Pharmacy Service, James J. Peters Veterans Affairs Medical Center, Bronx, New York 10468, USA.
Clin Ther. 2010 Mar;32(3):454-71. doi: 10.1016/j.clinthera.2010.03.013.
Besifloxacin is a topical ophthalmic fluoroquinolone that was approved by the US Food and Drug Administration (FDA) in May 2009 for the treatment of bacterial conjunctivitis caused by susceptible bacterial strains.
This article provides an overview of the pharmacology, clinical efficacy, and tolerability of ophthalmic besifloxacin when used for the treatment of bacterial conjunctivitis.
Relevant reports pertaining to the pharmacology, efficacy, and tolerability of besifloxacin were identified through a search of MEDLINE (1985-December 2009) and International Pharmaceutical Abstracts (1985-December 2009) using the terms besifloxacin, BOL-303224-A, ophthalmic fluoroquinolones, and bacterial conjunctivitis. Additional publications were identified by reviewing the reference lists of identified articles and searching the FDA Web site.
Besifloxacin has potent in vitro inhibitory activity against most common ocular bacterial pathogens (MIC90 values generally < or =4 microg/mL), including Staphylococcus aureus, Streptococcus pneumoniae, and Haemophilus influenzae. In an ocular pharmacokinetic study in 64 healthy volunteers, the C(max) in tears (mean [SD], 610 [540] microg/mL) was reached 10 minutes after a single ocular instillation of besifloxacin; concentrations > or =1.6 microg/g of tear were sustained for at least 24 hours; and the elimination t(1/2) was ~3.4 hours. In a study in 24 patients with a clinical diagnosis of bilateral bacterial conjunctivitis, systemic exposure (C(max)) after administration of besifloxacin ophthalmic suspension 3 times daily for 5 days was <0.5 ng/mL. In 2 randomized, double-masked, vehicle-controlled clinical trials, besifloxacin ophthalmic suspension was well tolerated and significantly more efficacious than vehicle in achieving clinical resolution (73.3% vs 43.1%, respectively, in one of the studies [P < 0.001]; 45.2% vs 33.0% in the other [P = 0.008]) and microbial eradication (88.3% vs 60.3% [P < 0.001] and 91.5% vs 59.7% [P < 0.001], respectively). In a randomized, double-masked, parallel-group, noninferiority trial comparing besifloxacin ophthalmic suspension 0.6% with moxifloxacin ophthalmic solution 0.5%, besifloxacin was found to be noninferior to moxifloxacin (predefined cutoff for noninferiority = -15), with no significant differences in rates of clinical resolution (58.3% and 59.4%, respectively; 95% CI, -9.48 to 7.29) or microbial eradication (93.3% and 91.1%; 95% CI, -2.44 to 6.74). Besifloxacin was generally well tolerated in these clinical trials, with the most common (> or =1.5%) ocular adverse events being nonspecific conjunctivitis (2.6%), blurred vision (2.1%), bacterial conjunctivitis (1.8%), and eye pain (1.5%). The recommended dose of besifloxacin is 1 drop in the affected eye(s) 3 times daily (4-12 hours apart) for 7 days.
Besifloxacin ophthalmic suspension 0.6% appeared to be well tolerated in the populations studied and was efficacious in the treatment of bacterial conjunctivitis caused by susceptible isolates.
贝西沙星是一种局部用眼科氟喹诺酮类药物，于 2009 年 5 月获得美国食品和药物管理局（FDA）批准，用于治疗敏感菌引起的细菌性结膜炎。
本文概述了贝西沙星的药理学、临床疗效和耐受性，用于治疗细菌性结膜炎。
通过在 MEDLINE（1985 年-2009 年 12 月）和国际药学文摘（1985 年-2009 年 12 月）中使用贝西沙星、BOL-303224-A、眼科氟喹诺酮类药物和细菌性结膜炎等术语搜索相关文献，确定了与贝西沙星的药理学、疗效和耐受性相关的报告。通过查看已确定文章的参考文献和搜索 FDA 网站，确定了其他出版物。
贝西沙星对大多数常见的眼部细菌病原体（MIC90 值通常为 < 或 = 4 μg/ml）具有强大的体外抑制活性，包括金黄色葡萄球菌、肺炎链球菌和流感嗜血杆菌。在 64 名健康志愿者的眼部药代动力学研究中，单次眼部滴注贝西沙星 10 分钟后，泪液中的 C（最大值）（平均[标准差]，610 [540]μg/ml）达到峰值；至少 24 小时内维持浓度>或 = 1.6μg/g 的泪液；消除半衰期（t（1/2））约为 3.4 小时。在 24 例临床诊断为双侧细菌性结膜炎的患者中进行的一项研究中，每天 3 次滴注贝西氟沙星眼用混悬液 5 天后，全身暴露量（C（最大值））< 0.5ng/ml。在 2 项随机、双盲、安慰剂对照的临床研究中，贝西氟沙星眼用混悬液耐受性良好，与安慰剂相比，在实现临床缓解方面更有效（分别为一项研究中的 73.3%和 43.1%，[P < 0.001]；另一项研究中的 45.2%和 33.0%，[P = 0.008]）和微生物清除率（分别为 88.3%和 60.3%[P < 0.001]和 91.5%和 59.7%[P < 0.001]）。在一项比较贝西沙星眼用混悬液 0.6%和莫西沙星眼用溶液 0.5%的随机、双盲、平行组非劣效性试验中，发现贝西沙星与莫西沙星相当（非劣效性预定截止值为 -15），临床缓解率（分别为 58.3%和 59.4%；95%置信区间，-9.48 至 7.29）或微生物清除率（分别为 93.3%和 91.1%；95%置信区间，-2.44 至 6.74）无显著差异。在这些临床试验中，贝西沙星通常具有良好的耐受性，最常见（> 或 = 1.5%）的眼部不良反应为非特异性结膜炎（2.6%）、视力模糊（2.1%）、细菌性结膜炎（1.8%）和眼痛（1.5%）。贝西沙星的推荐剂量为每天 3 次（12 小时一次），每次 1 滴，用于治疗敏感菌引起的细菌性结膜炎，共 7 天。
贝西沙星眼用混悬液 0.6%在研究人群中似乎具有良好的耐受性，在治疗敏感菌引起的细菌性结膜炎方面有效。
