Nakazawa S, Sato H, Narita A, Matsumoto K, Suzuki H, Nakazawa S, Chikaoka H, Koido R, Kamigaki M, Nakada Y
Jpn J Antibiot. 1987 Mar;40(3):613-29.
Cefuzonam (L-105, CZON) was studied in pediatric infections. A summary of the results it as follows: For recently isolated Staphylococcus aureus strains, Peak MICs of CZON were distributed between 0.39 and 0.78 micrograms/ml showing a greater susceptibility of S. aureus to CZON than to cefoperazone (CPZ), latamoxef (LMOX), and cefmenoxime (CMX). Peak MICs of CZON for Escherichia coli were 0.10-0.20 micrograms/ml, similar to those of CPZ, LMOX, and CMX. Ampicillin (ABPC)-resistant strains were also susceptible to CZON. MICs for Salmonella were similar to those for E. coli. Peak MICs of CZON for Vibrio parahaemolyticus were 0.20-0.39 micrograms/ml. The susceptibility of the bacteria to CZON was far greater than to ABPC, and was similar to CPZ, LMOX, and CMX. With 20 mg/kg drip infusion, serum concentrations reached their peaks at the end of administration with values of 20.6-68.7 micrograms/ml, which decreased to 0.43-1.70 micrograms/ml after 2 hours. Half-lives of CZON in serum were 0.68-1.2 hours. With 50 mg/kg drip infusion, serum concentrations reached their peaks at the end of administration with levels of 69.0-82.0 micrograms/ml, and at after 2 hours 1.85-3.45 micrograms/ml. Thus, an apparent dose response was observed. Half-lives of CZON in serum were 0.63-0.99 hours. Urinary recovery rates in 6 hours were 39.9-80.5%. A total of 44 cases of 10 different types of acute pediatric infections was treated by CZON intravenous drip infusion as the main therapeutic procedure. The efficacy rate was 93.2%, and the compound was effective on purulent infections, acute urinary tract infection, etc. with pathogens such as ABPC-resistant S. aureus, E. coli, and Enterococcus faecalis. Dosage levels per day were 50 to 80 mg/kg in most cases. In infections with S. aureus (8 strains), Streptococcus pneumoniae (3 strains), E. faecalis (1 strain), Haemophilus parahaemolyticus (1 strain), Haemophilus parainfluenzae (2 strains), Haemophilus influenzae (11 strains), Bordetella pertussis (1 strain), E. coli (3 strains), a total of 30 strains, bacterial elimination was noted with an exception of 1 strain of S. aureus. The compound was used for 4 to 15 days, but side effects observed clinically were only 1 case of diarrhea and 1 case of thrombocytosis.
对头孢唑南（L - 105，CZON）进行了儿科感染方面的研究。结果总结如下：对于近期分离出的金黄色葡萄球菌菌株，CZON的峰值最低抑菌浓度（MIC）分布在0.39至0.78微克/毫升之间，表明金黄色葡萄球菌对CZON的敏感性高于头孢哌酮（CPZ）、拉氧头孢（LMOX）和头孢甲肟（CMX）。CZON对大肠杆菌的峰值MIC为0.10 - 0.20微克/毫升，与CPZ、LMOX和CMX相似。耐氨苄西林（ABPC）菌株也对CZON敏感。沙门氏菌的MIC与大肠杆菌相似。CZON对副溶血性弧菌的峰值MIC为0.20 - 0.39微克/毫升。该细菌对CZON的敏感性远高于ABPC，与CPZ、LMOX和CMX相似。以20毫克/千克静脉滴注时，血清浓度在给药结束时达到峰值，值为20.6 - 68.7微克/毫升，2小时后降至0.43 - 1.70微克/毫升。CZON在血清中的半衰期为0.68 - 1.2小时。以50毫克/千克静脉滴注时，血清浓度在给药结束时达到峰值，水平为69.0 - 82.0微克/毫升，2小时后为1.85 - 3.45微克/毫升。因此，观察到明显的剂量反应。CZON在血清中的半衰期为0.63 - 0.99小时。6小时的尿回收率为39.9 - 80.5%。共有44例10种不同类型的小儿急性感染以CZON静脉滴注作为主要治疗方法进行治疗。有效率为93.2%，该化合物对化脓性感染、急性尿路感染等由耐ABPC的金黄色葡萄球菌、大肠杆菌和粪肠球菌等病原体引起的感染有效。大多数情况下每日剂量水平为50至80毫克/千克。在感染金黄色葡萄球菌（8株）、肺炎链球菌（3株）、粪肠球菌（1株）、副溶血性嗜血杆菌（1株）、副流感嗜血杆菌（2株）、流感嗜血杆菌（11株）、百日咳博德特氏菌（1株）、大肠杆菌（3株），共30株菌株的感染中，除1株金黄色葡萄球菌外均观察到细菌清除。该化合物使用4至15天，但临床观察到的副作用仅1例腹泻和1例血小板增多症。
