Jönsson Agnez, Foerster Sunniva, Golparian Daniel, Hamasuna Ryoichi, Jacobsson Susanne, Lindberg Magnus, Jensen Jörgen Skov, Ohnishi Makoto, Unemo Magnus
WHO Collaborating Centre for Gonorrhoea and other STIs, Department of Laboratory Medicine, Microbiology, Faculty of Medicine and Health, Örebro University, Örebro, Sweden.
Institute for Infectious Diseases, University of Bern, Bern, Switzerland.
APMIS. 2018 Jan;126(1):29-37. doi: 10.1111/apm.12777. Epub 2017 Nov 20.
Treatment of gonorrhoea is a challenge worldwide because of emergence of resistance in N. gonorrhoeae to all therapeutic antimicrobials available and novel antimicrobials are imperative. The newer-generation fluoroquinolone sitafloxacin, mostly used for respiratory tract infections in Japan, can have a high in vitro activity against gonococci. However, only a limited number of recent antimicrobial-resistant isolates from Japan have been examined. We investigated the sitafloxacin activity against a global gonococcal panel (250 isolates cultured in 1991-2013), including multidrug-resistant geographically, temporally and genetically diverse isolates, and performed time-kill curve analysis for sitafloxacin. The susceptibility to sitafloxacin (agar dilution) and seven additional therapeutic antimicrobials (Etest) was determined. Sitafloxacin was rapidly bactericidal, and the MIC range, MIC and MIC was ≤0.001-1, 0.125 and 0.25 mg/L, respectively. There was a high correlation between the MICs of sitafloxacin and ciprofloxacin; however, the MIC and MIC of sitafloxacin were 6-fold and >6-fold lower, respectively. Sitafloxacin might be an option for particularly dual antimicrobial therapy of gonorrhoea and for cases with ceftriaxone resistance or allergy. However, further in vitro and particularly in vivo evaluations of potential resistance, pharmacokinetics/pharmacodynamics and ideal dosing for gonorrhoea, as well as performance of randomized controlled clinical, trials are crucial.
由于淋病奈瑟菌对所有可用治疗性抗菌药物均出现耐药性，淋病的治疗在全球范围内都是一项挑战，因此新型抗菌药物势在必行。新一代氟喹诺酮类药物西他沙星在日本主要用于呼吸道感染，对淋球菌具有较高的体外活性。然而，最近来自日本的抗菌药物耐药分离株仅有少数得到检测。我们研究了西他沙星对一个全球淋球菌菌株库（1991 - 2013年培养的250株分离株）的活性，包括在地理、时间和基因上具有多样性的多重耐药分离株，并对西他沙星进行了时间杀菌曲线分析。测定了对西他沙星（琼脂稀释法）和另外七种治疗性抗菌药物（Etest法）的敏感性。西他沙星具有快速杀菌作用，其MIC范围、MIC₅₀和MIC₉₀分别为≤0.001 - 1、0.125和0.25mg/L。西他沙星和环丙沙星的MIC之间存在高度相关性；然而，西他沙星 的MIC₅₀和MIC₉₀分别低6倍和>6倍。西他沙星可能是淋病特别是双联抗菌治疗以及头孢曲松耐药或过敏病例的一种选择。然而进一步进行潜在耐药性的体外研究，特别是体内评估、药代动力学/药效学以及淋病的理想给药方案，以及开展随机对照临床试验至关重要。
