药品详细
Ezetimibe (依泽替米贝 )
化学结构式图
中文名
依泽替米贝
英文名
Ezetimibe
分子式
Not Available
化学名
(3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one
分子量
Average: 409.4252
Monoisotopic: 409.148949953
Monoisotopic: 409.148949953
CAS号
163222-33-1
ATC分类
C10A 未知
药物类型
small molecule
阶段
商品名
Ezedoc;Ezetrol;Zetia;
同义名
基本介绍
Ezetimibe is an anti-hyperlipidemic medication which is used to lower cholesterol levels. Specifically, it appears to bind to a critical mediator of cholesterol absorption, the Niemann-Pick C1-Like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells as well as in hepatocytes.
生产厂家
- Msp singapore co llc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
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剂型
| Form | Route | Strength |
|---|---|---|
| Tablet | Oral |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Zetia 10 mg tablet | 5.15 USD | tablet |
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
hyperlipidemi 高血脂;
药理
| Indication | For use as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia. |
| Pharmacodynamics | Ezetimibe is in a class of lipid-lowering compounds that selectively inhibits the intestinal absorption of cholesterol and related phytosterols. Ezetimibe, administered alone is indicated as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia. It is also used in combination therapy with HMG-CoA reductase inhibitors. Ezetimibe has a mechanism of action that differs from those of other classes of cholesterol-reducing compounds (HMG-CoA reductase inhibitors, bile acid sequestrants, fibric acid derivatives, and plant stanols). Ezetimibe does not inhibit cholesterol synthesis in the liver, or increase bile acid excretion but instead localizes and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood; this distinct mechanism is complementary to that of HMG-CoA reductase inhibitors. |
| Mechanism of action | Ezetimibe localizes and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. |
| Absorption | Not Available |
| Volume of distribution | Not Available |
| Protein binding | >90% |
| Metabolism |
Hepatic, intestinal wall |
| Route of elimination | Ezetimibe is primarily metabolized in the small intestine and liver via glucuronide conjugation (a phase II reaction) with subsequent biliary and renal excretion. In humans, ezetimibe is rapidly metabolized to ezetimibe-glucuronide. |
| Half life | 22 hours |
| Clearance | Not Available |
| Toxicity | Not Available |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | Not Available | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Cholestyramine | Cholestyramine may decrease the levels of ezetimibe. |
| Cyclosporine | Cyclosporine may increase the therapeutic and adverse effects of ezetimibe. |
食物相互作用
- Take without regard to meals.
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