Structure via PubChem · Public domain (PubChem)
依折麦布
Sign in to saveEzetimibe, sold under the brand name Zetia among others, is a medication used to treat high blood cholesterol and certain other lipid abnormalities. Generally it is used together with dietary changes and a statin. Alone, it is less preferred than a statin. It is taken by mouth. It is also available in the fixed-dose combinations ezetimibe/simvastatin, ezetimibe/atorvastatin, ezetimibe/rosuvastatin, and ezetimibe/bempedoic acid.
Key facts
- Drug.Watchedfields
- changed
- Drug.verifiedrevid
- 461098524
- Drug.image
- Ezetimibe.svg
- Drug.image_class
- skin-invert-image
- Drug.caption
- Above: molecular structure of ezetimibe Below: 3D representation of an ezetimibe molecule
- Drug.image2
- Ezetimibe 3D.png
- Drug.image_class2
- bg-transparent
- Drug.tradename
- Zetia, others
- Drug.MedlinePlus
- a603015
- Drug.DailyMedID
- Ezetimibe
- Drug.pregnancy_AU
- B3
- Drug.routes_of_administration
- By mouth
- Drug.class
- Cholesterol absorption inhibitor
- Drug.ATC_prefix
- C10
- Drug.ATC_suffix
- AX09
- Drug.legal_AU
- S4
- Drug.legal_CA
- Rx-only
- Drug.legal_UK
- POM
via Wikipedia infobox
Chemical data
- Formula
- C24H21F2NO3
- Molecular weight
- 409.4 g/mol
- IUPAC name
- (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
- SMILES
- C1=CC(=CC=C1[C@@H]2[C@H](C(=O)N2C3=CC=C(C=C3)F)CC[C@@H](C4=CC=C(C=C4)F)O)O
- InChIKey
- OLNTVTPDXPETLC-XPWALMASSA-N
- XLogP
- 4
- Polar surface area
- 60.8 Ų
- H-bond donors
- 2
- H-bond acceptors
- 5
- Formal charge
- 0
via PubChem
Drug data · ChEMBL
- Max clinical phase
- Approved
- Molecule type
- Small molecule
- First approval
- 2002
- Admin. routes
- oral
- Indications
- Hypercholesterolemia, metabolic syndrome, Disorder of lipid metabolism, chronic hepatitis C virus infection
via ChEMBL · EBI
Research
5,397 papers- Rosuvastatin/Ezetimibe: A Review in Hypercholesterolemia.American journal of cardiovascular drugs : drugs, devices, and other interventions · 2020
- Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions.Clinical pharmacokinetics · 2005
- Ezetimibe.American journal of cardiovascular drugs : drugs, devices, and other interventions · 2003
- Ezetimibe.Expert opinion on investigational drugs · 2002
- Ezetimibe/simvastatin.Expert opinion on drug safety · 2009
via PubMed
Wikidata facts
- Mass
- 409.14895
- Has use
- medication
Show 10 more facts
- chemical formula
- C₂₄H₂₁F₂NO₃
- route of administration
- oral administration
- isomeric SMILES
- C1=CC(=CC=C1[C@@H]2[C@H](C(=O)N2C3=CC=C(C=C3)F)CC[C@@H](C4=CC=C(C=C4)F)O)O
- canonical SMILES
- C1=CC(=CC=C1C2C(C(=O)N2C3=CC=C(C=C3)F)CCC(C4=CC=C(C=C4)F)O)O
- World Health Organisation international non-proprietary name
- ezetimibe
- defined daily dose
- 10
- physically interacts with
- NPC1 like intracellular cholesterol transporter 1
- Commons category
- Ezetimibe
- legal status (medicine)
- boxed warning
- significant drug interaction
- fenofibrate
Sources (6)
via Wikidata · CC0
Article · 中文
依折麦布(英語:Ezetimibe,商品名益适纯) (/ɛˈzɛt[不支援的輸入]mɪb/) 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(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。
Abstract from DBpedia / Wikipedia · CC BY-SA