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G. Atma Vemulakonda, MD; Seenu M. Hariprasad, MD; William F. Mieler, MD; Randall A. Prince, PharmD; Gaurav K. Shah, MD; Russell N. Van Gelder, MD, PhD

Arch Ophthalmol. 2008;126(1):18-22.

Objective  To determine the penetration of 1% voriconazole solution into the aqueous and vitreous following topical administration.

Methods  A prospective nonrandomized study of 13 patients scheduled for pars plana vitrectomy surgery. Aqueous and vitreous samples were obtained and analyzed after topical administration of 1% voriconazole every 2 hours for 24 hours before surgery. Drug concentration quantitation was performed using high-performance liquid chromatography.

Results  The mean (SD) sampling time after topical administration of the last voriconazole dose was 24 (14) minutes. The mean (SD) voriconazole concentrations in the aqueous and vitreous were 6.49 (3.04) µg/mL and 0.16 (0.08) µg/mL, respectively. Aqueous concentrations exceeded the minimum inhibitory concentration at which 90% of isolates are inhibited (MIC₉₀) for a wide spectrum of fungi and mold, including Aspergillus, Fusarium, and Candida species. Vitreous concentrations of voriconazole exceeded the MIC₉₀ for Candida albicans.

Conclusion  Topically administered voriconazole achieves therapeutic concentrations in the aqueous of the noninflamed human eye for many fungi and molds and achieves therapeutic levels in the vitreous for Candida species. Topical voriconazole may be a useful agent for the management of fungal keratitis and for prophylaxis against the development of fungal endophthalmitis.

Author Affiliations: Departments of Ophthalmology and Visual Sciences (Drs Vemulakonda, Shah, and Van Gelder) and Molecular Biology and Pharmacology (Dr Van Gelder), Washington University School of Medicine, and Barnes Retina Institute (Drs Hariprasad, Shah, and Van Gelder), St Louis, Missouri; Department of Ophthalmology and Visual Science, The University of Chicago, Chicago, Illinois (Dr Mieler); and College of Pharmacy, University of Houston, Houston, Texas (Dr Prince). Dr Vemulakonda is now with the Retina Division, Casey Eye Institute, Oregon Health and Science University, Portland. Dr Hariprasad is now with the Department of Ophthalmology and Visual Science, The University of Chicago. Dr Van Gelder is now with the Department of Ophthalmology, University of Washington Medical School, Seattle.