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Antimicrob Agents Chemother. 1979 August; 16(2): 127-133
Copyright © 1979, American Society for Microbiology. All Rights Reserved.

Human Pharmacology of Cefotaxime (HR 756), a New Cephalosporin

Ruedi Lüthy1, Reiner Münch1, Jürg Blaser2, Hansjörg Bhend1 and Walter Siegenthaler1

1 Department of Medicine, University of Zürich, CH-8091 Zürich, Switzerland
2 Institute for Biomedical Engineering, University of Zürich and Federal Institute of Technology, CH-8091 Zürich, Switzerland

ABSTRACT

Cefotaxime (HR 756) is a new semisynthetic parenteral cephalosporin with exceptional activity against gram-negative organisms and considerable stability against their ß-lactamases. To study its pharmacokinetic properties, 0.5-, 1-, and 2-g doses were administered to each of six volunteers intravenously over 15 min, followed by a sustaining infusions of 0.5, 1, and 2 g/h, respectively, for 3 consecutive hours. The loading doses produced mean peak levels of 41, 93, and 160 µg/ml, and mean steady-state serum concentrations were 27, 64, and 138 µg/ml, respectively. The mean terminal half-life was 75 ± 7 min. The total volume of distribution averaged 0.22 ± 0.03 liters/kg of body weight. Total body and renal clearances were 232 ± 30 and 145 ± 24 ml/min per 1.73 m2, respectively; 63 ± 9% of the administered dose was excreted through the kidneys in 24 h. To determine the effect of cefotaxime on the renal tubules, urinary alanine aminopeptidase excretion was measured before, during, and after the infusions. It remained within the normal range in all instances; however, 48 ± 14% of the total daily alanine aminopeptidase output was recovered during the infusion period. Side effects were dose related and included fatigue, loose stools, and night sweats. No significant changes in hematology, serum chemistry, or urinalysis were recorded.

Antimicrob Agents Chemother. 1979 August; 16(2): 127-133
Copyright © 1979, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Varghese, M., Khan, A. J., Kumar, K., Schaeffer, H. A., Pierro, M., Evans, H. E. (1984). Evaluation of Cefotaxime in Bacterial Infections. CLIN PEDIATR 23: 220-222 [Abstract]  


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