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0.5%氯替泼诺妥布酯眼用混悬液:术后抗炎使用的疗效与安全性。

Loteprednol etabonate ophthalmic suspension 0.5 %: efficacy and safety for postoperative anti-inflammatory use.

作者信息

Amon Michael, Busin Massimo

机构信息

Department of Ophthalmology, Hospital of the Brothers of Charity, Johannes von Gott Platz 1, Vienna, Austria.

出版信息

Int Ophthalmol. 2012 Oct;32(5):507-17. doi: 10.1007/s10792-012-9589-2. Epub 2012 Jun 16.

Abstract

Topical corticosteroids are routinely used as postoperative ocular anti-inflammatory drugs; however, adverse effects such as increased intraocular pressure (IOP) are observed with their use. While older corticosteroids such as dexamethasone and prednisolone acetate offer good anti-inflammatory efficacy, clinically significant increases in IOP (≥10 mmHg) are often associated with their use. Loteprednol etabonate, a novel C-20 ester-based corticosteroid, was retrometabolically designed to offer potent anti-inflammatory efficacy but with decreased impact on IOP. After exerting its therapeutic effects on the site of action, loteprednol etabonate is rapidly converted to inactive metabolites, resulting in fewer adverse effects. Randomized controlled studies have demonstrated the clinical efficacy and safety of loteprednol etabonate ophthalmic suspension 0.5 % for the treatment of postoperative inflammation in post-cataract patients with few patients, if any, exhibiting clinically significant increases (≥10 mmHg) in IOP. Furthermore, safety studies demonstrated a minimal effect of loteprednol etabonate on IOP with long-term use or in steroid responders with a much lower propensity to increase IOP relative to prednisolone acetate or dexamethasone. The anti-inflammatory treatment effect of loteprednol etabonate appears to be similar to that of rimexolone and difluprednate with less impact on IOP compared to difluprednate, although confirmatory comparative studies are needed. The available clinical data suggest that loteprednol etabonate is an efficacious and safe corticosteroid for the treatment of postoperative inflammation.

摘要

局部用皮质类固醇通常用作术后眼部抗炎药物;然而,使用过程中会观察到诸如眼压(IOP)升高之类的不良反应。虽然像地塞米松和醋酸泼尼松龙等传统皮质类固醇具有良好的抗炎效果,但使用它们时往往会出现具有临床意义的眼压升高(≥10 mmHg)。氯替泼诺醇乙酯是一种新型的基于C - 20酯的皮质类固醇,经过逆向代谢设计,以提供强效抗炎效果,但对眼压的影响较小。氯替泼诺醇乙酯在作用部位发挥治疗作用后,会迅速转化为无活性的代谢产物,从而减少不良反应。随机对照研究已证明0.5%氯替泼诺醇乙酯眼用混悬液在治疗白内障术后炎症方面的临床疗效和安全性,极少有患者(如果有的话)出现具有临床意义的眼压升高(≥10 mmHg)。此外,安全性研究表明,氯替泼诺醇乙酯长期使用对眼压影响极小;对于眼压升高倾向比醋酸泼尼松龙或地塞米松低得多的类固醇反应者,使用氯替泼诺醇乙酯也具有极小的眼压升高影响。氯替泼诺醇乙酯的抗炎治疗效果似乎与利美索龙和二氟泼尼酯相似,与二氟泼尼酯相比,对眼压的影响较小,不过仍需要进行确证性比较研究。现有临床数据表明,氯替泼诺醇乙酯是治疗术后炎症的一种有效且安全的皮质类固醇。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2c67/3459083/da8a24e2fcfe/10792_2012_9589_Fig1_HTML.jpg

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