Fundamental and clinical studies on cefuzoname in the pediatric field

: Cefuzoname (CZON) one of the aminothiazolyloxyiminoacetamido cephalosporins, was studied for its antibacterial activity, absorption and excretion, concentration in the cerebrospinal fluid (CSF) and the penetration, and clinical efficacy. The following are a summary of the results: 1. Antibacterial activity; The antibacterial activity of CZON was studied on clinically isolated Staphylococcus aureus (cefazolin (CEZ)-susceptible and CEZ-tolerant strains), Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis. Compared with CZON were cefmenoxime (CMX), latamoxef (LMOX), cefoperazone, cefmetazol (CMZ), cefotiam and CEZ, but for S. aureus cefamandole (CMD) was replaced for CPZ. Activities of CZON against S. aureus, both CEZ-susceptible and CEZ-tolerant strains, were superior to those of 6 control drugs. The distribution of MICs for the CEZ-susceptible strains was 0.10-12.5 micrograms/ml, and for the CEZ-tolerant strains 0.20-greater than 100 micrograms/ml. MIC peaks were 0.39 micrograms/ml and 0.78-1.56 micrograms/ml for CEZ-susceptible and CEZ-tolerant strains, respectively. Against both susceptible and tolerant strains, CZON showed superiority to CMZ and CMD, which are used prevalently and used for Methicillin-resistant S. aureus also. Distributions of MICs of CZON (and the peak of MICs) on E. coli, K. pneumoniae, and P. mirabilis were less than or equal to 0.025-1.56 (less than or equal to 0.025), less than or equal to 0.025-25 (less than or equal to 0.025-0.05), less than or equal to 0.025-25 (less than or equal to 0.025) micrograms/ml, respectively, showing CZON's similar antibacterial activity to those of cephalosporins, CMX and LMOX, which are 5th group. 2. Absorption and excretion: Eight patients, aged 10 months to 15 years, were administered with CZON 20 mg/kg, one shot intravenously. Serum concentrations somewhat varied from patient to patient, but the mean value was 48.7 micrograms/ml after 30 minutes of administration which decreased rapidly to 13.3 micrograms/ml after 1 hour, to 3.4 micrograms/ml after 2 hours, to 1.14 micrograms/ml after 4 hours, and to 0.15 microgram/ml after 6 hours. Half-lives were 0.67-1.47 hours, with the mean of 0.87 hour. Urinary recovery rates were 24.7-55.9%, with the mean of 45.1%, in 6 hours after administration. 3. CSF concentration and penetration rate: To 4 pediatric patients with purulent meningitis, CZON 25 mg/kg or 50 mg/kg was administered and the concentration in CSF was measured.(ABSTRACT TRUNCATED AT 400 WORDS)