cefuzonam and Staphylococcal-Infections

The validity of clinical use of cephem antibiotics for preventing the spread of methicillin-resistant Staphylococcus aureus (MRSA) was investigated using a methicillin-susceptible S. aureus (MSSA) carrying mecA gene. It became evident that drug with anti-staphylococcal activity, such as cefuzonam (CZON) or cefazolin (CEZ), has comparatively low selectivity of high-level methicillin resistant clones (methicillin MIC range from 25 to 800 micrograms/ml) from MSSA carrying mecA gene among cephem antibiotics tested. At concentrations over 1.56 micrograms/ml of both CZON and CEZ, about a 2-3 log10 decrease in viable count was observed. Therefore, it seems that much satisfactory disappearance of bacterial cells can be obtained in cooperation with host defence mechanisms.

Topics: Cefazolin; Ceftizoxime; Drug Resistance, Microbial; Genes, Bacterial; Humans; Immunity, Innate; Methicillin Resistance; Polymerase Chain Reaction; Staphylococcal Infections; Staphylococcus aureus

Fundamental and clinical studies on cefuzonam (CZON, L-105) were carried out and the results obtained are summarized below: MICs against 451 clinical isolates of Staphylococcus aureus were determined. Antibacterial activity of CZON on S. aureus was similar to that of cefazolin, inferior to that of cloxacillin, and superior to those of benzylpenicillin and cefotaxime. With one-shot intravenous injection of CZON, peak serum concentrations were 40.0 micrograms/ml and 97.5-145 micrograms/ml with a dose of 10 mg/kg and 20 mg/kg, respectively. Half-lives of the drug in serum were 34.2-47.9 minutes. Urinary excretion rates were 46.8-67.3% in 4 hours after injection. In all of 13 cases of pediatric infections tested, the clinical efficacy was excellent or good. Side effects observed were diarrhea in 4 patients, and elevated GOT and thrombocytosis in 1 patient each. From the above results, we have concluded that CZON is useful and safe antibiotic for treating various bacterial infections in children.

Topics: Age Factors; Blood Coagulation; Ceftizoxime; Cephalosporins; Child; Child, Preschool; Drug Evaluation; Drug Resistance, Microbial; Female; Humans; Infant; Intestines; Male; Staphylococcal Infections; Staphylococcus aureus

Concentrations of cefuzoname in cerebrospinal fluid (CSF) were determined in a total of 16 rabbits, 5 with healthy meninges, 5 with Staphylococcus aureus meningitis, and 6 with Escherichia coli meningitis. Mean percentages of the maximum concentration of the drug in CSF versus that in serum were 0.57, 3.37, and 4.40% for healthy rabbits, those with staphylococcal meningitis, and those with E. coli meningitis, respectively. The percentages of the area under the concentration-time curve of cefuzoname in CSF versus that in serum were, in the order of healthy group, staphylococcal meningitis group, and E. coli meningitis group, 0.61, 4.99, and 8.04% at 15 to 60 min, 1.44, 7.09, and 12.7% at 15 to 120 min, and 1.87, 8.07, and 15.8% at 15 to 180 min after administration, showing significant differences between the healthy and meningitis groups. All of the values in the E. coli meningitis group were greater than those of the staphylococcal meningitis group, but the differences were not significant. The ratios of the half-life of cefuzoname in CSF to that in serum were 2.10, 1.98, and 3.37 for the healthy, staphylococcal meningitis, and E. coli meningitis groups, respectively, with no significant difference between the three groups. Cefuzoname seems to be among the middle ranks of beta-lactam agents as far as penetration rate is concerned; however, when its potent antibacterial activity and broad spectrum are taken into account, the concentrations in CSF in patients with meningitis seem worth examining.

Topics: Animals; Ceftizoxime; Cephalosporins; Escherichia coli Infections; Half-Life; Meningitis; Rabbits; Staphylococcal Infections