Cefpiromeの基礎的検討

Abstract

新規注射用cephalosporin剤CPRの淋菌に対する抗菌力と前立腺, 腎臓の組織移行性を検討した.1)当科保存のNeisseria gonorrhoeae(非PPNG 34株, PPNG 20株)に対するCPRのMIC分布は非PPNGで≦0.003～0.1 μg/ml, PPNGで0.006～0.1 μg/mlで, MIC90はそれぞれ0.1 μg/ml, 0.05 μg/mlであった.2) CPR 1 g静注時の血中濃度と前立腺組織内濃度を30症例で検討した.組織内濃度は投与後15分で52.8 μg/gと最高値をとり, 以後経時的に漸減し, 60分平均値17.9 μg/g, 180分値10.1 μg/g, 320分値7.22 μg/g, 360分値2.70 μg/gであった.組織内濃度と組織採取時の血中濃度とは正相関をもち, 前立腺組織へは血中濃度に応じた組織移行が起こると考えられる.3)腎組織内濃度は4例で測定し, 投与90～100分後で皮質内濃度は107～148 μg/g, 髄質内濃度は80.6～88.6 μg/gといずれの症例も血中濃度を上回っていた.以上の点よりCPRは淋菌に対し優れた抗菌力を持つとともに十分な血中および組織内濃度を示し, 泌尿器感染症においても有用性が高い

The antibacterial activity of cefpirome (CPR), a new parenteral cephalosporin antibiotic having a cyclopentenopyridine group in the 3-position side chain, was evaluated against Neisseria gonorrhoeae and concentrations in human kidney and prostate was determined. The minimum inhibitory concentrations (MICs) of CPR against N. gonorrhoeae isolated clinically in our out-clinic (34 strains of non-PPNG and 20 of PPNG) were less than or equal to 0.003-0.1 microgram/ml in non-PPNG group and 0.006-0.1 microgram/ml in PPNG group. The 90% of MICs (MIC90s) was 0.1 microgram/ml in the non-PPNG group and 0.05 microgram/ml in the PPNG group. The concentration in the prostate was determined in 30 cases with benign prostatic hypertrophy. The maximum values was 52.8 micrograms/g at 15 minutes after administration of 1 g of CPR. The levels of CPR were gradually decreased with the lapse of time. The prostatic tissue concentration was 17.9 micrograms/g at 60 min., 10.1 micrograms/g at 180 min., 7.22 micrograms/g at 320 min. and 2.70 micrograms/g at 360 min. There was a positive correlation between concentration of the prostate and plasma collected at the time of the prostate. The concentration of CPR in human kidney, 90-100 min. after administration of 1 g to 4 cases with renal tumor, was 107-148 micrograms/g in the renal cortex, and 80.6-88.6 micrograms/g in the renal medulla. The concentration in kidney was higher than that in the plasma in all cases. In conclusion, CPR is suggested to be a useful drug for urological infection.