Itabashi T, Kawamura S, Sugita R, Fujimaki Y, Deguchi K, Fukayama S, Yokota N, Tanaka S, Nishimura Y, Yoshihara H
Jpn J Antibiot. 1986 Aug;39(8):1975-80.
We studied the concentration of ampicillin (ABPC) into middle ear effusions after administration of bacampicillin (BAPC). Nine patients with acute purulent otitis media were given orally single doses of the drug at a level of 10 mg/kg, and concentrations of ABPC which is the active antibiotic metabolite of BAPC were determined in middle ear effusions periodically after the administration. Bacteria present in effusions were identified, and their ability to produce beta-lactamase was also determined. ABPC concentrations in middle ear effusions were inversely related to the ability of bacteria detected from the intratympanic cavity to produce beta-lactamase. ABPC concentrations in middle ear effusions from which only beta-lactamase negative organisms were detected were higher by 5.2- and 2.3- fold at 60 and 120 minutes after the administration of BAPC, respectively, than those in effusions from which beta-lactamase positive organisms were detected. ABPC concentrations achieved in middle ear effusions in cases where only beta-lactamase negative organisms were detected exceeded MIC80's of the drug against main causative bacteria of acute purulent otitis media such as Streptococcus pneumoniae, Streptococcus pyogenes, and Haemophilus influenzae. Because only 10% or less of these species produces beta-lactamase, BAPC appears to be one of the highly effective drugs in the treatment of this disease.
我们研究了服用巴氨西林(BAPC)后中耳积液中氨苄西林(ABPC)的浓度。9例急性化脓性中耳炎患者口服单剂量10mg/kg的该药物,并在给药后定期测定中耳积液中作为BAPC活性抗生素代谢物的ABPC浓度。鉴定积液中存在的细菌,并测定其产生β-内酰胺酶的能力。中耳积液中的ABPC浓度与从鼓室内检测到的细菌产生β-内酰胺酶的能力呈负相关。在仅检测到β-内酰胺酶阴性菌的中耳积液中,给药后60分钟和120分钟时的ABPC浓度分别比检测到β-内酰胺酶阳性菌的积液中的浓度高5.2倍和2.3倍。在仅检测到β-内酰胺酶阴性菌的病例中,中耳积液中达到的ABPC浓度超过了该药物对急性化脓性中耳炎主要致病菌如肺炎链球菌、化脓性链球菌和流感嗜血杆菌的MIC80。由于这些菌种中只有10%或更少产生β-内酰胺酶,BAPC似乎是治疗这种疾病的高效药物之一。