glycylcyclines:比较与四环素审查。

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Zhanel GG, Homenuik K, Nichol K, Noreddin, Vercaigne L, Embil J,杜松子酒,Karlowsky是的,贺朋的DJ

glycylcyclines:比较与四环素审查。

药。2004;64 (1):63 - 88。

PubMed ID

14723559 (在PubMed

]

文摘

的四环素类抗生素具有广谱的活动对大量的病原体,包括革兰氏阳性和革兰氏阴性细菌,以及典型的生物。这些化合物抑菌,法案通过绑定到30年代细菌核糖体亚基,抑制蛋白质合成。四环素已成功地用于治疗各种各样的传染病包括社区获得性呼吸道感染和性传播疾病,在痤疮的管理。使用四环素治疗细菌感染近年来受到了限制,因为耐药生物的出现与射流和核糖体保护机制的阻力。研究必威国际app发现四环素类,规避这些耐药机制导致glycylcyclines的发展。最发达的glycylcycline 9-tert-butyl-glycylamido二甲胺四环素的导数,也称为tigecycline(雀鳝- 936)。四环素早些时候glycylcyclines展览抗菌活性的典型,但与更强的活动反对tetracycline-resistant生物与射流和核糖体保护机制的阻力。glycylcyclines活跃相对其它耐药病原体包括耐甲氧西林葡萄球菌、抗肺炎链球菌,vancomycin-resistant enterococci。Tigecycline仅可在临床使用的注射配方与目前市场四环素可用口服剂型。Tigecycline有显著更大体积的分布(> 10 L /公斤)比其他四环素(范围0.14 - 1.6 L /公斤)。 Protein binding is approximately 68%. Presently no human data are available describing the tissue penetration of tigecycline, although studies in rats using radiolabelled tigecycline demonstrated good penetration into tissues. Tigecycline has a half-life of 36 hours in humans, less than 15% of tigecycline is excreted unchanged in the urine. On the basis of available data, it does not appear that the pharmacokinetics of tigecycline are markedly influenced by patient gender or age. The pharmacodynamic parameter that best correlates with bacteriological eradication is time above minimum inhibitory concentration. Several animal studies have been published describing the efficacy of tigecycline. Human phase 1 and 2 clinical trials have been completed for tigecycline. Phase 2 studies have been conducted in patients with complicated skin and skin structure infections, and in patients with complicated intra-abdominal infections have been published as abstracts. Both studies concluded that tigecycline was efficacious and well tolerated. Few human data are available regarding the adverse effects or drug interactions resulting from tigecycline therapy; however, preliminary data report that tigecycline can be safely used, is well tolerated and that the adverse effects experienced were typical of the tetracyclines (i.e. nausea, vomiting and headache). Tigecycline appears to be a promising new antibacterial based on in vitro and pharmacokinetic/pharmacodynamic activity; however more clinical data are needed to fully evaluate its potential.

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
二甲胺四环素	16 s rrna	核苷酸	肠道细菌和其他真细菌	未知的	抑制剂	细节
二甲胺四环素	30年代核糖体蛋白S4	蛋白质	大肠杆菌(应变K12)	是的	抑制剂	细节
二甲胺四环素	30年代核糖体蛋白S9	蛋白质	大肠杆菌(应变K12)	是的	抑制剂	细节