Aqueous and vitreous concentrations following topical administration of 1% voriconazole in humans.
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) microg/mL and 0.16 (0.08) microg/mL, respectively. Aqueous concentrations exceeded the minimum inhibitory concentration at which 90% of isolates are inhibited (MIC(90)) for a wide spectrum of fungi and mold, including Aspergillus, Fusarium, and Candida species. Vitreous concentrations of voriconazole exceeded the MIC(90) for Candida albicans.


CONCLUSIONS
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.
Vemulakonda
G Atma
GA
Department of Ophthalmology and Visual Sciences, Washington University School of Medicine, St Louis, MO 63110, USA.
Hariprasad
Seenu M
SM
Mieler
William F
WF
Prince
Randall A
RA
Shah
Gaurav K
GK
Van Gelder
Russell N
RN
D000287:Administration, Topical; D000328:Adult; D000368:Aged; D000935:Antifungal Agents / Q000493:pharmacokinetics*; D001082:Aqueous Humor / Q000378:metabolism*; D001682:Biological Availability; D002175:Candida / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D008826:Microbial Sensitivity Tests; D008875:Middle Aged; D011446:Prospective Studies; D011743:Pyrimidines / Q000493:pharmacokinetics*; D014230:Triazoles / Q000493:pharmacokinetics*; D014821:Vitrectomy; D014822:Vitreous Body / Q000378:metabolism*; D065819:Voriconazole
D000935:Antifungal Agents; D011743:Pyrimidines; D014230:Triazoles; D065819:Voriconazole