新しいCephalosporin誘導体, Ceftezoleの基礎評価

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タイトル別名
  • IN VITRO AND IN VIVO EVALUATION OF CEFTEZOLE, A NEW CEPHALOSPORIN C DERIVATIVE
  • アタラシイ Cephalosproin ユウドウタイ Ceftezole ノ

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説明

Ceftezole (CTZ), a new cephalosporin C derivative, is a broad-spectrum bactericidal antibiotic. It has almost indentical antimicrobial activity against pathogenic organisms isolated from patients with that of cefazolin (CEZ) which is similar in chemical structure. The therapeutic effect of CTZ on experimental infections in mice was similar to that of CEZ and was superior to cephalothin (CET). The binding of CTZ to serum proteins was somewhat lower than that of CEZ. It is apparent from other bacteriological studies that CTZ and CEZ do not differ significantly in antibacterial properties. The serum levels of CTZ in the test animals and volunteers were determined after i.m. injection of 20mg/kg and after a single dose of 500mg, respectively. The serum levels of CTZ in volunteers peaked at 24.9μg/ml 15min after injection and remained effective (about 2.6μg/ml) at 4 hours. The serum half-life under the same conditions was 56min, i.e., about one half that of CEZ. The 24 hr. urinary recovery rate was 86.6%. Most of the administered CTZ was excreted unchanged mainly through the urinary tract. The biliary excretion rate in SD strain rats after i.m. injection of 20mg/kg was about 4.4%. As compared with commercially available cephalosporins, CTZ was second only to CEZ in biliary excretion rate. Various tissue levels of CTZ in animals were higher than CET, but with the exception of renal levels in the early stage after administration, were lower than CEZ.

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