[Pharmacokinetic and clinical evaluation of cefozopran in the pediatric field]

We conducted pharmacokinetic and clinical studies on cefozopran (CZOP, SCE-2787), an aminothiadiazolmethoxyiminoacetamido cephalosporin, and obtained the following results. 1. Concentrations in serum/excretion in urine We studied pharmacokinetic in children upon intravenous bolus injection and 30-minute intravenous drip infusion in single doses of 10 and 20 mg/kg. Upon intravenous bolus injection, mean serum concentrations 30 minutes after administration of 10 and 20 mg/kg were 27.8 and 52.3 micrograms/ml, respectively, and half-lives were 2.01 and 2.02 hours, respectively. Upon 30-minute intravenous drip infusion, mean serum concentrations on completion of the drip infusions of 10 and 20 mg/kg were 36.8 and 70.3 micrograms/ml, respectively, and half-lives were 1.74 and 4.11 hours, respectively. Their urinary recovery rates in the first 8 hours after administration were higher than 67.0% in the former regimen and between 23.2 to 98.0% in the latter. 2. Clinical results 54 patients were treated with CZOP for 32 cases of pneumonia, 11 cases of bronchitis, 3 cases of cervical lymphadenitis, 1 case of purulent tonsillitis, 2 cases of phlegmon, 2 cases of enterogastritis and 3 cases of urinary tract infections. CZOP gave "excellent" or "good" responses in 53 cases. 1 case of urinary tract infection showed fair response. Diarrhea was observed in 1 case. Abnormal laboratory test results were noted in 9 patients including elevations of eosinophils, GOT and GPT. In no cases the treatment had to be discontinued.