Penetration of voriconazole, 1%, eyedrops into human aqueous humor: a prospective open-label study.
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) microg/mL and after a single dosing every 6 hours (n = 5) was 0.94 (1.21) microg/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.
Lau
David
D
Department of Ophthalmology, Royal Victorian Eye and Ear Hospital, East Melbourne, Victoria, Australia.
Fedinands
Mervyn
M
Leung
Lok
L
Fullinfaw
Robert
R
Kong
David
D
Davies
Geoff
G
Daniell
Mark
M
D000368:Aged; D000369:Aged, 80 and over; D000935:Antifungal Agents / Q000493:pharmacokinetics*; D001082:Aqueous Humor / Q000378:metabolism*; D001682:Biological Availability; D006801:Humans; D009883:Ophthalmic Solutions / Q000493:pharmacokinetics*; D011446:Prospective Studies; D011743:Pyrimidines / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D014230:Triazoles / Q000493:pharmacokinetics*; D065819:Voriconazole
D000935:Antifungal Agents; D009883:Ophthalmic Solutions; D011743:Pyrimidines; D014230:Triazoles; D065819:Voriconazole