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Gabapentin immediate release

Theresa Zesiewicz, MD · FDA-approved active Small molecule

Gabapentin binds to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, reducing the release of excitatory neurotransmitters.

Gabapentin binds to the alpha-2-delta subunit of voltage-gated calcium channels in the central nervous system, reducing the release of excitatory neurotransmitters. Used for Postherpetic neuralgia, Partial-onset seizures (adjunctive therapy), Neuropathic pain.

At a glance

Generic nameGabapentin immediate release
Also known asNeurontin
SponsorTheresa Zesiewicz, MD
Drug classAnticonvulsant; gabapentinoid
TargetVoltage-gated calcium channel alpha-2-delta subunit
ModalitySmall molecule
Therapeutic areaNeurology
PhaseFDA-approved

Mechanism of action

By binding to presynaptic calcium channels, gabapentin decreases calcium influx and subsequently reduces the release of glutamate and other excitatory neurotransmitters. This leads to reduced neuronal excitability and is thought to underlie its analgesic and anticonvulsant effects. The exact mechanism in pain conditions remains incompletely understood but involves modulation of neuropathic pain pathways.

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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