新半合成セファロスポリン系抗生物質Cefoperazone (T-1551) の抗菌力, 吸収, 排泄, 代謝, 臓器移行性および外科臨床応用について

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  • STUDIES ON CEFOPERAZONE (T-1551) IN SURGERY Antibacterial Activity, Absorption, Excretion, Metabolism, Tissue Distribution and its Clinical Application
  • シン ハン ゴウセイ セファロスポリンケイ コウセイ ブッシツ Cefoper

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Fundamental and clinical studies on cefoperazone (CPZ, T-1551), a new semisynthetic cephalosporin, were investigated and the results obtained were summarized as follows.<BR>1) Antimicrobial spectrum<BR>CPZ showed a broad antimicrobial spectrum against both gram-positive and gramnegative bacteria.<BR>2) Antimicrobial activities against clinical isolates<BR>CPZ was less active than other cephalosporins against Staphylococcus aureus, but it was more active than most of the other cephalosporins against Escherichia coli, Klebsiella pneumoniae, Enterobacter sp., Serratia marcescens and Pseudornonas aeruginosa.<BR>3) Serum and urinary concentrations<BR>CPZ was intraveneously injected at the dose of 1, 000mg in three healthy human volunteers. For the results, blood levels of CPZ were reached the maximal levels of 280μg/ml at 1/12h and 6.9μg/ml at 6h after administration.<BR>The urinary concentrations showed the peak levels of 2, 600μg/ml at 30 min. after administration and the mean recovery rate was 26.0% within six hour's urine sample.<BR>4) Pharmacokinetics<BR>From the above data, the pharmacokinetic parameters were analysed to computer from the two compartment open model method, and the parameter of Kel, K12, K21, T1/2 (α), T1/2 (β) and Vd (I) was 1.17, 2.37, 2.20, 0.26, 1.40 and 2.71, respectively.<BR>5) In vivo metabolism<BR>The metabolites of CPZ were studied on human urine after administration. With bioautogram drawn up by TLC, it was revealed that CPZ was not metabolized in living body.<BR>6) Tissue concentration of rats<BR>According to results obtained with intramuscular injection of CPZ 20mg/kg to SD strain rats, the highest concentration was observed in the kidney and then liver, serum, in order.<BR>7) Result of clinical application<BR>CPZ was used for the treatment of 20 cases of surgical field infections and the results showed that 5 cases were excellent, 13 cases good and 2 cases poor.<BR>The efficacy rate was 90%.<BR>8) Side effects No severe side effects were observed clinically and in laboratory findings.

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