Influence of food on the pharmacokinetics of ketoconazole

T K Daneshmend, D W Warnock, M D Ene, E M Johnson, M R Potten, M D Richardson, P J Williamson

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75 Citations (Scopus)

Abstract

Eight healthy adults were given single oral doses of ketoconazole (200, 400, 600, and 800 mg) in the fasting state and with a standard breakfast at weekly intervals according to a balanced block design. Concentrations in serum were measured up to 32 h after the dose. Food did not reduce ketoconazole absorption or significantly alter peak ketoconazole concentrations in serum, though there was a food-related delay in achieving peak concentrations. At the 400- and 600-mg doses, food appeared to enhance absorption, but this effect was not seen at the 800-mg dose. With an increase in dose, the half-life and area under the serum concentration-time curve increased disproportionately, suggesting that the pharmacokinetics of ketoconazole may be dose dependent. Up to the 800-mg dose, the elimination of ketoconazole did not appear to be saturable. Administration of the drug with food is unlikely to be a cause of therapeutic failure.

Original languageEnglish
Pages (from-to)1-3
Number of pages3
JournalAntimicrobial Agents and Chemotherapy
Volume25
Issue number1
Publication statusPublished - Jan 1984

Keywords

  • Adult
  • Eating
  • Fasting
  • Female
  • Half-Life
  • Humans
  • Ketoconazole/blood
  • Kinetics
  • Male

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