LABORATORY AND CLINICAL STUDIES ON CEFTIZOXIME

Ceftizoxime was assessed for its antimicrobial activity, its concentrations in blood and recovery in urine following intramuscular injection, as well as for its clinical results in 10 cases of genito-urinary infection. 1) Comparison of antimicrobial activity showed that ceftizoxime is definitely mor...

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Published inCHEMOTHERAPY Vol. 28; no. Supplement5; pp. 681 - 695
Main Authors NAIDE, YORIO, FUJITA, TAMIO, ASANO, HARUYOSHI, YAMAGOE, TSUYOSHI, TAMAI, HIDEKI
Format Journal Article
LanguageJapanese
Published Japanese Society of Chemotherapy 01.01.1980
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Abstract Ceftizoxime was assessed for its antimicrobial activity, its concentrations in blood and recovery in urine following intramuscular injection, as well as for its clinical results in 10 cases of genito-urinary infection. 1) Comparison of antimicrobial activity showed that ceftizoxime is definitely more active against E. coil, Klesbiella and Enterobacter than ABPC, SBPC and CEZ, with only a few Enterobacter strains being resistant to the drug. In its activity against Serratia the drug was proven to be apparently more potent than SBPC and CEZ, although approximately one-third of the strains tested was found to be moderately or highly resistant. A majority of the organisms of the Proteus group was also susceptible to the drug. Agaisnt P.aeruginosa the drug gave a distribution pattern of MIC values similar to that of SBPC, however, the number of resistant strains was somewhat larger than in the case of GM. 2) The concentration of ceftizoxime in blood attained a maximum 15 to 30 minutes after intramuscular injection. The TX of the drug was estimated to be 1. 30 and 1.45 hours, respectively, following an intramuscular dose of 250 mg and 500 mg. These time intervals were shorter than a corresponding value for CEZ (injected intramuscularly by cross-over method) of 2.28 hours, but with only the difference between 250 mg of ceftizoxime and 500 mg of CEZ achieving statistical significance (P<0.05). The rate of urinary excretion of the drug was a little lower than that of CEZ. Thus, while 87.7% of the administered dose of CEZ was recovered in urine in 6 hours, corresponding figures for ceftizoxime following 250 mg and 500 mg doses were 66.4% and 67.1%, respectively. 3) Clinical results There were 4 cases of prostatitis treated with the drug. In one of these 4 cases where there was a concomitant DIC the therapeutic efficacy of the drug was considered unassessable because no causative organism could be detected and GM was used concurrently and also because fever was the only criterion available for evaluation of drug effectiveness. Of the remaining 3 cases, 2 were rated as having an excellent result and 1 as having a good result. Four cases of urinary tract infection treated with the drug (all having underlying disease) were all estimated as having a good result. The results of the drug in 1 case each of perinephritis and epididymitis were rated as good. One case with a fever developed after renal transplantation was excluded from the evaluation because of the absence of urinary tract infection. In none of the cases treated the use of the drug was attended by side effects. No abnormalities attributable to the drug were noted on laboratory tests.
AbstractList Ceftizoxime was assessed for its antimicrobial activity, its concentrations in blood and recovery in urine following intramuscular injection, as well as for its clinical results in 10 cases of genito-urinary infection. 1) Comparison of antimicrobial activity showed that ceftizoxime is definitely more active against E. coil, Klesbiella and Enterobacter than ABPC, SBPC and CEZ, with only a few Enterobacter strains being resistant to the drug. In its activity against Serratia the drug was proven to be apparently more potent than SBPC and CEZ, although approximately one-third of the strains tested was found to be moderately or highly resistant. A majority of the organisms of the Proteus group was also susceptible to the drug. Agaisnt P.aeruginosa the drug gave a distribution pattern of MIC values similar to that of SBPC, however, the number of resistant strains was somewhat larger than in the case of GM. 2) The concentration of ceftizoxime in blood attained a maximum 15 to 30 minutes after intramuscular injection. The TX of the drug was estimated to be 1. 30 and 1.45 hours, respectively, following an intramuscular dose of 250 mg and 500 mg. These time intervals were shorter than a corresponding value for CEZ (injected intramuscularly by cross-over method) of 2.28 hours, but with only the difference between 250 mg of ceftizoxime and 500 mg of CEZ achieving statistical significance (P<0.05). The rate of urinary excretion of the drug was a little lower than that of CEZ. Thus, while 87.7% of the administered dose of CEZ was recovered in urine in 6 hours, corresponding figures for ceftizoxime following 250 mg and 500 mg doses were 66.4% and 67.1%, respectively. 3) Clinical results There were 4 cases of prostatitis treated with the drug. In one of these 4 cases where there was a concomitant DIC the therapeutic efficacy of the drug was considered unassessable because no causative organism could be detected and GM was used concurrently and also because fever was the only criterion available for evaluation of drug effectiveness. Of the remaining 3 cases, 2 were rated as having an excellent result and 1 as having a good result. Four cases of urinary tract infection treated with the drug (all having underlying disease) were all estimated as having a good result. The results of the drug in 1 case each of perinephritis and epididymitis were rated as good. One case with a fever developed after renal transplantation was excluded from the evaluation because of the absence of urinary tract infection. In none of the cases treated the use of the drug was attended by side effects. No abnormalities attributable to the drug were noted on laboratory tests.
Author TAMAI, HIDEKI
NAIDE, YORIO
YAMAGOE, TSUYOSHI
FUJITA, TAMIO
ASANO, HARUYOSHI
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  organization: Department of Urology, School of Medicine, Fujitagakuen University
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References 2) NAIDE, Y.; T. KAWAMURA, K. MAXIMO, H. TAMURA & T. WATANABE: Prevalence of transferable drug resistance in drug-resistant bacteria isolated from urinary tract infections in Japan. jap. J. Microbiol. 11: 88-94, 1967
1) KAMIMURA, T.; Y. MATSUMOTO, N. OKADA, Y. MIME, M. NISHIDA, S. GOTO & S. KUWAHARA: Ceftizozime (FK 749), a new parenteral cephalosporin: In vitro and in vivo antibacterial activities. Antimicr. Agents & Chemoth. 16: 540-548, 1979
3) 大越正秋, 他: UTI薬効評価基準 (第2版). Chemotherapy 28: 324-341, 1980
4) 第26回日本化学療法学会東日本支部総会新薬シンポジウムFK749 (Ceftigoxime), 1979 (東京
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