1974 Volume 22 Issue 6 Pages 1080-1087
The characteristics of biliary excretion of cefazolin (CEZ), cephalothin (CET) and cephaloridine (CER) were studied6 preliminarily in rats. Based on these results, a suitable method of CEZ administration was evaluated for the treatment of bile tract infection in humans.
The relationship between dose and biliary levels of these cephalosporins was investigated in rats following an intramuscular injection. The bile levels of CEZ and CET increased as the dose increased, while CER did not show such response. Bile levels of CEZ and CET were higher than serum levels at the dose of 10-80mg/kg, whereas in CER administration serum levels were higher than bile levels.
Comparison was made, to obtain the highest bile level, among various administration routes of cephalosporins at the same dose.
Based on the results obtained from the studies in rats, a crossover study was carried out to compare the bile levels of CEZ and CER in 5 patients of cholethiasis with T-tube drainage of common bile duct after intravenous injection of 1g single dose. The peak concentration of CEZ was 0.85-21 mcg/ml and that of CER was 0.55-3. 9 mcg/ml.
In another crossover study of CEZ and CET in 5 patients after intravenous injection of 3g single dose, the peak concentration of CEZ in bile was 35.5-270 mcg/ml and that of CET was 0.3-64 mcg/ml. The sufficient bile levels of CEZ for the therapy of bile tract infection were obtained with the intravenous dose of 3g.
