The Scripps Clinic Medical Group, La Jolla, CA, USA.
Pharmaceutical Medical Affairs, Bausch + Lomb, Rochester, NY, USA.
Ophthalmol Ther. 2016 Jun;5(1):1-20. doi: 10.1007/s40123-016-0046-6. Epub 2016 Mar 24.
This comprehensive review summarizes the mechanism of action, pharmacokinetics, efficacy, and safety of besifloxacin ophthalmic suspension, 0.6% and examines its role in the treatment of ocular surface bacterial infections. Besifloxacin possesses balanced activity against bacterial topoisomerase II (also called DNA gyrase) and topoisomerase IV. It has shown a low potential to select for bacterial resistance in vitro and demonstrated strong in vitro activity against many Gram-positive, Gram-negative, and anaerobic organisms, including methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis (MRSA and MRSE, respectively). Ocular pharmacokinetic studies have shown that besifloxacin achieves high, sustained concentrations in the tear fluid and conjunctiva following topical administration, with negligible systemic exposure. Large randomized, controlled clinical trials have established the efficacy and safety of besifloxacin administered three times daily for 5 days for treatment of acute bacterial conjunctivitis in both adults and children, with high rates of clinical resolution (up to more than 70% by day 5) and bacterial eradication (more than 90% by day 5), and a low incidence of adverse events. Additionally, besifloxacin applied twice daily for 3 days demonstrated greater efficacy than vehicle in treating bacterial conjunctivitis. Case reports, a large retrospective chart review, and animal studies have provided supporting evidence for the efficacy of besifloxacin in the management of acute bacterial keratitis. There is some evidence to suggest that besifloxacin may provide an advantage over other current-generation fluoroquinolones in antimicrobial prophylaxis for ocular surgery. Besifloxacin is an appropriate option for treatment of bacterial conjunctivitis, and its use in the treatment of bacterial keratitis and lid disorders, as well as for surgical prophylaxis, appears promising and warrants further evaluation.
这篇全面的综述总结了 0.6%贝西沙星眼用混悬液的作用机制、药代动力学、疗效和安全性，并探讨了其在治疗眼表细菌感染中的作用。贝西沙星对细菌拓扑异构酶 II（也称为 DNA 回旋酶）和拓扑异构酶 IV 具有平衡的活性。它在体外选择细菌耐药性的潜力较低，并表现出对许多革兰氏阳性、革兰氏阴性和厌氧生物的强大体外活性，包括耐甲氧西林金黄色葡萄球菌和表皮葡萄球菌（分别为 MRSA 和 MRSE）。眼内药代动力学研究表明，贝西沙星经局部给药后，在泪液和结膜中达到高、持续的浓度，全身暴露可忽略不计。大型随机对照临床试验已经确立了贝西沙星每日三次给药 5 天治疗成人和儿童急性细菌性结膜炎的疗效和安全性，临床治愈率高（第 5 天高达 70%以上），细菌清除率高（第 5 天超过 90%），不良事件发生率低。此外，贝西沙星每日两次给药 3 天的疗效优于载体，用于治疗细菌性结膜炎。病例报告、大型回顾性图表审查和动物研究为贝西沙星在急性细菌性角膜炎管理中的疗效提供了支持证据。有一些证据表明，贝西沙星在眼外科抗菌预防方面可能优于其他新一代氟喹诺酮类药物。贝西沙星是治疗细菌性结膜炎的合适选择，其在细菌性角膜炎和眼睑疾病治疗以及手术预防方面的应用有前景，值得进一步评估。
