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. 1994 Jul;38(7):1476–1479. doi: 10.1128/aac.38.7.1476

Activity of levofloxacin in a murine model of tuberculosis.

S P Klemens 1, C A Sharpe 1, M C Rogge 1, M H Cynamon 1
PMCID: PMC284579  PMID: 7979275

Abstract

The activity of levofloxacin (LEV) was evaluated in a murine model of tuberculosis. Approximately 10(7) viable Mycobacterium tuberculosis ATCC 35801 were given intravenously to 4-week-old female outbred mice. In a dose-response study, treatment with LEV at 100, 200, and 400 mg/kg of body weight was started 1 day after infection and was given daily for 28 days. Viable cell counts were determined from homogenates of spleens and lungs. A dose-related reduction in organism cell counts in organs was noted for LEV. The activities of LEV at 100, 200, and 300 mg/kg were compared with those of first-line antituberculosis agents. Both isoniazid and rifampin were more active than LEV. There was no difference in activity between LEV and either ethambutol or pyrazinamide against splenic organisms. The activities of ethambutol and LEV at the two higher doses were comparable against lung organisms. LEV at 300 mg/kg was more active than pyrazinamide against lung organisms. The activity of LEV was compared with those of two other quinolones, ofloxacin and sparfloxacin. LEV at 200 mg/kg had more than twofold greater activity than ofloxacin at the same dose. Sparfloxacin at 100 mg/kg was more active than LEV at 200 mg/kg; however, the activities of sparfloxacin at 50 mg/kg and LEV at 200 mg/kg were comparable. The promising activity of LEV in M. tuberculosis-infected mice suggests that it is a good candidate for clinical development as a new antituberculosis agent.

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Selected References

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  1. Davidson P. T., Le H. Q. Drug treatment of tuberculosis--1992. Drugs. 1992 May;43(5):651–673. doi: 10.2165/00003495-199243050-00003. [DOI] [PubMed] [Google Scholar]
  2. Fu K. P., Lafredo S. C., Foleno B., Isaacson D. M., Barrett J. F., Tobia A. J., Rosenthale M. E. In vitro and in vivo antibacterial activities of levofloxacin (l-ofloxacin), an optically active ofloxacin. Antimicrob Agents Chemother. 1992 Apr;36(4):860–866. doi: 10.1128/aac.36.4.860. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Fujimoto T., Mitsuhashi S. In vitro antibacterial activity of DR-3355, the S-(-)-isomer of ofloxacin. Chemotherapy. 1990;36(4):268–276. doi: 10.1159/000238777. [DOI] [PubMed] [Google Scholar]
  4. Grosset J. Present and new drug regimens in chemotherapy and chemoprophylaxis of tuberculosis. Bull Int Union Tuberc Lung Dis. 1990 Jun-Sep;65(2-3):86–91. [PubMed] [Google Scholar]
  5. Ji B., Truffot-Pernot C., Grosset J. In vitro and in vivo activities of sparfloxacin (AT-4140) against Mycobacterium tuberculosis. Tubercle. 1991 Sep;72(3):181–186. doi: 10.1016/0041-3879(91)90004-c. [DOI] [PubMed] [Google Scholar]
  6. Kohno S., Koga H., Kaku M., Maesaki S., Hara K. Prospective comparative study of ofloxacin or ethambutol for the treatment of pulmonary tuberculosis. Chest. 1992 Dec;102(6):1815–1818. doi: 10.1378/chest.102.6.1815. [DOI] [PubMed] [Google Scholar]
  7. Lalande V., Truffot-Pernot C., Paccaly-Moulin A., Grosset J., Ji B. Powerful bactericidal activity of sparfloxacin (AT-4140) against Mycobacterium tuberculosis in mice. Antimicrob Agents Chemother. 1993 Mar;37(3):407–413. doi: 10.1128/aac.37.3.407. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Lamp K. C., Bailey E. M., Rybak M. J. Ofloxacin clinical pharmacokinetics. Clin Pharmacokinet. 1992 Jan;22(1):32–46. doi: 10.2165/00003088-199222010-00004. [DOI] [PubMed] [Google Scholar]
  9. Leysen D. C., Haemers A., Pattyn S. R. Mycobacteria and the new quinolones. Antimicrob Agents Chemother. 1989 Jan;33(1):1–5. doi: 10.1128/aac.33.1.1. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Mor N., Vanderkolk J., Heifets L. Inhibitory and bactericidal activities of levofloxacin against Mycobacterium tuberculosis in vitro and in human macrophages. Antimicrob Agents Chemother. 1994 May;38(5):1161–1164. doi: 10.1128/aac.38.5.1161. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Neu H. C., Chin N. X. In vitro activity of S-ofloxacin. Antimicrob Agents Chemother. 1989 Jul;33(7):1105–1107. doi: 10.1128/aac.33.7.1105. [DOI] [PMC free article] [PubMed] [Google Scholar]
  12. Stahlmann R. Safety profile of the quinolones. J Antimicrob Chemother. 1990 Nov;26 (Suppl 500):31–44. doi: 10.1093/jac/26.suppl_d.31. [DOI] [PubMed] [Google Scholar]
  13. Truffot-Pernot C., Ji B., Grosset J. Activities of pefloxacin and ofloxacin against mycobacteria: in vitro and mouse experiments. Tubercle. 1991 Mar;72(1):57–64. doi: 10.1016/0041-3879(91)90025-n. [DOI] [PubMed] [Google Scholar]
  14. Une T., Fujimoto T., Sato K., Osada Y. In vitro activity of DR-3355, an optically active ofloxacin. Antimicrob Agents Chemother. 1988 Sep;32(9):1336–1340. doi: 10.1128/aac.32.9.1336. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Yew W. W., Kwan S. Y., Ma W. K., Khin M. A., Chau P. Y. In-vitro activity of ofloxacin against Mycobacterium tuberculosis and its clinical efficacy in multiply resistant pulmonary tuberculosis. J Antimicrob Chemother. 1990 Aug;26(2):227–236. doi: 10.1093/jac/26.2.227. [DOI] [PubMed] [Google Scholar]

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