Iwai N, Sasaki A, Taneda Y, Inokuma K
Jpn J Antibiot. 1981 Jun;34(6):1002-18.
Studies on the antibacterial activity, absorption and excretion and also clinical investigation in the field of pediatrics have been carried out with cefotiam (SCE-963, CTM), a new cephalosporin antibiotic. 1) The MICs of CTM against the following clinical isolates were measured and compared with those of CEZ: S. aureus (81 strains), E. coli (27) and K. pneumoniae (27), with CTM being inferior by 1 tube in S. aureus, being superior by 2 to 3 tubes in E. coli and by about 2 - 3 tubes in K. pneumoniae. 2) Absorption and excretion. After intravenous one shot injection at dose levels of 10 mg/kg and 20 mg/kg, the peak in the serum concentration was shown in the 15-minute value with 18.1 and 36.6 mcg/ml for 10 mg/kg and 20 mg/kg, respectively. The half-life in ;the serum was 1.14 and 0.61 hours, respectively. In the case of 1-hour intravenous drip infusion at a dose level of 10 mg/kg, it was 14.3 mcg/ml, with 0.98-hour half-life in the serum. The recovery rates from the urine within 0 to 6 hours were 50.6% and 66.2% in the case of intravenous one shot injection at dose levels of 10 mg/kg and 20 mg/kg, respectively, with 71.1% in the case of the 1-hour intravenous drip infusion. 3) Two to 3 hours after intravenous one shot injection of CTM in H. influenzae-meningitis every 4 hours at a dose level of 62.5 mg/kg at one time, the cerebrospinal fluid concentration of CTM was only 2.12 to 10.0 mcg/ml, and this fact suggests that CTM is a useful cephalosporin for treating purulent meningitis. 4) CTM was administered in 19 clinical cases, with the results being: excellent in 4 out of 4 cases of bronchitis; excellent in 5 and good in 1 out of 6 cases of pneumonia; excellent in 3 cases of pyelitis; good in purulent parotitis, purulent meningitis and bacterial pericarditis; and excellent in peritonsillar abscess, purulent osteomyelitis and staphylococcal scalded skin syndrome (S.S.S.S.). No side effects have been observed in all cases. As for abnormal laboratory findings, 3 cases of eosinophilia were seen.
已对新型头孢菌素抗生素头孢替安(SCE - 963,CTM)进行了抗菌活性、吸收与排泄研究以及儿科领域的临床研究。1)测定了CTM对以下临床分离菌株的最低抑菌浓度(MIC),并与头孢唑林(CEZ)的进行比较:金黄色葡萄球菌(81株)、大肠杆菌(27株)和肺炎克雷伯菌(27株),结果显示CTM对金黄色葡萄球菌的MIC比CEZ低1管,对大肠杆菌的MIC比CEZ高2至3管,对肺炎克雷伯菌的MIC比CEZ高约2 - 3管。2)吸收与排泄。静脉注射剂量为10mg/kg和20mg/kg后,血清浓度峰值出现在15分钟时,10mg/kg剂量组为18.1mcg/ml,20mg/kg剂量组为36.6mcg/ml。血清半衰期分别为1.14小时和0.61小时。静脉滴注1小时、剂量为10mg/kg时,血清浓度为14.3mcg/ml,血清半衰期为0.98小时。静脉注射剂量为10mg/kg和20mg/kg时,0至6小时尿液回收率分别为50.6%和66.2%,静脉滴注1小时时为71.1%。3)在流感嗜血杆菌性脑膜炎患者中,一次静脉注射CTM 62.5mg/kg,每4小时一次,注射后2至3小时,脑脊液中CTM浓度仅为2.12至10.0mcg/ml,这表明CTM是治疗化脓性脑膜炎的一种有效头孢菌素。4)对19例临床病例使用了CTM,结果如下:4例支气管炎患者中4例疗效极佳;6例肺炎患者中5例疗效极佳,1例良好;3例肾盂炎患者疗效极佳;化脓性腮腺炎、化脓性脑膜炎和细菌性心包炎患者疗效良好;扁桃体周围脓肿、化脓性骨髓炎和葡萄球菌烫伤样皮肤综合征(S.S.S.S.)患者疗效极佳。所有病例均未观察到副作用。关于实验室检查异常,有3例出现嗜酸性粒细胞增多。