Tanihara Hidenobu, Inoue Toshihiro, Yamamoto Tetsuya, Kuwayama Yasuaki, Abe Haruki, Fukushima Atsuki, Suganami Hideki, Araie Makoto
Department of Ophthalmology, Faculty of Life Sciences, Kumamoto University, Kumamoto, Japan.
Department of Ophthalmology, Gifu University Graduate School of Medicine, Gifu, Japan.
Acta Ophthalmol. 2016 Feb;94(1):e26-34. doi: 10.1111/aos.12829. Epub 2015 Sep 4.
To investigate the intra-ocular pressure (IOP)-lowering effects and safety of 0.4% ripasudil (K-115), a Rho kinase inhibitor, twice daily for 52 weeks, in patients with open-angle glaucoma or ocular hypertension (OHT).
In this multicentre, prospective, open-label study, 388 patients with primary open-angle glaucoma, OHT or exfoliation glaucoma were enrolled and 354 of them were subdivided into four cohorts (monotherapy, 173; additive therapy to prostaglandin analogs, 62; β-blockers, 60; or fixed combination drugs, 59). The IOP reduction at trough and peak from baseline and adverse events was investigated.
Ripasudil showed IOP-lowering effects over 52 weeks in all the analyses of monotherapy, additive therapy and both subgroups (baseline IOP ≥21 mmHg and <21 mmHg) of monotherapy. The mean IOP reductions at trough and peak at week 52 were -2.6 and -3.7 mmHg for monotherapy, and -1.4 and -2.4, -2.2 and -3.0, and -1.7 and -1.7 mmHg, respectively, for additive therapy described above. The most frequently observed adverse events were conjunctival hyperaemia (n = 264, 74.6%), blepharitis (n = 73, 20.6%) and allergic conjunctivitis (n = 61, 17.2%). Most of the conjunctival hyperaemia findings were mild (97.0%), transient and resolved spontaneously (78.0%). Although 51 patients discontinued from the study due to blepharitis and/or allergic conjunctivitis (blepharitis, 28; allergic conjunctivitis, 17; both, 6), all the events resolved with or without treatment after the discontinuation of ripasudil administration.
Fifty-two week administration of 0.4% ripasudil revealed IOP-lowering effects and an acceptable safety profile when administered as monotherapy or as additive therapy, in patients with open-angle glaucoma or OHT.
研究0.4%的法舒地尔（K-115），一种Rho激酶抑制剂，每日两次给药，持续52周，对开角型青光眼或高眼压症（OHT）患者的降眼压效果及安全性。
在这项多中心、前瞻性、开放标签研究中，纳入了388例原发性开角型青光眼、高眼压症或剥脱性青光眼患者，其中354例被分为四个队列（单药治疗组，173例；前列腺素类似物的联合治疗组，62例；β受体阻滞剂组，60例；或固定复方药物组，59例）。研究了从基线开始的谷值和峰值眼压降低情况以及不良事件。
在单药治疗、联合治疗以及单药治疗的两个亚组（基线眼压≥21 mmHg和<21 mmHg）的所有分析中，法舒地尔在52周内均显示出降眼压效果。单药治疗在第52周时谷值和峰值眼压的平均降低分别为-2.6和-3.7 mmHg，上述联合治疗组分别为-1.4和-2.4 mmHg、-2.2和-3.0 mmHg、-1.7和-1.7 mmHg。最常观察到 的不良事件为结膜充血（n = 264，74.6%）、睑缘炎（n = 73，20.6%）和过敏性结膜炎（n = 61，17.2%）。大多数结膜充血表现为轻度（97.0%），短暂且可自发缓解（78.0%）。尽管有51例患者因睑缘炎和/或过敏性结膜炎退出研究（睑缘炎，28例；过敏性结膜炎，17例；两者均有，6例），但在停用法舒地尔给药后，所有这些事件无论是否接受治疗均得到缓解。
对于开角型青光眼或高眼压症患者，0.4%的法舒地尔每日两次给药52周，无论是作为单药治疗还是联合治疗，均显示出降眼压效果且安全性可接受。
