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Fosphenytoin

CEREBYX

Pronunciation: fos-FEN-i-toyn

Fosphenytoin ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Fosphenytoin ballicule
Fosphenytoin CEREBYX mascot mnemonic cartoon
Visual mnemonic: Fosphenytoin mascot
“Cerebral Fox phenytoin”
Variation of phenytoin mascot
Water-soluble phenytoin prodrug for IV/IM loading

What it isWater-soluble IV or IM prodrug of phenytoin; status epilepticus loading and short-term parenteral substitution.

Why this oneIt can be infused faster and causes less local tissue injury than IV phenytoin; IM administration is possible.

What limits itRapid IV infusion can cause severe hypotension and fatal arrhythmia—monitor ECG and blood pressure. Prescribe in phenytoin-equivalent units.

Fosphenytoin molecular structure (skeletal formula)
Molecular structure: Fosphenytoin

FDA-approved for

FDA label

BOXED WARNING Cardiovascular risk with rapid infusion: do not exceed 150 mg PE/min in adults and 2 mg PE/kg/min (or 150 mg PE/min) in pediatric patients; monitor cardiac/respiratory status.
FDA dosingPopulationStartTargetMax
Status epilepticusAdult15-20 mg PE/kg IV loading at 100-150 mg PE/minmaintenance 4-6 mg PE/kg/day dividedper level
Status epilepticusPediatric15-20 mg PE/kg IV loading at 2 mg PE/kg/min (or 150 mg PE/min, whichever slower)per levelper level
Non-emergent loading and maintenanceAdult10-20 mg PE/kg IV or IM loading4-6 mg PE/kg/day dividedper level
Non-emergent loading and maintenancePediatric10-15 mg PE/kg loading at 1-2 mg PE/kg/min (or 150 mg PE/min, whichever slower)2-4 mg PE/kg q12h at 1-2 mg PE/kg/minper level

Renal Monitor unbound phenytoin concentrations in renal disease or hypoalbuminemia

Hepatic Monitor unbound phenytoin concentrations in hepatic disease or hypoalbuminemia

Concentration is 50 mg PE/mL; a 10 mL vial contains 500 mg PE total.

Instructions

Available strengths

Contraindications

Cautions

Adverse reactions

Pregnancy Prenatal phenytoin (active metabolite) exposure may increase risk of congenital malformations and adverse developmental outcomes.

Lactation Undefined

Cost

Fosphenytoin (CEREBYX)
Strength#/mogeneric $/unitCostPlus
50 mg PE/mLinjper unitnot offered
NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Fosphenytoin is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2007

⚠ BOXED WARNING

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4
Overdose danger4 / 4
Weight-gain liability1 / 4
Sedation liability1 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryD

Defining liabilityCardiovascular collapse with rapid administration and phenytoin-related nonlinear toxicity.

Active metabolites

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