Nakazawa S, Sato H, Niino K, Hirama Y, Narita A, Suzuki H, Nakazawa S, Chikaoka H, Tazoe K, Irino Y, Nakada Y, Yoshihara T
Jpn J Antibiot. 1983 Apr;36(4):771-89.
Studies on T-1982 (cefbuperazone), a new cephamycin antibiotic, were carried out in the field of pediatrics, and the following results were obtained. 1. Peak MIC of T-1982 against S. pyogenes (group A) lately isolated was 0.39 micrograms/ml, and the drug was active even against highly resistant strains of macrolides, lincomycin, tetracycline and chloramphenicol. 2. Peak MICs of T-1982 were 0.78 microgram/ml against B. pertussis, 0.2 microgram/ml against E. coli and less than or equal to 0.05 microgram/ml against K. oxytoca, and the drug was also active against ampicillin-resistant bacteria. 3. Serum levels and urinary excretions of T-1982 were investigated in 6 cases. When given at a dose of 20-28 mg/kg by 1 hour intravenous drip infusion, serum concentrations of T-1982 attained the peak level of 63.5-75.9 micrograms/ml at the end of administration and sustained the level of 0.9-2.6 micrograms/ml at 6 hours, the serum half-life (T 1/2) ranging 70-82 minutes. Approximately 20-72% of the dose were excreted in the active form into urine within 6 hours. 4. Twenty-seven cases of acute pediatric infections were treated with T-1982 mainly by intravenous drip infusion, and satisfactory clinical results were obtained in all the cases of angina lacunaris, bronchitis, bronchopneumonia, pertussis, sepsis caused by Serratia and acute urinary tract infections caused by ampicillin-resistant E. coli. The efficacy rate was 96.3%. In this study the drug was administered chiefly at a daily dose of 50-70 mg/kg 2-3 times a day for 2-12 days. 5. Gram-positive cocci (S. aureus, S. pneumoniae, S. pyogenes) and Gram-negative rods (H. influenzae, H. parainfluenzae P. vulgaris, B. pertussis, S. marcescens, E. coli) were eradicated by the treatment with T-1982. 6. No noticeable side effects were observed, except for temporary increase of eosinophil in 2 cases and slight elevation of GOT in 1 case.
对新型头孢霉素抗生素T-1982(头孢布宗)进行了儿科领域的研究,获得了以下结果。1. T-1982对近期分离出的化脓性链球菌(A组)的最高MIC为0.39微克/毫升,该药物对大环内酯类、林可霉素、四环素和氯霉素的高度耐药菌株也有活性。2. T-1982对百日咳杆菌的最高MIC为0.78微克/毫升,对大肠杆菌为0.2微克/毫升,对产酸克雷伯菌小于或等于0.05微克/毫升,该药物对耐氨苄西林细菌也有活性。3. 对6例患者进行了T-1982的血清水平和尿排泄研究。以20 - 28毫克/千克的剂量通过1小时静脉滴注给药时,T-1982的血清浓度在给药结束时达到63.5 - 75.9微克/毫升的峰值水平,并在6小时时维持在0.9 - 2.6微克/毫升的水平,血清半衰期(T 1/2)为70 - 82分钟。约20 - 72%的剂量在6小时内以活性形式排泄到尿液中。4. 对27例小儿急性感染主要采用静脉滴注T-1982进行治疗,在所有咽峡炎、支气管炎、支气管肺炎、百日咳、沙雷氏菌引起的败血症以及耐氨苄西林大肠杆菌引起的急性尿路感染病例中均取得了满意的临床效果。有效率为96.3%。在本研究中,该药物主要以每日50 - 70毫克/千克的剂量,每天2 - 3次给药,持续2 - 12天。5. 通过T-1982治疗可根除革兰氏阳性球菌(金黄色葡萄球菌、肺炎链球菌、化脓性链球菌)和革兰氏阴性杆菌(流感嗜血杆菌、副流感嗜血杆菌、普通变形杆菌、百日咳杆菌、粘质沙雷氏菌、大肠杆菌)。6. 未观察到明显的副作用,仅有2例嗜酸性粒细胞暂时增加,1例谷草转氨酶轻度升高。