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Bile Binding ResinAka: Cholestyramine, Colestipol, Colesevelam, Welchol

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  1. Effects
    1. LDL Cholesterol decreased (15-30%)
    2. HDL Cholesterol increased (3-5%)
    3. Triglycerides increased
  2. Efficacy
    1. Reduces Myocardial Infarction risk
      1. Eggertsen (1984) JAMA 251(3):349
  3. Adverse effects
    1. Gastrointestinal
      1. Effects
        1. Constipation
        2. Flatulence
        3. Dyspepsia
      2. Reduce Adverse GI side effects
        1. Use moderate doses: 8-10 g per day
        2. Increase Dietary Fiber or supplement with Psyllium
        3. Colesevelam may have less GI intolerance
    2. Interferes with fat soluble Vitamin Absorption
      1. Take vitamin 2 hours before or 4 hours after Resin
      2. Colesevelam does not affect Vitamin Absorption
  4. Contraindications
    1. Absolute: Triglycerides >500 mg/dl
    2. Relative: Triglycerides >200 mg/dl
  5. Preparations
    1. Cholestyramine (Questran)
      1. Dose: 4g (9g packet) bid ($54) MAX: 24 g/day
    2. Colestipol (Colestid)
      1. Dose: 5g bid ($47) MAX: 30 g/day
    3. Colesevelam (Welchol)
      1. Most expensive agent of the class
      2. May be preferred agent of class
        1. Lower adverse effect profile (see above)
        2. May be taken concurrently with Statin
        3. Lowers A1C by 0.5%
          1. Zieve (2007) Clin Ther 29(1):74
      3. Dosing
        1. One Dose: Six 325 mg tablets daily with food, liquid
        2. Two Doses: Three 325 mg tablets bid with food, liquid
  6. References
    1. (2000) Med Lett Drugs Ther 42:102

Cholestyramine (C0008402)

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)
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD002792
EnglishCholestyramine, CHOLESTYRAMINE PREPARATION, Cholestyramine product, Cholestyramine Resin, Colestyramin, Colestyramine, Colestyramine product
Spanishcolestiramina, resina de colestiramina
Parent ConceptsAnticholesteremic Agents (C0003277), Antilipemic Agents (C0003367), Quaternary Ammonium Compounds (C0578399), Polystyrenes (C0032604), Nephroprotective Agent (C1514117), Antilipidemic Agent (C1516000), Anion Exchange Resins (C0003072), Bile Acids (C0005390), Cholestyramine (C0008402), Ion Exchange Resins (C0022014), Bile acid sequestrant antilipemic agent (C0304522)
SourcesCSP, MSH, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Colestipol (C0009279)

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.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD003084
EnglishColestipol, COLESTIPOL PREPARATION
Spanishcolestipol
Parent ConceptsAntilipemic Agents (C0003367), Polyamines (C0032433), Polymers (C0032521), Anion Exchange Resins (C0003072), Ion Exchange Resins (C0022014), Bile acid sequestrant antilipemic agent (C0304522)
SourcesCSP, MSH, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


colesevelam (C0541155)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC107058
Englishcolesevelam, COLESEVELAM PREPARATION
Parent ConceptsAntilipemic Agents (C0003367), Bile acid sequestrant antilipemic agent (C0304522)
SourcesMSH, NDFRT, RXNORM, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Welchol (C0939530)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC107058
EnglishWelchol
SourcesMSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)



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