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Gabapentin

NEURONTIN

What it isAlpha-2-delta calcium-channel subunit ligand for seizures and postherpetic neuralgia; also used off label for other neuralgia.

Why it mattersSaturable absorption produces diminishing exposure gains as the dose rises, unlike pregabalin.

What it changesReduce in renal impairment; accumulation sedates. Opioids add respiratory depression, and misuse is increasingly recognized.

FDA-approved for

Off-label

FDA label

FDA dosingPopulationStartTargetMax
Postherpetic neuralgiaAdults300 mg QD (day 1) → 300 mg BID (day 2) → 300 mg TID (day 3)600 mg TID (1800 mg/day)1800 mg/day
Partial onset seizures≥12 yr300 mg TID300–600 mg TID3600 mg/day
Partial onset seizuresPeds 3–11 yr10–15 mg/kg/day TID3–4 yr: 40 mg/kg/day; 5–11 yr: 25–35 mg/kg/day

Renal Adjust by creatinine clearance in patients ≥12 yr; reduce dose for renal impairment and supplement after hemodialysis

Hepatic Undefined

Max interval between doses ≤12 h

Instructions

Cautions

Adverse reactions

Pregnancy Available data do not indicate increased risk of major birth defects/miscarriage; developmental toxicity in animals; neonatal withdrawal reported with concomitant opioids near delivery

Lactation Secreted in human milk; effects on infant unknown

NO BOXED WARNINGS

Principal riskSedation and dizziness, additive with opioids

Cost, est. cash$4–$80/month

Generic entry2003

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger2 / 4
Weight-gain liability1 / 4
Sedation liability2 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryC

Defining liabilitySedation, dizziness and misuse potential; respiratory depression increases with opioids.

Mechanism of action: Gabapentin ballicule

Gabapentin ballicule: receptor binding, kinetics and half-life diagram

Open Gabapentin in the interactive console ↗

Memory aids: mascots and interaction avatars

Gabapentin NEURONTIN mascot mnemonic cartoon
“Gabba pen tin = Neuron tin”
Pens shaped like neurons with heads of Yo Gabba Gabba characters
Gabapentin no kinetic interactions avatar
no kinetic interactions

Open Gabapentin in the interactive console ↗