泊沙康唑药动学/药效学的状况。
文章的细节
-
引用
复制到剪贴板 -
李Y, Theuretzbacher U,克兰西CJ, Nguyen MH Derendorf H
泊沙康唑药动学/药效学的状况。
Pharmacokinet。2010年6月,49 (6):379 - 96。doi: 10.2165 / 11319340-000000000-00000。
- PubMed ID
-
20481649 (在PubMed]
- 文摘
-
泊沙康唑是一种最近批准的亲脂性的三唑抗真菌剂,有力的广谱抗真菌活性在体外和体内对多数念珠菌、新型隐球菌、曲霉菌,许多接合菌,真菌和真菌流行。记录,泊沙康唑有效力和频谱的活动类似于伊曲康唑和氟康唑优于临床念珠菌的重要分离。,c . neoformans和曲霉菌。这个新三唑了治疗真菌感染,最常发生在免疫系统严重受损患者,如器官移植患者或癌症患者接受化疗。自从posanconazole低溶解度在水和酸性介质,其吸收剂量是有限的和显著依赖于食物摄入量。时间达到最大血浆浓度被报道后5 - 8小时口服单剂量。泊沙康唑被估计的相对生物利用度明显不同的方案和被观察到显著增加了政府在分裂的剂量。泊沙康唑主要结合蛋白,蛋白结合的程度高(> 98%)。泊沙康唑有大量口服后平均表观分布容积(V (d) / F),大概是做L /公斤,建议广泛没有血管的分布和渗透到细胞内的空间。V (d) / F是受给药方案。因为食物大大提高其生物利用度,泊沙康唑应尽可能地一顿饱饭,以确保最佳的吸收。泊沙康唑主要循环在等离子体广泛分布到组织和正在慢慢消除。 Posaconazole is not metabolized to a significant extent through the cytochrome P450 (CYP) enzyme system and also has no effect on the CYP isoenzymes of 1A2, 2C8, 2C9, 2D6 and 2E1. The limited metabolism of posaconazole is mediated predominantly through phase 2 biotransformations via uridine diphosphate glucuronosyltransferase enzyme pathways. Therefore, inhibitors or inducers of these clearance pathways may affect posaconazole plasma concentrations. Since posaconazole is an inhibitor primarily of CYP3A4, plasma concentrations of drugs that are predominantly metabolized by CYP3A4 may be increased by posaconazole. Posaconazole has a median terminal elimination half-life of 15-35 hours. The renal elimination of posaconazole is less than 1 mL/h, which is negligible compared with the mean total oral clearance of 16.3 L/h. Posaconazole shows potent in vitro activity against yeasts such as Candida spp. and C. neoformans, and against a range of moulds such as Aspergillus spp., as well as many dimorphic fungi and dermatophytes. Posaconazole has been shown to improve survival and/or to reduce the fungal tissue burden in animals infected with Blastomyces dermatitidis, C. neoformans, Aspergillus fumigatus, Aspergillus flavus, Aspergillus terreus, Coccidioides immitis or Pseudallescheria boydii. The predictive pharmacokinetic/pharmacodynamic parameter for posaconazole treatment efficacy--the ratio between the mean free-drug area under the plasma concentration-time curve from 0 to 24 hours and the minimum inhibitory concentration (AUC(24)/MIC)--is about 17, which is similar to the value observed for other azoles in this infection model of disseminated Candida albicans infection.
beplay体育安全吗DrugBank数据引用了这篇文章
- 药物
- 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
在您的软件的交互溴麦角环肽 泊沙康唑 血清浓度的溴麦角环肽结合泊沙康唑时可以增加。 卡麦角林 泊沙康唑 卡麦角林的血清浓度可以增加时,结合泊沙康唑。 Dihydroergocornine 泊沙康唑 的血清浓度Dihydroergocornine结合泊沙康唑时可以增加。 Dihydroergocristine 泊沙康唑 的血清浓度Dihydroergocristine结合泊沙康唑时可以增加。 双氢麦角胺 泊沙康唑 双氢麦角胺的血清浓度可以增加时,结合泊沙康唑。 Ergoloid甲磺酸 泊沙康唑 的血清浓度Ergoloid甲磺酸结合泊沙康唑时可以增加。 麦角新碱 泊沙康唑 麦角新碱的血清浓度可以增加时,结合泊沙康唑。 麦角胺 泊沙康唑 的血清浓度麦角胺结合泊沙康唑时可以增加。 Lisuride 泊沙康唑 的血清浓度Lisuride结合泊沙康唑时可以增加。 Methylergometrine 泊沙康唑 的血清浓度Methylergometrine结合泊沙康唑时可以增加。
