In vitro and in vivo activities of levofloxacin against Mycobacterium tuberculosis
In vitro and in vivo activities of levofloxacin against Mycobacterium tuberculosis
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左氧氟沙星抗结核分枝杆菌的体外和体内活性
DOI：
10.1128/aac.39.6.1341
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发表时间：
1995
影响因子：
4.9
通讯作者：
Jacques H. Grosset
中科院分区：
文献类型：
--
作者：
B. Ji;N. Lounis;Chantal Truffot;Jacques H. Grosset
用18株结核分枝杆菌药敏菌株进行试验，左氧氟沙星（LVFX）抑制50%菌株的MIC比氧氟沙星（OFLO）抑制50%菌株的MIC低一个稀释度，但抑制90%菌株的MIC相似。LVFX体内抗M.与异烟肼、OFLO和司帕沙星（SPFX）的活性进行了比较。小鼠静脉内接种1.74 × 10（6）CFU的H37 Rv，第二天开始治疗，每周进行6次，持续4周。通过存活率、脾脏重量、大体肺病变和脾脏中CFU计数来评估感染的严重程度和治疗的有效性。在CFU计数方面，抗M.所用处理的抗结核活性按以下顺序运行：LVFX（300 mg/kg体重）= SPFX（100 mg/kg）>异烟肼> SPFX（50 mg/kg）> OFLO（300 mg/kg）= LVFX（150 mg/kg）> OFLO（150 mg/kg）= LVFX（50 mg/kg）。因此，似乎LVFX的体内活性与两倍大剂量的OFLO产生的活性相当。假设LVFX的最大临床耐受剂量与OFLO相似，即，800 mg/天，相当于小鼠中300 mg LVFX/kg。由于LVFX显示出强大的杀菌活性，如果患者接受最大临床耐受剂量的LVFX治疗，可能会对人类结核病产生有希望的效果。
In tests with 18 drug-susceptible strains of Mycobacterium tuberculosis, the MIC at which 50% of the strains are inhibited by levofloxacin (LVFX) was one dilution less than that at which 50% of the strains are inhibited by ofloxacin (OFLO), but the MICs at which 90% of the strains are inhibited were similar. The in vivo activity of LVFX against M. tuberculosis was compared with the activities of isoniazid, OFLO, and sparfloxacin (SPFX). Mice were inoculated intravenously with 1.74 x 10(6) CFU of H37Rv, and treatments began the next day and were carried out six times weekly for 4 weeks. The severity of infection and effectiveness of treatment were assessed by survival rate, spleen weights, gross lung lesions, and enumeration of CFU in the spleen. In terms of CFU counts, the ranking of the anti-M. tuberculosis activities of the treatments used ran in the following order: LVFX (300 mg/kg of body weight) = SPFX (100 mg/kg) > isoniazid > SPFX (50 mg/kg) > OFLO (300 mg/kg) = LVFX (150 mg/kg) > OFLO (150 mg/kg) = LVFX (50 mg/kg). It seems, therefore, that the in vivo activity of LVFX is comparable to that produced by a twofold-greater dosage of OFLO. It is assumed that the maximal clinically tolerated dosage of LVFX is similar to that of OFLO, i.e., 800 mg daily, which is equivalent to 300 mg of LVFX per kg in mice. Because LVFX displayed powerful bactericidal activity, promising effects against human tuberculosis may be achieved if patients are treated with the maximal clinically tolerated dosage of LVFX.