title: Relationship between pharmacokinetics and bioavailability of cefroxadine (CGP 9000) and renal function.
abstract: 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.
mesh_terms: D000328:Adult; D000368:Aged; D001681:Biological Assay; D001682:Biological Availability; D002511:Cephalosporins / Q000378:metabolism*; D002515:Cephradine / Q000031:analogs & derivatives / Q000097:blood / Q000378:metabolism* / Q000652:urine; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006207:Half-Life; D006801:Humans; D007674:Kidney Diseases / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D008875:Middle Aged
chemical_list: D002511:Cephalosporins; C012671:cefroxadine; D002515:Cephradine