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  Vol. 126 No. 3, March 2008 TABLE OF CONTENTS
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Penetration of Voriconazole, 1%, Eyedrops Into Human Aqueous Humor

A Prospective Open-Label Study

David Lau, BPharm, MRPharmS; Mervyn Fedinands, MBBS(Hons); Lok Leung, BPharm(Hons); Robert Fullinfaw, BSc, DSc; David Kong, PhD, BPharm, MPharm; Geoff Davies, BPharm; Mark Daniell, MBBS, MS, FRACS, FRANZCO

Arch Ophthalmol. 2008;126(3):343-346.

Objective  To determine the therapeutic efficacy of adjuvant use of voriconazole, 1%, eyedrops in the treatment of refractory fungal keratitis.

Methods  A prospective open-label trial was conducted to determine voriconazole levels obtained in human aqueous humor after administration of a 1% solution, preserved with 0.01% benzalkonium chloride, every 6 hours for 3 days, or hourly for 4 doses. Ten participants were selected among patients scheduled to undergo elective anterior segment surgery, and samples were tested using validated high-performance liquid chromatography.

Results  The mean (SD) voriconazole concentrations after hourly dosing (n = 5) was 1.90 (1.12) µg/mL and after a single dosing every 6 hours (n = 5) was 0.94 (1.21) µg/mL, respectively. The mean (SD) sampling times after the last administration of eyedrops were 1.1 (0.5) hours after hourly dosing and 2.1 (0.6) hours after a single dosing every 6 hours.

Conclusions  Voriconazole, 1%, eyedrops are well tolerated and penetrate into human aqueous humor when administered at hourly or 6-hourly intervals. They are effective in treating Candida and Aspergillus keratitis, are substantially more affordable than oral therapy, and have less potential to cause systemic adverse effects.


Author Affiliations: Department of Pharmacy, Eastern Health (Mr Lau); Departments of Ophthalmology (Messrs Fedinands and Daniell) and Pharmacy (Messrs Leung and Davies), Royal Victorian Eye and Ear Hospital; Department of Specialist Chemistry, Royal Melbourne Hospital (Dr Fullinfaw); and Department of Pharmacy Practice, Monash University (Dr Kong), Melbourne, Australia.



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