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贝西沙星:一种用于治疗细菌性结膜炎的新型抗感染药物。

Besifloxacin: a novel anti-infective for the treatment of bacterial conjunctivitis.

作者信息

Comstock Timothy L, Karpecki Paul M, Morris Timothy W, Zhang Jin-Zhong

机构信息

Global Medical Affairs, Pharmaceuticals, Bausch and Lomb, Inc., Rochester, NY, USA.

出版信息

Clin Ophthalmol. 2010 Apr 26;4:215-25. doi: 10.2147/opth.s9604.

Abstract

Bacterial conjunctivitis, commonly known as pink eye, is demographically unbiased in its prevalence and can be caused by a variety of aerobic and anaerobic bacteria. Timely empiric treatment with a broad-spectrum anti-infective, such as a topical fluoroquinolone, is critical in preventing potentially irreversible ocular damage. However, the rise in ocular methicillin- resistant Staphylococcus aureus isolates and the patterns of fluoroquinolone resistance for patients with other ocular bacterial infections mandate the need for new agents targeted for ocular use. Besifloxacin, a novel broad-spectrum fluoroquinolone, is approved for the treatment of bacterial conjunctivitis. It has a uniquely balanced dual-targeting activity that inhibits both DNA gyrase and topoisomerase IV and is associated with a lower incidence of resistance development. Besifloxacin is not marketed in other formulations, ensuring that its exposure is limited to bacterial populations in and around the eye. This specifically precludes any bacterial exposure to besifloxacin resulting from systemic use, which further reduces the likelihood of emergence of bacterial resistance. In vitro, besifloxacin has demonstrated equivalent or superior activity compared with other commonly used topical antibiotics. In clinical trials, besifloxacin has consistently demonstrated efficacy and safety in the treatment of patients with bacterial conjunctivitis. Besifloxacin is considered safe and is well tolerated with no observed contraindications.

摘要

细菌性结膜炎,俗称红眼病,其患病率在人群中无偏向性,可由多种需氧菌和厌氧菌引起。及时使用广谱抗感染药物进行经验性治疗,如局部用氟喹诺酮类药物,对于预防潜在的不可逆眼部损伤至关重要。然而,眼部耐甲氧西林金黄色葡萄球菌分离株的增加以及其他眼部细菌感染患者的氟喹诺酮耐药模式,使得需要有针对眼部使用的新型药物。贝西沙星是一种新型广谱氟喹诺酮类药物,已被批准用于治疗细菌性结膜炎。它具有独特的平衡双靶向活性,可抑制DNA旋转酶和拓扑异构酶IV,且耐药性发展发生率较低。贝西沙星没有其他剂型上市,确保其作用仅限于眼内及眼周的细菌群体。这特别排除了因全身使用导致细菌接触贝西沙星的情况,进一步降低了细菌耐药性出现的可能性。在体外,贝西沙星与其他常用局部抗生素相比已显示出同等或更高的活性。在临床试验中,贝西沙星在治疗细菌性结膜炎患者方面一直显示出疗效和安全性。贝西沙星被认为是安全的,耐受性良好,未观察到禁忌证。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2345/2861926/e1500ce195b8/opth-4-215f1.jpg

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