Fosphenytoin (Cerebyx)

Clin Neuropharmacol. 1997 Feb;20(1):1-12. doi: 10.1097/00002826-199702000-00001.

Abstract

Fosphenytoin is a phosphate ester prodrug of phenytoin developed as a replacement for standard injectable sodium phenytoin. After absorption, phenytoin is cleaved (conversion half-life 8-15 min) from fosphenytoin. Unlike phenytoin, fosphenytoin is freely soluble in aqueous solutions (including standard intravenous solutions) and rapidly absorbed by the intramuscular route. Fosphenytoin has been tested successfully for three indications in humans: intramuscular maintenance dosing, intramuscular loading dose administration, and intravenous treatment of status epilepticus. Local toxicity (pain, burning, itching) is less by the intramuscular or intravenous route for fosphenytoin than for standard injectable sodium phenytoin. Systemic toxicity is similar with both preparations except that hypotension is less common and paresthesias are more common with fosphenytoin.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Animals
  • Anticonvulsants / chemistry
  • Anticonvulsants / pharmacokinetics
  • Anticonvulsants / pharmacology*
  • Chemistry, Pharmaceutical
  • Humans
  • Phenytoin / analogs & derivatives*
  • Phenytoin / chemistry
  • Phenytoin / pharmacokinetics
  • Phenytoin / pharmacology
  • Prodrugs / chemistry
  • Prodrugs / pharmacokinetics
  • Prodrugs / pharmacology*

Substances

  • Anticonvulsants
  • Prodrugs
  • Phenytoin
  • fosphenytoin