Iwai N, Taneda Y, Sasaki A, Mizoguchi F, Nakamura H
Jpn J Antibiot. 1983 Apr;36(4):803-25.
T-1982 (cefbuperazone), a new cephamycin antibiotic, was basically and clinically studied in the field of pediatrics, and the following results were obtained. 1. The antibacterial activity of T-1982 was compared with that of CEZ, CMZ and ABPC. T-1982 was more active than the other drugs against Gram-negative bacteria, the sensitivity of E. coli (22 strains), K. pneumoniae (18 strains), P. mirabilis (19 strains), P. vulgaris (4 strains), P. morganii (5 strains) and K. oxytoca (4 strains) distributing less than 0.39, 0.1, 1.56, 0.39, 6.25 and 0.2 microgram/ml, respectively. Two of 3 strains of C. freundii were inhibited by 12.5 micrograms/ml. Against Gram-positive bacteria, the activity of T-1982 was inferior to that of the other drugs. S. pyogenes (28 strains) were inhibited by 0.78 microgram/ml or less, but the sensitivity of S. aureus (34 strains distributed 12.5-100 micrograms/ml). 2. T-1982 was administered to each 3 children at a dose of 20 mg/kg by one shot intravenous injection or 1 hour drip infusion, or at dose of 40 mg/kg by 1 hour drip infusion. The mean serum levels at 0.25, 0.5, 1, 2, 4 and 6 hours after one shot intravenous injection of 20 mg/kg were respectively 74.3, 56.3, 42.3, 17.6, 5.7 and 1.2 micrograms/ml with the mean half-life of 1.01 hours. The values were 32.9, 50.0, 73.7, 27.5, 12.4 and 4.5 micrograms/ml and 1.31 hours by intravenous drip infusion of 20 mg/kg and 50.4, 104.7, 136.3, 62.3, 18.6 and 6.9 micrograms/ml and 1.16 hours by intravenous drip infusion of 40 mg/kg. The mean urinary recovery rates within 6 hours were 47.7, 67.6 and 60.9%, respectively. 3. Treatment with T-1982 was made in 28 cases of pediatric infections; 1 case of acute bronchitis, 19 cases of acute bronchopneumonia or lobar pneumonia, 2 cases of acute purulent cervical lymphadenitis, 4 cases of acute pyelonephritis and each 1 case of subcutaneous abscess and suspected bacterial endocarditis. The clinical responses assessed in 27 cases were excellent in 21 cases, good in 5 cases and poor in 1 case, the efficacy rate being 96.3%. Bacteriologically, 2 strains of S. aureus, 3 strains of S. pneumoniae, 4 strains of H. influenzae, 2 strains of E. coli and 1 strain of P. mirabilis were eradicated. One strain of S. faecalis was reduced. No side effects were observed in any cases. Slight elevation of GOT and GPT and that of GOT were noted in each 1 case.
新型头孢霉素类抗生素T - 1982(头孢布宗)在儿科领域进行了基础和临床研究,获得了以下结果。1. 将T - 1982的抗菌活性与头孢唑啉(CEZ)、头孢孟多(CMZ)和氨苄青霉素(ABPC)进行比较。T - 1982对革兰氏阴性菌的活性比其他药物更强,对大肠杆菌(22株)、肺炎克雷伯菌(18株)、奇异变形杆菌(19株)、普通变形杆菌(4株)、摩根氏菌(5株)和产酸克雷伯菌(4株)的敏感性分别低于0.39、0.1、1.56、0.39、6.25和0.2微克/毫升。弗氏柠檬酸杆菌3株中有2株被12.5微克/毫升的浓度所抑制。对革兰氏阳性菌而言,T - 1982的活性不如其他药物。化脓性链球菌(28株)被0.78微克/毫升或更低的浓度所抑制,但金黄色葡萄球菌(34株)的敏感性分布在12.5 - 100微克/毫升之间。2. 分别对3名儿童以20毫克/千克的剂量进行单次静脉注射或1小时静脉滴注,或以40毫克/千克的剂量进行1小时静脉滴注,给予T - 1982。单次静脉注射20毫克/千克后0.25、0.5、1、2、4和6小时的平均血清浓度分别为74.3、56.3、42.3、17.6、5.7和1.2微克/毫升,平均半衰期为1.01小时。20毫克/千克静脉滴注时的值分别为32.9、50.0、73.7、27.5、12.4和4.5微克/毫升,半衰期为1.31小时;40毫克/千克静脉滴注时的值分别为50.4、104.7、136.3、62.3、18.6和6.9微克/毫升,半衰期为1.16小时。6小时内的平均尿回收率分别为47.7%、67.6%和60.9%。3. 对28例儿科感染病例使用T - 1982进行治疗;其中急性支气管炎1例,急性支气管肺炎或大叶性肺炎19例,急性化脓性颈淋巴结炎2例,急性肾盂肾炎4例,皮下脓肿和疑似细菌性心内膜炎各1例。对27例病例评估的临床反应中,21例为优,5例为良,1例为差,有效率为96.3%。细菌学方面,2株金黄色葡萄球菌、3株肺炎链球菌、4株流感嗜血杆菌、2株大肠杆菌和1株奇异变形杆菌被清除。1株粪肠球菌数量减少。所有病例均未观察到副作用。各有1例出现谷草转氨酶(GOT)和谷丙转氨酶(GPT)轻度升高以及GOT升高。