药品详细
Cholestyramine(消胆胺)
化学结构式图
中文名
消胆胺
英文名
Cholestyramine
分子式
Not Available
化学名
分子量
Not Available
CAS号
11041-12-6
ATC分类
C10A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Cholestyramine or colestyramine is a bile acid sequestrant. Bile acid sequestrants are polymeric compounds which serve as ion exchange resins. Cholestyramine resin is quite hydrophilic, but insoluble in water.
生产厂家
- Apothecon inc div bristol myers squibb
- Bristol myers co
- Ivax pharmaceuticals inc sub teva pharmaceuticals usa
- Par pharmaceutical inc
- Parke davis div warner lambert co
- Sandoz inc
- Teva pharmaceuticals usa
- Teva pharmaceuticals usa inc
- Upsher smith laboratories inc
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 | Indicated as adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet. Also for the relief of pruritus associated with partial biliary obstruction. |
| Pharmacodynamics | Cholesterol is probably the sole precursor of bile acids. During normal digestion, bile acids are secreted into the intestines. A major portion of the bile acids is absorbed from the intestinal tract and returned to the liver via the enterohepatic circulation. Only very small amounts of bile acids are found in normal serum. Cholestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. This results in a partial removal of bile acids from the enterohepatic circulation by preventing their absorption. |
| Mechanism of action | Cholestyramine binds bile in the gastrointestinal tract to prevent its reabsorption. The resin is a strong anion exchange resin, which means that it can exchange its chloride anions with anionic bile acids in the gastrointestinal tract and bind them strongly in the resin matrix. The functional group of the anion exchange resin is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer. |
| Absorption | Not absorbed from the gastrointestinal tract following oral administration. |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism |
Bile acids
|
| Route of elimination | Cholestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. |
| Half life | 6 minutes |
| Clearance | Not Available |
| Toxicity | Overdose may result in blockage of intestine or stomach. |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | |||||||
|---|---|---|---|---|---|---|---|
| State | solid | ||||||
| Experimental Properties |
|
||||||
| Predicted Properties | Not Available | ||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Acenocoumarol | The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of acenocoumarol by decreasing its absorption. |
| Anisindione | The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of anisindione by decreasing its absorption. |
| Bezafibrate | Bile acid sequestrants like cholestyramine may decrease the absorption of fibric acid derivatives like bezafibrate. Therapy modification should be considered. If concomitant therapy is used, separate doses by at least 2 hours to minimize this interaction. Fenofibric acid labeling recommends administration one hour prior to or 4-6 hours after a bile acid sequestrant. |
| Chlorothiazide | Bile acid sequestrants may decrease the absorption of thiazide diuretics such as chlorothiazide. The diuretic response is likewise decreased. Monitor for decreased therapeutic effects of thiazide diuretics if coadministered with a bile acid sequestrant. If these agents are used concomitantly, separate doses 2 or more hours to minimize the interaction. |
| Cholecalciferol | Bile acid sequestrants such as cholestyramine may decrease the serum concentration of Vitamin D analogs such as cholecalciferol. More specifically, bile acid sequestrants may impair absorption of Vitamin D analogs. Avoid concomitant administration of vitamin D analogs and bile acid sequestrants. Monitor plasma calcium concentrations in patients receiving combined therapy with these agents. This is particularly important in patients receiving higher doses of a bile acid sequestant (i.e., 30 g/day or more of cholestyramine or equivalent) or in patients experiencing bile acid sequestrant-induced steatorrhea. Specific recommendations regarding the separation of administration of these agents are not defined; however, it would seem prudent to separate the administration of these agents by several hours to minimize the potential risk of interaction. Similar precautions do not apply to parenterally administered vitamin D analogs. |
| Dicumarol | The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of dicumarol by decreasing its absorption. |
| Digoxin | The resin decreases the effect of digoxin |
| Ezetimibe | Cholestyramine may decrease the levels of ezetimibe. |
| Fluvastatin | Increased/decreased effect according to spacing |
| Hydrocortisone | Cholestyramine may decrease the effect of hydrocortisone. |
| Levothyroxine | The resin, cholestyramine, decreases the absorption of the thyroid hormone, levothyroxine. |
| Liothyronine | The resin, cholestyramine, decreases the absorption of the thyroid hormones, liothyronine. |
| Liotrix | The resin, cholestyramine, decreases the absorption of the thyroid hormone, liotrix. |
| Lomitapide | Bile acid sequestrants also used for treating high cholesterol may interfere with the absorption of oral medications, thus separate administration by 4 hours. |
| Methotrexate | Decreased levels of methotrexate |
| Raloxifene | The resin decreases the effect of raloxifene |
| Spironolactone | Increased risk of acidosis and hyperkalemia |
| Sulindac | The bile acid sequestrant, cholestyramine, may decrease the absorption of the NSAID, sulindac. Monitor for changes in the therapeutic and adverse effects of sulindac if cholestyramine is initiated, discontinued or dose changed. Administering the two agents 2 or more hours apart may reduce, but not eliminate, the risk of this interactions. |
| Tenoxicam | Cholestyramine may decrease the serum concentration of Tenoxicam by increasing clearance. Monitor for changes in Tenoxicam therapeutic and adverse effects if Cholestyramine is initiated, discontinued or dose changed. |
| Thyroglobulin | The resin, cholestyramine, decreases the absorption of the thyroid hormone, thyroglobulin. |
| Tiaprofenic acid | The bile acid sequestrant, Cholestyramine resin, may reduce Tiaprofenic acid absorption and therapeutic effect. |
| Tolmetin | Cholestyramine may decrease the absorption of Tolmetin. Monitor for changes in the therapeutic and adverse effects of Tolmetin if Cholestyramine is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction. |
| Torasemide | Cholestyramine may decrease the bioavailability of Torasemide by inhibiting Torasemide absorption. Monitor for changes in the therapeutic and adverse effects of Torasemide if Cholestyramine is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction. |
| Trichlormethiazide | The bile acid sequestrant, Cholestyramine resin, may inhibit the absorption of Trichlormethiazide. |
| Troglitazone | Decreases the effect of troglitazone |
| Ursodeoxycholic acid | The resin decreases the effect of ursodiol |
| Warfarin | The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of warfarin by decreasing its absorption. |
食物相互作用
- Take with food, do not mix with soft drinks.
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