Hirasawa S, Abe H, Bekki E, Hashimoto I, Sawada Y, Nakamura T, Mikami J, Watanabe Y
Jpn J Antibiot. 1980 Dec;33(12):1294-300.
A new antibiotic drug of cephalosporin, with marked resistance to beta-lactamase, cefoperazone (CPZ) for parenteral use was used in 10 patients with acute cholecystitis or cholangitis with cholelithiasis. CPZ was given by drip intravenous injection at a daily dose of 1 to 4 g. Clinical response was excellent in 1 case, good in 7 cases, fair in 2 cases and poor was none. Clinical adverse effect was not recognized. And CPZ in a dose of 1 g was given intravenously during the operation to 6 of those patients. Tissue specimens of different sites were taken from removed organs. The materials of A-bile and B-bile were subsequently taken at intervals. Determination of CPZ concentration was performed according to paper disk method with Micrococcus luteus ATCC 9341 strain. CPZ concentrations in the A-bile increased quickly soon after injection, and reached high level peak at 30-min. to 1 hour, then they were very slow decline. CPZ was observed in the B-bile through the gallbladder wall, and reached high level concentration comparative quickly after intravenous injection. CPZ concentration in the gallbladder wall, was directly proportional to the degree of pathological changes of inflammation. On the CPZ concentration in patients with acute cholecystitis, the concentration in A-bile, B-bile and gallbladder wall were observed extremely higher than the MIC or CPZ for Escherichia coli. CPZ therefore will be a very useful drug when used for chemotherapy of biliary tract infection.
一种新型头孢菌素类抗生素药物头孢哌酮(CPZ),对β-内酰胺酶具有显著抗性,用于10例急性胆囊炎或胆石症合并胆管炎患者的肠外给药。CPZ通过静脉滴注给药,每日剂量为1至4克。临床反应优1例,良7例,中2例,差0例。未发现临床不良反应。其中6例患者在手术期间静脉注射1克CPZ。从切除的器官中采集不同部位的组织标本。随后定期采集A胆汁和B胆汁样本。采用金黄色葡萄球菌ATCC 9341菌株纸片法测定CPZ浓度。注射后A胆汁中CPZ浓度迅速升高,在30分钟至1小时达到高水平峰值,然后下降缓慢。通过胆囊壁在B胆汁中观察到CPZ,静脉注射后较快达到高浓度。胆囊壁中CPZ浓度与炎症病理变化程度成正比。在急性胆囊炎患者的CPZ浓度方面,观察到A胆汁、B胆汁和胆囊壁中的浓度远高于大肠杆菌对CPZ的最低抑菌浓度(MIC)。因此,CPZ用于胆道感染化疗时将是一种非常有用的药物。