Motohiro T, Sakata Y, Nagai K, Morita J, Takagishi T, Matsuo Y, Hashimoto T, Yoshinaga Y, Hayashi M, Toyota A, Fujimoto T, Wada M, Kamizono S
Department of Pediatrics, School of Medicine, Kurume University.
Jpn J Antibiot. 1997 Dec;50(12):953-66.
Cefozopran (SCE-2787, CZOP), which is already on the market with a variety of approved indications in infectious diseases for adult patients, was administered to premature and newborn patients to evaluate the pharmacokinetics and the clinical efficacy. 1. Pharmacokinetics CZOP was intravenously administered at doses of 10.0 mg/kg, 21.4 mg/kg and 40.0 mg/kg to premature and newborn patients, and the blood concentrations and urinary excretion rate were examined. The blood CZOP concentrations were 31.7 and 65.5 micrograms/ml at 30 minutes after administration of 10.0 mg/kg and 40.0 mg/kg, respectively. The elimination half life was 1.78 hours and 2.31 hours, and the urinary recovery was 110.7% and 53.7% within 6 hours after administration, respectively. In the patient given 21.4 mg/kg, the blood CZOP concentration was 36.4 mg/kg at 1 an hour after administration and the elimination half life was 3.97 hours. The urinary recovery was 29.6% within 5 hours after administration. 2. Clinical results The clinical efficacy was evaluated in 19 patients and judged "good" or better in 13 of them with the efficacy rate or 68.4%. The bacteriological response was evaluated in 10 patients from whom Gram-positive cocci of S. aureus (6 strains), S. pneumoniae (1 strain) and E. faecalis (1 strain) and Gram-negative bacilli of H. influenzae (2 strains) and E. coli (2 strains) were isolated as possible causative organisms. With exception of 1 strain each of S aureus and H influenzae, which were not tested after the treatment with CZOP, all of these strains were found to be eradicated. 3. Adverse drug reactions (ADRs) of signs and symptoms and abnormal alterations of laboratory test values. Safety evaluation was made in 24 patients. ADRs of signs and symptoms were recognized in none of them. As abnormal alterations of laboratory test values, increased eosinophils in 3 patients, elevated GOT in one and elevated GPT in one were recognized. These results indicate that CZOP is a drug useful for treatment of infections in premature and newborn patients.
头孢唑兰（SCE - 2787，CZOP）已在市场上用于治疗成年患者的多种获批传染病适应症，此次对早产儿和新生儿患者给药以评估其药代动力学和临床疗效。1. 药代动力学 将CZOP以10.0mg/kg、21.4mg/kg和40.0mg/kg的剂量静脉注射给早产儿和新生儿患者，并检测血药浓度和尿排泄率。静脉注射10.0mg/kg和40.0mg/kg后30分钟时，血药浓度分别为31.7和65.5μg/ml。消除半衰期分别为1.78小时和2.31小时，给药后6小时内尿回收率分别为110.7%和53.7%。给予21.4mg/kg的患者，给药1小时后血药浓度为36.4mg/kg，消除半衰期为3.97小时。给药后5小时内尿回收率为29.6%。2. 临床结果 对19例患者的临床疗效进行评估，其中13例判定为“良好”或更好，有效率为68.4%。对10例患者进行了细菌学反应评估，从这些患者中分离出金黄色葡萄球菌（6株）、肺炎链球菌（1株）、粪肠球菌（1株）等革兰氏阳性球菌以及流感嗜血杆菌（2株）和大肠杆菌（2株）等革兰氏阴性杆菌作为可能的病原体。除1株金黄色葡萄球菌和1株流感嗜血杆菌在使用CZOP治疗后未进行检测外，所有这些菌株均被发现已被根除。3. 药物不良反应（ADR）的体征和症状以及实验室检查值的异常改变。对24例患者进行了安全性评估。未发现有体征和症状的ADR。作为实验室检查值的异常改变，3例患者嗜酸性粒细胞增多，1例谷草转氨酶升高，1例谷丙转氨酶升高。这些结果表明CZOP是一种可用于治疗早产儿和新生儿感染的药物。
