酮内酯抗生素对大环内酯类和:专注于呼吸道感染。

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Zhanel GG, Dueck M,贺朋的DJ, Vercaigne LM, Embil JM,杜松子酒,Karlowsky农协

酮内酯抗生素对大环内酯类和:专注于呼吸道感染。

药。2001;61 (4):443 - 98。

PubMed ID

11324679 (在PubMed

]

文摘

第一大环内酯物,红霉素,表现出广谱抗菌活性,主要用于呼吸道、皮肤和软组织感染。更新14 - 15 - 16国环大环内酯类,如克拉霉素和azalide,阿奇霉素,开发了解决红霉素的局限性。大环内酯类的主要结构部件是一个很大的内酯环,不同规模从12到16个原子。酮内酯抗生素一批新的拥有14个大环内酯类称为最近开发的一个3-keto L-cladinose的一部分。大环内酯类可逆地绑定到23 s rRNA,因此,抑制蛋白质合成阻断伸长。酮内酯抗生素的也有报告称,绑定到23 s rRNA及其作用机理类似于大环内酯类。大环内酯物耐药机制包括目标站点变更,变更在抗生素抗生素的运输和修改。酮内酯抗生素大环内酯类和具有活性好对革兰氏阳性需氧菌和革兰氏阴性需氧菌。Ketolides有优秀的活动与macrolide-resistant链球菌spp。包括mefA和ermB产生肺炎链球菌。新一代大环内酯类、酮内酯抗生素阿奇霉素、克拉霉素等,表现出更大的活动比红霉素对流感嗜血杆菌。 The bioavailability of macrolides ranges from 25 to 85%, with corresponding serum concentrations ranging from 0.4 to 12 mg/L and area under the concentration-time curves from 3 to 115 mg/L x h. Half-lives range from short for erythromycin to medium for clarithromycin, roxithromycin and ketolides, to very long for dirithromycin and azithromycin. All of these agents display large volumes of distribution with excellent uptake into respiratory tissues and fluids relative to serum. The majority of the agents are hepatically metabolised and excretion in the urine is limited, with the exception of clarithromycin. Clinical trials involving the macrolides are available for various respiratory infections. In general, macrolides are the preferred treatment for community-acquired pneumonia and alternative treatment for other respiratory infections. These agents are frequently used in patients with penicillin allergies. The macrolides are well-tolerated agents. Macrolides are divided into 3 groups for likely occurrence of drug-drug interactions: group 1 (e.g. erythromycin) are frequently involved, group 2 (e.g. clarithromycin, roxithromycin) are less commonly involved, whereas drug interactions have not been described for group 3 (e.g. azithromycin, dirithromycin). Few pharmacoeconomic studies involving macrolides are presently available. The ketolides are being developed in an attempt to address the increasingly prevalent problems of macrolide-resistant and multiresistant organisms.

DrugBank数据引用了这篇文章

药物靶点

药物	目标	类	生物	药理作用	行动
Dirithromycin	23 s核糖体核糖核酸	核苷酸	肠道细菌和其他真细菌	是的	抑制剂	细节