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The pharmacokinetic properties and clinical efficacy of iv mezlocillin were studied in 25 children (ages 2–17 years) with malignancies and normal renal and hepatic functions. The children received gentamicin in addition to mezlocillin. Administration of mezlocillin was over 30 min at two dosage regimens: (1) 50 mg/kg/dose every 4 h or (2) 75 mg/kg/dose every 4 h. After a 30 min infusion, mean serum concentrations of mezlocillin were 241±26 mg/l in group 1 and 278±34 mg/l in group 2 and at 4 h after infusion were 14±3 mg/1 and 45±16 mg/l in groups 1 and 2 respectively. The mean serum half-life was 50±4 min. The mean area under the curve was 354±38 mg-h/l. The mean volume of distribution was 0 24±0.03 1/kg and the mean total body clearance was 0.19±0.02 1/h/kg. These results suggest that the optimal dosage of mezlocillin in children should be 75 mg/kg/dose administered every 4 h and that this is a safe and effective antibiotic for therapy of serious infections when combined with an aminoglycoside antibiotic in children with cancer. [ABSTRACT FROM PUBLISHER]