Brogden R N, Campoli-Richards D M
ADIS Drug Information Services, Auckland, New Zealand.
Drugs. 1989 Oct;38(4):524-50. doi: 10.2165/00003495-198938040-00004.
Cefixime, previously designated FK027, FR17027 and CL284635, is an orally active cephalosporin with a broad spectrum of antibacterial activity in vitro. It is particularly active against many Enterobacteriaceae, Haemophilus influenzae. Streptococcus pyogenes, Streptococcus pneumoniae and Branhamella catarrhalis, and is resistant to hydrolysis by many beta-lactamases. Cefixime has little activity against Staphylococcus aureus and is inactive against Pseudomonas aeruginosa. Cefixime is distinguished by its 3-hour elimination half-life which permits twice daily, or in many instances once daily, administration. Comparative trials, though few, indicate that the clinical and bacteriological efficacy of cefixime 200 to 400mg daily administered as a single dose or in 2 divided doses, is comparable with that of multiple daily doses of co-trimoxazole (trimethoprim + sulphamethoxazole) or amoxycillin in acute uncomplicated urinary tract infection, with that of amoxycillin, amoxycillin/clavulanic acid and cefaclor in acute lower respiratory tract infections, and with that of amoxycillin and cefroxidine in adult patients with acute tonsillitis or pharyngitis. Several comparative trials in children with acute otitis media demonstrate the similar effectiveness of cefixime 8 mg/kg daily (in 2 divided doses, or as a single daily dose), cefaclor 20 to 40 mg/kg daily and amoxycillin 40 mg/kg daily in 3 divided doses. The most frequently reported adverse effects, diarrhoea and stool changes, are usually mild to moderate in severity, transient, and mostly occur in the first few days of treatment with cefixime. Thus, cefixime is an effective orally active cephalosporin with a relatively long elimination half-life permitting a simplified treatment regimen. It is a suitable alternative to cefaclor or amoxycillin in acute otitis media and acute upper and lower respiratory tract infections, and to amoxycillin or co-trimoxazole in acute uncomplicated urinary tract infections.
头孢克肟,曾被命名为FK027、FR17027和CL284635,是一种口服有效的头孢菌素,在体外具有广谱抗菌活性。它对许多肠杆菌科细菌、流感嗜血杆菌、化脓性链球菌、肺炎链球菌和卡他莫拉菌特别有效,并且对许多β-内酰胺酶的水解具有抗性。头孢克肟对金黄色葡萄球菌几乎没有活性,对铜绿假单胞菌无活性。头孢克肟的特点是其消除半衰期为3小时,这使得它可以每日给药两次,或者在许多情况下每日给药一次。尽管比较试验较少,但表明每日200至400mg的头孢克肟以单剂量或分2次给药,在急性单纯性尿路感染中的临床和细菌学疗效与每日多次剂量的复方新诺明(甲氧苄啶+磺胺甲恶唑)或阿莫西林相当,在急性下呼吸道感染中与阿莫西林、阿莫西林/克拉维酸和头孢克洛相当,在成年急性扁桃体炎或咽炎患者中与阿莫西林和头孢罗齐相当。在患有急性中耳炎的儿童中进行的几项比较试验表明,每日8mg/kg的头孢克肟(分2次给药,或作为每日单剂量)、每日20至40mg/kg的头孢克洛和每日40mg/kg分3次给药的阿莫西林效果相似。最常报告的不良反应,腹泻和大便改变,严重程度通常为轻至中度,是短暂的,并且大多发生在使用头孢克肟治疗的最初几天。因此,头孢克肟是一种有效的口服活性头孢菌素,具有相对较长的消除半衰期,允许简化治疗方案。在急性中耳炎以及急性上、下呼吸道感染中,它是头孢克洛或阿莫西林的合适替代品,在急性单纯性尿路感染中是阿莫西林或复方新诺明的合适替代品。