Intraocular penetration and effect on the retina of fluconazole.
The intraocular concentration of fluconazole was measured in nonvitrectomized and vitrectomized eyes after an intravenous administration of 5 or 25 mg/kg fluconazole in albino rabbits. Respective fluconazole concentrations in the aqueous, vitreous and serum 1 hour after administration were 2.87, 1.72 and 4.60 micrograms/ml at 5 mg/kg administration, and 14.93, 7.05 and 20.63 micrograms/ml at 25 mg/kg administration, indicating high and dose-dependent intraocular penetration of fluconazole. Intraocular penetration of intravenously administered fluconazole was moderately, not very much, enhanced by vitrectomy. The in-vitro electroretinogram (ERG) remained unchanged after perfusion with 20 micrograms/ml of fluconazole. The in-vivo ERG and the visual evoked potential was unchanged after the daily administration of 25 mg/kg fluconazole for 8 days. The toxicity of fluconazole on the retina would be low and within safety limits so far as it is used at clinical dosage. Fluconazole may have a place in the treatment of fungal ocular infections.
Mochizuki
K
K
Department of Ophthalmology, Kanazawa University School of Medicine, Japan.
Yamashita
Y
Y
Torisaki
T
T
Komatsu
K
K
Tanahashi
T
T
Sakai
H
H
D000818:Animals; D001082:Aqueous Humor / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D004596:Electroretinography / Q000187:drug effects; D005074:Evoked Potentials, Visual / Q000187:drug effects; D015725:Fluconazole / Q000493:pharmacokinetics* / Q000633:toxicity*; D007275:Injections, Intravenous; D011817:Rabbits; D012160:Retina / Q000187:drug effects*; D014821:Vitrectomy; D014822:Vitreous Body / Q000378:metabolism
D015725:Fluconazole