Pharmacokinetics and clinical study of cefotetan in bile: prophylactic use in biliary tract surgery.

The excretion of cefotetan, a 7 alpha-methoxy-cephalosporin, was studied in 27 patients undergoing biliary surgery. Pharmacokinetic parameters were determined after a single intravenous bolus dose of 1 g (10 patients) or 2 g (17 patients). Rapidly excreted in bile, cefotetan concentrations were considerably higher in bile [range: 92-2,594 mg.l-1 (1 g); 35-4,610 mg.l-1 (2 g)] than in plasma despite the presence of gall stones. Bile bactericidal activities against Staphylococcus aureus (MIC 8 mg.l-1) and Bacteroides fragilis (MIC 2 mg.l-1) correlated well with gall bladder cefotetan levels [r = 0.888 (1 g); r = 0.971 (2 g)]. No cefotetan was detected in the bile of 3 patients with nonfunctioning gall bladders. One other patient with very low activity and these three aside, the inhibitory quotients (cefotetan concentration/MIC) were > 4 for both doses against both bacteria.