Niinou K, Sato H
Department of Pediatrics, Oguchi Higashi General Hospital.
Jpn J Antibiot. 1993 Nov;46(11):978-90.
Pharmacokinetic and clinical studies on S-1108, a new oral cephem antibiotic, were performed in pediatric infections and the following results were obtained. 1. Pharmacokinetics studies Pharmacokinetics of S-1108 was studied in 4 children (3 y 7 m-11 y 1 m) using doses of 2 mg/kg (n = 2) and 4 mg/kg (n = 2). The average peak plasma level was 0.88 microgram/ml at 2 hours after administration of 2 mg/kg and 2.00 micrograms/ml at 3 hours after administration of 4 mg/kg, and plasma half-lives were 1.45 and 0.96 hours, respectively. Average cumulative urinary recovery rates at 0-6 hours were 30.0 and 34.8%, respectively. 2. Clinical studies S-1108 was administered to 32 patients with various infectious diseases (6 with acute tonsillitis, 2 each with pertussis and acute bronchitis, 3 with pneumonia, 4 with scarlet fever, 5 with impetigo contagiosa, 6 with acute urinary infection and 1 each with subcutaneous abscess, impetigo, vulvitis and urethritis) at daily doses between 6-12 mg/kg/day, t.i.d., for 5-12 days. Clinical responses were excellent in 17 patients, good in 13, and poor in 2, and the efficacy rate was 93.8%. Bacteria were identified and 33 strains of 12 species were found. The eradication rate was 93.9%. No side effects were observed in 43 patients. Abnormal laboratory test values were observed in 2 patients, 1 with elevation of eosin. and the other with elevations of GOT and GPT. The results suggest that S-1108 may be a very useful and safe drug for the treatment of pediatric infections.
对新型口服头孢菌素类抗生素S - 1108进行了儿科感染方面的药代动力学和临床研究,结果如下。1. 药代动力学研究 在4名儿童(3岁7个月至11岁1个月)中进行了S - 1108的药代动力学研究,给药剂量分别为2 mg/kg(n = 2)和4 mg/kg(n = 2)。给予2 mg/kg剂量后2小时的平均血浆峰浓度为0.88微克/毫升,给予4 mg/kg剂量后3小时的平均血浆峰浓度为2.00微克/毫升,血浆半衰期分别为1.45小时和0.96小时。0 - 6小时的平均累积尿回收率分别为30.0%和34.8%。2. 临床研究 对32例患有各种传染病的患者(6例急性扁桃体炎、2例百日咳和急性支气管炎各2例、3例肺炎、4例猩红热、5例脓疱疮、6例急性尿路感染以及1例皮下脓肿、脓疱病、外阴炎和尿道炎各1例)给予S - 1108,日剂量为6 - 12 mg/kg/天,分3次给药,持续5 - 12天。临床反应:17例优秀,13例良好,2例不佳,有效率为93.8%。鉴定出细菌,共发现12个菌种的33株菌株。根除率为93.9%。43例患者未观察到副作用。2例患者实验室检查值异常,1例嗜酸性粒细胞升高,另1例谷草转氨酶和谷丙转氨酶升高。结果表明,S - 1108可能是治疗儿科感染非常有用且安全的药物。