Ida S, Nishioka K, Takishima T, Satoh S, Kikuta Y, Ohnami K, Yamaki M, Kimura H, Kudo K, Mori S
First Department of Internal Medicine, School of Medicine, Tohoku University.
Jpn J Antibiot. 1988 Apr;41(4):415-26.
Seventy five patients with respiratory infections, including 40 cases of acute pneumonia, 33 cases of secondary infection after chronic pulmonary diseases and 2 cases of pulmonary abscess, were treated with cefotetan (CTT, Yamatetan) by drip infusion in order to evaluate its clinical efficacy. The overall rate of effectiveness was 83.8%. CTT was examined comparatively with other beta-lactam antibiotics for antibacterial activity on clinically isolated strains of 3 major respiratory pathogens including Haemophilus influenzae, Branhamella catarrhalis and Streptococcus pneumoniae. Minimum inhibitory concentrations (MIC's) of CTT on H. influenzae were less than 3.13 micrograms/ml regardless of the production of beta-lactamase by these organisms. As to B. catarrhalis, CTT also exerted an antibacterial activity enough to control the proliferation of all the strains at a level of 1.56 micrograms/ml. Against S. pneumoniae, on the other hand, CTT exhibited the lowest activity of all the drugs tested but still showed MIC's of 3.13 micrograms/ml or less. Drip infusion of CTT at a dose of 2 g brought about an average maximum blood concentration of 342 +/- 25.7 micrograms/ml and an average half-life in blood of 2.48 +/- 0.41 hours Maximum sputum concentration of the drug, however, was variable among the cases tested, ranging from 0.40 to 1.80 micrograms/ml. Side effects of the drug were observed in 5 cases or 6.7%. Four of them had some allergic symptoms; i.e., pyrexia and eruption. One patient was especially diagnosed as possible drug-induced interstitial pneumonia during the treatment with the drug. The diagnosis was confirmed by transbronchial lung biopsy and lymphocyte blastogenesis by CTT in vitro. As to abnormal laboratory findings, blood transaminases were elevated during drug administration in 13 cases or 17.3%, but were reduced back to the normal level after the withdrawal of the drug.
为评估头孢替坦(CTT,雅马替坦)的临床疗效,对75例呼吸道感染患者进行了治疗,其中包括40例急性肺炎、33例慢性肺部疾病继发感染和2例肺脓肿患者,采用静脉滴注给药。总有效率为83.8%。将CTT与其他β-内酰胺类抗生素进行比较,检测其对包括流感嗜血杆菌、卡他莫拉菌和肺炎链球菌在内的3种主要呼吸道病原菌临床分离株的抗菌活性。无论这些菌株是否产生β-内酰胺酶,CTT对流感嗜血杆菌的最低抑菌浓度(MIC)均小于3.13微克/毫升。对于卡他莫拉菌,CTT在1.56微克/毫升的水平也具有足够的抗菌活性以控制所有菌株的增殖。另一方面,对于肺炎链球菌,CTT在所有测试药物中表现出最低活性,但MIC仍为3.13微克/毫升或更低。静脉滴注2克CTT导致平均最高血药浓度为342±25.7微克/毫升,平均血药半衰期为2.48±0.41小时。然而,该药物在痰液中的最高浓度在测试病例中各不相同,范围为0.40至1.80微克/毫升。5例患者(6.7%)出现了药物副作用。其中4例有一些过敏症状,即发热和皮疹。1例患者在用药治疗期间被特别诊断为可能的药物性间质性肺炎。通过经支气管肺活检和CTT体外淋巴细胞增殖试验确诊。关于实验室检查异常,13例患者(17.3%)在给药期间出现血转氨酶升高,但停药后恢复至正常水平。