Cefamandoleに関する基礎的・臨床的研究 LABORATORY AND CLINICAL STUDIES ON CEFAMANDOLE
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従来のセファロスポリン系抗生物質より抗菌力の拡大と増強がなされたとされるCefamandole sodiumにつき基礎的・臨床的研究を行なった。呼吸器感染症の病原菌に対するMICのピーク値は, 肺炎球菌0.1μg/ml, 大腸菌0.78μg/ml, 肺炎桿菌0.78μg/ml, インフルエンザ菌0.39μg/mlで, 本剤の抗菌力の特徴はインフルエンザ菌に対する抗菌力が, CEZ, CEXよりも極めて優れ, アンピシリンに匹敵することである。ボランチアにおける本剤2gの点滴静注時血中ピーク値は57±19.16μg/ml, 血中半減期は37±1.73分, 尿中回収率は投与開始後5時間までに52.8±10.48%で, さらに連続投与による蓄積性もみられなかった。臨床的検討は呼吸器感染症16例, 尿路感染症3例, 細菌性心内膜炎2例, 敗血症1例, 肝膿瘍1例, 不明熱1例の計24例について行なった。呼吸器感染症に対する本剤の主たる投与量は慢性気管支炎1g×2・DI/日, 肺炎1～2g×2・DI/日で, 呼吸器感染症全体に対する有効率は75%であった。本剤が優れた抗菌力を示すインフルエンザ菌性呼吸器感染症4例中, 本剤の抗菌力と解離した臨床効果を呈した症例は嚢胞状気管支拡張症の1例だけであった。副作用は対象24例中1例のみにGOT, GPTの軽度上昇を認めたにすぎなかった。<BR>抗菌力および臨床的検討成績からみると, 本剤はインフルエンザ菌性呼吸器感染症をはじめとした感染症に極めて有用であると結論することができる。
Laboratory and clinical studies on cefamandole sodium were performed with following results.<BR>1. Antibacterial activity of cefamandole sodium against respiratory pathogenic bacteria isolated from sputum was measured.<BR>1. Antibacterial activity of cefamandole sodium against respiratory pathogenic bacteria isolated from sputum was measured.<BR>1) MIC values against 53 strains of<I>Haemophilus influenzae</I>ranged from 0.2 to 12.5μg/ml. Only a few strains of this organism were resistant to cefamandole sodium. Cefamandole sodium was active almost the same as ampicillin and its antibacterial activity was 32 to 64 times superior to those of CEZ and CEX.<BR>2) MIC values against 50 strains of<I>Streptococcus pneumoniae</I>, 7 strains of<I>Escherichia coli</I>and 19 strains of<I>Klebsiella pneumoniae</I>, ranged from 0.05 to 0.39μg/ml, 0.20 to 12.5μg/ml and 0.20 to 3.13μg/ml respectively.<BR>2. After intramuscular administration of cefamandole sodium 20mg/kg in rats, the tissue concentrations reached peak level at 15 minutes and they were in the following order of kidney, serum, lung and liver. One to two hours later, cefamandole was not detectable in all organs.<BR>3. Two grams of cefamandole sodium was administered intravenously to three healthy subjects over two hours. The mean values of the peak serum levels and serum half-life values were 57.00±19.16μg/ml and 37.00±1.73 minutes. Excretion rate in the urine during five hours was 52.80±10.48 percent.<BR>4. In the study on the three healthy subjects, repeated administration of 2g of cefamandole sodium had no influence on the peak serum levels, serum half-llife and urine concentration.<BR>5. Cefamandole sodium was given to 16 patients with respiratory tract infections, 3 patients with acute cystitis, 2 patients with bacterial endocarditis, one patient with sepsis and one patient with liver abscess. The dosage was 1 to 3g and the drug was administered mainly by instillation every 12 hours.<BR>In the cases with respiratory tract infections (2 cases with acute bronchitis, 8 cases with chronic bronchitis, 5 cases with acute pneumonia and 1 case with bronchiectasis), cefamandole sodium was evaluated to be “excellent” in 2 cases, “good” in 10 cases and “poor” in 4 cases. Four cases that failed to respond satisfactorily to cefamandole sodium included each case with<I>Pseudomonas aeruginosa</I>and<I>Mycoplasma pneumoniae</I>infection, one case with acute pneumonia complicated with apoplexia and one case of saccural bronchiectasis. Clinical recovery was observed in 12 (75%) in 16 patients with respiratory tract infections. In the cases with respiratory tract infection due to<I>Haemophilus influenzae</I>, clinical recovery with correlated MIC except for one case of saccural bronchiectasis.<BR>On the other hand, this antibiotic was evaluated to be “excellent” and “good” in all cases with acute cystitis, “fair” or “poor” in the two cases with bacterial endocarditis, and “good” in the each case of sepsis and liver abscess.<BR>6. As side effects S-GOT and S-GPT increased in one case, but they returned to normal by discontinuation of the antibiotic.
CHEMOTHERAPY 27(Supplement5), 321-333, 1979
Japanese Society of Chemotherapy