Nakamura T, Hashimoto I, Sawada Y, Mikami J, Yoshimoto M, Nishindai H, Nakanishi Y
Jpn J Antibiot. 1986 Sep;39(9):2355-66.
Cefsulodin (CFS), a new antipseudomonal cephalosporin, shows a potent antibacterial activity against Pseudomonas aeruginosa and some Gram-positive bacteria, whereas it shows low activity against many Gram-negative rods. Against clinical isolates of P. aeruginosa, CFS was about 10 times more active than sulbenicillin and carbenicillin, and had a similar activity to gentamicin and dibekacin. The CFS was administered by an intravenous bolus injection at a dose of 1 g to each of 14 patients operated for acute peritonitis with drainage or radical mastectomy with drainage to treat breast cancer. These cases included 3 of localized peritonitis due to perforative appendicitis, 3 of diffuse peritonitis due to perforative duodenal ulcer, 2 of panperitonitis due to intestinal obstruction and perforative sigmoid colon cancer, 4 of subacute cholangitis, localized peritonitis T-tube choledochal drainage due to choledocholithiasis, and 2 of breast cancer. Materials from drain exudate were taken at intervals with sterilized paper discs and CFS concentrations were determined by the paper disc bioassay method with P. aeruginosa NCTC 10490 as the test organism. Serum concentrations of CFS just after injection reached 135.4 +/- 66.1 micrograms/ml, and they were 2.7 +/- 1.5 micrograms/ml at 6 hours after injection. Concentrations in purulent exudates of patients with acute peritonitis increased quickly after intravenous bolus injections, and reached maximum levels relatively early after injection in cases 2 to 3 days after operation. In cases 10 to 13 days after operation, CFS levels were comparatively low and reached to peak levels at 4 to 5 hours after injection. Levels of CFS in purulent exudate tended to increase in proportion to the severity of symptoms, as did CFS levels in appendix wall. Pseudomonas spp. were not isolated in this study, but MICs of CFS were mostly around 1.56 to 3.13 micrograms/ml when clinically isolated Pseudomonas spp. were present at 10(6) cells/ml. Levels of CFS in infected exudate were higher than the above MIC values against Pseudomonas spp. Therefore, CFS were a useful drug for the chemotherapy against pseudomonal infections.
头孢磺啶（CFS）是一种新型抗假单胞菌头孢菌素，对铜绿假单胞菌和一些革兰氏阳性菌显示出强大的抗菌活性，而对许多革兰氏阴性杆菌活性较低。针对铜绿假单胞菌的临床分离株，CFS的活性比磺苄西林和羧苄西林高约10倍，与庆大霉素和地贝卡星活性相似。对14例因急性腹膜炎行引流手术或因乳腺癌行根治性乳房切除术并引流的患者，静脉推注1g剂量的CFS。这些病例包括3例因穿孔性阑尾炎导致的局限性腹膜炎、3例因十二指肠溃疡穿孔导致的弥漫性腹膜炎、2例因肠梗阻和乙状结肠穿孔癌导致的全腹膜炎、4例亚急性胆管炎、因胆总管结石导致的局限性腹膜炎经T管胆总管引流、以及2例乳腺癌。每隔一段时间用无菌纸盘采集引流渗出物样本，以铜绿假单胞菌NCTC 10490作为测试菌株，通过纸盘生物测定法测定CFS浓度。注射后即刻CFS血清浓度达到135.4±66.1微克/毫升，注射后6小时为2.7±1.5微克/毫升。急性腹膜炎患者静脉推注后，脓性渗出物中的浓度迅速升高，在术后2至3天的病例中注射后相对较早达到最高水平。在术后10至13天的病例中，CFS水平相对较低，在注射后4至5小时达到峰值水平。脓性渗出物中CFS水平往往与症状严重程度成比例增加，阑尾壁中的CFS水平也是如此。本研究中未分离出假单胞菌属，但当临床分离的假单胞菌属以10(6)个细胞/毫升存在时，CFS的最低抑菌浓度大多在1.56至3.13微克/毫升左右。感染渗出物中CFS水平高于上述针对假单胞菌属的最低抑菌浓度值。因此，CFS是治疗假单胞菌感染的一种有用药物。
