Experimental intravitreal ketoconazole in DMSO.
Ketoconazole is a weakly dibasic synthetic imidazole with a broad spectrum of antifungal activity. Topical, subconjuctival, and systemic administrations provide poor concentrations in the vitreous. To determine the ocular toxicity of intravitreal ketoconazole, the authors injected doses varying between 15 micrograms to 2240 micrograms dissolved in 0.1 ml of 100% DMSO into the vitreous bodies of 24 rabbits. Doses of 540 micrograms or less resulted in no toxicity to the eyes. Doses of 720 micrograms revealed electroretinographic abnormalities and photoreceptor degeneration by electron microscopy. Doses of 2,240 micrograms resulted in severe histopathologic and electroretinographic alterations. This study suggests that a single intravitreal dose of 540 micrograms or less of ketoconazole in DMSO may be safely used in the treatment of fungal endophthalmitis.
Yoshizumi
M O
MO
Jules Stein Eye Institute, Department of Ophthalmology, UCLA School of Medicine 90024.
Banihashemi
A R
AR
D000287:Administration, Topical; D000818:Animals; D004121:Dimethyl Sulfoxide; D004596:Electroretinography; D009877:Endophthalmitis / Q000188:drug therapy*; D007654:Ketoconazole / Q000008:administration & dosage / Q000633:toxicity*; D011817:Rabbits; D012162:Retinal Degeneration / Q000139:chemically induced; D014822:Vitreous Body
D007654:Ketoconazole; D004121:Dimethyl Sulfoxide