局部抗青光眼药物的研究及应用进展  

Progress in research and application of local anti-glaucoma drugs

作　　者：穆婉 丁英卓 席宇飞 贲申煜 陈彬 葛玲[2] MU Wan;DING Ying-zhuo;XI Yu-fei;BEN Shen-yu;CHEN Bin;CE Ling(Department of Pharmacy,Shanghai Eye Diseases Prevention&Treatment Center/Shanghai Eye Hospital,School of Medicine,Tongji University,SHANGHAI 200331,China;Department of Ophthalmology,Shanghai Eye Diseases Prevention&Treatment Center/Shanghai Eye Hospital,School of Medicine,Tongji University,SHANGHAI 200331,China)

机构地区：[1]上海市眼病防治中心/同济大学附属眼科医院药剂科,上海200331 [2]上海市眼病防治中心/同济大学附属眼科医院眼科,上海200331

出　　处：《中国新药与临床杂志》2024年第8期574-581,共8页Chinese Journal of New Drugs and Clinical Remedies

基　　金：上海市眼病防治中心基础研究项目(2021JC006);上海市眼病防治中心临床研究项目(22LC01007)。

摘　　要：青光眼是导致全球不可逆性致盲性眼病的主要原因之一,病理性眼压升高是青光眼的主要危险因素,故其临床治疗宗旨是降低眼压至个体目标眼压水平。目前临床经典的局部抗青光眼药物主要有前列腺素类似物、肾上腺素β受体阻滞药、肾上腺素α2受体激动剂、碳酸酐酶抑制剂和胆碱能受体激动剂五类,作用机制包括减少房水产生,增加小梁网途径和经葡萄膜巩膜通路的房水外流,以及收缩瞳孔括约肌开放房角等。其中,前列腺素类似物因疗效和安全性较好,目前已成为临床上开角型青光眼患者控制眼压的首选药物。近年来,新型抗青光眼药物(包括Rho激酶抑制剂和一氧化氮供体抗青光眼药物等)的上市,以及相关药物缓释制剂(眼内及眼外药物递送系统)的研发,为青光眼的治疗提供了新的药物选择。Glaucoma,a leading cause of irreversible blindness worldwide,primarily involves pathological elevation of intraocular pressure(IOP),which is its main risk factor,so the clinical goal in treating glaucoma is to reduce IOP to individual target levels.Currently,the classical local anti-glaucoma drugs include five categories:prostaglandin analogues(PGAs),β-adrenergic receptor blockers,α2-adrenergic receptor agonists,carbonic anhydrase inhibitors,and cholinergic receptor agonists.These drugs mainly work by reducing aqueous humor production,increasing aqueous outflow through the trabecular pathway and the uveal scleral pathway,and contracting the pupil sphincter to open the chamber angle.Among these,PGAs have become the preferred choice for controlling IOP in primary open-angle glaucoma patients due to their efficacy and safety.In recent years,the introduction of novel glaucoma medications,including Rho kinase inhibitors and nitric oxide-donating anti-glaucoma drugs,along with the development of related drug-releasing formulations(intraocular and extraocular drug delivery systems),offers new options for glaucoma treatment.

关 键 词：青光眼 眼压 前列腺素类似物 RHO激酶抑制剂 一氧化氮供体 缓释凝胶 

分 类 号：R969[医药卫生—药理学] R775[医药卫生—药学]