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[用于治疗开角型青光眼和高眼压症的ROCK(Rho激酶抑制剂)]

[ROCK (RHO-KINASE INHIBITORS) FOR THE TREATMENT OF OPEN-ANGLE GLAUCOMA AND OCULAR HYPERTENSION].

作者信息

Hayat Hagay, Achiron Asaf, Masarwa Dua, Goldberg Mordechai

机构信息

Ophthalmology Department, Barzilai Medical Center, Ashkelon Israel, Israel.

Sourasky Tel Aviv Hospital, Sackler Faculty of Medicine, Israel.

出版信息

Harefuah. 2023 Mar;162(3):160-164.

PMID:36966373
Abstract

Netarsudil ophthalmic solution 0.02% is a new treatment for open-angle glaucoma and ocular hypertension, which was approved for treatment in the United States and in the European Commission. The drug is a rho- kinase inhibitor (ROCK) that lowers intraocular pressure by enhancing the outflow at the trabecular meshwork and decreasing both aqueous humor production and episcleral venous pressure. This literature review aims to present this new treatment, characterize its specific mechanism of action, and discuss its effect and adverse events profile. The efficacy and safety of the drug were studied in the ROCKET and MERCURY clinical trials, in which Netarsudil was compared to other common drugs, including Timolol (Beta-blocker), Latanoprost (Prostaglandin analog), and a combination drop containing Netarsudil and Latanoprost. These trials showed a reduction of 16%-21% in the intraocular pressure (IOP) when using Netarsudil. Moreover, it was found that when using a combination of Netarsudil and Latanoprost, 64.5% of these patients achieved ≥30% reduction in mean diurnal IOP versus 28.8% of patients treated only with Netarsudil and 37.2% of patients treated only with Latanoprost (P<0.0001). The most common adverse event reported was conjunctival hyperemia, which was more frequent in patients using Netarsudil. However, this did not significantly affect the drug tolerance.

摘要

0.02%奈他地尔眼药水是一种用于治疗开角型青光眼和高眼压症的新型药物,已获美国和欧盟委员会批准用于治疗。该药物是一种Rho激酶抑制剂(ROCK),通过增强小梁网房水流出、减少房水生成和降低巩膜静脉压来降低眼压。这篇文献综述旨在介绍这种新型治疗方法,阐述其具体作用机制,并讨论其疗效和不良事件情况。在ROCKET和MERCURY临床试验中研究了该药物的疗效和安全性,将奈他地尔与其他常用药物进行了比较,包括噻吗洛尔(β受体阻滞剂)、拉坦前列素(前列腺素类似物)以及含有奈他地尔和拉坦前列素的复方滴眼液。这些试验表明,使用奈他地尔时眼压降低了16%-21%。此外,研究发现,使用奈他地尔和拉坦前列素联合用药时,64.5%的患者平均日眼压降低≥30%,而仅使用奈他地尔治疗的患者为28.8%,仅使用拉坦前列素治疗的患者为37.2%(P<0.0001)。报告的最常见不良事件是结膜充血,在使用奈他地尔的患者中更为常见。然而,这并未显著影响药物耐受性。

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