Kazuoka K, Shimizu S, Kawamura Y, Kamiya H, Sakurai M
Jpn J Antibiot. 1983 Apr;36(4):826-37.
T-1982 (cefbuperazone), a new injectable cephamycin antibiotic, was studied for its antibacterial activity, concentration in serum and urine, penetration into cerebrospinal fluid (CSF) as well as clinical application. The following results were obtained. 1. Antibacterial activity: The susceptibilities of clinically isolated K. pneumoniae, E. coli and E. cloacae to T-1982 were superior to those of CEZ CMZ, and ABPC. T-1982 seemed to be useful for various infections due to Gram-negative rods. 2. Concentration in serum and urine: Subjects were 10 children with congenital heart failure but no abnormal renal and liver functions. T-1982 was given intravenously to 3 groups at 200 mg/kg by one shot (4 cases), 20 mg/kg by 1 hour drip infusion (3 cases) and 10 mg/kg by 1 hour drip infusion (3 cases). The half-lives were 60, 78 and 85 minutes, respectively. 3. Penetration into cerebrospinal fluid: Three children with malignant tumor were injected 20 mg/kg intravenously. A small amount of T-1982 was penetrated into CSF. 4. Clinical efficacy: T-1982 was administered daily 40-116 mg/kg t.i.d. or q.i.d. for 2-14 days to 17 children comprising 1 bronchopneumonia, 1 bronchitis, 4 tonsillitis, 1 lymphadenitis, 1 sepsis, 1 pharyngitis, 1 impetigo, 1 acute sinusitis and 6 pyelonephritis. Clinical efficacy was excellent in 10, good in 2, fair and poor in 3, and the efficacy rate was 70.6%. Bacteriological effect was as follows; eradicated in 9 cases and unknown in 8 cases. As side effect, GOT and GPT elevations unrelated to the drug were observed in 2 cases. Other abnormal findings were not found. T-1982 seems to be safe antibiotic in the field of pediatrics.
T - 1982(头孢布宗)是一种新型注射用头孢霉素类抗生素,对其抗菌活性、血清和尿液中的浓度、脑脊液(CSF)穿透率以及临床应用进行了研究。获得了以下结果。1. 抗菌活性:临床分离的肺炎克雷伯菌、大肠杆菌和阴沟肠杆菌对T - 1982的敏感性优于头孢唑林(CEZ)、头孢美唑(CMZ)和氨苄青霉素(ABPC)。T - 1982似乎对革兰氏阴性杆菌引起的各种感染有效。2. 血清和尿液中的浓度:受试者为10名先天性心力衰竭儿童,但肝肾功能无异常。将T - 1982分别以200mg/kg单次静脉注射(4例)、20mg/kg 1小时静脉滴注(3例)和10mg/kg 1小时静脉滴注(3例)的方式给予3组儿童。半衰期分别为60、78和85分钟。3. 脑脊液穿透率:3名患有恶性肿瘤的儿童静脉注射20mg/kg。少量T - 1982穿透进入脑脊液。4. 临床疗效:对17名儿童每日给予T - 1982 40 - 116mg/kg,分3次或4次给药,疗程2 - 14天,其中包括1例支气管肺炎、1例支气管炎、4例扁桃体炎、1例淋巴结炎、1例败血症、1例咽炎、1例脓疱病、1例急性鼻窦炎和6例肾盂肾炎。临床疗效优者10例,良者2例,中者和差者3例,有效率为70.6%。细菌学疗效如下:9例根除,8例不明。作为副作用,2例观察到与药物无关的谷草转氨酶(GOT)和谷丙转氨酶(GPT)升高。未发现其他异常。T - 1982在儿科领域似乎是一种安全的抗生素。