Nakagawa K
Jpn J Antibiot. 1982 Feb;35(2):283-95.
Cefuroxime (CXM) is a new injectable cephalosporin stable against beta-lactamases. The results of preclinical and clinical studies so far carried out in Japan on cefuroxime are summarized in this paper. 1. CXM is stable to various kinds of beta-lactamases except the one produced by P. vulgaris GN 76 (RICHMOND type Ic). Reflecting this action, CXM has been shown to have antibacterial activity, not only against organisms which respond to conventional cephalosporins, but also against Citrobacter, Enterobacter, Hafnia, and Indole positive Proteus which are resistant to conventional cephalosporins. 2. After an intravenous or an intramuscular injection, satisfactory blood levels of CXM are attained with the half-life about 1 hour, and CXM is excreted into urine via kidney in an active form. Transfer of CXM to tissues or various body fluids such as bile, cerebrospinal fluid, prostatic fluid, etc., is also satisfactory. 3. Of the total 826 evaluable cases treated in the open clinical study, 243 cases (29%) were assessed as 'excellent' and 404 (49%), as 'good,' and the efficacy ratio ('excellent' and 'good') was as high as 78%. 4. In a double-blind comparative study vs. cefazolin in patients with respiratory or urinary tract infections, CXM was proven to be superior to CEZ in either the infection, both in terms of clinical efficacy and global utility. 5. Incidence of side effect was very low. Of the total 1,057 cases treated in the open and double-blind clinical studies, side effects, mostly skin hypersensitivity and pyrexia, were noted only in 26 cases (2.5%).
头孢呋辛(CXM)是一种新型的对β-内酰胺酶稳定的注射用头孢菌素。本文总结了迄今为止在日本进行的关于头孢呋辛的临床前和临床研究结果。1. 除普通变形杆菌GN 76产生的β-内酰胺酶(RICHMOND Ic型)外,CXM对各种β-内酰胺酶均稳定。反映这种作用,CXM不仅对常规头孢菌素敏感的细菌具有抗菌活性,而且对耐常规头孢菌素的柠檬酸杆菌、肠杆菌、哈夫尼菌和吲哚阳性变形杆菌也有抗菌活性。2. 静脉注射或肌肉注射后,CXM能达到满意的血药浓度,半衰期约为1小时,且CXM以活性形式经肾脏排泄到尿液中。CXM向组织或各种体液如胆汁、脑脊液、前列腺液等的转运也令人满意。3. 在开放临床研究中治疗的826例可评估病例中,243例(29%)被评为“优”,404例(49%)被评为“良”,有效率(“优”和“良”)高达78%。4. 在呼吸道或泌尿系统感染患者中与头孢唑林进行的双盲对照研究中,CXM在感染方面,无论是临床疗效还是总体效用,均被证明优于头孢唑林。5. 副作用发生率很低。在开放和双盲临床研究中治疗的1057例患者中,仅26例(2.5%)出现副作用,主要为皮肤过敏和发热。