Topical medication for the posterior part of the eye. The principles and the investigation of efficient drugs

(1)局部应用伊甘地平（一种水溶性钙拮抗剂）和尼普拉地洛尔（一种具有一氧化氮释放作用的α - β拮抗剂），具有增加兔视神经头循环的作用。(2)氯美定（钙拮抗剂）和倍他洛尔（具有钙拮抗剂作用的β拮抗剂）对大鼠视网膜神经节细胞或Muller细胞有神经保护作用。(3)在家兔实验中，局部应用伊加地平渗透到视网膜表面，浓度足以发挥内皮素-1引起血管收缩的抑制作用。(4)放射自显影研究表明，局部应用的伊加地平或尼普地洛能以足够的浓度渗入眼后部或球周组织。(5)长期外用尼帕地洛尔、倍他洛尔或伊加地平对正常人视神经头循环的影响越来越大。

(1) Topically applied iganidipine (a water-soluble calcium antagonist) and nipradilol (an alpha-beta antagonist with nitric oxide releasing effect) showed the effects of increasing circulation in the optic nerve head of rabbits.(2) Lomeridine (a calcium antagonist) and betaxolol (a beta antagonist with calcium antagonistic effect) showed neuroprotective effects on the retinal ganglion cells or Muller cells of rats.(3) In rabbits, topically applied iganidipine penetrated into the retinal surface with the concentration sufficient to exert the inhibiting effects of vascular constriction caused with endothlin-1.(4) Autoradiography studies showed that topically applied iganidipine or nipradilol penetrated into the posterior portion of eye or into peribulbar tissues with sufficient concentration.(5) Long-term topical application of nipradilol, betaxolol, or iganidipine showed increasing effects on the optic nerve head circulation of normal humans.