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Penetration of Voriconazole, 1%, Eyedrops Into Human Aqueous HumorA 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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