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奈帕芬胺:一种用于白内障手术后疼痛的眼科用非甾体类抗炎药。

Nepafenac: an ophthalmic nonsteroidal antiinflammatory drug for pain after cataract surgery.

机构信息

College of Pharmacy, University of Georgia, Athens, GA, USA.

出版信息

Ann Pharmacother. 2013 Jun;47(6):892-6. doi: 10.1345/aph.1R757. Epub 2013 May 28.

DOI:10.1345/aph.1R757
PMID:23715071
Abstract

OBJECTIVE

To examine the efficacy of nepafenac in the treatment of pain and inflammation in patients after cataract surgery using evidence from controlled clinical studies.

DATA SOURCES

Citations in Google Scholar, PubMed, and Web of Science from January 1, 2005, to March 25, 2013, were identified using nepafenac and cataract as search terms.

STUDY SELECTION AND DATA EXTRACTION

The literature search was limited to human studies published in English. Three trials that compared nepafenac with other nonsteroidal antiinflammatory drugs (NSAIDs) were included.

DATA SYNTHESIS

The pharmacokinetics and pharmacodynamics of nepafenac 0.1% suspension (and its active metabolite, amfenac) were compared with bromfenac 0.09% solution and ketorolac 0.4% solution with respect to aqueous humor concentrations and ability to reduce cyclooxygenase 1 and 2 (COX-1 and COX-2) enzymes. The maximum concentration (C(max)) values of ketorolac and amfenac were statistically similar, while the C(max) of bromfenac was significantly lower than that of amfenac. Ketorolac most effectively inhibited COX-1 enzymes; COX-2 enzymes were most effectively reduced by amfenac. When nepafenac 0.1% suspension was compared with placebo and ketorolac 0.5% solution, nepafenac achieved a higher percentage cure rate than placebo at day 14 (p = 0.0241). Significant differences in cure rates between nepafenac and ketorolac were not observed. Nepafenac 0.1%, bromfenac 0.09%, and ketorolac 0.45% were compared to determine which most effectively reduced prostaglandin E₂ (PGE₂) following surgery. PGE₂ concentrations were significantly lowest in the ketorolac group, followed by the bromfenac and nepafenac groups, respectively. Topical nepafenac 0.1% suspension was approved in 2005. A 0.3% suspension was approved in October 2012. The 0.3% product may have some advantages over its predecessor: it is dosed once rather than thrice daily, which may increase patient adherence and improve outcomes. The price and dosing frequency of the 0.3% product are comparable to those of bromfenac 0.09% solution.

CONCLUSIONS

The 2 nepafenac products appear to be equally efficacious, with a slightly increased adverse event rate in patients using the 0.3% versus 0.1% formulation. Head-to-head clinical trials that compare the 0.3% product with the 0.1% product or other commercially available NSAIDs are unavailable.

摘要

目的

通过对照临床试验的证据,研究奈帕芬那在白内障手术后患者疼痛和炎症治疗中的疗效。

资料来源

从 2005 年 1 月 1 日至 2013 年 3 月 25 日,在 Google Scholar、PubMed 和 Web of Science 中,以奈帕芬那和白内障为检索词,检索文献。

研究选择和数据提取

文献检索仅限于发表在英语文献中的人类研究。共纳入了 3 项比较奈帕芬那与其他非甾体抗炎药(NSAIDs)的试验。

数据分析

奈帕芬那 0.1%混悬剂(及其活性代谢物氨芬酸)的药代动力学和药效学与溴芬那 0.09%溶液和酮咯酸 0.4%溶液进行了比较,比较指标包括房水浓度和对环氧化酶 1 和 2(COX-1 和 COX-2)的抑制能力。酮咯酸和氨芬酸的最大浓度(C(max))值统计学相似,而溴芬酸的 C(max)明显低于氨芬酸。酮咯酸最有效地抑制 COX-1 酶;氨芬酸最有效地降低 COX-2 酶。与安慰剂和酮咯酸 0.5%溶液相比,奈帕芬那 0.1%混悬剂在第 14 天的治愈率更高(p = 0.0241)。奈帕芬那与酮咯酸之间的治愈率无显著差异。奈帕芬那 0.1%、溴芬那 0.09%和酮咯酸 0.45%被用于比较哪种药物能最有效地减少手术后前列腺素 E₂(PGE₂)的生成。在酮咯酸组中 PGE₂浓度最低,溴芬那组和奈帕芬那组次之。奈帕芬那 0.1%滴眼混悬剂于 2005 年获得批准。0.3%混悬剂于 2012 年 10 月获得批准。0.3%的产品可能优于其前身:每日使用一次而不是三次,这可能会增加患者的依从性并改善治疗效果。0.3%产品的价格和使用频率与溴芬那 0.09%溶液相当。

结论

两种奈帕芬那产品似乎同样有效,使用 0.3%制剂的患者不良反应发生率略有增加。尚未进行比较 0.3%产品与 0.1%产品或其他市售 NSAIDs 的头对头临床试验。

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