straight when I was bodybuilding and became physically addicted. Did a 6 month taper but I don't think my nervous system ever fully recovered. I mean I don't have seizures or electric shocks and shit but I have muscle spasms all over my body regularly that I never used to have. And I get bad muscle cramps when I work out now that I also never used to get. However, some of that could be age and 17 years of working out.
 
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