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头孢呋辛酯。对其抗菌活性、药代动力学特性及治疗效果的综述。

Cefuroxime axetil. A review of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy.

作者信息

Perry C M, Brogden R N

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1996 Jul;52(1):125-58. doi: 10.2165/00003495-199652010-00009.

Abstract

Cefuroxime axetil is an oral cephalosporin which is rapidly hydrolysed to the active parent compound, cefuroxime. Cefuroxime has a broad spectrum of in vitro antibacterial activity which encompasses methicillin-sensitive staphylococci and the common respiratory pathogens Streptococcus pneumoniae, Haemophilus influenzae, Moraxella (Branhamella) catarrhalis and group A beta-haemolytic streptococci. Cefuroxime has broad spectrum activity against the beta-lactamase positive respiratory pathogens H. influenzae and M. catarrhalis; it is also active against penicillin-susceptible and -intermediate strains of S. pneumoniae. In clinical trials, cefuroxime axetil (administered twice daily) has been evaluated in the treatment of upper and lower respiratory tract infections and has demonstrated similar efficacy to established antibacterial agents, including amoxicillin/clavulanic acid and cefaclor. Five days' treatment with cefuroxime axetil was recently shown to be as effective as 10 days' treatment with either cefuroxime axetil or amoxicillin/clavulanic acid in patients with acute otitis media or acute bronchitis. Cefuroxime axetil was at least as effective as phenoxymethylpenicillin (penicillin V) in the treatment of patients with group A beta-haemolytic streptococcal tonsillopharyngitis. A number of studies have evaluated the efficacy of cefuroxime axetil as the oral component of intravenous to oral sequential therapy in hospitalised patients with lower respiratory tract infection. In each study patients received parenteral cefuroxime for approximately 2 days followed by cefuroxime axetil for 5 to 10 days. In comparative studies, cefuroxime sequential therapy was as effective as amoxicillin/ clavulanic acid sequential therapy and full courses of parenteral cefuroxime, cefotiam or cefoperazone. Adults with urinary tract infections and skin infections were also effectively treated with cefuroxime axetil, as were adults and adolescents with early stage lyme disease. Cefuroxime axetil is associated with a low incidence of adverse events, with gastrointestinal disturbances being the most frequently observed. Thus, cefuroxime axetil is an effective and convenient treatment for a wide range of infections and may be considered a therapeutic option when empirical treatment of community-acquired infections is required. Moreover, given the promising results of several intravenous/oral sequential treatment studies, cefuroxime axetil may also become established as an oral component of sequential treatment regimens.

摘要

头孢呋辛酯是一种口服头孢菌素,可迅速水解为活性母体化合物头孢呋辛。头孢呋辛具有广泛的体外抗菌活性,涵盖对甲氧西林敏感的葡萄球菌以及常见的呼吸道病原体,如肺炎链球菌、流感嗜血杆菌、卡他莫拉菌(布兰汉菌属)和A组β溶血性链球菌。头孢呋辛对β-内酰胺酶阳性的呼吸道病原体流感嗜血杆菌和卡他莫拉菌具有广谱活性;它对青霉素敏感和中度敏感的肺炎链球菌菌株也有活性。在临床试验中,已对头孢呋辛酯(每日给药两次)治疗上、下呼吸道感染进行了评估,结果显示其疗效与已有的抗菌药物,包括阿莫西林/克拉维酸和头孢克洛相似。最近的研究表明,在患有急性中耳炎或急性支气管炎的患者中,用头孢呋辛酯治疗5天与用头孢呋辛酯或阿莫西林/克拉维酸治疗10天的效果相同。在治疗A组β溶血性链球菌扁桃体咽炎患者时,头孢呋辛酯至少与苯氧甲基青霉素(青霉素V)一样有效。多项研究评估了头孢呋辛酯作为住院下呼吸道感染患者静脉-口服序贯治疗口服部分的疗效。在每项研究中,患者接受大约2天的静脉注射头孢呋辛,随后接受5至10天的头孢呋辛酯治疗。在比较研究中,头孢呋辛序贯治疗与阿莫西林/克拉维酸序贯治疗以及全程静脉注射头孢呋辛、头孢替安或头孢哌酮的疗效相同。患有尿路感染和皮肤感染的成人以及患有早期莱姆病的成人和青少年也可用头孢呋辛酯有效治疗。头孢呋辛酯的不良事件发生率较低,最常见的是胃肠道不适。因此,头孢呋辛酯是治疗多种感染的有效且方便的药物,在需要对社区获得性感染进行经验性治疗时可作为一种治疗选择。此外,鉴于多项静脉/口服序贯治疗研究取得了令人鼓舞的结果,头孢呋辛酯也可能成为序贯治疗方案的口服部分。

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