达托霉素
 | |
| 临床资料 | |
|---|---|
| 商品名 | Cubicin |
| AHFS/Drugs.com | Monograph |
| 给药途径 | 静脉注射 |
| ATC码 | |
| 法律规范状态 | |
| 法律规范 | |
| 药物动力学数据 | |
| 生物利用度 | n/a |
| 血浆蛋白结合率 | 90–95% |
| 药物代谢 | 肾 (推测)[1] |
| 生物半衰期 | 7–11 h (对肾功能不全者可达28h) |
| 排泄途径 | 尿液 (78%; 未经代谢排出); 粪便 (5.7%) |
| 识别信息 | |
| |
| CAS号 | 103060-53-3  |
| PubChem CID | |
| DrugBank | |
| ChemSpider | |
| UNII | |
| KEGG | |
| ChEMBL | |
| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.116.065 |
| 化学信息 | |
| 化学式 | C72H101N17O26 |
| 摩尔质量 | 1619.7086 g/mol |
| 鉴定 | |
|---|---|
| 标志 | ? |
| TCDB | 1.D.15 |
| OPM家族 | 172 |
| OPM蛋白 | 1t5n |
达托霉素 （Daptomycin），是脂蛋白抗生素，用来治疗威胁系统和生命的革兰氏阳性菌所造成的感染。达托霉素自然存在于土壤腐生营养玫瑰孢链霉菌中。
作用机制
[编辑]达托霉素的机制与大多数抗生素不同。达托霉素会利用磷酸酰甘油让其插入细胞膜中，并且凝集，改变细胞膜的曲度并穿孔，进而引发细胞去极化，最终导致细胞坏死。[2]
2. 达托霉素相互凝集
3. 导致细胞穿孔、去极化
微生物学
[编辑]达托霉素仅对革兰氏阳性菌具有杀菌作用，已证明其对肠球菌（包括耐糖肽的肠球菌(GRE)）、葡萄球菌（包括耐甲氧西林金黄色葡萄球菌）、链球菌、[3]棒状杆菌和静止期伯氏疏螺旋体持留细菌具有体外活性。[4]
参考资料
[编辑]- ^ Woodworth JR, Nyhart EH, Brier GL, Wolny JD, Black HR. = long&pmid = 1318678 Single-dose pharmacokinetics and antibacterial activity of daptomycin, a new lipopeptide antibiotic, in healthy volunteers 请检查
|url=值 (帮助). Antimicrob Agents Chemother. February 1992, 36 (2): 318–25. PMC 188435
. PMID 1318678. doi:10.1128/aac.36.2.318.[永久失效链接]
- ^ Pogliano J, Pogliano N, Silverman JA. Daptomycin-mediated reorganization of membrane architecture causes mislocalization of essential cell division proteins. Journal of Bacteriology. September 2012, 194 (17): 4494–504. PMC 3415520 . PMID 22661688. doi:10.1128/JB.00011-12.
- ^ Shoemaker DM, Simou J, Roland WE. A review of daptomycin for injection (Cubicin) in the treatment of complicated skin and skin structure infections. Therapeutics and Clinical Risk Management. June 2006, 2 (2): 169–174. PMC 1661656 . PMID 18360590. doi:10.2147/tcrm.2006.2.2.169.
- ^ Feng J, Weitner M, Shi W, Zhang S, Zhang Y. Eradication of Biofilm-Like Microcolony Structures of Borrelia burgdorferi by Daunomycin and Daptomycin but not Mitomycin C in Combination with Doxycycline and Cefuroxime. Frontiers in Microbiology. 2016, 7: 62. PMC 4748043 . PMID 26903956. doi:10.3389/fmicb.2016.00062 .
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