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[Levofloxacin in the field of dermatology]
Abstract:
1. Minimum inhibitory concentrations (MICs) of levofloxacin (LVFX, DR-3355), ofloxacin (OFLX), tosufloxacin (TFLX), norfloxacin (NFLX) were determined, with an inoculum size of 10(6) cfu/ml, against 122 strains of Staphylococcus aureus isolated from lesions of skin infections. LVFX showed most frequent MIC values of 0.20 micrograms/ml. OFLX, TFLX, and NFLX showed most frequent MIC values of 0.39 micrograms/ml, less than or equal to 0.05 micrograms/ml and 0.78 micrograms/ml, respectively. 2. Serum and skin levels of LVFX after oral administration (10 mg/kg, fasting) were determined in rats. Serum levels were 1.79, 1.29, 0.60, 0.43 and 0.18 micrograms/ml, and corresponding skin levels were 1.63, 1.77, 1.04, 0.87 and 0.64 micrograms/g (wet weight) at 0.5, 1, 2, 4 and 8 hours after administration (n = 5), respectively. 3. LVFX was used clinically in 43 cases at doses of 200-300 mg divided into 2 or 3 doses, and evaluated for final overall clinical efficacy in 41 cases. Cure was observed in 21 cases, remarkable improvement in 13 cases, improvement in 4 cases, unchanged in 1 case, aggravation in 1 case, and remarkable aggravation in 1 case. Diarrhea was observed in 2 cases, diffuse erythema with feverishness in 1 case and slight dyspnea in 1 case. Transient slight eosinophilia, elevation of Al-P, anemia and leukopenia were observed.
Insights
Levofloxacin (LVFX) demonstrates potent activity against Staphylococcus aureus skin infections, showing favorable MIC values and effective serum and skin penetration in preclinical models. Clinical trials indicate significant efficacy in treating skin infections with manageable side effects.
Area of Science:
- Microbiology and Infectious Diseases
- Pharmacology and Toxicology
- Dermatology
Context:
- Staphylococcus aureus is a common pathogen in skin infections.
- Fluoroquinolones are a class of antibiotics used to treat bacterial infections.
- Understanding the efficacy and pharmacokinetic profiles of antibiotics is crucial for effective treatment.
Purpose:
- To evaluate the in vitro activity of levofloxacin (LVFX) and other fluoroquinolones against Staphylococcus aureus.
- To determine the pharmacokinetic properties of LVFX in rat serum and skin.
- To assess the clinical efficacy and safety of LVFX in patients with skin infections.
Summary:
- Levofloxacin exhibited the lowest minimum inhibitory concentrations (MICs) against Staphylococcus aureus compared to ofloxacin, tosufloxacin, and norfloxacin. In rats, LVFX achieved significant serum and skin concentrations after oral administration, indicating good penetration. Clinical evaluation in 43 patients showed an overall efficacy rate of 85.4% (cure or improvement) for skin infections, with adverse events including diarrhea and transient laboratory abnormalities.
Impact:
- Levofloxacin demonstrates promising efficacy and favorable pharmacokinetic properties for treating Staphylococcus aureus skin infections.
- The findings support the use of levofloxacin as a therapeutic option for skin infections caused by susceptible S. aureus strains.
- Further research could explore optimal dosing regimens and comparative effectiveness against other antibiotics.