Document Type


Original Publication Date


Journal/Book/Conference Title

Antimicrobial Agents and Chemotherapy





First Page


Last Page


DOI of Original Publication



Originally published at At time of publishing, Gary R. Matzke was at University of Minnesota.

Date of Submission

November 2015


The impact of renal insufficiency on the dispositions of 300 mg of orally administered ceftibuten-cis, a new broad-spectrum oral cephalosporin, and its primary metabolite ceftibuten-trans was characterized in 30 adult subjects. Subjects were divided into five groups of six subjects each on the basis of their 24-h ambulatory creatinine clearances (CLCR). The apparent total body clearance (CLP/F; where F is absolute bioavailability) and renal clearance of ceftibuten-cis were significantly lower in subjects with end-stage renal disease (on maintenance hemodialysis; group V) and in those with severe (CLCR, 5 to 29 ml/min; group IV) and moderate (CLCR, 30 to 49 ml/min; group III) renal insufficiency than in those with mild renal insufficiency (CLCR, 50 to 80 ml/min; group II) or normal renal function (CLCR, greater than 80 ml/min; group I). A significant correlation was observed between CLCR and ceftibuten-cis CLP/F. The mean apparent steady-state volume of distribution (V beta/F) of ceftibuten-cis ranged from 0.21 to 0.24 liter/kg in subjects in group I, II, III, and IV. V beta/F was significantly greater in the group V subjects with end-stage renal disease (V beta/F, 0.39 +/- 0.27 liters/kg). These changes in V beta/F cannot be separated from possible changes in bioavailability. The maximum concentration of ceftibuten-trans in plasma was significantly higher and occurred significantly later in group IV subjects than it did in subjects in the other groups. The terminal elimination half-life of ceftibuten-trans was significantly and progressively prolonged as CLCR declined (2.63 ± 1.02, 5.37 ± 1.93, 14.29 ± 10.84, and 19.46 ± 9.69 h in groups I, II, III, and IV, respectively). The hemodialysis clearance of ceftibuten-cis was 76.9 ± 18.0 ml/min, and the fraction of the administered dose of ceftibuten-cis removed during ~3 h of hemodialysis-was 39 ±%. Ceftibuten dosage adjustments are proposed for subjects with renal insufficiency.


Copyright © 1991, the American Society for Microbiology. All rights reserved.

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VCU Pharmacotherapy and Outcomes Science Publications