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局部外用药Retapamulin的药理与临床研究进展 被引量：2

Pharmacological and clinical properties of retapamulin for topical use
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摘要 Retapamulin(SB-275833)是截短侧耳素类化合物的半合成衍生物,为一种选择性细菌蛋白质合成抑制剂,在体外对G+菌包括金葡球菌、化脓链球菌和一些G-菌(如流感嗜血杆菌、卡他莫拉菌)均有极好的抗菌活性。2007年4月通过美国FDA审批,目前该产品尚未在中国上市,文中对其作用机制、抗菌活性、药动学、临床研究及不良反应等做一综述。 Retapamulin （SB-275833） is a semisynthetic derivative from the compound pleuromutilin and has excellent in vitro antibacterial activity against gram-positive bacteria, including Staphylococcus aureus, Streptococcus pyogenes and some gram-negative bacteria （such as Haemophilus infiuenzae and Moraxella catarrhalis）. This review summarizes the pharmacological mechanism, antibacterial potency pharmacokinetics, clinical studies and adverse reactions of retapamulin .
作者 兰杨 杜小莉
机构地区 中国医学科学院中国协和医科大学北京协和医院药剂科
出处 《中国新药杂志》 CAS CSCD 北大核心 2007年第24期2079-2082,共4页 Chinese Journal of New Drugs
关键词 retapamulin 截短侧耳素类抗生素 作用机制 临床研究 retapamulin pleuromutilin antibacterial mechanism clinical studies
分类号 R978.1 [医药卫生—药品]
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参考文献12

  • 1JONES RN, FRITSCHE TR, SADER HS, et al. Activity of Retapamulin( SB-275833 ), a Novel Pleuromutilin, against Selected Resistant Gran-Positive Cocci[J]. Antimicrob Agents Chemother, 2006, 50(7): 2583-2586.
  • 2YAN K, MADDEN L, CHOUDHRY AE, etal. Biochemical Characterization of the Interactions of the Novel Pleuromutilin Derivative Retapamulin with Bacterial Ribosomes[J]. Antimicrob Agents Chemother, 2006, 50 ( 11 ) : 3875 - 3881.
  • 3LONG KS, HANSEN LH, JAKOBSEN L, et al. Interaction of Pleuromutilin Derivatives with the Ribosomal Peptidyl Transferase Center [ J ]. Antlmlcrob Agents Chemother, 2006, 50 ( 4 ) : 1458 - 1462.
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  • 5European Medicines Agency. European Public Assessment Report [ EB/OL]. [2007 - 06 - 11 ]. http://www.emea.europa. eu/humandocs/PD Fs/EPAR/altargo/H-757-PI-en. pdf.
  • 6RITTENHOUSE S, BISWAS S, BROSKEY J, et al. Selection of Retapamulin, a Novel Pleuromutilin for Topical Use[ J ]. Antimicrob Agents Chemother, 2006, 50( 11 ) : 3882 - 3885.
  • 7GOLDSTEIN EJ, CITRON DM, MERRIAM CV, et al. Comparative In Vitro Activities of Retapamulin( SB-275833 )against 141 Clinical Isolates of Propionibacterium spp. , Including 117 P. acnes Isolates[ J]. Antimicrob Agents Chemother, 2006, 50 ( 1 ) : 379 - 381.
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同被引文献26

  • 1汤建林,应懿,徐颖,黄永平,周世文.反相高效液相色谱法测定人血浆中薁磺酸钠浓度[J].第三军医大学学报,2004,26(21):1964-1966. 被引量：2
  • 2郭万正.动物专用抗生素——泰妙菌素及使用[J].养殖与饲料,2005,4(12):29-32. 被引量：2
  • 3邹祥.高效液相色谱法测定发酵液中截短侧耳素的含量[J].食品与发酵工业,2006,32(3):83-85. 被引量：5
  • 4新型抗生素Altabax获FDA审批[J].齐鲁药事,2007,26(2):84-84. 被引量：1
  • 5杨海峰,王权,于生兰.畜禽专用抗生素泰妙菌素的研究进展[J].饲料工业,2007,28(10):56-57. 被引量：4
  • 6Hogenauer G, Egger H, Ruf C,et al. Affinity labeling of Escherichia coil ribosomes with a eovalenty binding derivatives of the antibiotic Pleuromutilin [ J ]. Biochemistry, 1981,20:516 - 522.
  • 7Poulsen S M,Karlsson M,Johansson L B,et al. The pleuromutilin drugs tianmulin and valnemulin bind to the RNA at the peptidyl transferase centre on the ribosome[J]. Mol Microbiol,2001,41 (5) : 1091 - 1099.
  • 8Schlunzen F,Pyetan E,Fucini P, et al. Inhibition of petide bond formation by pleueomutilins:the structure of 50S ribosomal subunit from Deinococcus radiodurans in complex with tiamulin [ J ]. Mol Microbiol, 2004,54 ( 5 ) : 1287 - 1294.
  • 9Springer D M,Sorenson M E, Huang S, et al. Synthesis and activity of a C - 8 keto pleuromutilin derivative [ J ]. Bioorg Med Chem Lett,2003,13(10) :1751 - 1753.
  • 10Hannan P C,Windsor H M, Ripley P H. In vitro susceptibilities of recent field isolates of mycoplasma hyopneumoniae and mycoplasma hyosynovie to valnemulin,tiamulin and enrofloxacin and the in vitro development of resistance to certain anti - microbial agents inmy coplasma hyopneumoniae [J]. Res Vet Sci,1997,63(2) :157 - 160.

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二级引证文献13

中国新药杂志
2007年 第24期

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