Kager L, Liljeqvist L, Malmborg A S, Nord C E, Pieper R
Antimicrob Agents Chemother. 1982 Aug;22(2):208-12. doi: 10.1128/AAC.22.2.208.
The influence of a combination of ampicillin and a beta-lactamase inhibitor, sulbactam, on colonic bacterial flora was studied in patients undergoing colorectal surgery. Drug concentrations were determined in serum, intestinal mucosa, and feces. The results of the drug concentrations were correlated with changes in the numbers of aerobic and anaerobic bacterial bowel flora. Ampicillin and sulbactam were given intravenously to 21 patients in 500-mg doses of each drug every 8 h for 2 days. The first dose was given when anesthesia was begun. The concentrations of ampicillin in serum were significantly higher (0.01 greater than P greater than 0.001) than those of sulbactam. In contrast, at all time intervals, the concentrations of sulbactam in intestinal mucosa were significantly higher than those of ampicillin (0.05 greater than P greater than 0.01). The serum half-life of the two drugs was the same at 2.2 h. After one dose of the antibiotics, sulbactam was detectable in the feces of four patients, and ampicillin was detectable in the feces of 11 patients. During the 2 days of ampicillin and sulbactam prophylaxis, no measurable decrease occurred in the anaerobic flora of the bowel; a mean decrease of 3 logs occurred in the anaerobic bowel flora. The results of this study show that ampicillin and sulbactam prophylaxis had a greater effect on the anaerobic bowel flora than on the aerobic bowel flora. In light of the in vitro spectrum of ampicillin and sulbactam activity, it was surprising that bowel aerobic flora was unchanged.
在接受结直肠手术的患者中,研究了氨苄西林与β-内酰胺酶抑制剂舒巴坦联合使用对结肠细菌菌群的影响。测定了血清、肠黏膜和粪便中的药物浓度。将药物浓度结果与需氧和厌氧肠道细菌菌群数量的变化进行关联分析。对21例患者静脉给予氨苄西林和舒巴坦,每种药物剂量为500mg,每8小时一次,共给药2天。在开始麻醉时给予首剂。血清中氨苄西林的浓度显著高于舒巴坦(0.01>P>0.001)。相反,在所有时间间隔,肠黏膜中舒巴坦的浓度均显著高于氨苄西林(0.05>P>0.01)。两种药物的血清半衰期相同,均为2.2小时。一剂抗生素后,4例患者的粪便中可检测到舒巴坦,11例患者的粪便中可检测到氨苄西林。在进行氨苄西林和舒巴坦预防的2天内,肠道厌氧菌数量没有出现可测量的减少;肠道厌氧菌数量平均减少了3个对数级。本研究结果表明,氨苄西林和舒巴坦预防对厌氧肠道菌群的影响大于对需氧肠道菌群的影响。鉴于氨苄西林和舒巴坦的体外活性谱,肠道需氧菌群未发生变化这一点令人惊讶。