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Fosphenytoin is a prodrug of phenytoin that is rapidly converted to phenytoin, a voltage-gated sodium channel blocker, in vivo.1,2,3 It induces less tissue damage compared with two other phenytoin prodrugs in rats following subcutaneous and intramuscular administration.1 Fosphenytoin has anticonvulsant activity in a mouse model of maximal electroshock seizures similar to that of phenytoin (ED50s = 16 and 8 mg/kg, respectively).2 It also has antiarrhythmic activity in isolated guinea pig atria and in anesthetized dogs. Formulations containing fosphenytoin have been used in the treatment of status epilepticus.
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1. Phenytoin prodrugs VI: In vivo evaluation of a phosphate ester prodrug of phenytoin after parenteral administration to rats. J. Pharm. Sci. 73(8), 1087-1090 (1984).
2. Pharmacology of ACC-
3. Fosphenytoin: A novel phenytoin prodrug. Pharmacotherapy 16(5), 777-791 (1996).