Penetration of voriconazole, 1%, eyedrops into human aqueous humor: a prospective open-label study

Arch Ophthalmol. 2008 Mar;126(3):343-6. doi: 10.1001/archophthalmol.2007.71.


Objective: To determine the therapeutic efficacy of adjuvant use of voriconazole, 1%, eyedrops in the treatment of refractory fungal keratitis.

Methods: A prospective open-label trial was conducted to determine voriconazole levels obtained in human aqueous humor after administration of a 1% solution, preserved with 0.01% benzalkonium chloride, every 6 hours for 3 days, or hourly for 4 doses. Ten participants were selected among patients scheduled to undergo elective anterior segment surgery, and samples were tested using validated high-performance liquid chromatography.

Results: The mean (SD) voriconazole concentrations after hourly dosing (n = 5) was 1.90 (1.12) microg/mL and after a single dosing every 6 hours (n = 5) was 0.94 (1.21) microg/mL, respectively. The mean (SD) sampling times after the last administration of eyedrops were 1.1 (0.5) hours after hourly dosing and 2.1 (0.6) hours after a single dosing every 6 hours.

Conclusions: Voriconazole, 1%, eyedrops are well tolerated and penetrate into human aqueous humor when administered at hourly or 6-hourly intervals. They are effective in treating Candida and Aspergillus keratitis, are substantially more affordable than oral therapy, and have less potential to cause systemic adverse effects.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Aged, 80 and over
  • Antifungal Agents / pharmacokinetics*
  • Aqueous Humor / metabolism*
  • Biological Availability
  • Humans
  • Ophthalmic Solutions / pharmacokinetics*
  • Prospective Studies
  • Pyrimidines / pharmacokinetics*
  • Tissue Distribution
  • Triazoles / pharmacokinetics*
  • Voriconazole


  • Antifungal Agents
  • Ophthalmic Solutions
  • Pyrimidines
  • Triazoles
  • Voriconazole