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头孢地尼:新一代广谱口服头孢菌素。

Cefdinir: an advanced-generation, broad-spectrum oral cephalosporin.

作者信息

Guay David R P

机构信息

Institute for the Study of Geriatric Pharmacotherapy, College of Pharmacy, University of Minnesota, Minneapolis 55455, USA.

出版信息

Clin Ther. 2002 Apr;24(4):473-89. doi: 10.1016/s0149-2918(02)85125-6.

DOI:10.1016/s0149-2918(02)85125-6
PMID:12017394
Abstract

BACKGROUND

Cefdinir is an advanced-generation, broad-spectrum cephalosporin antimicrobial agent that has been approved for the treatment of community-acquired pneumonia, acute bacterial exacerbations of chronic bronchitis, acute maxillary sinusitis, pharyngitis/tonsillitis, acute bacterial otitis media, and uncomplicated skin and skin-structure infections in adult and pediatric patients.

OBJECTIVE

The purpose of this article was to review the in vitro antimicrobial activity, pharmacokinetics, clinical efficacy, safety, and potential role of cefdinir.

METHODS

Studies were identified by a MEDLINE search (January 1983-September 2001) of the English-language medical literature, a review of identified articles and their bibliographies, and a review of data on file with the manufacturer. Clinical efficacy data were selected from all published trials mentioning cefdinir. Information concerning in vitro susceptibility, safety, chemistry, and the pharmacokinetic profile of cefdinir also was reviewed.

RESULTS

Cefdinir has a broad spectrum of activity against many gram-negative and gram-positive aerobic organisms, including Streptococcus pneumoniae, Staphylococcus aureus, Streptococcus pyogenes, Haemophilus influenzae, and Moraxella catarrhalis. Cefdinir is stable to hydrolysis by 13 of the common beta-lactamases. It is rapidly absorbed from the gastrointestinal tract (mean time to peak plasma concentration, 3 hours) and is almost entirely eliminated via renal clearance of unchanged drug. The terminal disposition half-life of cefdinir is approximately 1.5 hours. Efficacy has been demonstrated in 19 clinical trials in adults and children with upper and lower respiratory tract infections (eg, pharyngitis, sinusitis, acute otitis media, acute bronchitis, acute bacterial exacerbation of chronic bronchitis, community-acquired pneumonia), and skin and skin-structure infections. The adverse-event profile is similar to that of comparator agents, although in 4 adult and adolescent studies and 1 adult study, diarrhea occurred significantly more frequently in cefdinir recipients than in recipients of penicillin V, cephalexin, cefaclor, and cefprozil.

CONCLUSIONS

Cefdinir is an alternative to other antimicrobial agents and can be dosed once or twice daily for the treatment of upper and lower respiratory tract infections and skin and skin-structure infections. Similar to other oral expanded-spectrum cephalosporins, cefdinir has activity against common pathogens of the respiratory tract and skin and is stable in the presence of selected beta-lactamases. The clinical choice of an oral expanded-spectrum cephalosporin will be based on patient acceptance, frequency of administration, and cost.

摘要

背景

头孢地尼是新一代广谱头孢菌素抗菌剂,已被批准用于治疗成人和儿童的社区获得性肺炎、慢性支气管炎急性细菌感染、急性上颌窦炎、咽炎/扁桃体炎、急性细菌性中耳炎以及单纯性皮肤和皮肤结构感染。

目的

本文旨在综述头孢地尼的体外抗菌活性、药代动力学、临床疗效、安全性及潜在作用。

方法

通过检索MEDLINE(1983年1月至2001年9月)英文医学文献、查阅已识别文章及其参考文献以及查阅生产商存档数据来确定研究。临床疗效数据选自所有提及头孢地尼的已发表试验。还综述了有关头孢地尼体外敏感性、安全性、化学性质和药代动力学特征的信息。

结果

头孢地尼对许多革兰氏阴性和革兰氏阳性需氧菌具有广谱活性,包括肺炎链球菌、金黄色葡萄球菌、化脓性链球菌、流感嗜血杆菌和卡他莫拉菌。头孢地尼对13种常见β-内酰胺酶的水解作用稳定。它从胃肠道迅速吸收(血浆浓度达峰平均时间为3小时),几乎完全通过肾脏清除原形药物而消除。头孢地尼的终末消除半衰期约为1.5小时。在19项针对成人和儿童上、下呼吸道感染(如咽炎、鼻窦炎、急性中耳炎、急性支气管炎、慢性支气管炎急性细菌感染、社区获得性肺炎)以及皮肤和皮肤结构感染的临床试验中已证明其疗效。不良事件情况与对照药物相似,不过在4项成人和青少年研究以及1项成人研究中,接受头孢地尼治疗的患者腹泻发生率明显高于接受青霉素V、头孢氨苄、头孢克洛和头孢丙烯治疗的患者。

结论

头孢地尼可作为其他抗菌剂的替代药物,可每日给药一次或两次,用于治疗上、下呼吸道感染以及皮肤和皮肤结构感染。与其他口服广谱头孢菌素类似,头孢地尼对呼吸道和皮肤的常见病原体具有活性,并且在某些β-内酰胺酶存在的情况下稳定。口服广谱头孢菌素的临床选择将基于患者的接受程度、给药频率和成本。

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