1977 Volume 25 Issue 8 Pages 2361-2370
An experimental pyelonephritis model was prepared in rats by infecting E. coli C-11 ascendently from the urethral orifice 3 days after the intraperitoneal administration of 150 mg/kg of 2-bromoethyl-amine hydrobromide. In this model, the lesion was confined to renal papillary tips, and BUN value in the blood was remarkably increased. Three days after infection of E. coli, 20 mg/kg doses of CTZ, CEZ and CER, respectively, were administered intramuscularly to rats induced pyelonephritis, and the levels of each drug in sera, kidneys and livers were determined.
The results showed that the decreasing tendencies in serum and tissue levels of CTZ with time-course showed similar patterns to those in normal rats. On the other hand, the decrease in serum and tissue levels of CEZ and CER was hardly observed.
The urinary excretion of CTZ, CEZ and CER was compared after intramuscular administration of 20, 40 and 80 mg/kg doses. It was found that the mean urinary, excretion rates in 24 hours after administration were 87-90% in CTZ, while they were 38-49% in CEZ and 33-42% in CER. These data indicated that urinary excretion in experimental pyelonephritis rats was much less disturbed in case of CTZ than in CEZ and CER.
Four patients with uremia, operated ureterostomia bilateralis, were administered intramuscularly with 1 g of CTZ and CEZ, respectively, by the cross-over method, and the serum levels and urinary excretion rates of each drug in 6 hours after administration were compared. The results showed that the urinary excretion rates of CTZ were higher than those of CEZ in all cases.
The relationship between the above results and the clinical effects of CTZ against urinary tract infections were discussed.
