局部应用尼普地洛（一种具有α受体阻断和硝酸甘油样活性的β受体阻滞剂）对房水动力学和眼底循环的影响。

Effects of topical nipradilol, a beta-blocking agent with alpha-blocking and nitroglycerin-like activities, on aqueous humor dynamics and fundus circulation.

作者信息

Kanno M, Araie M, Tomita K, Sawanobori K

机构信息

Department of Ophthalmology, University of Tokyo School of Medicine, Japan.

出版信息

Invest Ophthalmol Vis Sci. 1998 Apr;39(5):736-43.

PMID:9538880

Abstract

PURPOSE

To study the effects of nipradilol, a nonselective beta-blocker with alpha 1-blocking activity and nitroglycerin-like activity, on aqueous humor dynamics and optic nerve head (ONH) circulation in albino rabbits.

METHODS

Experiments were carried out during the dark phase, in conscious rabbits conditioned to a schedule of alternating 12-hour periods of light and dark. The blood-aqueous barrier permeability and the aqueous flow rate were determined fluorophotometrically. The effect on outflow to general blood circulation and uveoscleral outflow were determined by using the fluorophotometric Diamox technique, and the effect on the uveoscleral outflow was further assessed by using the anterior chamber perfusion method. The ONH circulation was estimated by using the laser speckle method.

RESULTS

Unilateral topical administration of 0.25% nipradilol solution lowered intraocular pressure (IOP) with relatively weak contralateral effects in a dose-dependent manner with a maximum reduction of 6 mm Hg and an effect duration of 6 hours. Twice-daily instillation for 14 days showed no attenuation of the effects. Single instillation of 0.25% nipradilol showed no significant effect on blood-aqueous barrier permeability and decreased aqueous flow rate in the treated eye (17%; P < 0.01) and in the contralateral eye (9%, P < 0.05). Nipradilol produced no significant effect on outflow facility to general blood circulation, whereas it substantially increased uveoscleral outflow. Twice-daily 0.25% nipradilol instillation increased ONH tissue blood velocity by 13% (P < 0.01), which was probably attributable to locally penetrating drug.

CONCLUSIONS

Because of its ability to lower IOP and to increase uveoscleral outflow and optic nerve head circulation in rabbits, further studies are warranted to determine whether nipradilol has potential as an antiglaucoma agent in humans.

摘要

目的

研究尼普地洛（一种具有α1受体阻断活性和硝酸甘油样活性的非选择性β受体阻滞剂）对白化兔房水动力学和视神经乳头（ONH）循环的影响。

方法

实验在黑暗期进行，实验对象为适应12小时明暗交替作息的清醒家兔。采用荧光光度法测定血-房水屏障通透性和房水流量。通过荧光光度法地高辛技术测定对全身血液循环流出和葡萄膜巩膜流出的影响，并采用前房灌注法进一步评估对葡萄膜巩膜流出的影响。采用激光散斑法评估ONH循环。

结果

单侧局部应用0.25%尼普地洛溶液可降低眼压（IOP），对侧效应相对较弱，呈剂量依赖性，最大降幅为6 mmHg，作用持续时间为6小时。每日滴眼两次，连续14天，效果无减弱。单次滴注0.25%尼普地洛对血-房水屏障通透性无显著影响，治疗眼房水流量降低（17%；P<0.01），对侧眼降低（9%，P<0.05）。尼普地洛对全身血液循环流出系数无显著影响，但可显著增加葡萄膜巩膜流出。每日两次滴注0.25%尼普地洛可使ONH组织血流速度增加（13%，P<0.01），这可能归因于局部渗透的药物。