II. Effects

  1. LDL Cholesterol decreased (15-30%)
  2. HDL Cholesterol increased (3-5%)
  3. Triglycerides increased

III. Efficacy

  1. Lowers cardiovascular mortality by 30%
  2. Reduces Myocardial Infarction risk
    1. Eggertsen (1984) JAMA 251(3):349-50 [PubMed]

IV. 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

V. Contraindications

  1. Absolute
    1. Serum Triglycerides >500 mg/dl
    2. Bowel Obstruction
    3. Complete biliary obstruction
  2. Relative
    1. Triglycerides >200 mg/dl

VI. 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):74-83 [PubMed]
    3. Dosing
      1. One Dose: Six 325 mg tablets daily with food, liquid
      2. Two Doses: Three 325 mg tablets bid with food, liquid

VII. Drug Interactions

  1. Take at least 2 hours apart from Warfarin, Digoxin and Amiodarone
  2. Take with water or orange juice before meals

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Cost: Medications

cholestyramine (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
CHOLESTYRAMINE LIGHT PACKET Generic $1.90 each
CHOLESTYRAMINE LIGHT POWDER Generic $0.23 per gram
CHOLESTYRAMINE PACKET Generic $1.66 each
CHOLESTYRAMINE POWDER Generic $0.21 per gram
colestipol (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
COLESTIPOL HCL 1 GM TABLET Generic $0.83 each
COLESTIPOL HCL GRANULES PACKET Generic $2.93 each
COLESTIPOL MICRONIZED 1 GM TAB Generic $0.83 each
welchol (on 5/17/2017 at Medicaid.Gov Survey of pharmacy drug pricing)
WELCHOL 3.75G PACKET $19.08 each
WELCHOL 625 MG TABLET $3.17 each

Ontology: Cholestyramine Resin (C0008402)

Definition (MSH) A strongly basic anion exchange resin whose main constituent is polystyrene trimethylbenzylammonium Cl(-) anion.
Definition (NCI) An anion exchange resin with hypolipidemic activity. Cholestyramine resin adsorbs and combines with bile acids in the intestine to form an insoluble complex, which is then excreted in the feces, 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.
Definition (CSP) strongly basic anion exchange resin used to extract bile salts and cholesterol, to treat diarrhea and biliary obstruction, and as an antipruritic.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D002792
SnomedCT 72824008, 317391006, 319945002, 387408001
English Colestyramin, Colestyramine, Resin, Cholestyramine, Cholestyramine [diarr], Cholestyramine [lipid low], Cholestyramine [antidiarrheal use], Cholestyramine [antidiarrhoeal use], Cholestyramine [lipid lowering use], cholestyramine, cholestyramine (medication), Cholestyramine Resins, Cholestyramines, Cholestyramine Resin, Cholestyramine, Colestyramins, Resins, Cholestyramine, Colestyramines, CHOLESTYRAMINE, Cholestyramine Resin [Chemical/Ingredient], cholestyramine resin, colestyramine, Colestyramine [antidiarrheal use], Cholestyramine [lipid lowering use] (product), Cholestyramine [antidiarrheal use] (product), Colestyramine [lipid lowering use], Colestyramine [antidiarrhoeal use], Cholestyramine resin, Cholestyramine product, Cholestyramine (product), Cholestyramine (substance), Cholestyramine [antidiarrheal use] (substance), Cholestyramine [lipid lowering use] (substance), Colestyramine product
Finnish Kolestyramiini
Russian KHOLESTIRAMIN, KOLESTIRAMIN, ХОЛЕСТИРАМИНОВАЯ СМОЛА, ХОЛЕСТИРАМИН, KHOLESTIRAMINOVAIA SMOLA, MK-135, КОЛЕСТИРАМИН
Japanese コレスチラミン樹脂, クエストラン, コレスチラミン
French Colestyramine, Résine de cholestyramine, Cholestyramine
Italian Colestiramina, Resina colestiramina
Portuguese Colestiramina, Resina de Colestiramina, Resina Colestiramina
Spanish Colestiramina, Resina de Colestiramina, colestiramina [uso como antidiarreico] (producto), colestiramina [uso como antidiarreico], colestiramina (como hipolipemiante), colestiramina (como hipolipemiante) (producto), colestiramina (producto), colestiramina (sustancia), colestiramina (uso como hipolipemiante) (producto), colestiramina (uso como hipolipemiante), colestiramina, resina de colestiramina
Croatian KOLESTIRAMIN
Swedish Kolestyraminresin
Czech cholestyraminová pryskyřice, cholestyramin
Polish Cholestyramina, Żywica cholestyraminowa
Norwegian Kolestyramin
German Cholestyramin-Harz, Cholestyramin, Colestyramin

Ontology: Colestipol (C0009279)

Definition (NCI) A positively charged, non-digestible, triamine and epoxypropane copolymer anion-exchange resin that binds to bile acids in the intestine to form an insoluble complex, which is excreted in the feces.
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 Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D003084
SnomedCT 372811005, 66971004
English Colestipol, colestipol, Colestipol [Chemical/Ingredient], COLESTIPOL, Colestipol (product), Colestipol (substance)
Swedish Kolestipol
Czech kolestipol
Finnish Kolestipoli
Russian KOLESTIPOL, КОЛЕСТИПОЛ
Japanese コレスチポール
Polish Kolestipol
Norwegian Kolestipol
Spanish colestipol (producto), colestipol (sustancia), colestipol, Colestipol
French Colestipol
German Colestipol
Italian Colestipolo
Portuguese Colestipol

Ontology: colesevelam (C0541155)

Definition (NCI) A non-absorbed polymer that binds bile acids in the intestine, impedes their reabsorption and lowers serum lipids. In patients with type 2 diabetes mellitus, colesevelam also lowers blood glucose levels by an unknown mechanism.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C107058
SnomedCT 442510005, 441851004
English Colesevelam, Colesevelam (substance), Colesevelam (product), colesevelam [Chemical/Ingredient], colesevelam, Allylamine Polymer with 1-chloro-2,3-epoxypropane, (6-(allylamino)hexyl)trimethylammonium Chloride and N-allyldecylamine, COLESEVELAM
Spanish colesevelam, colesevelam (sustancia), colesevelam (producto)

Ontology: Welchol (C0939530)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C107058
English Welchol, welchol