Sekiguchi T, Miyao M, Kokawa T, Yuasa Y, Uyama Y, Tanaka H
Jpn J Antibiot. 1982 Jan;35(1):160-70.
Laboratory and clinical studies were performed as follows on ceftizoxime (CZX), a new cephalosporin antibiotic. 1. Susceptibility of clinically isolated bacteria to CZX and cefotiam (CTM) or sulbenicillin (SBPC). Antibacterial activities of CZX and CTM were compared against S. aureus, E. coli, K. pneumoniae, E. cloacae, H. influenzae and E. aerogenes; CZX was compared with SBPC against Ps. aeruginosa. CZX and CTM were nearly equal in activity against S. aureus, but CZX was found to be more active than CTM by 1--10 tubes against E. coli, K. pneumoniae, E. cloacae, H. influenzae and E. aerogenes. Against Ps. aeruginosa, CZX and SBPC were nearly equal in activity. 2. Serum concentration and urinary recovery. Serum concentrations of CZX were measured in 6 patients given CZX for prophylactic purpose during cardiac catheterization. In 2 patients given 20 mg/kg of CZX intravenously, the average serum concentration was 38.9 micrograms/ml at 30 minutes after intravenous bolus injection. In 3 patients given 10 mg/kg of CZX by intravenous drip infusion, the peak average serum concentration was 28.1 micrograms/ml at the end of infusion. Urinary recovery in 2 patients tested was 81.1% and 92.5% until 6--7 hours after intravenous bolus injection. 3. Clinical efficacy. CZX was given intravenously to 24 patients in doses of 30--111 mg/kg (57.1 mg/kg on an average) t.i.d. or q.i.d. for 3--16 days (5.5 days on an average): 1 with lacunar tonsillitis, 4 with acute bronchitis, 12 with pneumonia, 2 with enterocolitis, 2 with soft tissue infection, 2 with lymphadenitis and 1 with UTI. The overall efficacy rate was 95.8%, i.e., efficacy was excellent in 10 (41.7%), good in 13 (54.2%), and poor in 1 (4.2%). Bacteriological efficacy was excellent, i.e. 21 of the 23 strains disappeared. One patient had mild and transient diarrhea, but no other laboratory abnormalities were observed during treatment. The above results suggest that CZX is 1 of the most useful antibiotics for treating pediatric infections, especially due to Gram negative bacteria.
对新型头孢菌素抗生素头孢唑肟（CZX）进行了如下实验室和临床研究。1. 临床分离细菌对CZX与头孢替安（CTM）或磺苄西林（SBPC）的敏感性。比较了CZX和CTM对金黄色葡萄球菌、大肠杆菌、肺炎克雷伯菌、阴沟肠杆菌、流感嗜血杆菌和气杆菌的抗菌活性；比较了CZX与SBPC对铜绿假单胞菌的抗菌活性。CZX和CTM对金黄色葡萄球菌的活性几乎相同，但发现CZX对大肠杆菌、肺炎克雷伯菌、阴沟肠杆菌、流感嗜血杆菌和气杆菌的活性比CTM高1 - 10个稀释度。对于铜绿假单胞菌，CZX和SBPC的活性几乎相同。2. 血清浓度和尿回收率。在6例因心脏导管插入术接受CZX预防性治疗的患者中测量了CZX的血清浓度。在2例静脉注射20mg/kg CZX的患者中，静脉推注后30分钟时平均血清浓度为38.9μg/ml。在3例静脉滴注10mg/kg CZX的患者中，输注结束时平均血清峰值浓度为28.1μg/ml。在2例受试患者中，静脉推注后6 - 7小时内尿回收率分别为81.1%和92.5%。3. 临床疗效。对24例患者静脉注射CZX，剂量为30 - 111mg/kg（平均57.1mg/kg），每日3次或4次，持续3 - 16天（平均5.5天）：1例患有陷窝性扁桃体炎，4例患有急性支气管炎，12例患有肺炎，2例患有小肠结肠炎，2例患有软组织感染，2例患有淋巴结炎，1例患有尿路感染。总有效率为95.8%，即疗效优秀者10例（41.7%），良好者13例（54.2%），差者1例（4.2%）。细菌学疗效优秀，即23株菌株中有21株消失。1例患者出现轻度短暂腹泻，但治疗期间未观察到其他实验室异常。上述结果表明，CZX是治疗儿科感染尤其是革兰氏阴性菌感染最有用的抗生素之一。
