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Sitafloxacin
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Rhonda L. Stuart, Ashwin Swaminathan
Sitafloxacin (as sitafloxacin hydrate) is available as 50-mg tablets under the name Gracevit, and as a 10% fine granular preparation. Sitafloxacin inhibits bacterial topoisomerase II (DNA gyrase) and topoisomerase IV and is bactericidal. Sitafloxacin has a broad spectrum of activity and is currently licensed for clinical use and marketed in Japan and Thailand for a broad range of infections, including respiratory tract, urinary tract, odontogenic, and otorhinolaryngological infections and as a component of salvage combination therapies for Helicobacter pylori. Sitafloxacin’s potential market outside of Asia is limited due to the risk of cutaneous phototoxicity in Caucasian patients (Ghebremedhin, 2012; MIMS, n.d.).
A randomized, controlled, multicenter clinical trial to evaluate the efficacy and safety of oral sitafloxacin versus moxifloxacin in adult patients with community-acquired pneumonia
Published in Current Medical Research and Opinion, 2021
Ying Li, Demei Zhu, Yiqiang Peng, Zhaohui Tong, Zhuang Ma, Jinfu Xu, Shenghua Sun, Huaping Tang, Qingyu Xiu, Yongjie Liang, Xiongbiao Wang, Xiaoju Lv, Yuanrong Dai, Yingqun Zhu, Yuejin Qu, Kaifeng Xu, Yijiang Huang, Shiman Wu, Guoxiang Lai, Xi Li, Xiaowen Han, Zegang Yang, Jifang Sheng, Zhuola Liu, Hui Li, Yiqiang Chen, Huili Zhu, Yingyuan Zhang
Previous studies have shown that sitafloxacin has broad spectrum antimicrobial activity in vitro and in vivo. Sitafloxacin is highly active against most gram-positive bacteria, gram-negative organisms, anaerobes and atypical pathogens. Several studies in Japan8–11,19–21 demonstrated that sitafloxacin was superior to levofloxacin, ciprofloxacin, tosufloxacin, trovafloxacin, moxifloxacin, garenoxacin and gatifloxacin in in vitro antimicrobial activity against most bacterial pathogens. Its MIC90 value (mg/L) was 0.06–0.5 against methicillin-susceptible S. aureus, 0.5–2 against methicillin-resistant S. aureus, 0.03–0.06 against S. pneumoniae, 0.004 against H. influenzae, 0.008–0.015 against M. catarrhalis and 0.12–0.25 against K. pneumoniae. Studies have indicated that the antimicrobial activity of sitafloxacin against S. pneumoniae and E. coli is not affected by their resistance to other fluoroquinolones, suggesting no cross-resistance to sitafloxacin in these two bacterial species10. Oral administration of sitafloxacin 100 mg qd can result in an effective antimicrobial level of sitafloxacin in plasma against S. aureus, S. pneumoniae, E. coli, H. influenzae and M. catarrhalis. Sitafloxacin penetrates well into alveolar epithelial lining fluid in critically ill patients with pneumonia after a single oral dose of 200 mg22. But sitafloxacin 100 mg bid should be used for infections caused by P. aeruginosa10.
A randomized, active-controlled, multicentre clinical trial to evaluate the efficacy and safety of oral sitafloxacin versus levofloxacin in Chinese adults with acute uncomplicated or complicated urinary tract infection
Published in Annals of Medicine, 2021
Ying Li, Yousheng Yin, Xiaomei Peng, Hongguang Zheng, Fajun Fu, Zhenxiang Liu, Xiongfei Wu, Xiaoyan Wu, Song Zheng, Nan Chen, Leye He, Laicheng Ren, Zhaohui Ni, Detian Li, Peiyu Liang, Xiaoju Lv, Yingyuan Zhang
Sitafloxacin is a fluoroquinolone antimicrobial agent developed by Daiichi Sankyo Company, Limited (Tokyo, Japan). It was approved and launched onto Japan market in 2008. Sitafloxacin is indicated for treatment of UTIs such as pyelonephritis and cystitis, and respiratory tract infections such as pneumonia, and the infections secondary to chronic respiratory diseases, as well as otitis media, nasal sinusitis, periodontitis, pericoronitis and oral infections [7]. Daiichi Sankyo (China) Holdings Co., Ltd. (Shanghai, China) sponsored this clinical study in Chinese adults with UTI for the purpose to facilitate and promote the clinical use of sitafloxacin in China. The result of this clinical study is reported as follows.