Moorthi K, Fleckenstein G, Nies B
Krankenhaus Neu-Mariahilf, Göttingen, FRG.
Methods Find Exp Clin Pharmacol. 1990 May;12(4):287-90.
Cefixime is a new oral cephalosporin antibiotic with improved activity against Gram-negative pathogens comparable to the parenteral third generation cephalosporins, high beta-lactamase stability and a long elimination half-life of about 3 h. 15 patients undergoing cholecystectomy received 2 x 200 mg/day cefixime for two days before surgery. The last application was administered 13-17 h preoperatively. Intraoperatively, the mean biliary level of cefexime was 199.3 micrograms/ml (8.8 micrograms/ml-1163.8 micrograms/ml). The mean level in gallbladder wall was 25.02 micrograms/g (0.68 micrograms/g-61.20 micrograms/g). Serum samples were taken simultaneously. Despite relevant concentrations in bile and gallbladder wall, no cefixime could be detected in the serum samples of two patients. The other 13 patients, however, showed relevant serum levels between 0.28 micrograms/ml and 2.98 micrograms/ml (mean 1.01 micrograms/ml). Side effects as well as an influence on laboratory parameters were not seen. After administration of cefixime in bile and gallbladder tissue high antibiotic levels were achieved, even 13-17 hours after the last application.
头孢克肟是一种新型口服头孢菌素抗生素,对革兰氏阴性病原体的活性有所提高,可与胃肠外第三代头孢菌素相媲美,具有较高的β-内酰胺酶稳定性,消除半衰期约为3小时。15例接受胆囊切除术的患者在手术前两日每日服用2次,每次200mg头孢克肟。最后一次用药在术前13 - 17小时进行。术中,头孢克肟的平均胆汁浓度为199.3微克/毫升(8.8微克/毫升 - 1163.8微克/毫升)。胆囊壁中的平均浓度为25.02微克/克(0.68微克/克 - 61.20微克/克)。同时采集血清样本。尽管胆汁和胆囊壁中有相应浓度,但在两名患者的血清样本中未检测到头孢克肟。然而,其他13例患者的血清水平在0.28微克/毫升至2.98微克/毫升之间(平均1.01微克/毫升)。未观察到副作用以及对实验室参数的影响。在胆汁和胆囊组织中给予头孢克肟后,即使在最后一次用药13 - 17小时后仍能达到较高的抗生素浓度。