Stern W H, Guerin C J, Erickson P A, Lewis G P, Anderson D H, Fisher S K
Am J Ophthalmol. 1983 Jul;96(1):43-51. doi: 10.1016/0002-9394(83)90453-1.
The retinal and corneal toxicity of fluorouracil in the rabbit eye after lensectomy and vitrectomy depended on both the dosage and the frequency of intraocular injection and was reversible at certain dosages. All eyes in Group 1 (1.25 mg of fluorouracil every 12 hours for four days and then every 24 hours for three days) had opaque corneas by three days; these did not clear for four weeks. Histologic studies showed loss of photoreceptor outer segments and loss of ribosomes in all the retinal cells examined. The electroretinographic b-wave decreased to 0% of the baseline value (no b-wave), and did not recover after three weeks. In Group 2 eyes (1.25 mg of fluorouracil every 24 hours for seven days), corneal opacification increased to a maximum after two weeks and gradually decreased by four weeks. The electroretinographic b-wave diminished to 9.6% of the baseline value at two weeks but later recovered to 62.5% of the baseline value at three weeks. Histologic studies showed loss of photoreceptor outer segments and ribosomes at nine days; both returned to near normal after five weeks. Clinical, electrophysiologic, and histologic studies showed no toxicity in Group 3 eyes (0.5 mg of fluorouracil every 24 hours for seven days). This dosage of fluorouracil exerts a significant antiproliferative effect on injected retinal pigment epithelial cells and is well tolerated by the rabbit eye.
晶状体切除和玻璃体切除术后，氟尿嘧啶对兔眼视网膜和角膜的毒性取决于眼内注射的剂量和频率，且在一定剂量下是可逆的。第1组所有眼睛（每12小时注射1.25mg氟尿嘧啶，共4天，然后每24小时注射1.25mg氟尿嘧啶，共3天）在3天时角膜均出现混浊，4周后仍未消退。组织学研究显示，在所检查的所有视网膜细胞中，光感受器外节丢失，核糖体减少。视网膜电图b波降至基线值的0%（无b波），3周后仍未恢复。第2组眼睛（每24小时注射1.25mg氟尿嘧啶，共7天），角膜混浊在2周时增至最大，4周时逐渐减轻。视网膜电图b波在2周时降至基线值的9.6%，但在3周时恢复至基线值的62.5%。组织学研究显示，9天时光感受器外节和核糖体减少，5周后两者均恢复至接近正常水平。临床、电生理和组织学研究显示，第3组眼睛（每24小时注射0.5mg氟尿嘧啶，共7天）无毒性。该剂量的氟尿嘧啶对注射的视网膜色素上皮细胞具有显著的抗增殖作用，且兔眼耐受性良好。
