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Primidone

MYSOLINE

What it isAntiepileptic with direct and phenobarbital-mediated GABA-A enhancement; essential tremor and seizures.

Why this oneWith propranolol it is one of only two first-line treatments for essential tremor.

What limits itA severe acute reaction on the first dose is common, so start at a fraction of the target. It is an enzyme inducer through its phenobarbital metabolite.

FDA-approved for

Off-label

FDA label

FDA dosingPopulationStartTargetMax
Epilepsy (grand mal, psychomotor, focal), no prior treatmentAdult & child ≥8 yr100-125 mg QHS250 mg TID500 mg QID (2000 mg/day)
EpilepsyPediatric <8 yr50 mg QHS125-250 mg TID (or 10-25 mg/kg/day divided)250 mg TID

Titration Increase approximately every 3 days per initiation schedule (Days 1-3, 4-6, 7-9, then maintenance)

Renal Undefined

Hepatic Undefined

Target serum primidone level 5-12 mcg/mL

Instructions

Contraindications

Cautions

Adverse reactions

Pregnancy Undefined

Lactation Undefined

NO BOXED WARNINGS

Principal riskSedation; converts to phenobarbital

Cost, est. cash$5–$150/month

Generic entry2001

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4
Overdose danger4 / 4
Weight-gain liability1 / 4
Sedation liability3 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk3 / 4

Legacy pregnancy categoryD

Defining liabilitySedation, dependence and phenobarbital-mediated respiratory/CNS depression in overdose.

Active metabolites

Mechanism of action: Primidone ballicule

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

Open Primidone in the interactive console ↗

Memory aids: mascots and interaction avatars

Primidone MYSOLINE mascot mnemonic cartoon
“Prima donna’s Missile line”
“Shredder” inducer
Metabolized to phenobarbital, similar theme
Pan-inducer, affecting substrates shown on the paper
Primidone CYP2C19 inducer avatar
CYP2C19 inducer (moderate)
Primidone CYP3A4 inducer avatar
CYP3A4 inducer (strong)
Primidone P-gp inducer avatar
P-gp inducer (strong)
Primidone UGT1A4 inducer avatar
UGT1A4 inducer

Open Primidone in the interactive console ↗