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Related Experiment Videos

[Antituberculosis effect of levofloxacin].

Y Lu1, L Zhu, L Duan

  • 1Beijing Institute of Tuberculosis and Thoracic Tumor, Beijing 101149, China.

Zhonghua Jie He He Hu Xi Za Zhi = Zhonghua Jiehe He Huxi Zazhi = Chinese Journal of Tuberculosis and Respiratory Diseases
|January 10, 2002
PubMed
Summary

Levofloxacin (LVLX) demonstrates potent in vitro and in vivo activity against Mycobacterium tuberculosis, showing twice the efficacy of ofloxacin (OFLX). This new antituberculosis drug offers comparable effectiveness with fewer side effects.

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Area of Science:

  • Microbiology and Infectious Diseases
  • Pharmacology and Pharmaceutical Sciences
  • Clinical Medicine

Background:

  • Tuberculosis remains a significant global health challenge, necessitating the development of effective and safe therapeutic agents.
  • Fluoroquinolones, including ofloxacin, have been utilized in tuberculosis treatment, but resistance and side effects are concerns.
  • Levofloxacin, a fluoroquinolone, presents a potential alternative for tuberculosis therapy.

Purpose of the Study:

  • To evaluate the in vitro and in vivo antimycobacterial activities of levofloxacin (LVLX) against Mycobacterium tuberculosis.
  • To assess the pharmacokinetics of LVLX and compare its efficacy and safety with ofloxacin (OFLX) in treating pulmonary tuberculosis.

Main Methods:

  • Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) of LVLX and OFLX were determined using the tube doubling dilution method.

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  • In vivo efficacy was assessed in a murine tuberculosis model by measuring the half survival time.
  • Pharmacokinetic parameters were analyzed using High-Performance Liquid Chromatography (HPLC) in 138 newly diagnosed and retreatment pulmonary tuberculosis patients.

    • Main Results:

    • LVLX exhibited MIC and MBC values two dilutions lower than OFLX, indicating superior in vitro activity.
    • In a murine model, LVLX demonstrated significantly greater antimycobacterial activity than OFLX at equivalent doses.
    • Clinical trials showed high sputum conversion rates (97% for LVLX group) and X-ray resolution rates, with low incidence of adverse drug reactions for LVLX compared to OFLX.

    Conclusions:

    • Levofloxacin possesses strong in vitro and in vivo activity against Mycobacterium tuberculosis, exceeding that of ofloxacin.
    • LVLX and OFLX share similar favorable pharmacokinetic profiles.
    • LVLX at 300 mg/d is an effective and safe alternative to OFLX at 600 mg/d for pulmonary tuberculosis treatment, with a better safety profile.