Tajima T, Kondo Y, Negishi S, Kawashima S, Hagiwara N, Iizuka T, Kubota K, Abe T
Department of Pediatrics, School of Medicine, Teikyo University.
Jpn J Antibiot. 1994 Nov;47(11):1457-63.
Pharmacokinetic, bacteriological and clinical studies on cefozopran (CZOP) were performed in children. The results were as followed: 1. A total of 13 patients were treated with CZOP. The tested dose was 20 mg/kg (50 mg/kg in maxillary sinusitis), and the drug administered via intravenous bolus injection or 30-minute intravenous drip infusion 3 times daily, for 3-11 days. Clinical efficacies of CZOP in 13 patients with bacterial infections (11 with pneumonia, 1 with otitis media and 1 with maxillary sinusitis) were evaluated as excellent in 13 with an efficacy rate of 100%. Any adverse reactions or abnormal laboratory test results were not observed in any patients. Fourteen causative strains were found in 10 patients. Streptococcus pneumoniae in 4 cases out of 4, Streptococcus pyogenes in 1/1, Moraxella (Branhamella) catarrhalis in 3/3, Haemophilus influenzae in 4/6 were eradicated. 2. Pharmacokinetic studies. The mean serum concentration immediately after intravenous drip infusion over 30-minute of 20 mg/kg was 39.1 micrograms/ml (range: 25.6-52.5 micrograms/ml). The mean urinary recovery rate over 8 hours after administration was 49.0% (range: 45.2-51.8%). Based on the above results and the broad spectrum and great antibacterial activity of CZOP, it is considered that CZOP is a promising antibiotic usable as a single agent for the primary therapy of acute bacterial infections ranging from mild to severe in children.
对儿童进行了头孢唑兰(CZOP)的药代动力学、细菌学和临床研究。结果如下:1. 共有13例患者接受了CZOP治疗。测试剂量为20mg/kg(上颌窦炎时为50mg/kg),药物通过静脉推注或30分钟静脉滴注给药,每日3次,持续3 - 11天。评估了CZOP对13例细菌感染患者(11例肺炎、1例中耳炎和1例上颌窦炎)的临床疗效,13例均为优,有效率为100%。未观察到任何患者出现不良反应或实验室检查结果异常。10例患者中发现了14株病原菌。4株肺炎链球菌中的4例、1株化脓性链球菌中的1例、3株卡他莫拉菌(布兰汉菌)中的3例、6株流感嗜血杆菌中的4例被根除。2. 药代动力学研究。20mg/kg静脉滴注30分钟后即刻的平均血清浓度为39.1μg/ml(范围:25.6 - 52.5μg/ml)。给药后8小时的平均尿回收率为49.0%(范围:45.2 - 51.8%)。基于上述结果以及CZOP的广谱和强大抗菌活性,认为CZOP是一种有前景的抗生素,可作为单一药物用于儿童轻至重度急性细菌感染的初始治疗。