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Methsuximide

CELONTIN

What it isSuccinimide T-type calcium channel blocker; absence seizures refractory to ethosuximide.

Why this oneIt penetrates better than ethosuximide and has some activity in focal seizures.

What limits itBlood dyscrasias require counts. More CNS toxicity than ethosuximide; it inhibits CYP2C19.

FDA-approved for

Off-label

FDA label

FDA dosingPopulationStartTargetMax
Absence (petit mal) seizuresadult/peds300 mg/day for first weekup to 1.2 g/day1.2 g/day

Titration May increase at weekly intervals by 300 mg/day (over the 3 weeks following the first week)

Renal Undefined

Hepatic Undefined

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Anticonvulsants associated with elevated incidence of birth defects; do not discontinue in patients where used to prevent major seizures

Lactation Undefined

NO BOXED WARNINGS

Principal riskBlood dyscrasias; more CNS toxicity than ethosuximide

Cost, est. cash$10–$500/month

Generic entry2023

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: Methsuximide ballicule

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

Open Methsuximide in the interactive console ↗