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Rho激酶抑制剂在青光眼治疗中的应用:当前观点与未来方向

Rho Kinase Inhibitors in Glaucoma Management: Current Perspectives and Future Directions.

作者信息

Chatzimichail Eleftherios, Christodoulaki Eirini, Konstas Panagiotis A G, Tsiropoulos Georgios N, Amaxilati Efstratia, Gugleta Konstantin, Gatzioufas Zisis, Panos Georgios D

机构信息

Department of Ophthalmology, University Hospital of Basel, Basel, 4031, Switzerland.

Eye Centre of Greece, Pylaia, Thessaloniki, Greece.

出版信息

Drug Des Devel Ther. 2025 Apr 2;19:2519-2531. doi: 10.2147/DDDT.S515166. eCollection 2025.

Abstract

Glaucoma is a group of eye conditions characterised by optic nerve damage and visual field loss, representing the leading cause of irreversible blindness worldwide. Glaucoma exerts substantial global impact on visual impairment and blindness. The management of glaucoma has traditionally relied on medications such as prostaglandin analogs, beta-blockers, alpha agonists, and carbonic anhydrase inhibitors, which aim to lower intraocular pressure through various mechanisms. Rho kinase (ROCK) inhibitors have recently emerged as a novel class of antiglaucoma drugs, offering an alternative approach by enhancing aqueous humour outflow through the conventional pathway. Recent clinical studies assessing the efficacy and safety of Ripasudil (K-115) and Netarsudil (AR-13324) have demonstrated promising outcomes in the treatment of various types of glaucoma. Comparative studies have shown that ROCK inhibitors are non-inferior to traditional antiglaucomatous medications, such as beta-blockers and prostaglandins. Additionally, emerging evidence suggests their neuroprotective properties, which may play a role in preserving retinal ganglion cells. Furthermore, positive outcomes have been observed when these agents are used in conjunction with glaucoma filtering surgery, potentially enhancing surgical success rates. Adverse effects, including conjunctival hyperemia, cornea verticillata, conjunctivitis, and blepharitis, have been reported following the use of ROCK inhibitors. However, those side effects appear to be subtle in most cases. This review aims to provide an overview of ROCK inhibitors, focusing on their mechanisms of action, clinical efficacy, safety profiles, and additional benefits for eye health. Furthermore, further potential applications of ROCK inhibitors in glaucoma management are going to be discussed.

摘要

青光眼是一组以视神经损伤和视野缺损为特征的眼部疾病,是全球不可逆性失明的主要原因。青光眼对视力损害和失明具有重大的全球影响。传统上,青光眼的治疗依赖于前列腺素类似物、β受体阻滞剂、α激动剂和碳酸酐酶抑制剂等药物,这些药物旨在通过各种机制降低眼压。 Rho激酶(ROCK)抑制剂最近已成为一类新型抗青光眼药物,通过传统途径增强房水流出提供了一种替代方法。最近评估ripasudil(K-115)和netarsudil(AR-13324)疗效和安全性的临床研究在治疗各种类型青光眼方面显示出了有前景的结果。比较研究表明,ROCK抑制剂不劣于传统抗青光眼药物,如β受体阻滞剂和前列腺素。此外,新出现的证据表明它们具有神经保护特性,这可能在保护视网膜神经节细胞中发挥作用。此外,当这些药物与青光眼滤过手术联合使用时,观察到了积极的结果,可能提高手术成功率。使用ROCK抑制剂后已报告有不良反应,包括结膜充血、角膜涡状浑浊、结膜炎和睑缘炎。然而,这些副作用在大多数情况下似乎并不明显。本综述旨在概述ROCK抑制剂,重点介绍其作用机制、临床疗效、安全性概况以及对眼部健康的其他益处。此外,还将讨论ROCK抑制剂在青光眼治疗中的进一步潜在应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8709/11972570/386c59ffe20b/DDDT-19-2519-g0001.jpg

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