Topical fluorouracil: Pharmacokinetics in normal rabbit eyes

Francisco E. Fantes, Dale K. Heuer, Richard K. Parrish, Nunzio Sossi, Michael G. Gressel

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28 Scopus citations


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 preferable 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 μg/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.

Original languageEnglish (US)
Pages (from-to)953-955
Number of pages3
JournalArchives of ophthalmology
Issue number7
StatePublished - Jul 1985

ASJC Scopus subject areas

  • Ophthalmology


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