Jacobs M R
Department of Pathology, Case Western Reserve University, Cleveland, Ohio 44106.
Am J Med. 1991 Dec 30;91(6A):31S-34S. doi: 10.1016/0002-9343(91)90307-j.
Although the fluoroquinolones share many properties, these agents differ in their ability to kill the same bacterial strain. The bactericidal activity of temafloxacin against a number of pathogens has been compared with that of other fluoroquinolones by determination of minimal bactericidal concentration, time-kill kinetics, and postantibiotic effect. Studies have demonstrated that temafloxacin has equivalent or superior ability to kill when compared with other fluoroquinolones. Temafloxacin, ciprofloxacin, and PD 117558 were more active than other fluoroquinolones against Mycobacterium avium complex, with 90% minimal bactericidal concentrations (MBC90S; 8-16 micrograms/mL) four- to eightfold greater than 90% minimal inhibitory concentrations (MIC90S; 2 micrograms/mL). Against Chlamydia trachomatis the MIC90 and MBC90 of temafloxacin were both 0.25 microgram/mL; ciprofloxacin was less active (MBC90 twice the MIC90), and norfloxacin was least active. Temafloxacin demonstrated more rapid killing kinetics than did ciprofloxacin or ofloxacin at all concentrations tested against Streptococcus pyogenes. Findings were similar against Streptococcus pneumoniae at antibiotic concentrations of 1-2 micrograms/mL. Similar time-kill curves against Escherichia coli were observed for temafloxacin, ciprofloxacin, and difloxacin. Time-kill kinetics of temafloxacin against methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-sensitive S. aureus (MSSA) were superior to those of ciprofloxacin and ofloxacin. Postantibiotic effect with temafloxacin against Legionella pneumophila showed a considerable delay in regrowth, and temafloxacin delayed regrowth of MRSA and MSSA to a greater extent than did ciprofloxacin or ofloxacin. By the three methods used in the studies to assess bactericidal activity that are currently published, temafloxacin had equivalent or superior activity to the comparative fluoroquinolones tested. Other organisms remain to be tested and the significance of these findings determined in clinical studies.
尽管氟喹诺酮类药物有许多共同特性,但这些药物在杀灭同一菌株的能力上存在差异。通过测定最低杀菌浓度、时间杀菌动力学和抗生素后效应,已将替马沙星对多种病原体的杀菌活性与其他氟喹诺酮类药物进行了比较。研究表明,与其他氟喹诺酮类药物相比,替马沙星具有同等或更强的杀菌能力。替马沙星、环丙沙星和PD 117558对鸟分枝杆菌复合群的活性比其他氟喹诺酮类药物更强,其90%最低杀菌浓度(MBC90s;8 - 16微克/毫升)比90%最低抑菌浓度(MIC90s;2微克/毫升)高4至8倍。对于沙眼衣原体,替马沙星的MIC90和MBC90均为0.25微克/毫升;环丙沙星活性较低(MBC90是MIC90的两倍),诺氟沙星活性最低。在针对化脓性链球菌测试的所有浓度下,替马沙星的杀菌动力学比环丙沙星或氧氟沙星更快。在抗生素浓度为1 - 2微克/毫升时,对肺炎链球菌的研究结果相似。观察到替马沙星、环丙沙星和双氟沙星对大肠杆菌的时间杀菌曲线相似。替马沙星对耐甲氧西林金黄色葡萄球菌(MRSA)和甲氧西林敏感金黄色葡萄球菌(MSSA)的时间杀菌动力学优于环丙沙星和氧氟沙星。替马沙星对嗜肺军团菌的抗生素后效应显示其再生长有相当大的延迟,并且替马沙星比环丙沙星或氧氟沙星更能延迟MRSA和MSSA的再生长。通过目前已发表的研究中用于评估杀菌活性的三种方法,替马沙星与所测试的对照氟喹诺酮类药物具有同等或更强的活性。其他微生物仍有待测试,这些发现的临床意义有待在临床研究中确定。