Kusumoto Y, Akita H, Sato Y, Iwata S, Takeuchi Y, Abe T, Sunakawa K, Yokota T
Department of Pediatrics, Social Insurance Saitama Central Hospital.
Jpn J Antibiot. 1994 Jul;47(7):921-31.
Bacteriological and clinical studies in the pediatric field have been performed on biapenem (L-627), a newly-developed carbapenem antibiotic, and the following results were obtained. 1. In the pharmacokinetic study, the plasma concentration of L-627 showed dose-dependant change: Cmax was 14.6 micrograms/ml and AUC was 15.4 micrograms.hr/ml with the administration of 6 mg/kg, while Cmax was 49.2 micrograms/ml and AUC was 60.1 micrograms.hr/ml with the administration of 12 mg/kg. After the administration of 6 mg/kg, the urinary concentration reached maximum within 2 hours and the cumulative urinary excretion rate in the first 6 hours was 49.4%. 2. Antibacterial activities of L-627 against 27 strains of clinical isolates were determined. MICs of L-627 against such Gram-positive cocci as Staphylococcus aureus, Streptococcus pneumoniae and Streptococcus pyogenes were sufficiently low, and those against such Gram-negative rods as Haemophilus influenzae, Escherichia coli and Bordetella pertussis were satisfactory and as low as those of imipenem or ceftazidime. 3. Clinical efficacies of L-627 were evaluated in 36 cases of bacterial infections. The overall efficacy rate was 100%, and excellent responses in 26 cases and good in 10 cases were obtained. As for bacteriological efficacies, all strains except 1 of B. pertussis were eradicated and a high eradication rate of 96.6% was obtained. 4. No side effects were observed in 37 evaluated cases. As abnormal laboratory test results, eosinophilia was noted in 2 cases (5.4%), but they returned to normal values rapidly after the drug was discontinued. From these results, it has been concluded that L-627 is a safe and effective drug to be used in treatment of pediatric infectious diseases.
对新开发的碳青霉烯类抗生素比阿培南（L-627）进行了儿科领域的细菌学和临床研究，获得了以下结果。1. 在药代动力学研究中，L-627的血浆浓度呈剂量依赖性变化：给予6mg/kg时，Cmax为14.6μg/ml，AUC为15.4μg·hr/ml；给予12mg/kg时，Cmax为49.2μg/ml，AUC为60.1μg·hr/ml。给予6mg/kg后，尿浓度在2小时内达到最高，前6小时的累积尿排泄率为49.4%。2. 测定了L-627对27株临床分离株的抗菌活性。L-627对金黄色葡萄球菌、肺炎链球菌和化脓性链球菌等革兰氏阳性球菌的MICs足够低，对流感嗜血杆菌、大肠杆菌和百日咳博德特氏菌等革兰氏阴性杆菌的MICs令人满意，且与亚胺培南或头孢他啶的MICs一样低。3. 对36例细菌感染病例评估了L-627的临床疗效。总有效率为100%，26例为优效反应，10例为良好反应。在细菌学疗效方面，除1株百日咳博德特氏菌外，所有菌株均被根除，根除率高达96.6%。4. 在37例评估病例中未观察到副作用。作为异常的实验室检查结果，2例（5.4%）出现嗜酸性粒细胞增多，但停药后迅速恢复正常。从这些结果得出结论，L-627是一种用于治疗儿科传染病的安全有效的药物。
