The distribution of
ceftezole in blood and tissues and its excretion after intramuscular or
intravenous administration of single doses of 10 and 20 mg/kg were compared with those of
cefazolin,
cephaloridine and
cephalothin. Blood levels of
ceftezole in rats and rabbits were lower than those of
cefazolin, and higher than those of
cephaloridine and
cephalothin. Retention time of
ceftezole in the blood was somewhat shorter than that of
cefazolin. However, blood levels of
ceftezole in dogs were nearly the same as those of
cefazolin and
cephaloridine. The rate of urinary excretion of
ceftezole in 24-hour urine after administration in rats and rabbits was found to be higher than those of the other
antibiotics tested. In dogs, however, the rate of urinary excretion of
ceftezole was nearly the same as that of
cefazolin and higher than those of
cephaloridine and
cephalothin. The biliary excretion of
ceftezole in rats and dogs was much higher than those of
cephaloridine and
cephalothin, but lower than that of
cefazolin. Tissue distribution of
ceftezole in rats was compared with that of the other
antibiotics by intramuscular and
intravenous administration. The initial level of
ceftezole in the kidneys was found to be substantially higher than those of the other
antibiotics. The initial level of
ceftezole in the liver and lungs was also slightly higher than those of the other drugs when administered intramuscularly. Tissue levels of
ceftezole were somewhat lower than those of
cefazolin in rabbits after
intravenous administration.
Ceftezole attained a higher maximum level in rat lymph by intramuscular administration than the other
antibiotics tested. The maximum concentration of
ceftezole present in the exudate in the rat inflammatory pouch was higher than that of
cefazolin. In rabbits with cerebrospinal
meningitis induced by
infection of Streptococcus pyogenes, the level of
ceftezole in the cerebrospinal fluid was several times higher than that in normal rabbits. The serum level and urinary excretion of
ceftezole was examined in 6 healthy male volunteers after intramuscular administration of a single dose of 500 mg.
Ceftezole attained a mean maximum serum level of 22.9 mug/ml 30 minutes after administration and disappeared from the blood in about 6 hours. It was excreted rapidly in the urine. The concentration in 1-hour urine was the highest (mean level: 2,667 mug/ml) and the total excretion rate was 92.6%. No metabolites with antimicrobial activity were observed in the urine. No changes in the pattern of plasma level and urinary excretion and no accumulation in the tissues were observed after repeated intramuscular administration of 20 mg/kg of
ceftezole in rabbits, 26 times, for 14 days.