Iwai N, Taneda Y, Shibata M, Mizoguchi F, Nakamura H, Katayama M
Jpn J Antibiot. 1985 Oct;38(10):2903-16.
A fundamental and clinical study of ceftizoxime (CZX) suppositories was performed in pre-school and school-age children. The average time courses of CZX serum and urinary concentrations after administration of CZX suppository 250 mg (i.e. per kg body weight doses of 8.3-10.9 mg) to 4 school-age children were as follows. Serum concentrations: 6.1 micrograms/ml at 15 minutes, 6.3 micrograms/ml at 30 minutes, 3.8 micrograms/ml at 1 hour, 1.7 microgram/ml at 2 hours, 0.5 microgram/ml at 4 hours and 0.2 microgram/ml at 6 hours with a biological half-life of 1.43 hours. Urinary concentrations: 885 micrograms/ml for 0-2 hours, 209 micrograms/ml for 2-4 hours and 112 micrograms/ml for 4-6 hours with an average 6-hour urinary recovery rate of 25.6%. The clinical and biological effectiveness and adverse reactions were studied in 11 infants and school-age children afflicted with various infections (acute purulent tonsillitis, 1; acute bronchitis, 3; acute pneumonia, 4; and UTI, 3). The clinical responsiveness was "excellent" in 8, "good" in 2, and "failure" was recorded in 1, with an overall efficacy of 90.9% inclusive of "excellent" and "good". The microbiological effectiveness of CZX suppositories on presumed pathogenic organisms comprising 4 strains of H. influenzae, 1 strain of H. parainfluenzae, and 3 strains of E. coli was satisfactory, as evidenced by the substantially high eradication rate of 87.5%. The only organism that survived CZX suppository treatment was 1 strain of H. influenzae which however was greatly decreased. The only side effect was diarrhea in 1 patient, which however did not necessitate withdrawal of the drug. The only laboratory test abnormality was GOT and GPT elevation in 1 patient which was normalized within 8 days. In conclusion, CZX suppositories were found to be efficacious and safe for treatment of bacterial infections in children.
对头孢唑肟（CZX）栓剂进行了一项针对学龄前和学龄儿童的基础与临床研究。给4名学龄儿童使用250mg CZX栓剂（即每千克体重剂量为8.3 - 10.9mg）后，CZX血清和尿液浓度的平均时间进程如下。血清浓度：15分钟时为6.1微克/毫升，30分钟时为6.3微克/毫升，1小时时为3.8微克/毫升，2小时时为1.7微克/毫升，4小时时为0.5微克/毫升，6小时时为0.2微克/毫升，生物半衰期为1.43小时。尿液浓度：0 - 2小时为885微克/毫升，2 - 4小时为209微克/毫升，4 - 6小时为112微克/毫升，6小时平均尿液回收率为25.6%。对11名患有各种感染（急性化脓性扁桃体炎1例、急性支气管炎3例、急性肺炎4例、尿路感染3例）的婴儿和学龄儿童进行了临床和生物学有效性及不良反应研究。临床反应“优秀”的有8例，“良好”的有2例，“失败”的有1例，“优秀”和“良好”的总体有效率为90.9%。CZX栓剂对包括4株流感嗜血杆菌、1株副流感嗜血杆菌和3株大肠杆菌在内的推测致病微生物的微生物学有效性令人满意，根除率高达87.5%即可证明。CZX栓剂治疗后唯一存活的菌株是1株流感嗜血杆菌，但其数量大幅减少。唯一的副作用是1例患者出现腹泻，但无需停药。唯一的实验室检查异常是1例患者谷草转氨酶和谷丙转氨酶升高，8天内恢复正常。总之，发现CZX栓剂对治疗儿童细菌感染有效且安全。
