Tsuburaya H, Watanabe I, Endo S, Oikawa M
Jpn J Antibiot. 1985 Jan;38(1):31-40.
Basic and clinical studies in 37 patients with biliary tract disease on comparison between cefmenoxime (CMX) and cefotiam (CTM) were studied and the following results were obtained. In vitro antibacterial activities of CMX and CTM against 25 strains (15 organisms) isolated from bile of patients with biliary tract disease were stronger than that of cefazolin (CEZ). In cholecystectomized patients, CMX (2 g) or CTM (2 g) was injected intravenously, followed by determination of concentration in bile and gallbladder tissue about 2 hours after administration. In CMX administration, the mean concentration in gallbladder bile was 812.1 micrograms/ml, and the mean concentration in duct bile was 1,050.6 micrograms/ml, and the mean concentration in gallbladder tissue was 100.7 micrograms/g. In CTM administration, the mean values were, 1,092.5 micrograms/ml, 1,287.8 micrograms/ml, 28.5 micrograms/g, respectively. The concentration of CMX and CTM were almost similarly. The bile concentration of CMX (i.v.) was compared with CTM (i.v.) by cross-over method in cases of T-tube drainage. The peak bile concentrations of CMX and CTM were as high as 172.4 micrograms/ml and 182.2 micrograms/ml, respectively, 1 approximately 2 hours after 2 g intravenous administrations. Furthermore, the concentration of them were highly gained, 16.1 micrograms/ml of CMX and 33.8 micrograms/ml of CTM, even at 5 approximately 6 hours. In choledochostomized patients, CMX (4 g/day) was injected intravenously, followed by determination of concentration in intraperitoneal exudate. The mean concentration of CMX was 15.3 micrograms/ml on the first day after the operation, and 6.0 micrograms/ml even on the third day after the operation. Those results suggest that the high antibacterial activity of CMX against organism in bile and, the high penetration of CMX to bile, gallbladder tissue and intraperitoneal exudate will promise its important role in treatment of biliary tract infections.
对37例胆道疾病患者进行了头孢甲肟（CMX）和头孢替安（CTM）的基础和临床研究，获得了以下结果。CMX和CTM对从胆道疾病患者胆汁中分离出的25株菌株（15种微生物）的体外抗菌活性强于头孢唑林（CEZ）。在胆囊切除患者中，静脉注射CMX（2g）或CTM（2g），给药后约2小时测定胆汁和胆囊组织中的浓度。在给予CMX时，胆囊胆汁中的平均浓度为812.1微克/毫升，胆管胆汁中的平均浓度为1050.6微克/毫升，胆囊组织中的平均浓度为100.7微克/克。在给予CTM时，平均值分别为1092.5微克/毫升、1287.8微克/毫升、28.5微克/克。CMX和CTM的浓度几乎相似。在T管引流病例中，采用交叉法比较了CMX（静脉注射）和CTM（静脉注射）的胆汁浓度。静脉注射2g后约1至2小时，CMX和CTM的胆汁峰值浓度分别高达172.4微克/毫升和182.2微克/毫升。此外，即使在5至6小时时，它们的浓度也很高，CMX为16.1微克/毫升，CTM为33.8微克/毫升。在胆总管造口患者中，静脉注射CMX（4g/天），然后测定腹腔渗出液中的浓度。术后第一天CMX的平均浓度为15.3微克/毫升，术后第三天甚至为6.0微克/毫升。这些结果表明，CMX对胆汁中微生物的高抗菌活性以及CMX对胆汁、胆囊组织和腹腔渗出液的高渗透性将使其在胆道感染治疗中发挥重要作用。
