药品详细
Colesevelam (Colesevelam )
化学结构式图
中文名
Colesevelam
英文名
Colesevelam
分子式
Not Available
化学名
分子量
Not Available
CAS号
182815-44-7
ATC分类
C10A 未知
药物类型
small molecule
阶段
商品名
CholestaGel;Welchol;
同义名
Colesevelam hydrochloride;
基本介绍
Colesevelam is a bile acid sequestrant. Colesevelam is used with exercise and diet changes (restriction of cholesterol and fat intake) to reduce the amount of cholesterol and certain fatty substances in the blood. It works by binding bile acids in the intestine. Bile acids are made when cholesterol is broken down in the body. Removing these bile acids helps to lower blood cholesterol.
生产厂家
- Daiichi sankyo inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Tablet, film coated | Oral |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Welchol 625 mg tablet | 1.96 USD | tablet |
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
|
适应症
Diabetes 糖尿病;hyperlipidemi 高血脂;
药理
| Indication | For use, alone or in combination with an HMG-CoA reductase inhibitor, as adjunctive therapy to diet and exercise for the reduction of elevated LDL cholesterol in patients with primary hypercholesterolemia (Fredrickson Type IIa). |
| Pharmacodynamics | Colesevelam is a high capacity bile-acid binding molecule. Colesevelam binds to bile acids in the intestine which reduces the amount of bile acids that are returned to the liver via enterohepatic circulation. Clinical studies have demonstrated that elevated levels of total cholesterol (total-C), LDL-C, and apolipoprotein B (Apo B, a protein associated with LDL-C) are associated with an increased risk of atherosclerosis in humans. Similarly, decreased levels of high-density lipoprotein cholesterol (HDL-C) are associated with the development of atherosclerosis. Epidemiological investigations have established that cardiovascular morbidity and mortality vary directly with the levels of total-C and LDL-C, and inversely with the level of HDL-C. The combination of colesevelam and an HMG-CoA reductase inhibitor is effective in further lowering serum total-C and LDL-C levels beyond that achieved by either agent alone. |
| Mechanism of action | Colesevelam 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 hydrolyzed by digestive enzymes and is not absorbed. |
| 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 | Excretion: In 16 healthy volunteers, an average of 0.05% of administered radioactivity from a single 14C-labeled colesevelam hydrochloride dose was excreted in the urine. |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Symptoms of overdose may include eye irritation, constipation, abdominal cramps, nausea, vomiting, diarrhea, and hypersensitivity. However, as colesevelam is not absorbed, the risk of systemic toxicity is low. Doses in excess of 4.5 g per day have not been tested. |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | |||||||
|---|---|---|---|---|---|---|---|
| State | solid | ||||||
| Melting point | Not Available | ||||||
| Experimental Properties |
|
||||||
| Predicted Properties | Not Available | ||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Sulindac | The bile acid sequestrant, colesevelam, may decrease the absorption of the NSAID, sulindac. Sulindac should be administered at least 1 hour before or 4 hours after colesevelam. Monitor for changes in the therapeutic and adverse effects of sulindac if colesevelam is initiated, discontinued or dose changed. |
| Tiaprofenic acid | The bile acid sequestrant, Colesevelam, may reduce Tiaprofenic acid absorption and therapeutic effect. |
| Tolmetin | Colesevelam may decrease the absorption of Tolmetin. Monitor for changes in the therapeutic and adverse effects of Tolmetin if Colesevelam is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction. |
| Torasemide | Colesevelam may decrease the bioavailability of Torasemide by inhibiting Torasemide absorption. Monitor for changes in the therapeutic and adverse effects of Torasemide if Colesevelam is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction. |
| Trichlormethiazide | The bile acid sequestrant, Colesevelam, may inhibit the absorption of Trichlormethiazide. |
食物相互作用
- Drink liberally.
- Take with a meal.
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