Extent of urinary excretion of p-hydroxyphenytoin in healthy subjects given phenytoin

R. G. Dickinson, W. D. Hooper, M. Patterson, M. J. Eadie, B. Maguire

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58 Scopus citations

Abstract

Urinary excretion of p-hydroxyphenytoin and its glucuronide conjugate was measured in eight healthy young adults in a comparative bioavailability study of oral sodium phenytoin (~5 mg/kg/dose). Among these subjects the percentage of the phenytoin dose converted to p-hydroxyphenytoin and appearing in urine was relatively similar (mean 79%, range 67-88%). The great majority of the p-hydroxyphenytoin appeared in urine as conjugates; only 1.4-3.4% of the excreted /j-hydroxyphenytoin was in the form of unconjugated metabolite. The proportion of a single phenytoin dose excreted in urine as /?-hydroxyphenytoin or its conjugate increased from the first dose (mean ± SD) 74.9 ± 4.6% to the second dose, given 2 weeks later 79.3 ± 4.6% (p < 0.05). This finding suggests that autoinduction of phenytoin metabolism may occur after relatively brief exposure to the drug.

Original languageEnglish (US)
Pages (from-to)283-289
Number of pages7
JournalTherapeutic Drug Monitoring
Volume7
Issue number3
DOIs
StatePublished - Sep 1985

Keywords

  • Autoinduction
  • Bioavailability
  • Metabolism
  • Phenytoin

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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