Levofloxacin (LVFX), an optical isomer of ofloxacin (OFLX), is twice as potent as OFLX against gram-positive and gram-negative bacteria such as Haemophilus influenzae, Streptococcus pneumoniae and Pseudomonas aeruginosa, while it has been shown to be as safe as OFLX in animal experiments. Phase 1 study showed that the pharmacokinetics of LVFX were similar to those of OFLX. We carried out a multicenter collaborative trial at 69 institutions to determine the clinical efficacy and safety of LVFX in the field of internal medicine, mainly in the treatment of respiratory tract infections. LVFX was orally administered to 463 patients in daily doses of 200 mg to 600 mg for 7 to 14 consecutive days. Out of the total patients enrolled, the clinical efficacy was evaluated in 423 patients and was 84.9% (321/378) against respiratory tract infections, 78.8% (26/33) against urinary tract infections, 100% (9/9) against infectious enteritis and 100% (3/3) against other infections. As for respiratory tract infections, the efficacy rate was 90.6% (77/85) for pharyngitis and tonsillitis, 80.2% (174/217) for infectious exacerbation of chronic respiratory disease and 91.8% (67/73) for pneumonia. The efficacy rate, as a function of the daily dose, was 79.2% (38/48) with 100mg b.i.d., 85.5% (253/296) with 100mg t.i.d., 87.7% (50/57) with 200mg t.i.d., and 81.8% (18/22) with other dose regimens. The bacteriological response was evaluated in 179 patients and showed an eradication rate of 77.4% (123/159) for monomicrobial infections and 40.0% (8/20) for polymicrobial infections. The MIC was determined for 78 strains, and the eradication rate was 78.9% (56/71) for strains with an MIC value of 1.56 µg/ml or lower and 0.0% (0/7) for strains with an MIC value of 3.13 µg/ml or higher. Out of 454 patients, clinical adverse reactions were recorded in 17 (3.7%), consisting of gastrointestinal disorder in 9, neurogenic symptoms in 7 and other symptoms in 1. Abnormal laboratory findings were recorded in 41 (10.0%) out of 409 patients, the main item being elevation of the eosinophil count and the transaminase level. None of them were serious. Based on the above results, we concluded that LVFX is a useful antibacterial agent for the treatment of infections in the field of internal medicine, mainly respiratory tract infections.
|Number of pages||23|
|Publication status||Published - May 1992|
All Science Journal Classification (ASJC) codes
- Pharmacology (medical)
- Infectious Diseases
- Drug Discovery