Pharmacology of Cefazolin and Other Cephalosporins in Patients with Renal Insufficiency

The pharmacokinetic behavior of cefazolin and cephalothin was compared in patients with normal and impaired renal function. With equivalent doses, total levels of cefazolin in serum exceeded those of cephalothin by four- to sixfold, and concentrations of free cefazolin were three times higher. This...

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Bibliographic Details
Published in:The Journal of infectious diseases 1973-10, Vol.128 (Supplement-2), p.S347-S353
Main Authors: Craig, Wlliiam A., Welling, Peter G., Jackson, Thomas C., Kunin, Calvin M.
Format: Article
Language:English
Subjects:
Blood
Blood proteins
Blood Proteins - metabolism
Cephalosporins
Cephalosporins - blood
Cephalosporins - metabolism
Cephalothin - metabolism
Dialysis
Dosage
Half lives
Half-Life
Humans
Kidney - physiopathology
Kidney Failure, Chronic - metabolism
Kidney Failure, Chronic - physiopathology
Pharmacokinetics
Protein Binding
Renal clearance
Renal Dialysis
Renal function
Sulfides - metabolism
Tetrazoles - metabolism
Thiadiazoles - metabolism
Urine
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Summary:The pharmacokinetic behavior of cefazolin and cephalothin was compared in patients with normal and impaired renal function. With equivalent doses, total levels of cefazolin in serum exceeded those of cephalothin by four- to sixfold, and concentrations of free cefazolin were three times higher. This can be explained largely by the greater binding of cefazolin to serum proteins (83.9% compared with 65.2% for cephalothin) and its lower rate of renal clearance. Binding of cefazolin to serum proteins was markedly reduced in uremic patients despite adequate concentration of albumin in serum. The kidney was the principle route of excretion for both drugs, but the effect of renal failure on persistence of antibiotic in the body was more pronounced for cefazolin. The half-life of cefazolin in serum of normal persons was 1.9 hr and as long as 35 hr in severely uremic patients; it was only modestly influenced by hemodialysis. High concentrations of cefazolin were obtained in urine even in uremic patients whose clearance exceeded 10 ml per min. The drug was well tolerated when injected im. No accumulation was noted, and presumably good therapeutic levels were obtained when cefazolin was given at 8-hr intervals.
ISSN:0022-1899
1537-6613
DOI:10.1093/infdis/128.Supplement_2.S347