Last reviewed · How we verify

Standard dose gabapentin

Mario Negri Institute for Pharmacological Research · FDA-approved active Small molecule

Gabapentin reduces neuronal excitability by binding to the alpha-2-delta subunit of voltage-gated calcium channels, thereby decreasing calcium influx and neurotransmitter release.

Gabapentin reduces neuronal excitability by binding to the alpha-2-delta subunit of voltage-gated calcium channels, thereby decreasing calcium influx and neurotransmitter release. Used for Postherpetic neuralgia (neuropathic pain following herpes zoster), Partial-onset seizures (adjunctive therapy), Neuropathic pain conditions.

At a glance

Generic nameStandard dose gabapentin
Also known asStandard gabapentin
SponsorMario Negri Institute for Pharmacological Research
Drug classAnticonvulsant; gabapentinoid
TargetAlpha-2-delta-1 subunit of voltage-gated calcium channels
ModalitySmall molecule
Therapeutic areaNeurology
PhaseFDA-approved

Mechanism of action

Gabapentin is a structural analogue of gamma-aminobutyric acid (GABA) that crosses the blood-brain barrier and binds to the alpha-2-delta-1 subunit of presynaptic voltage-gated calcium channels. This binding reduces calcium entry into nerve terminals, which decreases the release of excitatory neurotransmitters including glutamate, noradrenaline, and substance P. The net effect is reduced neuronal firing and pain signal transmission.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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