1982 Volume 30 Issue 6 Pages 646-661
Ceftizoxime (FK 749, CZX), a new parenteral cephalosporin antibiotic resistant to β-lactamase, was studied with special reference to excretion into bile and tissue concentrations of gallbladder and liver. The following results were obtained;
1) Antibacterial activity
Antibacterial activities of CZX against 21 strains isolated from bile of patients with cholecystectomy were superior to that of CEZ or CTM. CZX was more active against Escherichia coli and Klebsiella pneumoniae which were frequently isolated from bile than that of CEZ or CTM, and was highly active against strains of Proteus morganii, Serratia marcescens and Enterobacter aerogenes which were almost resistant to CEZ and CTM.
2) Bile and tissue levels
Bile and tissue levels of CZX and CEZ were determined at about 2 hours following intravenous bolus injection of 2 grams in 11 cases and 8 cases with cholecystectomy. Mean bile levels in gallbladder and common duct were 159.4 and 154.0μg/ml in CZX group, on the other hand were 138.7 and 128.8μg/ml in CEZ group. Mean tissue levels in wall of gallbladder was 31.9μg/g in CZX group, on the other hand was 29.9μg/g in CEZ group.
Biliary level of CZX was higher than that of CEZ.
3) Biliary levels in patients with external biliary fistula
Peak level in bile was obtained with 131.9μg/ml in average from 1 to 2 hour following intravenous bolus injection of 2g CZX, and thereafter was decreased but high level in bile was also obtained with 18.9μg/ml in average from 5 to 6 hour.
In 4 cases, biliary levels of CZX were compared with that of CEZ by cross-over method. As a result, biliary level of CZX was higher than that of CEZ during 1 to 5 hour following injection.
4) Clinical results
Out of 13 cases treated with CZX for surgical infections including postoperative meningitis and diffuse peritonitis, the results were excellent in 4 cases, good in 5 cases, and the overall efficacy was 69.2%. Especially, in 2 cases of postoperative meningitis, 3 cases of peritonitis due to perforation of appendix or pyometra, each one case of lymphangitis, mastitis, osteomyelitis and phlegmon, satisfactory effects were obtained in all cases.
No adverse reaction was observed in any of the cases, nor was there any marker changes due to administration of CZX in laboratory findings including peripheral blood examinations, hepatic and renal functions.
From above mentioned results with antibacterial activity, excretion into bile, tissue concentrations of common duct and clinical applications, ceftizoxime seemed to be a useful cephalosporin antibiotic in surgical infections such as a biliary tract infection in particular.
