Intraocular penetration and effect on the retina of fluconazole.

Abstract

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.

• Authors: K Mochizuki, Y Yamashita, T Torisaki, K Komatsu, T Tanahashi, H Sakai
• Journal: Lens and eye toxicity research (Lens Eye Toxic Res) Vol. 9 Issue 3-4 Pg. 537-46 ( 1992) ISSN: 1042-6922 [Print] United States
• PMID: 1301802 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Fluconazole

Topics

• Animals
• Aqueous Humor (metabolism)
• Chromatography, High Pressure Liquid
• Electroretinography (drug effects)
• Evoked Potentials, Visual (drug effects)
• Fluconazole (pharmacokinetics, toxicity)
• Injections, Intravenous
• Rabbits
• Retina (drug effects)
• Vitrectomy
• Vitreous Body (metabolism)