Yamaguchi H, Nishikawa K, Ogawa A, Kuno K, Kondo K
Jpn J Antibiot. 1980 Aug;33(8):841-51.
As a result of conducting experimental and clinical tests with the newly developed cephalosporin, cefoperazone (CPZ), the following conclusions were obtained: (1) When tested against 10 strains of Staphylococcus aureus and 16 strains of Staphylococcus epidermidis, the antibacterial activity of CPZ was found to be weaker than that of CEZ. Against 5 strains of A-beta-Streptococcus and 4 strains of Streptococcus pneumoniae, both CPZ and CEZ exhibited similar excellent antibacterial activity. CPZ was effective against 18 strains of Escherichia coli though its activity was influenced by the amount of inoculated bacteria present. Against 15 strains of Haemophilus influenzae and 10 strains of Haemophilus parahaemolyticus, CPZ was found to be more effective than CEZ though several high-resistant strains were noted. CPZ also showed more excellent antibacterial activity than CEZ against 4 strains of Haemophilus parainfluenzae, 5 strains of Klebsiella pneumoniae, 8 strains of Salmonella sp., 4 strains of Pseudomonas aeruginosa and 4 strains of Proteus sp. (2) The mean half-life in the blood following intravenous injections of 25 mg/kg and 10 mg/kg of CPZ to three children was 70 minutes. (3) One hour after intravenous injection of 25 mg/kg of CPZ to 3 cases of aseptic meningitis, drug concentration in the cerebrospinal fluid (CSF) was 1.20 mcg/ml, less than 0.39 mcg/ml and 1.55 mcg/ml. In one case, the CSF/serum ratio was 2.7%. (4) The average recovery rate in the urine of children who had received intravenous administrations of 25 mg/kg (3 children) and 10 mg/kg (1 child) was 17.8% between 0 and 6 hours. (5) Eighteen pediatric patients received CPZ in doses ranging from 48 to 170 mg/kg divided three-four times a day. They were RTI in 7, URI in 5, UTI in 5, SSSS in 1 and enteritis in 1 children. The clinical effectiveness of CPZ was judged to be remarkedly effective in 11 children, effective in 5 children and ineffective in 3 children, with an overall effective rate of 84.2%. One patient of tonsillitis combined sinusitis was considered 2 cases. The three cases in which the drug was found to e ineffective were 2 cases of pyothorax and 1 case of sinusitis. (6) Side effects were 1 case of eosinophilia, 2 cases of elevation of GOT and GPT, and 1 case of mild elevation of GOT. All were considered to be minor.
通过对新开发的头孢菌素头孢哌酮(CPZ)进行实验和临床试验,得出以下结论:(1)在对10株金黄色葡萄球菌和16株表皮葡萄球菌进行测试时,发现CPZ的抗菌活性比头孢乙腈(CEZ)弱。对于5株A组β溶血性链球菌和4株肺炎链球菌,CPZ和CEZ均表现出相似的优异抗菌活性。CPZ对18株大肠杆菌有效,但其活性受接种菌量的影响。对于15株流感嗜血杆菌和10株副溶血性嗜血杆菌,尽管发现了几株高耐药菌株,但CPZ比CEZ更有效。在4株副流感嗜血杆菌、5株肺炎克雷伯菌、8株沙门氏菌、4株铜绿假单胞菌和4株变形杆菌中,CPZ也比CEZ表现出更优异的抗菌活性。(2)对三名儿童静脉注射25mg/kg和10mg/kg的CPZ后,血液中的平均半衰期为70分钟。(3)对3例无菌性脑膜炎患者静脉注射25mg/kg的CPZ 1小时后,脑脊液(CSF)中的药物浓度分别为1.20mcg/ml、低于0.39mcg/ml和1.55mcg/ml。在1例患者中,脑脊液/血清比值为2.7%。(4)接受25mg/kg(3名儿童)和10mg/kg(1名儿童)静脉给药的儿童在0至6小时内尿液中的平均回收率为17.8%。(5)18名儿科患者接受了CPZ治疗,剂量为48至170mg/kg,每日分三至四次给药。其中7例为呼吸道感染(RTI),5例为上呼吸道感染(URI),5例为泌尿系统感染(UTI),1例为葡萄球菌烫伤样皮肤综合征(SSSS),1例为肠炎。CPZ的临床疗效判定为显著有效11例,有效5例,无效3例,总有效率为84.2%。1例扁桃体炎合并鼻窦炎患者计为2例。发现药物无效的3例患者为2例脓胸和1例鼻窦炎。(6)副作用为1例嗜酸性粒细胞增多、2例谷草转氨酶(GOT)和谷丙转氨酶(GPT)升高以及1例GOT轻度升高。所有这些均被认为是轻微的。