Pharmacology of Cefazolin and Other Cephalosporins in Patients with Renal Insufficiency

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Abstract
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.

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