cefroxadine and Kidney-Diseases

The pharmacokinetics and bioavailability of cefroxadine were studied in 15 patients with different renal functions after administration of 0.5 g as oral capsules and as intravenous infusions. Microbiological assays by agar diffusion and high-pressure liquid chromatography may both be used for this agent since no metabolite can be found. The bioavailability is near 100% of the oral dose regardless of renal function. Urinary recovery varied from about 50% in renal glomerular filtration rates (GFR) of less than 7 ml/min to nearly 100% in normal renal function. The serum concentrations, serum elimination half-life and total body clearance were significantly influenced by reduced renal function. Nonrenal elimination occurred in reduced renal function; the maximum serum elimination half-life was 24.6 h. Dose modifications according to renal function are suggested with from three doses/24 in normal renal function to one dose/24 h in patients with GFR of 10 ml/min. The relative distribution volume corresponded to approximately 30% of the body weight. Tubular secretion of cefroxadine took place. The concentrations in urine remained above 32 mg/l for 12 h in all subjects regardless of renal function.

Topics: Adult; Aged; Biological Assay; Biological Availability; Cephalosporins; Cephradine; Chromatography, High Pressure Liquid; Female; Half-Life; Humans; Kidney Diseases; Kinetics; Male; Middle Aged

The pharmacokinetics of cefroxadine, a new orally active broad-spectrum cephalosporin, was studied in healthy volunteers and patients with impaired renal function after a single oral dose of 500 mg. The pharmacokinetic parameters of cefroxadine were obtained by analysing the serum level data of the drug based on a one-compartment open model. The mean serum half-life of cefroxadine was 0.97 h in healthy subjects, and was prolonged to 41.7 h in patients with a creatinine clearance of less than 5 ml/min. There was a significant linear correlation (p less than 0.001) between the elimination rate constant of the drug and the creatinine clearance. In healthy subjects, 71% of the administered dose was excreted in the urine collected over the first 6 h.

Topics: Adult; Aged; Cephalosporins; Cephradine; Creatinine; Humans; Kidney Diseases; Kinetics; Middle Aged