Lamb Harriet M, Ormrod Douglas, Scott Lesley J, Figgitt David P
Adis International Limited, 41 Centorian Drive, PB 65901, Mairangi Bay, Auckland 10, New Zealand.
Drugs. 2002;62(7):1041-89. doi: 10.2165/00003495-200262070-00005.
Ceftriaxone is a parenteral third-generation cephalosporin with a long elimination half-life which permits once-daily administration. It has good activity against Streptococcus pneumoniae, methicillin-susceptible staphylococci, Haemophilus influenzae, Moraxella catarrhalis and Neisseria spp. Although active against Enterobacteriaceae, the recent spread of derepressed mutants which hyperproduce chromosomal beta-lactamases and extended-spectrum beta-lactamases has diminished the activity of all third-generation cephalosporins against these pathogens necessitating careful attention to sensitivity studies. Extensive data from randomised clinical trials confirm the efficacy of ceftriaxone in serious and difficult-to-treat community-acquired infections including meningitis, pneumonia and nonresponsive acute otitis media. Ceftriaxone also has efficacy in other community-acquired infections including uncomplicated gonorrhoea, acute pyelonephritis and various infections in children. In the nosocomial setting, extensive data also confirm the efficacy of ceftriaxone with or without an aminoglycoside in serious Gram-negative infections, pneumonia, spontaneous bacterial peritonitis and as surgical prophylaxis. Outpatient use of ceftriaxone, either as part of a step-down regimen or parenterally, is a distinguishing feature of the data gathered on the agent over the last decade. The review focuses on new applications of the drug and its use in infections in which the causative pathogens or their resistance patterns have changed over the past decade. Ceftriaxone has a good tolerability profile, the most common events being diarrhoea, nausea, vomiting, candidiasis and rash. Ceftriaxone may cause reversible biliary pseudolithiasis, notably at higher dosages of the drug (>/=2 g/day); however, the incidence of true lithiasis is <0.1%. Injection site discomfort or phlebitis can occur after intramuscular or intravenous administration.
As a result of its strong activity against S. pneumoniae, ceftriaxone holds an important place, either alone or as part of a combination regimen, in the treatment of invasive pneumococcal infections, including those with reduced beta-lactam susceptibility. Its once-daily administration schedule allows simplification of otherwise complex regimens in a hospital setting and has also contributed to its popularity as a parenteral agent in an ambulatory setting. These properties, together with a well characterised tolerability profile, mean that ceftriaxone is likely to retain its place as an important third-generation cephalosporin in the treatment of serious community-acquired and nosocomial infections.
头孢曲松是一种肠外第三代头孢菌素，消除半衰期长，允许每日给药一次。它对肺炎链球菌、甲氧西林敏感葡萄球菌、流感嗜血杆菌、卡他莫拉菌和奈瑟菌属有良好活性。虽然对肠杆菌科有活性，但最近过度产生染色体β-内酰胺酶和超广谱β-内酰胺酶的去阻遏突变体的传播，削弱了所有第三代头孢菌素对这些病原体的活性，因此需要仔细关注敏感性研究。来自随机临床试验的大量数据证实了头孢曲松在严重且难以治疗的社区获得性感染（包括脑膜炎、肺炎和无反应性急性中耳炎）中的疗效。头孢曲松在其他社区获得性感染（包括单纯性淋病、急性肾盂肾炎和儿童的各种感染）中也有疗效。在医院环境中，大量数据也证实了头孢曲松单独使用或与氨基糖苷类联合使用在严重革兰氏阴性感染、肺炎、自发性细菌性腹膜炎以及作为手术预防用药方面的疗效。过去十年收集的数据的一个显著特点是门诊使用头孢曲松，无论是作为降阶梯治疗方案的一部分还是肠外给药。本综述重点关注该药物的新应用及其在过去十年中致病病原体或其耐药模式发生变化的感染中的应用。头孢曲松具有良好的耐受性，最常见的不良反应是腹泻、恶心、呕吐、念珠菌病和皮疹。头孢曲松可能导致可逆性胆汁假性结石形成，尤其是在药物剂量较高（≥2g/天）时；然而，真正结石形成 的发生率<0.1%。肌内或静脉注射后可能会出现注射部位不适或静脉炎。
由于头孢曲松对肺炎链球菌有强大活性，它在侵袭性肺炎球菌感染（包括β-内酰胺敏感性降低的感染）的治疗中，单独或作为联合治疗方案的一部分，都占有重要地位。其每日一次的给药方案可简化医院环境中原本复杂的治疗方案，也使其在门诊环境中作为肠外用药广受欢迎。这些特性，连同其良好的耐受性特征，意味着头孢曲松在严重社区获得性和医院感染的治疗中可能会继续保持其作为重要第三代头孢菌素的地位。
