Topical fluorouracil. Pharmacokinetics in normal rabbit eyes

F. E. Fantes, D. K. Heuer, Richard K Parrish, N. Sossi, M. G. Gressel

Research output: Contribution to journalArticle

26 Citations (Scopus)

Abstract

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
Pages (from-to)953-955
Number of pages3
JournalArchives of Ophthalmology
Volume103
Issue number7
StatePublished - Dec 1 1985

Fingerprint

Fluorouracil
Pharmacokinetics
Rabbits
Conjunctiva
Cornea
Lenses
Filtering Surgery
Topical Administration
Serum
Glaucoma
Carbon
Cell Culture Techniques
Fibroblasts
Injections

ASJC Scopus subject areas

  • Ophthalmology

Cite this

Fantes, F. E., Heuer, D. K., Parrish, R. K., Sossi, N., & Gressel, M. G. (1985). Topical fluorouracil. Pharmacokinetics in normal rabbit eyes. Archives of Ophthalmology, 103(7), 953-955.

Topical fluorouracil. Pharmacokinetics in normal rabbit eyes. / Fantes, F. E.; Heuer, D. K.; Parrish, Richard K; Sossi, N.; Gressel, M. G.

In: Archives of Ophthalmology, Vol. 103, No. 7, 01.12.1985, p. 953-955.

Research output: Contribution to journalArticle

Fantes, FE, Heuer, DK, Parrish, RK, Sossi, N & Gressel, MG 1985, 'Topical fluorouracil. Pharmacokinetics in normal rabbit eyes', Archives of Ophthalmology, vol. 103, no. 7, pp. 953-955.
Fantes FE, Heuer DK, Parrish RK, Sossi N, Gressel MG. Topical fluorouracil. Pharmacokinetics in normal rabbit eyes. Archives of Ophthalmology. 1985 Dec 1;103(7):953-955.
Fantes, F. E. ; Heuer, D. K. ; Parrish, Richard K ; Sossi, N. ; Gressel, M. G. / Topical fluorouracil. Pharmacokinetics in normal rabbit eyes. In: Archives of Ophthalmology. 1985 ; Vol. 103, No. 7. pp. 953-955.
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