药品详细
Chenodeoxycholic acid(鹅去氧胆酸)
化学结构式图
中文名
鹅去氧胆酸
英文名
Chenodeoxycholic acid
分子式
C24H40O4
化学名
(4R)-4-[(1S,2S,5R,7S,9R,10R,11S,14R,15R)-5,9-dihydroxy-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadecan-14-yl]pentanoic acid
分子量
Average: 392.572
Monoisotopic: 392.292659768
Monoisotopic: 392.292659768
CAS号
474-25-9
ATC分类
A05A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Chenodeoxycholic acid (or Chenodiol) is an epimer of ursodeoxycholic acid (DB01586). Chenodeoxycholic acid is a bile acid naturally found in the body. It works by dissolving the cholesterol that makes gallstones and inhibiting production of cholesterol in the liver and absorption in the intestines, which helps to decrease the formation of gallstones. It can also reduce the amount of other bile acids that can be harmful to liver cells when levels are elevated.
生产厂家
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes | Not Available |
| Substructures | Not Available |
适应症
药理
| Indication | Chenodiol is indicated for patients with radiolucent stones in well-opacifying gallbladders, in whom selective surgery would be undertaken except for the presence of increased surgical risk due to systemic disease or age. Chenodiol will not dissolve calcified (radiopaque) or radiolucent bile pigment stones. |
| Pharmacodynamics | It acts by reducing levels of cholesterol in the bile, helping gallstones that are made predominantly of cholesterol to dissolve. Chenodeoxycholic acid is ineffective with stones of a high calcium or bile acid content. |
| Mechanism of action | Chenodiol suppresses hepatic synthesis of both cholesterol and cholic acid, gradually replacing the latter and its metabolite, deoxycholic acid in an expanded bile acid pool. These actions contribute to biliary cholesterol desaturation and gradual dissolution of radiolucent cholesterol gallstones in the presence of a gall-bladder visualized by oral cholecystography. Bile acids may also bind the the bile acid receptor (FXR) which regulates the synthesis and transport of bile acids. |
| Absorption | Chenodiol is well absorbed from the small intestine. |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism |
Chenodiol is well absorbed from the small intestine and taken up by the liver where it is converted to its taurine and glycine conjugates and secreted in bile. At steady-state, an amount of chenodiol near the daily dose escapes to the colon and is converted by bacterial action to lithocholic acid. About 80% of the lithocholate is excreted in the feces; the remainder is absorbed and converted in the liver to its poorly absorbed sulfolithocholyl conjugates. During chenodiol therapy there is only a minor increase in biliary lithocholate, while fecal bile acids are increased three- to fourfold.
|
| Route of elimination | About 80% of its bacterial metabolite lithocholate is excreted in the feces. |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Hepatotoxic. |
| Affected organisms | Not Available |
| Pathways | Not Available |
理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Colesevelam | Bile Acid Sequestrants may decrease the serum concentration of Chenodiol. Consider administration of chenodiol 5 hours or more after bile acid sequestrants to reduce chenodiol adsorption in the gastrointestinal tract. Monitor for decreased therapeutic effects of chenodiol in patients receiving bile acid sequestrants. |
食物相互作用
Not Available
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