Ji B, Truffot-Pernot C, Grosset J
Faculté de Medicine Pitié Salpêtrière, Paris, France.
Tubercle. 1991 Sep;72(3):181-6. doi: 10.1016/0041-3879(91)90004-c.
The in vitro and in vivo activities of sparfloxacin (AT-4140) against M. tuberculosis are reported. The MICs of sparfloxacin for 50% and 90% of 18 clinical isolates were, respectively, 0.25 and 0.5 mg/l, one or two dilutions lower than that of ciprofloxacin and ofloxacin. In mice infected intravenously with 0.1 mg M. tuberculosis H37Rv strain, the minimal effective dosage of sparfloxacin, as assessed by survival rate, spleen enlargement and gross lung lesions, was 12.5 mg/kg. The activities of various regimens were in the following rank order: INH 25 mg/kg = sparfloxacin 50-100 mg/kg greater than ofloxacin 300 mg/kg greater than (or =) sparfloxacin 25 mg/kg greater than sparfloxacin 12.5 mg/kg greater than (or =) ofloxacin 200 mg/kg greater than ofloxacin 100 mg/kg greater than (or =) negative control. Therefore, on a weight to weight basis, sparfloxacin was six to eight-fold more active against M. tuberculosis infection in mice than ofloxacin. In addition, WIN 57273, a new broad-spectrum fluoroquinolone, at a dosage of 100 mg/kg daily, was inactive against M. tuberculosis infection.
报告了司帕沙星（AT - 4140）对结核分枝杆菌的体外和体内活性。司帕沙星对18株临床分离株中50%和90%的最低抑菌浓度（MIC）分别为0.25和0.5mg/l，比环丙沙星和氧氟沙星低1或2个稀释度。在静脉注射0.1mg结核分枝杆菌H37Rv株感染的小鼠中，根据生存率、脾脏肿大和肺部大体病变评估，司帕沙星的最小有效剂量为12.5mg/kg。各种治疗方案的活性按以下顺序排列：异烟肼25mg/kg = 司帕沙星50 - 100mg/kg＞氧氟沙星300mg/kg＞（或 =）司帕沙星25mg/kg＞司帕沙星12.5mg/kg＞（或 =）氧氟沙星200mg/kg＞氧氟沙星100mg/kg＞（或 =）阴性对照。因此，以重量计，司帕沙星对小鼠结核分枝杆菌感染的活性比氧氟沙星高6至8倍。此外，新型广谱氟喹诺酮类药物WIN 57273，每日剂量100mg/kg，对结核分枝杆菌感染无活性。
