pharmocology of gabapentin

[laCster]

i have recently been prescribed gabapentin and this substance is starting to intrigue me. i am about 3grams of it right now titrated over several hours (300mg every hour) and potentiated by food and naproxen sodium...and i feel... ummm.. numb but energetic, talkative, and a little dumb.

my question is how does gabapentin affect the brain? i have looked over the internet and read about some literature that gabapentin binds to NMDA receptors; is this true?? gaba is such a wierd drug and i can't to seem an exact answer as to why it "works" so to say. i guess i wanted to see (or read lol) what people had to say on BL.

any opinions, experiences, or thoughts on gabapentin would be cool to read aswell


thanks...
-lacster

 

[Epsilon Alpha]

Here's a good review to start at, it more focuses on seizure disorders but it goes pretty well into the known pharmacology.
http://works.bepress.com/cgi/viewco...arch="gabapentinoids mechanism action review"

There's also talk of it upregulating GABA biosynthesis, so you might want to look into that as well.

 

[laCster]

very good read! thank you epsilon alpha

could gabapentin increase GABA synthesis by inducing the activity of GAD?..

 

[alkap555]

I messed around with gabapentin for a few weeks, mostly to explore any recreational and therapeutic applications. Definately a unique drug, hard to explain the subjective effects... in higher doses it definitely Zombified my though. I didn't notice any pronounced anxiolytic effects, just a general sense of "fuzziness" in most sensory aspects.

By GAD do you mean glutamic acid decarboxylase? I haven't read about the pharmacodynamics of gabapentin in a while but I do think I remember something about augmenting glutamic acid decarboxylase activity, which as you know convert Glutamate-->GABA. So the answer to your question is yes, possibly. On second thought, here is what I found in a quick search. If you want full text access to the journal I can get it for you if you don't have free university access. Its a pretty old paper but seems legit:

http://www.ncbi.nlm.nih.gov/pubmed/9686247

 

[laCster]

yes by GAD i was refering to glutamic acid decarboxylase

interesting, good post and read