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Pharmacology of Gabapentin

The exact mechanisms through which gabapentin exerts its analgesic and antiepileptic actions are unknown, However, according to the information from the FDA-approved label for the gabapentin drug product, gabapentin has no effect on GABA binding, uptake or degradation. In-vitro studies have shown gabapentin binds to auxiliary α2-δ subunits of voltage-gated Ca channels on neurons hereby 2+ resulting in a decrease in neuronal excitability.

At clinically therapeutic doses (900-3600 mg/day), gabapentin does not bind to GABAA or GABAB receptors, nor does it bind to benzodiazepine sites.

The FDA-approved product label for gabapentin mentions adverse reactions such as dizziness, somnolence (drowsiness), peripheral edema (swelling), ataxia (incoordination), fatigue and nystagmus (involuntary rapid eye movement). According to a published study which analyzed online information from 32 websites, gabapentin use, similar to pregabalin, is associated with sedative and/or psychedelic effects.

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