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头孢替坦:抗菌活性、药代动力学特性及治疗用途综述

Cefotetan. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.

作者信息

Ward A, Richards D M

出版信息

Drugs. 1985 Nov;30(5):382-426. doi: 10.2165/00003495-198530050-00002.

Abstract

Cefotetan is a new semisynthetic cephamycin antibiotic administered intravenously or intramuscularly. It has a broad spectrum of activity against Gram-negative aerobic and most clinically important Gram-positive and anaerobic bacteria, and is generally more active against Gram-negative bacteria than the 'first and second generation' agents. Cefotetan is particularly active against Enterobacteriaceae but has little activity against Pseudomonas aeruginosa. An extended plasma elimination half-life of about 3.5 hours, and relatively high achievable serum and tissue levels, enables cefotetan to be administered on a twice daily basis in the treatment of mild to severe infections. Cefotetan has shown good clinical efficacy in intra-abdominal, obstetric and gynaecological infections, postoperative wound infections, and infections in immunocompromised patients - all of which are often complicated due to their polymicrobial nature or by the presence of anaerobic pathogens. A satisfactory clinical response is achieved in over 90% of paediatric patients with acute otorhinolaryngological infections, whereas in the treatment of chronic disease, as with other agents, the efficacy is dramatically reduced. Like other cephalosporins, cefotetan is effective in treating patients with complicated urinary tract infections and lower respiratory tract infections. Its efficacy in urinary tract infections is at least as good as cefoxitin, although in this and some other clinical areas its activity relative to that of other cephamycins and cephalosporins remains to be assessed. Thus, with its convenient twice daily dosage schedule, cefotetan would appear to be a useful addition to a rapidly expanding group of antibacterial agents.

摘要

头孢替坦是一种新型半合成头孢霉素类抗生素,可静脉注射或肌肉注射。它对革兰氏阴性需氧菌以及大多数临床上重要的革兰氏阳性菌和厌氧菌具有广谱抗菌活性,并且通常对革兰氏阴性菌的活性比“第一代和第二代”药物更强。头孢替坦对肠杆菌科细菌特别有效,但对铜绿假单胞菌几乎没有活性。其血浆消除半衰期约为3.5小时,且血清和组织水平相对较高,这使得头孢替坦能够每日给药两次,用于治疗轻至重度感染。头孢替坦在腹腔内、妇产科感染、术后伤口感染以及免疫功能低下患者的感染中均显示出良好的临床疗效——所有这些感染往往因其微生物种类多样或存在厌氧病原体而变得复杂。超过90%的患有急性耳鼻喉感染的儿科患者获得了满意的临床反应,而在治疗慢性病时,与其他药物一样,疗效会显著降低。与其他头孢菌素一样,头孢替坦对治疗复杂性尿路感染和下呼吸道感染的患者有效。其在尿路感染方面的疗效至少与头孢西丁相当,尽管在这一及其他一些临床领域,其相对于其他头孢霉素类和头孢菌素类药物的活性仍有待评估。因此,鉴于其方便的每日两次给药方案,头孢替坦似乎是快速扩充的抗菌药物群体中的一个有用补充。

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