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拉坦前列素治疗青光眼

Latanoprost in the treatment of glaucoma.

作者信息

Alm Albert

机构信息

Department of Neuroscience, Ophthalmology, University Hospital, Uppsala, Sweden.

出版信息

Clin Ophthalmol. 2014 Sep 26;8:1967-85. doi: 10.2147/OPTH.S59162. eCollection 2014.

Abstract

Prostaglandins are approved by the European Glaucoma Society guidelines as first-line treatment for glaucoma. This review focuses on latanoprost, an ester prodrug of prostaglandin (PG) F2α, which was the first of the currently available topical PGF2α analogs to be launched for glaucoma or ocular hypertension and which still accounts for the majority of prescriptions. It is better absorbed than the parent compound through the cornea, and peak concentration of the active drug is in the aqueous humor 1-2 hours after topical dosing (15-30 ng/mL). Metabolism occurs mainly in the liver. Latanoprost (0.005%) has been very well studied in clinical trials and meta-analyses that show it to be generally as effective as the other PG analogs (bimatoprost, travoprost, and tafluprost) and more effective than timolol, dorzolamide, and brimonidine. Latanoprost has good short- and long-term safety and tolerability profiles. In common with other prostaglandins, it lacks systemic effects, but can cause ocular adverse events such as conjunctival hyperemia, pigmentation of the iris, periocular skin or eyelashes, hypertrichosis, and ocular surface effects or irritation. Latanoprost is significantly better tolerated than either bimatoprost or travoprost. Patients treated with latanoprost have better compliance and persist with therapy longer than those that are given other drugs. An improved formulation of latanoprost without the preservative benzalkonium chloride has recently been developed. It is as effective as conventional latanoprost, has a lower incidence of hyperemia, and can be stored at room temperature. In conclusion, latanoprost has the best efficacy-tolerability ratio of the PG analogs available for glaucoma treatment, and has good compliance and persistence. These factors should be improved further by the recent development of preservative-free latanoprost.

摘要

前列腺素已被欧洲青光眼协会指南批准为青光眼的一线治疗药物。本综述聚焦于拉坦前列素,它是前列腺素(PG)F2α的酯前药,是目前可用的局部用PGF2α类似物中首个用于青光眼或高眼压症的药物,且至今仍占大多数处方量。它比母体化合物更易通过角膜吸收,局部给药后1 - 2小时活性药物在房水中达到峰值浓度(15 - 30 ng/mL)。代谢主要发生在肝脏。拉坦前列素(0.005%)在临床试验和荟萃分析中得到了充分研究,结果表明它总体上与其他PG类似物(比马前列素、曲伏前列素和他氟前列素)效果相当,且比噻吗洛尔、多佐胺和溴莫尼定更有效。拉坦前列素具有良好的短期和长期安全性及耐受性。与其他前列腺素一样,它没有全身作用,但可引起眼部不良事件,如结膜充血、虹膜色素沉着、眼周皮肤或睫毛色素沉着、多毛症以及眼表效应或刺激。拉坦前列素的耐受性明显优于比马前列素或曲伏前列素。接受拉坦前列素治疗的患者比接受其他药物治疗的患者依从性更好,坚持治疗的时间更长。最近已开发出一种不含防腐剂苯扎氯铵的拉坦前列素改良制剂。它与传统拉坦前列素效果相同,充血发生率更低,且可在室温下储存。总之,拉坦前列素在可用于青光眼治疗的PG类似物中具有最佳的疗效 - 耐受性比,且具有良好的依从性和持续性。无防腐剂拉坦前列素的最新研发应会进一步改善这些因素。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/24bb/4196887/e58eb0b9622e/opth-8-1967Fig1.jpg

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