Iwai N, Taneda Y, Shibata M, Mizoguchi F, Katayama M
Jpn J Antibiot. 1984 Oct;37(10):1859-79.
Microbiological, pharmacokinetic and clinical studies on sulbactam/cefoperazone (SBT/CPZ) were carried out in the field of pediatrics. Antimicrobial activity The MIC80 of SBT/CPZ was 6.25 micrograms/ml for clinically isolated 24 strains of S. aureus (24 beta-lactamase producing strains), 0.39 micrograms/ml for 17 strains of S. pyogenes, 3.13 micrograms/ml for 24 strains of E. coli (22 beta-lactamase producing strains), 3.13 micrograms/ml for 22 strains of K. pneumoniae (22 beta-lactamase producing strains), 1.56 micrograms/ml for 22 strains of P. mirabilis and 0.20 microgram/ml for 15 strains of H. influenzae (13 beta-lactamase producing strains). In comparison with CPZ in respect to the MIC, SBT/CPZ exhibited synergistic effect on 31 strains out of 81 beta-lactamase producing strains (included 6 strains of S. aureus, 9 of E. coli, 5 of K. pneumoniae and 11 of H. influenzae) which was scarcely observed against 43 non-beta-lactamase producing strains. Absorption and excretion Serum levels and urinary excretion of SBT/CPZ were studied in 7 children aged 5 to 12 years. The mean serum concentration of SBT at 15 minutes following a single intravenous injection of 10 mg/kg of SBT/CPZ was 14.2 micrograms/ml and that of CPZ was 30.4 micrograms/ml. The mean urinary recovery rates at 6 hours following the intravenous injection were 57.8% and 18.3%, respectively. The mean serum concentrations of SBT and CPZ after 1-hour infusion of 10 mg/kg of SBT/CPZ were 10.9 micrograms/ml and 17.6 micrograms/ml, respectively. The urinary recovery rates of SBT and CPZ at 7 hours after the infusion were 100.0% and 27.7% on average, respectively. The mean serum levels of SBT and CPZ at 15 minutes after a single intravenous injection of 20 mg/kg of SBT/CPZ were 25.6 micrograms/ml and 66.0 micrograms/ml, respectively and urinary elimination until up to 6 hours were 72.5% on average for SBT and 21.1% for CPZ. Clinical study SBT/CPZ was used for the treatment of a total of 20 pediatric patients aged 1 month to 14 years to evaluate its clinical effectiveness, bacteriological efficacy and adverse effects. The clinical efficacy in 6 patients with acute pneumonia, 3 with staphylococcal scalded skin syndrome, 2 each with acute purulent tonsillitis and acute pyelonephritis, 1 each with acute purulent lymphadenitis, acute sinusitis, acute bronchitis, peritonitis and acute enteritis was judged to be excellent in 15 cases and good in 3 cases with an efficacy ratio of 100%. The clinical efficacy in 6 patients whose infections were caused by beta-lactamase producing strains was judged to be excellent in all the cases.(ABSTRACT TRUNCATED AT 400 WORDS)
在儿科领域开展了关于舒巴坦/头孢哌酮(SBT/CPZ)的微生物学、药代动力学及临床研究。抗菌活性:对于临床分离出的24株金黄色葡萄球菌(24株产β-内酰胺酶菌株),SBT/CPZ的MIC80为6.25微克/毫升;对于17株化脓性链球菌,为0.39微克/毫升;对于24株大肠杆菌(22株产β-内酰胺酶菌株),为3.13微克/毫升;对于22株肺炎克雷伯菌(22株产β-内酰胺酶菌株),为3.13微克/毫升;对于22株奇异变形杆菌,为1.56微克/毫升;对于15株流感嗜血杆菌(13株产β-内酰胺酶菌株),为0.20微克/毫升。与头孢哌酮相比,就MIC而言,SBT/CPZ对81株产β-内酰胺酶菌株中的31株(包括6株金黄色葡萄球菌、9株大肠杆菌、5株肺炎克雷伯菌和11株流感嗜血杆菌)表现出协同作用,而对43株不产β-内酰胺酶菌株几乎未观察到协同作用。吸收与排泄:对7名5至12岁儿童研究了SBT/CPZ的血清水平及尿排泄情况。单次静脉注射10毫克/千克SBT/CPZ后15分钟,SBT的平均血清浓度为14.2微克/毫升,头孢哌酮为30.4微克/毫升。静脉注射后6小时的平均尿回收率分别为57.8%和18.3%。静脉输注10毫克/千克SBT/CPZ 1小时后,SBT和头孢哌酮的平均血清浓度分别为10.9微克/毫升和17.6微克/毫升。输注后7小时SBT和头孢哌酮의尿回收率平均分别为100.0%和27.7%。单次静脉注射20毫克/千克SBT/CPZ后15分钟,SBT和头孢哌酮의平均血清水平分别为25.6微克/毫升和66.0微克/毫升,至6小时的尿排泄平均分别为72.5%(SBT)和21.1%(头孢哌酮)。临床研究:SBT/CPZ用于治疗共20例1个月至14岁的儿科患者,以评估其临床有效性、细菌学疗效及不良反应。6例急性肺炎、3例葡萄球菌烫伤样皮肤综合征、2例急性化脓性扁桃体炎和急性肾盂肾炎、1例急性化脓性淋巴结炎、急性鼻窦炎、急性支气管炎、腹膜炎和急性肠炎患者中,临床疗效判定为优15例,良3例,有效率100%。6例由产β-内酰胺酶菌株引起感染的患者,临床疗效均判定为优。(摘要截选至400字)