The pharmacokinetics of ketoconazole after chronic administration in adults

Eur J Clin Pharmacol. 1987;33(5):531-4. doi: 10.1007/BF00544251.


We have studied the pharmacokinetics of the anti-mycotic ketoconazole in seven patients who took it for 1-6 months at a dose of 200 mg daily. The mean elimination half-life of the drug was 3.3 h, and although the ketoconazole was given only once daily, a satisfactory clinical response was obtained in all seven individuals. Only a small fraction of the absorbed drug (mean 0.22%) was excreted unchanged in the urine, suggesting almost complete metabolism. Our results support the concept that anti-mycotic activity in the tissues continues after the plasma drug concentration has fallen below a critical level. Our results also support the concept of a change in pharmacokinetics with chronic dosing.

MeSH terms

  • Adult
  • Aged
  • Drug Administration Schedule
  • Female
  • Half-Life
  • Humans
  • Ketoconazole / administration & dosage
  • Ketoconazole / blood
  • Ketoconazole / pharmacokinetics*
  • Male
  • Middle Aged


  • Ketoconazole