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.
1.Varia, S.A., and Stella, V.J.Phenytoin prodrugs VI: In vivo evaluation of a phosphate ester prodrug of phenytoin after parenteral administration to ratsJ. Pharm. Sci.73(8)1087-1090(1984) 2.Smith, R.D., Brown, B.S., Maher, R.W., et al.Pharmacology of ACC-9653 (phenytoin prodrug)Epilepsia30(Suppl. 2)S15-S21(1989) 3.Boucher, B.A.Fosphenytoin: A novel phenytoin prodrugPharmacotherapy16(5)777-791(1996)
















