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依折麦布

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依折麦布
臨床資料
商品名英语Drug nomenclatureZetia
AHFS/Drugs.comMonograph
MedlinePlusa603015
懷孕分級
  • : C
给药途径Oral
ATC碼
法律規範狀態
法律規範
藥物動力學數據
生物利用度35–65%
血漿蛋白結合率>90%
药物代谢肠壁,肝脏
生物半衰期19–30 小时
排泄途徑肾脏11%, 粪便78%
识别信息
  • (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
CAS号163222-33-1  checkY
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.207.996 編輯維基數據鏈接
化学信息
化学式C24H21F2NO3
摩尔质量409.4 g·mol−1
3D模型(JSmol英语JSmol
熔点164至166 °C(327至331 °F)
  • Fc1ccc(cc1)[C@@H](O)CC[C@H]4C(=O)N(c2ccc(F)cc2)[C@@H]4c3ccc(O)cc3
  • InChI=1S/C24H21F2NO3/c25-17-5-1-15(2-6-17)22(29)14-13-21-23(16-3-11-20(28)12-4-16)27(24(21)30)19-9-7-18(26)8-10-19/h1-12,21-23,28-29H,13-14H2/t21-,22+,23-/m1/s1 checkY
  • Key:OLNTVTPDXPETLC-XPWALMASSA-N checkY

依折麦布(英語:Ezetimibe,商品名益适纯)/ɛˈzɛtɪmɪb, -mb/) 是一种用来降低血清胆固醇浓度的药物。其作用機理為阻斷Niemann-Pick C1-like 1 (NPC1L1)protein,藉此抑制小腸和肝臟細胞吸收膽固醇,進而增加肝臟細胞 LDL receptor 表現量。臨床上可以用於使用他汀類有無法 接受副作用的患者、severe primary hypercholesterolemia 患者、單用他汀類成效不彰者,但因為目前研究無法證明單用依澤替米貝 (ezetimibe) 的效益,因此美国心脏协会(AHA)和美国心血管学院(ACC)建議對他汀類有無法接受副作用的患者仍應該同時服用最高耐受劑量的他汀類

研究顯示針對有急性冠狀動脈疾病且 LDL 濃度低於 125 mg/dl 的病患, 合用依澤替米貝 (ezetimibe) 和 simvastatin 可以降低 2% 復發型心血管事件發生風險,而另外一個分組實驗也顯示合用兩藥的組別 LDL 濃度平均為 54 mg/dl,單用 simvastatin 之 LDL 濃度平均則為 70 mg/dl,由此可見其與他汀類藥物合用之效益。[1]

引用

[编辑]
  1. ^ Michos, Erin D.; McEvoy, John W.; Blumenthal, Roger S. Lipid Management for the Prevention of Atherosclerotic Cardiovascular Disease. New England Journal of Medicine. 2019-10-17, 381 (16): 1557–1567. ISSN 0028-4793. PMID 31618541. doi:10.1056/NEJMra1806939. 
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依折麦布
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