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贝西沙星(BSFX)是美国博士伦公司开发的一种用于治疗由敏感菌引起的细菌性结膜炎的新氟喹诺酮类抗菌药。本品对包括耐药株在内的常见结膜炎致病菌具有广谱抗菌活性。研究表明,0.6%BSFX混悬滴眼剂具有给药频次少,不良反应发生率低且轻微,耐受性良好,临床疗效(成功率和微生物清除率均不劣于莫西沙星)明确等优势。尤其是它对DNA促旋酶和拓扑异构酶的抑制活性趋于平衡,且目前仅限于治疗细菌性结膜炎,故与其他广泛使用的同类药物相比,本品的耐药选择压力很小。本文对BSFX的制备方法、作用机制/耐药机制、抗菌活性、药动学与药效学及临床研究等进展进行较系统综述。
Beixifloxacin (BSFX) is a new fluoroquinolone antibacterial agent developed by Bausch & Lomb in the United States for the treatment of bacterial conjunctivitis caused by susceptible bacteria. This product, including resistant strains, including common conjunctivitis pathogens with broad-spectrum antibacterial activity. Studies have shown that 0.6% BSFX suspension eye drops with less frequent administration, low and mild adverse reactions, good tolerability, clinical efficacy (success rate and microbial clearance are not inferior to moxifloxacin) clear advantages . Especially its DNA gyrase and topoisomerase inhibitory activity tends to balance, and is currently limited to the treatment of bacterial conjunctivitis, so compared with other widely used similar drugs, the pressure of drug resistance choice is very small . This article systematically reviews the progress of BSFX preparation methods, mechanism of action / mechanism of resistance, antibacterial activity, pharmacokinetics and pharmacodynamics and clinical research.