Ocular uptake of fluconazole following oral administration

Arch Ophthalmol. 1990 Jul;108(7):1006-8. doi: 10.1001/archopht.1990.01070090108050.

Abstract

The ocular penetration and distribution of oral fluconazole was studied in Dutch-belted rabbits. Measured by high-pressure liquid chromatography, fluconazole readily penetrated all ocular tissues and fluids. No difference was observed between the levels obtained in phakic and aphakic eyes. Four hours after a single oral dose of 20 mg/kg, the mean levels and SEs were as follows: cornea, 13.3 +/- 1.4 micrograms/g; aqueous, 7.4 +/- 0.3 mg/L; vitreous, 9.8 +/- 0.9 mg/L; and choroid/retina, 5.2 +/- 0.4 micrograms/g. These levels were approximately twice those obtained with a 10-mg/kg dose. The corneal concentrations correlated highly with serum levels (r = .89). A steady accumulation in both normal corneas and corneas infected with Candida albicans was noted when 17.5 mg/kg of fluconazole was administered twice daily over a 5-day period. Drug levels did not increase in the cornea when fluconazole was administered as a single daily dose of 35 mg/kg. In view of its excellent ocular pharmacokinetic profile, fluconazole merits further attention as an orally administered agent for ocular fungal infections.

Publication types

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

MeSH terms

  • Administration, Oral
  • Animals
  • Aqueous Humor / metabolism
  • Choroid / metabolism
  • Cornea / metabolism
  • Dose-Response Relationship, Drug
  • Eye / metabolism*
  • Fluconazole / administration & dosage
  • Fluconazole / blood
  • Fluconazole / pharmacokinetics*
  • Lens, Crystalline / metabolism
  • Rabbits
  • Retina / metabolism
  • Time Factors
  • Tissue Distribution
  • Vitreous Body / metabolism

Substances

  • Fluconazole