Clinical pharmacokinetics and safety of high doses of ceforanide (BL-S786R) and cefazolin.

Antimicrobial Agents and Chemotherapy
R D SmythG H Hottendorf

Abstract

The pharmacokinetics and safety of ceforanide and cefazolin were compared in normal subjects after 30-min intravenous infusions of 2-, 3-, and 4-g single doses and 4-g twice-daily doses for 10 days. No significant differences were observed in plasma-renal pharmacokinetic parameters between single and multiple doses of ceforanide. Half-life (t((1/2)), 2.8 h), plasma clearance (Cl(p), 48 ml/min per 1.73 m(2)), and renal clearance (Cl(0-12h) (r), 47 ml/min per 1.73 m(2); tubular secretion, 44%, and glomerular filtration, 56%) did not change with increased dose or on multiple dosing. No significant change was observed in t((1/2)) (1.9 h), area under the plasma concentration-time curve, Cl(r) (60 ml/min per 1.73 m(2); tubular secretion, 80%, and glomerular filtration, 20%), or Cl(p) (75 ml/min per 1.73 m(2)) for 4-g single doses compared with twice-daily administration of cefazolin. A small increase in cefazolin clearance was observed when plasma concentrations were greater than 100 mug/ml, when the single dose was increased from 2 to 4 g; this was a result of the decrease in percentage of plasma protein binding and increased renal clearance due to increased glomerular filtration. The increase in renal clearance resulted in a lack o...Continue Reading

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Citations

Feb 1, 1981·Antimicrobial Agents and Chemotherapy·R H CooperJ Mills
Apr 1, 1981·Antimicrobial Agents and Chemotherapy·F H LeeD R Van Harken
Feb 1, 1982·Antimicrobial Agents and Chemotherapy·A S DajaniR D Smyth
Feb 1, 1982·Antimicrobial Agents and Chemotherapy·S RipaM Pfeffer
May 1, 1983·Antimicrobial Agents and Chemotherapy·D E Kenady, M D Ram
Apr 1, 1985·Antimicrobial Agents and Chemotherapy·J T DiPiroJ P Rissing
Jan 1, 1986·Antimicrobial Agents and Chemotherapy·A L BarryR R Packer
Oct 1, 1986·Antimicrobial Agents and Chemotherapy·M N DudleyR Quintiliani
Nov 1, 1988·Drug Intelligence & Clinical Pharmacy·B H AckermanB H Harrison
Jul 1, 1985·Drug Intelligence & Clinical Pharmacy·P O Anderson
Mar 1, 1985·Drug Intelligence & Clinical Pharmacy·T A Tartaglione, R E Polk
Sep 1, 1983·Drug Intelligence & Clinical Pharmacy·W J CadyW R Hamsa
Nov 1, 1982·Pharmacotherapy·S L Barriere, J Mills
Nov 4, 2020·Antimicrobial Agents and Chemotherapy·Maxwell J LaskoJoseph L Kuti

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