第四代氟喹诺酮类眼科制剂的细菌清除率。

Rate of bacterial eradication by ophthalmic solutions of fourth-generation fluoroquinolones.

机构信息

Molecular Pathogenesis of Eye Infections Research Center, Dean A. McGee Eye Institute, Oklahoma City, Oklahoma, USA.

出版信息

Adv Ther. 2009 Apr;26(4):447-54. doi: 10.1007/s12325-009-0018-5. Epub 2009 Apr 16.

DOI:10.1007/s12325-009-0018-5

PMID:19381523

Abstract

INTRODUCTION

Antibacterial activity of ophthalmic fourth-generation fluoroquinolones has traditionally been evaluated by comparing only their active ingredients, gatifloxacin and moxifloxacin. However, ophthalmic formulations of fourth-generation fluoroquinolones differ in terms of the inclusion of preservatives. While gatifloxacin ophthalmic solution 0.3% (Zymar; Allergan, Inc., Irvine, CA, USA) contains 0.005% benzalkonium chloride (BAK), moxifloxacin ophthalmic solution 0.5% (Vigamox; Alcon Laboratories, Inc., Fort Worth, TX, USA) is preservative-free. Recent studies have demonstrated that the presence of BAK dramatically affects the antibacterial activity of the ophthalmic formulation of gatifloxacin. This study was designed to compare the kill rates of ophthalmic solutions of fourth-generation fluoroquinolones against isolates of common ocular bacterial pathogens.

METHODS

Approximately 5.6 log(10) colony-forming units (CFU)/mL of Haemophilus influenzae (n=1), Streptococcus pneumoniae (n=1), Staphylococcus aureus (n=2), methicillin-resistant Staphylococcus aureus (MRSA) (n=4), methicillinresistant Staphylococcus epidermidis (MRSE) (n=4), and fluoroquinolone-resistant S. epidermidis (n=1) were incubated with ophthalmic solutions of either gatifloxacin or moxifloxacin. Viable bacteria were quantified at specific time points up to 60 minutes.

RESULTS

Gatifloxacin 0.3% completely eradicated H. influenzae and Strep. pneumoniae in 5 minutes, one of two S. aureus isolates in 15 minutes, and the other S. aureus isolate in 60 minutes. Gatifloxacin 0.3% completely killed all MRSA, MRSE, and fluoroquinolone-resistant S. epidermidis isolates in 15 minutes. Moxifloxacin 0.5% completely eradicated Strep. pneumoniae and one of four MRSA isolates in 60 minutes. All other isolates incubated with moxifloxacin 0.5% retained viable bacteria ranging from 1.8 to 4.4 log(10) CFU/mL.

CONCLUSIONS

The ophthalmic solution of gatifloxacin 0.3% eradicated bacteria that frequently cause postoperative ocular infections substantially faster than did the ophthalmic solution of moxifloxacin 0.5%.

摘要

简介

传统上，通过比较第四代氟喹诺酮类药物的活性成分加替沙星和莫西沙星，来评估其抗菌活性。然而，第四代氟喹诺酮类药物的眼用制剂在防腐剂的使用方面存在差异。加替沙星 0.3%眼用溶液（Zymar；Allergan，Inc.，Irvine，CA，USA）中含有 0.005%苯扎氯铵（BAK），而莫西沙星 0.5%眼用溶液（Vigamox；Alcon Laboratories，Inc.，Fort Worth，TX，USA）则不含防腐剂。最近的研究表明，BAK 的存在会极大地影响加替沙星眼用制剂的抗菌活性。本研究旨在比较第四代氟喹诺酮类眼用制剂对常见眼部细菌病原体分离株的杀灭率。

方法

将约 5.6 log(10) 个菌落形成单位（CFU）/mL 的流感嗜血杆菌（n=1）、肺炎链球菌（n=1）、金黄色葡萄球菌（n=2）、耐甲氧西林金黄色葡萄球菌（MRSA）（n=4）、耐甲氧西林表皮葡萄球菌（MRSE）（n=4）和氟喹诺酮耐药表皮葡萄球菌（n=1）与加替沙星或莫西沙星的眼用溶液孵育。在特定时间点测量活菌数量，最长达 60 分钟。

结果

加替沙星 0.3% 在 5 分钟内完全清除了流感嗜血杆菌和肺炎链球菌，在 15 分钟内清除了两种金黄色葡萄球菌分离株中的一种，在 60 分钟内清除了另一种金黄色葡萄球菌分离株。加替沙星 0.3% 在 15 分钟内完全杀死了所有耐甲氧西林金黄色葡萄球菌、耐甲氧西林表皮葡萄球菌和氟喹诺酮耐药表皮葡萄球菌分离株。莫西沙星 0.5% 在 60 分钟内完全清除了肺炎链球菌和 4 株耐甲氧西林金黄色葡萄球菌分离株中的一株。用莫西沙星 0.5% 孵育的所有其他分离株保留的活菌数为 1.8 至 4.4 log(10) CFU/mL。