How Does GABA Affect the Brain Differently Than GABA Receptors?

[JasonP]

Okay, so from what I heard is that drugs like klonopin don't create GABA they just activate the GABA-a receptors.

My question is that if there is an increase in GABA does that mean that there will be more of an inhibitory effect on the brain when the GABA-a receptor is activated?

The reason I ask is because some people are helped from tinnitus by a combination of Neurontin and Klonopin. Whereas, from what I understand Neurontin helps increase GABA and then Klonopin activates the GABA-a receptor.

Can you all tell me if I am wrong here or explain the differences?

Also, to the people who have tried this and it worked, how long can this work without building up tolerance?

 

[Beste]

Amazing thread. I also wonder this. And I'd like to add that is it good to take clonazepam for your T if it was also benzo w/d induced? Will it make it worse?

 

[JasonP]

Amazing thread. I also wonder this. And I'd like to add that is it good to take clonazepam for your T if it was also benzo w/d induced? Will it make it worse?

Great question. I don't know. Have you read this article? I don't know if it will help but I figure I can post it.

http://www.ncbi.nlm.nih.gov/pubmed/18821451

 

[hartje5]

As GABA activates the GABA receptor an increase in GABA concentration will activate the GABA receptor more. Indeed GABA receptor activation leads to relative inhibition of the receiving neuron. (Says my husband who's a neuroscientist )

 

[undecided]

The reason I ask is because some people are helped from tinnitus by a combination of Neurontin and Klonopin. Whereas, from what I understand Neurontin helps increase GABA and then Klonopin activates the GABA-a receptor.

Neurontin is a calcium channel blocker and has a small affinity for NMDA receptors.
Although it has been synthesized to be chemically similar to the GABA molecule, it does not act on the GABA receptors.
I'd say that that getting enough neurontin in your system will make you a bit uncoordinated and less caring about your tinnitus (perception change mostly, maybe a slight volume decrease). Adding klonopin or any other benzo into that happy mix will just amplify the effect.

 

[JasonP]

As GABA activates the GABA receptor an increase in GABA concentration will activate the GABA receptor more. Indeed GABA receptor activation leads to relative inhibition of the receiving neuron. (Says my husband who's a neuroscientist )

Oh cool! Can you please ask your husband to answer this question? Please https://www.tinnitustalk.com/thread...na-channels-during-long-term-benzo-use.16170/

 

[JasonP]

Neurontin is a calcium channel blocker and has a small affinity for NMDA receptors.
Although it has been synthesized to be chemically similar to the GABA molecule, it does not act on the GABA receptors.
I'd say that that getting enough neurontin in your system will make you a bit uncoordinated and less caring about your tinnitus (perception change mostly, maybe a slight volume decrease). Adding klonopin or any other benzo into that happy mix will just amplify the effect.

I think you are right about the calcium channels, but according to this report Neurontin also increases GABA.

http://www.ncbi.nlm.nih.gov/pubmed/22871916

 

[undecided]

I think you are right about the calcium channels, but according to this report Neurontin also increases GABA.

http://www.ncbi.nlm.nih.gov/pubmed/22871916

What I understand from this report is that GABA increase seems relative to each individuals base GABA levels prior to administration of Gabapentin which sounds a bit random and individualized.
This could explain why some people don't feel much on it while others fall asleep driving after small doses.
I believe Pfizer has never come clean on the actual mechanism of action for Neurontin, which might be the reason why they're still paying tons in class action lawsuits (and it being prescribed for any off label use a doctor might come up with).

Anyway, just to share my opinion, Neurontin works nicely sometimes at > 1800mg doses, separated throughout the day, with a bit of Lyrica thrown in from time to time... Will sleep like a baby on them.
Useful dope.

 

[JasonP]

What I understand from this report is that GABA increase seems relative to each individuals base GABA levels prior to administration of Gabapentin which sounds a bit random and individualized.
This could explain why some people don't feel much on it while others fall asleep driving after small doses.
I believe Pfizer has never come clean on the actual mechanism of action for Neurontin, which might be the reason why they're still paying tons in class action lawsuits (and it being prescribed for any off label use a doctor might come up with).

Anyway, just to share my opinion, Neurontin works nicely sometimes at > 1800mg doses, separated throughout the day, with a bit of Lyrica thrown in from time to time... Will sleep like a baby on them.
Useful dope.

I just took 200mg this morning for the first time and it was relaxing. I wonder how the Neurontin "forms" GABA. I know normally GABA is made from Glutamate.

 

[JasonP]

As GABA activates the GABA receptor an increase in GABA concentration will activate the GABA receptor more. Indeed GABA receptor activation leads to relative inhibition of the receiving neuron. (Says my husband who's a neuroscientist )

Oh and I also have another question for your husband. Today I was prescribed a "calcium channel blocker" medicine called Neurontin. My question is, if it blocks the calcium, where does the calcium go? Does it store up in the brain and cause problems? This may sound like a stupid question to him but I am not a neuroscientist Thanks for all your help.

 

[hartje5]

Calcium, as other elements, is part of homeostasis (the tendency of the body to keep things constant). There is an enormous buffering capacity for calcium in your body. In bones, in muscles, in fact in every living cel in your body. The shift in calcium that is blocked is minute in relation to the calcium concentrations that exist in the intracellular and extracellular fluid. So no need to worry about storing calcium in your brain while on Neurontin.

There is really no easy answer to your question for it requires a lot of knowledge of the cell, electrolytes and fysiologie to start to understand the mechanism.

 

[undecided]

I just took 200mg this morning for the first time and it was relaxing. I wonder how the Neurontin "forms" GABA. I know normally GABA is made from Glutamate.

Gabapentin is basically a GABA molecule, the sort that comes in food supplements I'd guess, onto which they probably slap a hexane ring or something to make it liposoluble. That would help it cross the blood brain barrier and make it work its magic.
Your typical synthesized, basic GABA molecules (like the Solgar stuff for example) just flow around in the bloodstream and gut until pooped out.