Stapley E O, Birnbaum J, Miller A K, Wallick H, Hendlin D, Woodruff H B
Merck Institute for Therapeutic Research, Rahway, New Jersey 07065.
Rev Infect Dis. 1979 Jan-Feb;1(1):73-89. doi: 10.1093/clinids/1.1.73.
The cephamycins are a family of beta-lactam antibiotics that are produced by actinomycetes and are structurally similar to the cephalosporins. They are characterized by the presence of a 7-alpha-methoxyl group, which confers unusually high resistance to beta-lactamases. Cefoxitin, the first semisynthetic cephamycin, is resistant to almost all beta-lactamases. Cefoxitin retains the 3-carbamoyl group of cephamycin C and thus has excellent metabolic stability. Cefoxitin is bactericidal and almost devoid of any inoculum effect. Active against many cephalothin-resistant gram-negative bacteria, cefoxitin demonstrates a very broad spectrum that includes indole-positive Proteus and many strains of Serratia. In contrast to that of the cephalosporins, cefoxitin's spectrum of activity against anaerobic pathogens includes Bacteroides fragilis. The therapeutic effectiveness of cefoxitin in experimental infections in mice confirms the excellent characteristics of this semisynthetic cephamycin and indicates that it should be a very valuable agent for treatment of bacterial infections.
头霉素类是一族由放线菌产生的β-内酰胺抗生素，其结构与头孢菌素相似。它们的特点是含有7-α-甲氧基，这赋予了对β-内酰胺酶异常高的抗性。第一代半合成头霉素头孢西丁对几乎所有β-内酰胺酶都有抗性。头孢西丁保留了头霉素C的3-氨甲酰基，因此具有出色的代谢稳定性。头孢西丁具有杀菌作用，几乎没有任何接种量效应。头孢西丁对许多耐头孢噻吩的革兰氏阴性菌有活性，显示出非常广泛的抗菌谱，包括吲哚阳性变形杆菌和许多沙雷氏菌菌株。与头孢菌素不同，头孢西丁对厌氧病原体的抗菌谱包括脆弱拟杆菌。头孢西丁在小鼠实验性感染中的治疗效果证实了这种半合成头霉素的优异特性，并表明它应该是治疗细菌感染的一种非常有价值的药物。
