药品详细
Colestipol (Colestipol )
化学结构式图
中文名
Colestipol
英文名
Colestipol
分子式
Not Available
化学名
(2-aminoethyl)[2-({2-[(2-aminoethyl)amino]ethyl}amino)ethyl]amine; 2-(chloromethyl)oxirane
分子量
Average: 281.826
Monoisotopic: 281.198238250
Monoisotopic: 281.198238250
CAS号
50925-79-6
ATC分类
C10A 未知
药物类型
small molecule
阶段
商品名
Cholestabyl;Colestid;
同义名
Colestipolum [INN-Latin];
基本介绍
Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels. [PubChem]
生产厂家
- Impax laboratories inc
- Pharmacia and upjohn co
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Granule | Oral | |
| Tablet | Oral |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Colestid 90 5 gm Packets Box | 252.5 USD | box |
| Colestid 30 5 gm Packets Box | 81.11 USD | box |
| Colestid Flavored 5 gm/7.5 gm Packets | 3.29 USD | packet |
| Colestid 5 g Powder Packet | 1.04 USD | packet |
| Colestid Orange 5 g Powder Packet | 1.04 USD | packet |
| Colestid 1 gm tablet | 0.86 USD | tablet |
| Colestipol hcl 1 gm tablet | 0.66 USD | tablet |
| Colestid 5 gm Granules | 0.33 USD | gm |
| Colestid Flavored 5 gm Granules | 0.31 USD | gm |
| Colestid flavored granules | 0.3 USD | g |
| Colestid 1 g Tablet | 0.29 USD | tablet |
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
|
适应症
hyperlipidemi 高血脂;
药理
| Indication | For use, as adjunctive therapy to diet, for the reduction of elevated serum total and LDL-C in patients with primary hypercholesterolemia (elevated LDL-C) who do not respond adequately to diet. |
| Pharmacodynamics | Cholesterol is the major, and probably the sole precursor of bile acids. During normal digestion, bile acids are secreted via the bile from the liver and gall bladder into the intestines. Bile acids emulsify the fat and lipid materials present in food, thus facilitating absorption. A major portion of the bile acids secreted is reabsorbed from the intestines and returned via the portal circulation to the liver, thus completing the enterohepatic cycle. Only very small amounts of bile acids are found in normal serum. Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces. This nonsystemic action results in a partial removal of the bile acids from the enterohepatic circulation, preventing their reabsorption. Since colestipol hydrochloride is an anion exchange resin, the chloride anions of the resin can be replaced by other anions, usually those with a greater affinity for the resin than the chloride ion. |
| Mechanism of action | Colestipol is a non-absorbed, lipid-lowering polymer that binds bile acids in the intestine, impeding their reabsorption. As the bile acid pool becomes depleted, the hepatic enzyme, cholesterol 7-(alpha)-hydroxylase, is upregulated, which increases the conversion of cholesterol to bile acids. This causes an increased demand for cholesterol in the liver cells, resulting in the dual effect of increasing transcription and activity of the cholesterol biosynthetic enzyme, hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase, and increasing the number of hepatic low-density lipoprotein (LDL) receptors. These compensatory effects result in increased clearance of LDL cholesterol (LDL-C) from the blood, resulting in decreased serum LDL-C levels. Serum triglyceride levels may increase or remain unchanged. The end result is increased clearance of LDL-cholesterol from the blood with decreased serum LDL-cholesterol. |
| Absorption | Not absorbed from the gastrointestinal tract. |
| Volume of distribution | Not Available |
| Protein binding | Not applicable (not hydrolyzed by digestive enzymes and not absorbed). |
| Metabolism |
Not applicable (not hydrolyzed by digestive enzymes and not absorbed). |
| Route of elimination | Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces. In humans, less than 0.17% of a single 14C-labeled colestipol hydrochloride dose is excreted in the urine when given following 60 days of chronic dosing of 20 grams of colestipol hydrochloride per day. The increased fecal loss of bile acids due to colestipol hydrochloride administration leads to an increased oxidation of cholesterol to bile acids. |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Oral LD50 in rats is > 1000 mg/kg. Symptoms of overdose may include eye irritation, constipation, abdominal cramps, nausea, vomiting, diarrhea, and hypersensitivity. However, as colestipol is not absorbed, the risk of systemic toxicity is low. |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | Not Available | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
|
||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
||||||||||||||||||||||||||||||||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Acenocoumarol | The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of acenocoumarol by decreasing its absorption. |
| Anisindione | The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of anisindione by decreasing its absorption. |
| Dicumarol | The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of dicumarol by decreasing its absorption. |
| Digoxin | The resin decreases the effect of digoxin |
| Fluvastatin | Increased/decreased effect according to spacing |
| Hydrocortisone | Cholestyramine decreases the effect of hydrocortisone |
| Levothyroxine | The resin, colestipol, decreases the absorption of the thyroid hormone, levothyroxine. |
| Liothyronine | The resin, colestipol, decreases the absorption of the thyroid hormone, liothyronine. |
| Liotrix | The resin, colestipol, decreases the absorption of the thyroid hormone, liotrix. |
| Raloxifene | The resin decreases the effect of raloxifene |
| Sulindac | The bile acid sequestrant, colestipol, may decrease the absorption of the NSAID, sulindac. Monitor for changes in the therapeutic and adverse effects of sulindac if colestipol 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. |
| Thyroglobulin | The resin, colestipol, decreases the absorption of the thyroid hormone, thyroglobulin. |
| Tiaprofenic acid | The bile acid sequestrant, Colestipol, may reduce Tiaprofenic acid absorption and therapeutic effect. |
| Tolmetin | Colestipol may decrease the absorption of Tolmetin. Monitor for changes in the therapeutic and adverse effects of Tolmetin if Colestipol is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction. |
| Torasemide | Colestipol may decrease the bioavailability of Torasemide by inhibiting Torasemide absorption. Monitor for changes in the therapeutic and adverse effects of Torasemide if Colestipol is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction. |
| Trichlormethiazide | The bile acid sequestrant, Colestipol, may inhibit the absorption of Trichlormethiazide. |
| Ursodeoxycholic acid | The resin decreases the effect of ursodiol |
| Warfarin | The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of warfarin by decreasing its absorption. |
食物相互作用
- Take with food.
收藏