Todd P A, Brogden R N
Adis Drug Information Services, Auckland, New Zealand.
Drugs. 1990 Oct;40(4):608-51. doi: 10.2165/00003495-199040040-00008.
Cefotaxime was the first 'third generation' cephalosporin to be marketed and is administered intramuscularly or intravenously. Similar to other agents of this class, it has a broad spectrum of in vitro activity, particularly against Enterobacteriaceae, including beta-lactamase-producing strains. Cefotaxime forms a metabolite, desacetylcefotaxime, which is antibacterially effective against many bacteria per se and acts additively or synergistically with cefotaxime against many strains. Since the first review of cefotaxime in the Journal, further studies have confirmed its value in the treatment of various infections: complicated urinary tract infections, lower respiratory tract infections, bacteraemia, meningitis, uncomplicated gonorrhoea, infections of skin and soft tissue and of bone and joints, and obstetric and gynaecological infections. Cefotaxime is effective as an empirical treatment of suspected infection due to susceptible organisms in immunocompromised patients and is of proven efficacy in serious, life-threatening infections in general. Cefotaxime reduces the incidence of postsurgical infection but the role of third generation cephalosporins in prophylaxis remains to be determined. The indications for which cefotaxime and other 'third generation' cephalosporins would be considered the most appropriate therapy remain largely dependent upon such factors as varied as cost, local medical custom, decisions of regulatory agencies and geographical patterns of bacterial resistance. Cefotaxime nevertheless represents a valuable 'third generation' cephalosporin of great clinical value in certain infectious conditions, in particular those which are serious and life-threatening and where resistance to therapies is creating a clinical problem.
头孢噻肟是首个上市的“第三代”头孢菌素，可通过肌肉注射或静脉注射给药。与该类的其他药物相似，它具有广泛的体外活性谱，尤其对肠杆菌科细菌有效，包括产β-内酰胺酶的菌株。头孢噻肟形成一种代谢产物去乙酰头孢噻肟，其本身对许多细菌具有抗菌活性，并且与头孢噻肟对许多菌株起相加或协同作用。自《杂志》首次对头孢噻肟进行综述以来，进一步的研究证实了其在治疗各种感染中的价值：复杂性尿路感染、下呼吸道感染、菌血症、脑膜炎、非复杂性淋病、皮肤和软组织感染以及骨和关节感染，以及妇产科感染。头孢噻肟作为免疫功能低下患者疑似由敏感菌引起感染的经验性治疗有效，并且总体上在严重的、危及生命的感染中已证实具有疗效。头孢噻肟可降低术后感染的发生率，但第三代头孢菌素在预防中的作用仍有待确定。头孢噻肟和其他“第三代”头孢菌素被认为是最合适治疗方法的适应症在很大程度上仍取决于多种因素，如成本、当地医疗习惯、监管机构的决定以及细菌耐药性的地理模式。然而，头孢噻肟在某些感染性疾病中，特别是那些严重且危及生命以及对治疗产生耐药性从而造成临床问题的疾病中，是一种具有重要临床价值的宝贵“第三代”头孢菌素。
