Evaluation of concentration of voriconazole in aqueous humor after topical and oral administration in horses

To determine penetration of topically and orally administered voriconazole into ocular tissues and evaluate concentrations of the drug in blood and signs of toxicosis after topical application in horses. 11 healthy adult horses. Each eye in 6 horses was treated with a single concentration (0.5%, 1.0...

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Bibliographic Details
Published in:	American journal of veterinary research Vol. 67; no. 2; pp. 296 - 301
Main Authors:	Clode, A.B, Davis, J.L, Salmon, J, Michau, T.M, Gilger, B.C
Format:	Journal Article
Language:	English
Published:	United States 01-02-2006
Subjects:	Administration, Oral Administration, Topical adverse effects Animals Antifungal Agents - administration & dosage Antifungal Agents - adverse effects Antifungal Agents - blood Antifungal Agents - pharmacokinetics aqueous humor Aqueous Humor - chemistry blood plasma chemical concentration Dose-Response Relationship, Drug drug evaluation drug toxicity eyes Female horses Horses - metabolism Male oral administration poisoning Pyrimidines - administration & dosage Pyrimidines - adverse effects Pyrimidines - blood Pyrimidines - pharmacokinetics topical application triazole fungicides Triazoles - administration & dosage Triazoles - adverse effects Triazoles - blood Triazoles - pharmacokinetics Voriconazole
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Summary:	To determine penetration of topically and orally administered voriconazole into ocular tissues and evaluate concentrations of the drug in blood and signs of toxicosis after topical application in horses. 11 healthy adult horses. Each eye in 6 horses was treated with a single concentration (0.5%, 1.0%, or 3.0%) of a topically administered voriconazole solution every 4 hours for 7 doses. Anterior chamber paracentesis was performed and plasma samples were collected after application of the final dose. Voriconazole concentrations in aqueous humor (AH) and plasma were measured via high-performance liquid chromatography. Five horses received a single orally administered dose of voriconazole (4 mg/kg); anterior chamber paracentesis was performed, and voriconazole concentrations in AH were measured. Mean +/- SD voriconazole concentrations in AH after topical administration of 0.5%, 1.0%, and 3.0% solutions (n = 4 eyes for each concentration) were 1.43 +/- 0.37 microg/mL, 2.35 +/- 0.78 microg/mL, and 2.40 +/- 0.29 microg/mL, respectively. The 1.0% and 3.0% solutions resulted in significantly higher AH concentrations than the 0.5% solution, and only the 3.0% solution induced signs of ocular toxicosis. Voriconazole was detected in the plasma for 1 hour after the final topically administered dose of all solutions. Mean +/- SD voriconazole concentration in AH after a single orally administered dose was 0.86 +/- 0.22 microg/mL. Results indicated that voriconazole effectively penetrated the cornea in clinically normal eyes and reached detectable concentrations in the AH after topical administration. The drug also penetrated noninflamed equine eyes after oral administration. Low plasma concentrations of voriconazole were detected after topical administration.
ISSN:	0002-9645 1943-5681
DOI:	10.2460/ajvr.67.2.296