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Bile Binding ResinAka: Cholestyramine, Colestipol, Colesevelam, Welchol
- Effects
- LDL Cholesterol decreased (15-30%)
- HDL Cholesterol increased (3-5%)
- Triglycerides increased
- Efficacy
- Reduces Myocardial Infarction risk
- Eggertsen (1984) JAMA 251(3):349
- Adverse effects
- Gastrointestinal
- Effects
- Constipation
- Flatulence
- Dyspepsia
- Reduce Adverse GI side effects
- Use moderate doses: 8-10 g per day
- Increase Dietary Fiber or supplement with Psyllium
- Colesevelam may have less GI intolerance
- Interferes with fat soluble Vitamin Absorption
- Take vitamin 2 hours before or 4 hours after Resin
- Colesevelam does not affect Vitamin Absorption
- Contraindications
- Absolute: Triglycerides >500 mg/dl
- Relative: Triglycerides >200 mg/dl
- Preparations
- Cholestyramine (Questran)
- Dose: 4g (9g packet) bid ($54) MAX: 24 g/day
- Colestipol (Colestid)
- Dose: 5g bid ($47) MAX: 30 g/day
- Colesevelam (Welchol)
- Most expensive agent of the class
- May be preferred agent of class
- Lower adverse effect profile (see above)
- May be taken concurrently with Statin
- Lowers A1C by 0.5%
- Zieve (2007) Clin Ther 29(1):74
- Dosing
- One Dose: Six 325 mg tablets daily with food, liquid
- Two Doses: Three 325 mg tablets bid with food, liquid
- References
- (2000) Med Lett Drugs Ther 42:102
Cholestyramine (C0008402)
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| Definition (MSH) | A strongly basic anion exchange resin whose main constituent is polystyrene trimethylbenzylammonium as Cl(-) anion. It exchanges chloride ions with bile salts, thus decreasing their concentration and that of cholesterol. It is used as a hypocholesteremic in diarrhea and biliary obstruction, and as an antipruritic. |
| Definition (CSP) | strongly basic anion exchange resin used to extract bile salts and cholesterol, to treat diarrhea and biliary obstruction, and as an antipruritic. |
| Definition (NCI) | An anion exchange resin. Cholestyramine resin adsorbs and combines with bile acids in the intestine to form an insoluble complex, which is then excreted in the feces. As a result, the absorption of bile acids from the enterohepatic circulation is partially prevented, resulting in an increased oxidation of cholesterol to bile acids, a decrease in low density lipoprotein in the plasma, and a decrease in serum cholesterol levels. Cholestyramine also increases the elimination of methotrexate and leflunomide, thereby potentially decreasing related toxicities. (NCI04) |
| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | Cholestyramine, CHOLESTYRAMINE PREPARATION, Cholestyramine product, Cholestyramine Resin, Colestyramin, Colestyramine, Colestyramine product |
| Spanish | colestiramina, resina de colestiramina |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Definition (MSH) | Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels. |
| Definition (CSP) | highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic, it may also may reduce triglyceride levels. |
| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
|
| English | Colestipol, COLESTIPOL PREPARATION |
| Spanish | colestipol |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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| Concepts | Organic Chemical (T109)
, Pharmacologic Substance (T121)
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| English | colesevelam, COLESEVELAM PREPARATION |
| Credits | Derived from the NIH UMLS (Unified Medical Language System)
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