Oshika T, Araie M, Sugiyama T, Nakajima M, Azuma I
Department of Ophthalmology, University of Tokyo, School of Medicine, Japan.
Arch Ophthalmol. 1991 Nov;109(11):1569-74. doi: 10.1001/archopht.1991.01080110105046.
We investigated the effects of topical administration of bunazosin hydrochloride, a new selective alpha 1-adrenergic antagonist, on intraocular pressure and aqueous humor dynamics in normal human eyes. In the single-dose study, all concentrations of bunazosin (0.025%, 0.05%, 0.1%, and 0.2%) significantly lowered intraocular pressure in a concentration-dependent manner. Administration of multiple doses of 0.1% bunazosin revealed no occurrence of tachyphylaxis after 1 week. Single application of 0.1% bunazosin had no significant influence on aqueous flow rate, tonographic outflow facility, or episcleral venous pressure, suggesting that bunazosin reduces intraocular pressure by increasing uveoscleral outflow. Aqueous protein concentration was found to be unaltered by bunazosin, indicating that blood-aqueous barrier permeability to protein molecules remained unchanged. We conclude that bunazosin may be a possible new antiglaucoma agent with a mechanism of action different from those currently in use for treating ocular hypertension.
我们研究了新型选择性α1肾上腺素能拮抗剂盐酸布那唑嗪局部给药对正常人眼内压和房水动力学的影响。在单剂量研究中，所有浓度的布那唑嗪（0.025%、0.05%、0.1%和0.2%）均以浓度依赖方式显著降低眼内压。多次给予0.1%布那唑嗪1周后未出现快速耐受现象。单次应用0.1%布那唑嗪对房水流量、眼压描记流出易度或巩膜静脉压无显著影响，提示布那唑嗪通过增加葡萄膜巩膜流出降低眼内压。发现布那唑嗪未改变房水蛋白浓度，表明血-房水屏障对蛋白质分子的通透性保持不变。我们得出结论，布那唑嗪可能是一种新型抗青光眼药物，其作用机制与目前用于治疗高眼压症的药物不同。
