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July 1985

Topical Fluorouracil: Pharmacokinetics in Normal Rabbit Eyes

Author Affiliations

From the Department of Ophthalmology, Bascom Palmer Eye Institute, University of Miami School of Medicine. Dr Heuer is now with the Department of Ophthalmology, University of Florida College of Medicine, Gainesville. Dr Gressel is now with the Department of Ophthalmology, Cleveland Clinic Foundation.

Arch Ophthalmol. 1985;103(7):953-955. doi:10.1001/archopht.1985.01050070079034

• Postoperative subconjunctival fluorouracil injections may be a useful adjunct to standard glaucoma filtering surgery in eyes that are at high risk of failure. Topical administration would be perferable to subconjunctival administration; however, there are no data on the ocular penetration of topically applied fluorouracil. Consequently, we investigated the pharmacokinetics of topically administered fluorouracil labeled with carbon 14 in normal rabbit eyes. One drop (approximately 2.4 mg) of fluorouracil resulted in the following concentrations at 0.5 and six hours, respectively: 17.3 and 0.9 μg/g of conjunctiva; 24.3 and 1.3 μg/g of cornea; 14.6 and 0.2 μg/mL of aqueous; 0.8 and 0.5 μg/g of lens; 1.1 and 0.3 μg/g of vitreous; and 0.2 and less than 0.1 μg/mL of serum. Three drops (approximately 7.2 mg) of fluorouracil resulted in the following concentrations at 0.5 and eight hours, respectively: 589.8 and 1.3 μg/g of conjunctiva; 502.9 and 1.8 μg/g of cornea; 199.6 and 0.8 μg/mL of aqueous; 6.2 and 0.5 μg/g of lens; 6.8 and 0.5 pg/g of vitreous; and 1.3 and 0.2 μg/mL of serum. Since a fluorouracil concentration of 0.2 μg/mL inhibits rabbit conjunctival fibroblast proliferation in cell culture by 50%, these data suggest that topically applied fluorouracil achieves sufficient levels in the ocular compartments and tissues to have potential therapeutic applications.

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