酮内酯抗生素的:一个评论。
文章的细节
-
引用
复制到剪贴板 -
Zhanel GG,沃尔特斯M, Noreddin Vercaigne LM, Wierzbowski, Embil JM,杜松子酒,杜思韦特年代,贺朋的DJ
酮内酯抗生素的:一个评论。
药。2002;62 (12):1771 - 804。
- PubMed ID
-
12149046 (在PubMed]
- 文摘
-
Ketolides是大环内酯类的一个新类设计尤其是对抗呼吸道获得性耐药病原体大环内酯类。酮内酯抗生素的半合成衍生物的14名成员组成的大环内酯物红霉素A,并保留红霉素macrolactone环形结构以及D-desosamine糖附加在位置5。酮内酯抗生素的定义特征的删除是中性糖、L-cladinose 3环的位置和后续的氧化3-hydroxyl 3-keto官能团。酮内酯抗生素,目前正在开发另外包含11、12环氨基甲酸酯键的两个羟基的红霉素和arylalkyl或arylallyl链,传授体外活动等于或优于新型大环内酯类。Telithromycin是这个新类的第一个成员批准临床使用,而abt - 773是目前发展的第三阶段。Ketolides有行动的机制非常类似于红霉素的派生。他们通过互动接近强有力地抑制蛋白质合成肽基转移酶的细菌核糖体亚基的50年代。Ketolides与核糖体结合亲和力高于大环内酯类。酮内酯抗生素的具有活性好对革兰氏阳性需氧菌和革兰氏阴性需氧菌,对耐药肺炎链球菌和有优秀的活动,其中包括macrolide-resistant (mefA和ermB肺炎链球菌菌株)。Ketolides如telithromycin显示优良的药物动力学允许一次剂量管理和广泛的组织分布相对于血清。 Evidence suggests the ketolides are primarily metabolised in the liver and that elimination is by a combination of biliary, hepatic and urinary excretion. Pharmacodynamically, ketolides display an element of concentration dependent killing unlike macrolides which are considered time dependent killers. Clinical trial data are only available for telithromycin and have focused on respiratory infections including community-acquired pneumonia, acute exacerbations of chronic bronchitis, sinusitis and streptococcal pharyngitis. Bacteriological and clinical cure rates have been similar to comparators. Limited data suggest very good eradication of macrolide-resistant and penicillin-resistant S. pneumoniae. As a class, the macrolides are well tolerated and can be used safely. Limited clinical trial data suggest that ketolides have similar safety profiles to the newer macrolides. Telithromycin interacts with the cytochrome P450 enzyme system (specifically CYP 3A4) in a reversible fashion and limited clinically significant drug interactions occur. In summary, clinical trials support the clinical efficacy of the ketolides in upper and lower respiratory tract infections caused by typical and atypical pathogens including strains resistant to penicillins and macrolides. Considerations such as local epidemiology, patterns of resistance and ketolide adverse effects, drug interactions and cost relative to existing agents will define the role of these agents. The addition of the ketolides in the era of antibacterial resistance provides clinicians with more options in the treatment of respiratory infections.
beplay体育安全吗DrugBank数据引用了这篇文章
- 药物酶
-
药物 酶 类 生物 药理作用 行动 Telithromycin 细胞色素P450 3 a4 蛋白质 人类 未知的底物抑制剂细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
-
药物 交互 整合药物之间
在您的软件的交互
