Aqueous humor concentration of voriconazole after topical administration in rabbits

Abstract

In AH, therapeutic drug levels that cover the minimum inhibitory concentrations (MIC) of most fungi can be reached. To achieve a sustained high level of voriconazole as an effective antifungal therapy for corneal keratitis, voriconazole should be topically administered every 30 min.

Severe Arthrographis kalrae Keratomycosis in an Immunocompetent Patient

“…7 Voriconazole can reach effective levels in the eye when used systemically and topically. 1,8 In our patient, despite systemic and topical voriconazole treatment for almost 1 year, the A. kalrae infection could only be stabilizied but not eliminated. The infection recurred repeatedly.…”

Infectious Keratitis After Boston Type 1 Keratoprosthesis Implantation

“…23 Voriconazole can reach effective intraocular levels when used systemically and/or topically. 22,24 It can penetrate through corneas with intact epithelium because of its highly lipophilic nature and may penetrate more rapidly than amphotericin because of its smaller size. 22 The systemic side-effect profile of voriconazole appears to be relatively safe with side effects of extreme swelling, mild and transient skin rashes, and liver enzyme elevations reported.…”

Voriconazole

“…In the rabbit, administration of 1% VCZ topically did penetrate the aqueous humor and achieved MICs, but dosing frequency to attain these levels requires administration every 30 minutes, which is impractical. 41 The majority of other studies of VCZ have used the rodent models for human fungal disease. 42 In a mouse study with inoculated blastomycosis and grapefruit juice provision, oral VCZ at 40 mg/kg once a day resulted in greater suppression of CFU than when administered at 5 or 20 mg/kg once a day and 40 mg/kg three times a week, and prolonged survival in a dose-dependent fashion.…”