Author Topic: Does gabapentin effect gaba receptors?  (Read 460 times)

[Buddie]

Does gabapentin effect gaba receptors?
« on: May 10, 2022, 03:39:16 pm »
?
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[Buddie]

Re: Does gabapentin effect gaba receptors?
« Reply #1 on: May 23, 2022, 09:42:40 pm »
I am wanting to know the same thing, too, Foxclover. My orthopedist wants me to take it for back pain (intensified by benzo nerve pain), and I do need something to get functional again. But the pain from benzo withdrawal can be worse than an injury. Prednisone threw me into a HUGE wave-- worse than the first months of acute. I am so nervous about all meds (and supplements, and tinctures and so on...)

I'm not sure they know exactly how or why it works. I have been looking at a few sites to get an idea of the current thinking, but that's hard to do during an anxiety spike. Everything sounds so ominous and forbidding.  :-\

[...]
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[Buddie]

Re: Does gabapentin effect gaba receptors?
« Reply #2 on: May 23, 2022, 10:26:46 pm »
Not according to the recently updated publication from the US National Institutes of Health cited below.

Quote
The exact mechanism of action with the GABA receptors is unknown; however, researchers know that gabapentin freely passes the blood-brain barrier and acts on neurotransmitters. Gabapentin has a cyclohexyl group to the structure of neurotransmitter GABA as a chemical structure. Even though it has a similar structure to GABA, it does not bind to GABA receptors and does not influence the synthesis or uptake of GABA. Gabapentin works by showing a high affinity for binding sites throughout the brain correspondent to the presence of the voltage-gated calcium channels, especially alpha-2-delta-1, which seems to inhibit the release of excitatory neurotransmitters in the presynaptic area which participate in epileptogenesis. Even though there is no evidence for direct action at the serotonin, dopamine, benzodiazepine, or histamine receptors, research has shown gabapentin to increase total-blood levels of serotonin in healthy control subjects.

The elimination half-life of gabapentin is 5 to 7 hours, and it takes two days for the body to eliminate gabapentin from its system.

Citation:
Gabapentin - StatPearls - NCBI Bookshelf
https://www.ncbi.nlm.nih.gov/books/NBK493228/
Last Update: May 2, 2022
Suggestions, opinions and/or advice provided by the author of this post should not be regarded as medical advice; nor should it substitute for professional medical care. Consult your doctor before making any changes to your medication. Please read our Community Policy Documents board for further information.

[Buddie]

Re: Does gabapentin effect gaba receptors?
« Reply #3 on: May 24, 2022, 01:51:37 am »
I am wanting to know the same thing, too, Foxclover. My orthopedist wants me to take it for back pain (intensified by benzo nerve pain), and I do need something to get functional again. But the pain from benzo withdrawal can be worse than an injury. Prednisone threw me into a HUGE wave-- worse than the first months of acute. I am so nervous about all meds (and supplements, and tinctures and so on...)

I'm not sure they know exactly how or why it works. I have been looking at a few sites to get an idea of the current thinking, but that's hard to do during an anxiety spike. Everything sounds so ominous and forbidding.  :-\

[...]
Someone I know so knows about these drugs told me no, it doesn't.
Suggestions, opinions and/or advice provided by the author of this post should not be regarded as medical advice; nor should it substitute for professional medical care. Consult your doctor before making any changes to your medication. Please read our Community Policy Documents board for further information.

[Buddie]

Re: Does gabapentin effect gaba receptors?
« Reply #4 on: May 25, 2022, 05:19:41 pm »
Grateful for this thread. I wanted to know too.
Suggestions, opinions and/or advice provided by the author of this post should not be regarded as medical advice; nor should it substitute for professional medical care. Consult your doctor before making any changes to your medication. Please read our Community Policy Documents board for further information.

[Buddie]

Re: Does gabapentin effect gaba receptors?
« Reply #5 on: May 25, 2022, 05:53:29 pm »
it does increase gaba concentrations in the brain, though -

"This study will use magnetic resonance spectroscopy (MRS) and the drug gabapentin to examine the role of the brain chemical gamma-amino-butyric acid (GABA) in regulating emotions in healthy people. Gabapentin, which is used to treat epilepsy, increases GABA concentrations in the brain. MRS, similar to magnetic resonance imaging (MRI), is a diagnostic test that uses a magnetic field and radio waves to produce images of the brain."

https://clinicaltrials.gov/ct2/show/NCT00094510
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[Buddie]

Re: Does gabapentin effect gaba receptors?
« Reply #6 on: May 25, 2022, 07:54:56 pm »
I'm on gabapentin 900mg for fibro.  It helps.  Is it supposed to help/hurt with withdrawal?  I'm about 9 days out since starting my detox from Klonopin 2mg.  So far, only huge side effect was a day of severe vertigo. So far, nothing big. 
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[Buddie]

Re: Does gabapentin effect gaba receptors?
« Reply #7 on: June 06, 2022, 12:31:08 am »
The link is to a clinical trial without the published results. It says something very confusing:

"The effects of GBP (gabapentin) on brain amino acid neurotransmitters are not completely understood. GBP significantly increases brain GABA levels in humans after one hour of the first oral dose, although it does not seem to directly affect GABA-specific enzymes, GABA receptors, and GABA uptake. In vitro, GBP stimulates the enzyme glutamic acid decarboxylase that is involved in the synthesis of GABA."

No wonder it's hard to know what to think of it. The researchers themselves are scratching their heads.
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[Buddie]

Re: Does gabapentin effect gaba receptors?
« Reply #8 on: June 06, 2022, 12:32:38 pm »
I was told that it can help with the anxiety from withdrawal. Not sure if this is true.  I'm on mine due to Fibro. It works well for that.
Suggestions, opinions and/or advice provided by the author of this post should not be regarded as medical advice; nor should it substitute for professional medical care. Consult your doctor before making any changes to your medication. Please read our Community Policy Documents board for further information.