Inhibition of experimental intraocular proliferation with intravitreal 5-fluouracil

Abstract

5-Fluorouracil was used to inhibit experimental intraocular proliferation in rabbit eyes, produced by homologe fibroblast implantation. Two different concentrations were used, 1 and 5 mg in a single intravitreal injection. The eyes were followed up over 4 weeks. Proliferation and resulting traction detachment was reduced from 75% to 30% in the 1-mg 5-fluouracil group. In addition, we observed retinal and vascular changes in a considerable number of eyes treated with 1 mg and much more pronounced alterations in most of the eyes treated with 5 mg fluouracil.

High-Energy Electrons Used to Inhibit Experimental Intraocular Proliferation and Detachment

“…With doses higher than 3,000 rad or with inaccurate application of radiation treatment [Kinyoun et al, 1984], however, tissue dam age may not be excluded. In this connection, it should also be mentioned that toxic effects on the retina may be equally produced by higher doses of antimetabolites [Binder et al, 1983;Santana et al, 1984], Furthermore, the question of the degree of retinal damage pro duced by strong bluelight. by mechanical manipulations as well as by intraocular sili cone tamponades [Binder et al, 1983;Gonvers, 1986] still awaits further clarification.…”

“…Antiproliferative preparations, such as dexamethasone alcohol, triamcinolone acetonide, 5-fluoracil and daunomicin, have proven their effectiveness in experimental conditions [Tano ct al., 1980;Binder, 1982;Blumenkranz et al, 1983: Binder et al, 1983Kulnig et al, 1984]. Their disadvantages, however, have also become manifest, as e.g.…”

Resultados a longo prazo do uso de drogas antiproliferativas na trabeculectomia primária

“…O uso de agentes antiproliferativos promove uma melhora nos índices de sucesso desta cirurgia por inibir a proliferação fibroblástica e a biosíntese de colágeno e material extracelular (1)(2) . O 5-Fluorouracil (5-FU) é uma droga capaz de inibir a proliferação de fibroblastos in vitro e in vivo, reduzindo a síntese de colágeno e a formação da cicatriz (3)(4) . A droga pode ser injetada no espaço subconjuntival no período pós-operatório (5) , ou aplicada sob o retalho conjuntival durante o procedimento cirúrgico.…”

Liposome-encapsulated3H-5FU in rabbits

“…Therapeutic intraocular levels of 5FU can be achieved by intravitreal or subconjunctival administration [7]. However, frequent injections are needed to maintain therapeutic levels, and potentially toxic levels can occur immediately following an intravitreal injection of 1 mg into the rabbit eye [13,2]. A method that would increase the ocular penetration of a drug after subconjunctival injection, or slowly release the drug after intravitreal injection to increase its half-life, would be advantageous.…”