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Tiagabine

GABITRIL

What it isGAT-1 GABA-reuptake inhibitor; adjunctive treatment of focal seizures.

Why this oneNo other marketed antiepileptic uses selective GABA-transporter blockade.

What limits it⚑ It can provoke seizures or nonconvulsive status in people without epilepsy; dizziness, tremor, and CYP3A4 interactions also matter.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Partial seizures, adjunctive (enzyme-inducing AEDs)Adults4 mg QD32-56 mg/day divided BID-QID56 mg/day
Partial seizures, adjunctive (enzyme-inducing AEDs)Adolescents 12-18 yr4 mg QDdivided BID-QID32 mg/day

Titration Increase by 4 mg at start of week 2, then by 4-8 mg at weekly intervals

Renal Undefined

Hepatic Undefined

Instructions

Cautions

Adverse reactions

Pregnancy Animal studies show teratogenicity; use in pregnancy only if clearly needed; encourage NAAED Pregnancy Registry enrollment

Lactation Undefined

NO BOXED WARNINGS

Principal riskIt provokes seizures in people without epilepsy

Cost, est. cash$10–$300/month

Generic entry2011

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability1 / 4
Sedation liability1 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilitySedation, dizziness and agent-specific rash, behavioral, hepatic, hematologic or teratogenic toxicity.

Mechanism of action: Tiagabine ballicule

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

Open Tiagabine in the interactive console ↗

Memory aids: mascots and interaction avatars

Tiagabine GABITRIL mascot mnemonic cartoon
“Tiger beans (on the) GABA trail”
Tiagabine CYP3A4 substrate avatar
CYP3A4 substrate

Open Tiagabine in the interactive console ↗