Nishimura K, Shirasawa E, Kinoshita M, Hikida M, Kuwayama Y
Central Research Laboratories, Santen Pharmaceutical Company Limited, Osaka, Japan.
Nippon Ganka Gakkai Zasshi. 1991 Aug;95(8):746-51.
Effects of topically applied bunazosin, an alpha 1-adrenoceptor blocker, on intraocular pressure (IOP) and pupillary diameter were investigated in normotensive rabbits and cats, in addition to experimentally hypertensive rabbits. Bunazosin (0.005% to 0.1%) applied to both eyes significantly lowered IOP in a concentration-dependent manner in normotensive rabbits and cats. The unilateral application of 0.1% bunazosin significantly lowered the IOP in the treated eye, whereas it caused no significant change in the contralateral eye, suggesting that the effect of bunazosin is due mainly to a direct and local action and is not systemic. Bunazosin was also effective in experimentally hypertensive models induced both by water-loading and by alpha-chymotrypsin in rabbits. There was a significant correlation between the IOP decrease caused by bunazosin and the IOP value before the application, indicating that the IOP-lowering action of bunazosin is dependent on the height of the original IOP level. Bunazosin had no influence on pupillary diameter even when 0.5% was applied to rabbits. Topically applied bunazosin may be useful as a new antiglaucoma agent.
除了实验性高血压兔外,还在血压正常的兔和猫身上研究了局部应用α1肾上腺素能受体阻滞剂布那唑嗪对眼压(IOP)和瞳孔直径的影响。在血压正常的兔和猫中,双眼应用布那唑嗪(0.005%至0.1%)以浓度依赖的方式显著降低眼压。单侧应用0.1%布那唑嗪可显著降低治疗眼的眼压,而对侧眼无明显变化,这表明布那唑嗪的作用主要是直接和局部的,而非全身性的。布那唑嗪对兔水负荷诱导的和α-糜蛋白酶诱导的实验性高血压模型也有效。布那唑嗪引起的眼压降低与用药前的眼压值之间存在显著相关性,表明布那唑嗪的降眼压作用取决于初始眼压水平的高度。即使向兔应用0.5%的布那唑嗪,对瞳孔直径也没有影响。局部应用布那唑嗪可能作为一种新型抗青光眼药物有用。