Drug intelligence / Profile preview

gabapentin

Development stage
Approved
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

Gabapentin is an anticonvulsant medication and a gamma-aminobutyric acid (GABA) analogue primarily used to treat neuropathic pain and partial seizures in epilepsy. It is also approved for postherpetic neuralgia (nerve pain after shingles) and moderate-to-severe restless legs syndrome. Gabapentin works by binding to the α2δ-1 subunit of voltage-gated calcium channels in the central nervous system, reducing the release of excitatory neurotransmitters such as glutamate. This action decreases abnormal neuronal excitation associated with seizures and neuropathic pain. Gabapentin was first developed by Parke-Davis (a subsidiary of Pfizer), received FDA approval in 1993, and has been available as a generic since 2004[1][2][3][4][5][7].

Brand names
NeurontinGraliseHorizantGabaroneFanatrexgabapentin
Other names
gabapentin
02

Targets

CACNA2D2 (Voltage-gated calcium channel subunit alpha-2/delta-2)CACNA2D1 (Voltage-gated calcium channel subunit alpha2/delta-1)

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