Effects of renal dysfunction on the pharmacokinetics of loracarbef.
Loracarbef, the first carbacephem antibiotic to undergo clinical development, is excreted primarily unchanged in the urine (> 90%). Data analyzed from subjects with various degrees of renal dysfunction who were given single oral doses of loracarbef indicated a linear relationship between creatinine clearance (CLCR) and plasma clearance [CLP (L/hr) = 0.106.CLCR (ml/min/1.73 m2)]. The mean area under the plasma concentration-time curve in normal subjects and in patients with severe renal insufficiency (no dialysis/receiving dialysis) was 32 micrograms.hr/ml and 1085 micrograms.hr/ml/103 micrograms.hr/ml, respectively. Therefore, for individuals with moderate renal insufficiency (CLCR, 10 to 49 ml/min/1.73 m2), the dose should be halved or the dosing interval doubled; patients with severe renal insufficiency who are not receiving dialysis should be treated with the normal dose given once every 3 to 5 days. Loracarbef is readily cleared from plasma by hemodialysis; dosing should be repeated after a hemodialysis treatment.
Lilly Research Laboratories, Indianapolis, IN.
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Therasse
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Farlow
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Davidson
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Quadracci
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Hatcher
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Cerimele
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DeSante
D000328:Adult; D002511:Cephalosporins / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D007676:Kidney Failure, Chronic / Q000378:metabolism* / Q000503:physiopathology / Q000628:therapy; D007677:Kidney Function Tests; D008297:Male; D008875:Middle Aged; D006435:Renal Dialysis
D002511:Cephalosporins; C054920:loracarbef