Gabapentin

Gabapentin is a small molecule pharmaceutical compound primarily used as an anticonvulsant and for the treatment of neuropathic pain (PubChem CID 3446). The specific phrase 'Gabapentin in the gastrointestinal lumen' refers to the drug's presence in the digestive tract prior to absorption, rather than a biological target. Gabapentin itself is a ligand that targets the alpha-2/delta-1 subunit of voltage-gated calcium channels (CACNA2D1) in the central nervous system (StatPearls, 2023). Its absorption from the gastrointestinal lumen into the systemic circulation is mediated by the Large Neutral Amino Acid Transporter 1 (LAT1/SLC7A5), a process that is saturable and leads to non-linear pharmacokinetics (DrugBank DB00996). By binding to its molecular target, Gabapentin reduces the influx of calcium into presynaptic terminals, which inhibits the release of excitatory neurotransmitters like glutamate and substance P (FDA Neurontin Label). It is commonly prescribed for postherpetic neuralgia and partial-onset seizures, and it is characterized by a lack of significant hepatic metabolism, being excreted unchanged by the kidneys (PubMed: 10907668).

Other names

Neurontin1-(Aminomethyl)cyclohexaneacetic acidGraliseHorizant

Gabapentin binds with high affinity to the alpha-2/delta-1 subunit of voltage-gated calcium channels (CACNA2D1), which reduces the presynaptic release of excitatory neurotransmitters in the central nervous system (StatPearls, 2023).