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奈他地尔:一种用于治疗慢性原发性开角型青光眼和高眼压症的新型眼科药物。

Netarsudil: A new ophthalmic drug in the treatment of chronic primary open angle glaucoma and ocular hypertension.

作者信息

Batra Mansi, Gupta Sumeet, Nair Anroop B, Dhanawat Meenakshi, Sandal Suraj, Morsy Mohamed Aly

机构信息

Department of Clinical Practice, M. M. College of Pharmacy, M. M. (Deemed to be University), Mullana (Ambala), Haryana, India.

Department of Pharmacology, M. M. College of Pharmacy, M. M. (Deemed to be University), Mullana (Ambala), Haryana, India.

出版信息

Eur J Ophthalmol. 2021 Sep;31(5):2237-2244. doi: 10.1177/11206721211008783. Epub 2021 Apr 10.

DOI:10.1177/11206721211008783
PMID:33843288
Abstract

BACKGROUND

Vision impairment remains a major health problem worldwide. Elevated intraocular pressure is a prime risk factor for blindness in the elderly. Netarsudil is a Rho-associated protein kinase (ROCK) inhibitor, which also inhibits norepinephrine transport. This narrative review summarizes the properties and clinical significance of netarsudil, a promising drug in topical glaucoma therapy.

METHODS

We searched PubMed, Medline and Scopus databases using relevant keywords to retrieve information on the physicochemical properties, formulation, mechanism of action, clinical pharmacokinetics, dose and toxicity of netarsudil.

RESULTS

Netarsudil showed promising effects in lowering the elevated intraocular pressure by two mechanisms. The US FDA approved netarsudil for clinical use in 2017 under the trademark of Rhopressa while European Medicines Agency approved Rhokiinsa in 2019. This drug is available as a 0.02% ophthalmic solution for once-daily topical application.

CONCLUSION

The discovery of netarsudil is a breakthrough in the therapy of glaucoma with proven efficacy in a wide range of eye pressures and is well tolerated in cases with ocular hypertension and chronic glaucoma.

摘要

背景

视力损害仍是全球主要的健康问题。眼压升高是老年人失明的主要危险因素。奈他地尔是一种Rho相关蛋白激酶(ROCK)抑制剂,它也抑制去甲肾上腺素转运。本叙述性综述总结了奈他地尔的特性及临床意义,奈他地尔是一种在局部青光眼治疗中有前景的药物。

方法

我们使用相关关键词搜索了PubMed、Medline和Scopus数据库,以检索有关奈他地尔的理化性质、剂型、作用机制、临床药代动力学、剂量和毒性的信息。

结果

奈他地尔通过两种机制在降低升高的眼压方面显示出有前景的效果。美国食品药品监督管理局(US FDA)于2017年批准奈他地尔以Rhopressa为商标用于临床,而欧洲药品管理局于2019年批准了Rhokiinsa。该药物有0.02%的眼药水剂型,每日一次局部使用。

结论

奈他地尔的发现是青光眼治疗的一项突破,在广泛的眼压范围内已证实其疗效,并且在高眼压症和慢性青光眼患者中耐受性良好。

相似文献

1
Netarsudil: A new ophthalmic drug in the treatment of chronic primary open angle glaucoma and ocular hypertension.奈他地尔:一种用于治疗慢性原发性开角型青光眼和高眼压症的新型眼科药物。
Eur J Ophthalmol. 2021 Sep;31(5):2237-2244. doi: 10.1177/11206721211008783. Epub 2021 Apr 10.
2
Netarsudil ophthalmic solution 0.02% for the treatment of patients with open-angle glaucoma or ocular hypertension.0.02%奈他地尔眼药水用于治疗开角型青光眼或高眼压症患者。
Drugs Today (Barc). 2018 Aug;54(8):467-478. doi: 10.1358/dot.2018.54.8.2849627.
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Two Phase 3 Clinical Trials Comparing the Safety and Efficacy of Netarsudil to Timolol in Patients With Elevated Intraocular Pressure: Rho Kinase Elevated IOP Treatment Trial 1 and 2 (ROCKET-1 and ROCKET-2).两项比较奈立定(netarsudil)和噻吗洛尔(timolol)安全性和疗效的 3 期临床试验: Rho 激酶升高的眼压治疗试验 1 和 2(ROCKET-1 和 ROCKET-2)。
Am J Ophthalmol. 2018 Feb;186:116-127. doi: 10.1016/j.ajo.2017.11.019. Epub 2017 Dec 1.
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Netarsudil Ophthalmic Solution 0.02%: First Global Approval.奈他舒地尔滴眼液 0.02%:全球首次获批。
Drugs. 2018 Mar;78(3):389-396. doi: 10.1007/s40265-018-0877-7.
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Netarsudil and latanoprost ophthalmic solution for the reduction of intraocular pressure in open-angle glaucoma or ocular hypertension.尼达尼布滴眼液和拉坦前列素滴眼液降低开角型青光眼或高眼压症患者的眼内压。
Expert Rev Clin Pharmacol. 2019 Dec;12(12):1073-1079. doi: 10.1080/17512433.2019.1701435.
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Phase 2 Randomized Clinical Study of Netarsudil Ophthalmic Solution in Japanese Patients with Primary Open-Angle Glaucoma or Ocular Hypertension.网织红细胞生成素眼部溶液治疗日本原发性开角型青光眼或高眼压症患者的 2 期随机临床试验。
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A multicenter, open-label study of netarsudil for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension in a real-world setting.一项在真实世界环境中评估奈他舒地尔降低开角型青光眼或高眼压症患者眼内压的多中心、开放性研究。
Curr Med Res Opin. 2021 Jun;37(6):1011-1020. doi: 10.1080/03007995.2021.1901222. Epub 2021 Mar 27.
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Comparison of safety and efficacy of Netarsudil 0.02% and Bimatoprost 0.01% monotherapy and combination therapy in primary open-angle glaucoma and ocular hypertension.比较 Netarsudil 0.02%与单独使用比马前列素 0.01%及联合治疗原发性开角型青光眼和高眼压症的安全性和疗效。
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Long-term Safety and Ocular Hypotensive Efficacy Evaluation of Netarsudil Ophthalmic Solution: Rho Kinase Elevated IOP Treatment Trial (ROCKET-2).罗库溴铵用于全身麻醉诱导的随机对照研究
Am J Ophthalmol. 2019 Apr;200:130-137. doi: 10.1016/j.ajo.2019.01.003. Epub 2019 Jan 15.
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New glaucoma medications: latanoprostene bunod, netarsudil, and fixed combination netarsudil-latanoprost.新型青光眼药物:拉坦前列素苯并磺胺、奈立定和奈拉滨/拉坦前列素固定组合。
Eye (Lond). 2020 Jan;34(1):72-88. doi: 10.1038/s41433-019-0671-0. Epub 2019 Nov 6.

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