[Pharmacokinetics and clinical evaluation of ceftizoxime (author's transl)]

Abstract

Pharmacokinetics of ceftizoxime (CZX), a new cephalosporin antibiotic, was investigated in 9 children with normal renal and hepatic function. In addition, the clinical effect of CZX was evaluated in 26 pediatric patients with various infections. In 4 of the 9 children with normal renal and hepatic function, intravenous bolus injection of CZX in a dose of 20 mg/kg yielded a mean peak serum level of 36.5 micrograms/ml at 1/2 hour after infusion, and mean serum levels of 12.5 micrograms/ml at 2 hours and 6.0 micrograms/ml at 4 hours after infusion. The biological half-lives of CZX were estimated to be 1.25--2.55 hours. In another child, serum levels of CZX at 1/2, 2 and 4 hours after intravenous bolus injection in a dose of 10 mg/kg were 19.60, 5.96 and 2.06 micrograms/ml, respectively. The clear difference in dose response between 20 mg/kg and 10 mg/kg reflected the doubled dose levels. In the remaining 4 children, drip infusion of CZX in a dose of 20 mg/kg (1 child 17 mg/kg) over 0.5--1.5 hours yielded peak serum levels at the end of infusion. The biological half-lives of CZX were estimated to be 0.95--1.50 hours. About 80% of CZX was excreted in the urine within 6 hours after infusion in the 4 children tested. Twenty-six pediatric patients with various infections were treated with CZX intravenous doses of 20 mg/kg to 118 mg/kg b.i.d.--q.i.d. for 3--14 days. Of the 12 patients with acute bronchitis and pneumonia, 5 showed excellent response, 6 good and 1 fair response. Of the 5 patients with urinary tract infection, 4 showed excellent response and 1 good response. One patient each with colitis, tonsillitis and facial cellulitis, pharyngitis showed excellent response and 1 patient each with purulent thyroiditis and gluteal abscess showed good response. The single patients with sepsis showed excellent response. One patient each with pyothorax, purulent arthritis and cerebral abscess showed poor response. Overall effectiveness rate was 84.6%. although 22 of all 26 patients treated had serious underlying diseases such as APL, AML. A mild increase in GOT and GPT was observed in 1 patient during treatment with CZX, and the values returned to normal after discontinuation of the drug. These results suggest that ceftizoxime is 1 of the most important antibiotics for treating a wide range of infections in children as well as in adults.