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一种Rho相关蛋白激酶抑制剂对兔的眼内降压作用。

Ocular hypotensive effects of a Rho-associated protein kinase inhibitor in rabbits.

作者信息

Kamaruddin Muhammad Irfan, Nakamura-Shibasaki Momoko, Mizuno Yu, Kiuchi Yoshiaki

机构信息

Department of Ophthalmology and Visual Sciences, Graduate School of Biomedical Sciences, Hiroshima University, Hiroshima, Japan.

Department of Ophthalmology, Hasanuddin University, Makassar, South Sulawesi, Indonesia.

出版信息

Clin Ophthalmol. 2017 Mar 31;11:591-597. doi: 10.2147/OPTH.S131416. eCollection 2017.

Abstract

PURPOSE

Ripasudil is a novel Rho-associated protein kinase inhibitor that is used to treat ocular hypertension. However, the comparison of the intraocular pressure (IOP)-lowering effects between ripasudil alone and other ocular hypotensive drugs has not been studied thoroughly. The purpose of this study is to examine the ocular hypotensive effects of 0.4% ripasudil, 2% pilocarpine, 0.5% timolol and 0.1% dorzolamide in rabbits. We also studied the IOP changes when 0.4% ripasudil was combined with 2% pilocarpine, 0.5% timolol or 0.1% dorzolamide.

METHODS

One drop of saline solution, 0.4% ripasudil, 0.5% timolol, 2% pilocarpine or 1% dorzolamide or a combination of these agents was applied topically to the left eyes of eight healthy albino rabbits. Posttreatment changes in the IOP of albino rabbits were monitored using a rebound tonometer over a 5-h time course. Changes in IOP after application of saline served as the control. One-way analysis of variance and Dunnett's post hoc tests were used for statistical analyses.

RESULTS

After topical instillation, 0.4% ripasudil resulted in significant decreases in IOP at 0.5 and 1 h compared with the control group. Treatment with timolol, pilocarpine or dorzolamide had no significant effect on IOP. Treatment with timolol, pilocarpine or dorzolamide in combination with ripasudil resulted in significant reductions in IOP at 1 h. However, none of these agents enhanced the IOP-lowering effects of ripasudil.

CONCLUSION

Ripasudil has stronger IOP-lowering effects than timolol, pilocarpine or dorzolamide hypotensive agents in our rabbit model. Addition of timolol, pilocarpine or dorzolamide did not enhance the IOP-lowering effects of ripasudil alone.

摘要

目的

ripasudil是一种新型的Rho相关蛋白激酶抑制剂,用于治疗高眼压症。然而,ripasudil单独使用与其他降眼压药物之间降低眼压(IOP)效果的比较尚未得到充分研究。本研究的目的是检测0.4%ripasudil、2%毛果芸香碱、0.5%噻吗洛尔和0.1%多佐胺对兔眼压的降低作用。我们还研究了0.4%ripasudil与2%毛果芸香碱、0.5%噻吗洛尔或0.1%多佐胺联合使用时的眼压变化。

方法

将一滴盐溶液、0.4%ripasudil、0.5%噻吗洛尔、2%毛果芸香碱或1%多佐胺或这些药物的组合局部应用于8只健康白化兔的左眼。使用回弹眼压计在5小时的时间过程中监测白化兔治疗后眼压的变化。应用盐溶液后的眼压变化作为对照。采用单因素方差分析和Dunnett事后检验进行统计分析。

结果

局部滴注后,与对照组相比,0.4%ripasudil在0.5小时和1小时时眼压显著降低。噻吗洛尔、毛果芸香碱或多佐胺治疗对眼压无显著影响。噻吗洛尔、毛果芸香碱或多佐胺与ripasudil联合治疗在1小时时眼压显著降低。然而,这些药物均未增强ripasudil的降眼压作用。

结论

在我们的兔模型中,ripasudil比噻吗洛尔、毛果芸香碱或多佐胺降压剂具有更强降眼压作用。添加噻吗洛尔、毛果芸香碱或多佐胺并不能增强ripasudil单独使用时的降眼压作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/64a9/5383069/10ecc9cd3948/opth-11-591Fig1.jpg

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