Dudley M N, Quintiliani R, Nightingale C H
Clin Pharm. 1984 Jan-Feb;3(1):23-32.
The in vitro activity, pharmacokinetics, adverse effects, and clinical efficacy of cefonicid are reviewed. Also discussed are formulary considerations and bacterial resistance. Cefonicid, an investigational agent near approval, is less active than other currently available first- and second-generation cephalosporins against gram-positive cocci, particularly Staphylococcus. Cefonicid and cefamandole have similar activity that is superior to the first-generation cephalosporins against Escherichia coli, Klebsiella, Citrobacter spp., Enterobacter spp., indole-negative Proteus spp., and Providencia spp. Organisms such as Serratia marcescens, Acinetobacter, Pseudomonas, and Bacteroides fragilis are resistant to cefonicid. Despite a small volume of distribution and high protein binding, cefonicid achieves high tissue concentrations. Approximately 90% of an administered dose is excreted unchanged in the urine, and the elimination half-life is approximately four hours. Cefonicid is usually well tolerated. In treating skin infections, cefonicid was usually less effective than cefazolin against Staphylococcus aureus. In genitourinary infections, cefonicid 1 g daily (as the sodium salt) in a single dose has shown comparable efficacy to cefamandole or amoxicillin given in multiple daily doses. Based on available data, single daily dosing of cefonicid in the therapy of Staph. aureus endocarditis is not effective. In studies of patients undergoing hysterectomy, cesarean section, cholecystectomy, and colorectal surgery, cefonicid 1 g given as a single preoperative dose has produced results comparable with those of cefoxitin 1-2 g (as the sodium salt) given preoperatively and for several doses postoperatively. The major clinical uses of cefonicid will probably be as a possible cost-reducing alternative (based on a single daily dose) to currently available first- and second-generation cephalosporins for the treatment of community-acquired pneumonia and infections caused by enteric organisms. It may also be useful as a possible cost-reducing alternative to cefoxitin for prophylaxis in hysterectomy and biliary tract surgery.
本文综述了头孢尼西的体外活性、药代动力学、不良反应及临床疗效。还讨论了其在处方方面的考量及细菌耐药性。头孢尼西作为一种即将获批的研究用药物,对革兰氏阳性球菌,尤其是葡萄球菌的活性低于其他现有的第一代和第二代头孢菌素。头孢尼西和头孢孟多的活性相似,对大肠杆菌、克雷伯菌、柠檬酸杆菌属、肠杆菌属、吲哚阴性变形杆菌属和普罗威登斯菌属的活性优于第一代头孢菌素。粘质沙雷氏菌、不动杆菌、铜绿假单胞菌和脆弱拟杆菌等微生物对头孢尼西耐药。尽管头孢尼西的分布容积小且蛋白结合率高,但它能在组织中达到较高浓度。给药剂量的约90%以原形经尿液排出,消除半衰期约为4小时。头孢尼西通常耐受性良好。在治疗皮肤感染时,头孢尼西对金黄色葡萄球菌的疗效通常不如头孢唑林。在治疗泌尿生殖系统感染时,每日单剂量给予1g头孢尼西(钠盐)已显示出与每日多次给药的头孢孟多或阿莫西林相当的疗效。根据现有数据,每日单剂量使用头孢尼西治疗金黄色葡萄球菌性心内膜炎无效。在对接受子宫切除术、剖宫产、胆囊切除术和结肠直肠手术的患者进行的研究中,术前单剂量给予1g头孢尼西的结果与术前给予1 - 2g头孢西丁(钠盐)并在术后给予数剂的结果相当。头孢尼西的主要临床用途可能是作为一种可能降低成本的替代药物(基于每日单剂量),用于治疗社区获得性肺炎和由肠道微生物引起的感染,替代现有的第一代和第二代头孢菌素。它也可能作为一种可能降低成本的替代药物,用于子宫切除术和胆道手术的预防,替代头孢西丁。