Drug intelligence / Profile preview

fosphenytoin

Development stage
Approved
Lead developer
Pfizer
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

Fosphenytoin is a water-soluble prodrug of phenytoin, used primarily in hospital settings for the management of generalized convulsive status epilepticus and for the prevention and treatment of seizures during neurosurgery. It is administered intravenously or intramuscularly when oral administration of phenytoin is not feasible. After administration, it is rapidly converted by endogenous phosphatases to phenytoin, which exerts anticonvulsant effects by blocking frequency-dependent, use-dependent, and voltage-dependent neuronal sodium channels. This action limits repetitive firing of action potentials in neurons. Fosphenytoin's pharmacological effects are essentially those of phenytoin but with improved solubility and safety profile for parenteral use[1][5][6][8].

Brand names
Cerebyx
Other names
fosphenytoin sodium
02

Targets

ATP1A (Sodium/potassium-transporting ATPase)CACNA1C (Voltage-dependent L-type calcium channel subunit alpha-1C)NaV (Voltage-gated sodium channels)

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