DT-Web

DB01432 - Cholestyramine


Identification
Name Cholestyramine
Accession Number DB01432
Type small molecule
Description Cholestyramine or colestyramine is a bile acid sequestrant. Bile acid sequestrants are polymeric compounds which serve as ion exchange resins. Cholestyramine resin is quite hydrophilic, but insoluble in water.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight Not Available
Groups approved
Monoisotopic Weight Not Available
Pharmacology
Indication Indicated as adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet. Also for the relief of pruritus associated with partial biliary obstruction.
Mechanism of action Cholestyramine binds bile in the gastrointestinal tract to prevent its reabsorption. The resin is a strong anion exchange resin, which means that it can exchange its chloride anions with anionic bile acids in the gastrointestinal tract and bind them strongly in the resin matrix. The functional group of the anion exchange resin is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer.
Absorption Not absorbed from the gastrointestinal tract following oral administration.
Protein binding Not Available
Biotransformation Bile acids
Route of elimination Cholestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces.
Toxicity Overdose may result in blockage of intestine or stomach.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Acenocoumarol The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of acenocoumarol by decreasing its absorption.
Anisindione The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of anisindione by decreasing its absorption.
Bezafibrate Bile acid sequestrants like cholestyramine may decrease the absorption of fibric acid derivatives like bezafibrate. Therapy modification should be considered. If concomitant therapy is used, separate doses by at least 2 hours to minimize this interaction. Fenofibric acid labeling recommends administration one hour prior to or 4-6 hours after a bile acid sequestrant.
Chlorothiazide Bile acid sequestrants may decrease the absorption of thiazide diuretics such as chlorothiazide. The diuretic response is likewise decreased. Monitor for decreased therapeutic effects of thiazide diuretics if coadministered with a bile acid sequestrant. If these agents are used concomitantly, separate doses 2 or more hours to minimize the interaction.
Cholecalciferol Bile acid sequestrants such as cholestyramine may decrease the serum concentration of Vitamin D analogs such as cholecalciferol. More specifically, bile acid sequestrants may impair absorption of Vitamin D analogs. Avoid concomitant administration of vitamin D analogs and bile acid sequestrants. Monitor plasma calcium concentrations in patients receiving combined therapy with these agents. This is particularly important in patients receiving higher doses of a bile acid sequestant (i.e., 30 g/day or more of cholestyramine or equivalent) or in patients experiencing bile acid sequestrant-induced steatorrhea. Specific recommendations regarding the separation of administration of these agents are not defined; however, it would seem prudent to separate the administration of these agents by several hours to minimize the potential risk of interaction. Similar precautions do not apply to parenterally administered vitamin D analogs.
Dicumarol The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of dicumarol by decreasing its absorption.
Digoxin The resin decreases the effect of digoxin
Ezetimibe Cholestyramine may decrease the levels of ezetimibe.
Fluvastatin Increased/decreased effect according to spacing
Hydrocortisone Cholestyramine may decrease the effect of hydrocortisone.
Levothyroxine The resin, cholestyramine, decreases the absorption of the thyroid hormone, levothyroxine.
Liothyronine The resin, cholestyramine, decreases the absorption of the thyroid hormones, liothyronine.
Liotrix The resin, cholestyramine, decreases the absorption of the thyroid hormone, liotrix.
Lomitapide Bile acid sequestrants also used for treating high cholesterol may interfere with the absorption of oral medications, thus separate administration by 4 hours.
Methotrexate Decreased levels of methotrexate
Raloxifene The resin decreases the effect of raloxifene
Spironolactone Increased risk of acidosis and hyperkalemia
Sulindac The bile acid sequestrant, cholestyramine, may decrease the absorption of the NSAID, sulindac. Monitor for changes in the therapeutic and adverse effects of sulindac if cholestyramine 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.
Tenoxicam Cholestyramine may decrease the serum concentration of Tenoxicam by increasing clearance. Monitor for changes in Tenoxicam therapeutic and adverse effects if Cholestyramine is initiated, discontinued or dose changed.
Thyroglobulin The resin, cholestyramine, decreases the absorption of the thyroid hormone, thyroglobulin.
Tiaprofenic acid The bile acid sequestrant, Cholestyramine resin, may reduce Tiaprofenic acid absorption and therapeutic effect.
Tolmetin Cholestyramine may decrease the absorption of Tolmetin. Monitor for changes in the therapeutic and adverse effects of Tolmetin if Cholestyramine is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction.
Torasemide Cholestyramine may decrease the bioavailability of Torasemide by inhibiting Torasemide absorption. Monitor for changes in the therapeutic and adverse effects of Torasemide if Cholestyramine is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction.
Trichlormethiazide The bile acid sequestrant, Cholestyramine resin, may inhibit the absorption of Trichlormethiazide.
Troglitazone Decreases the effect of troglitazone
Ursodeoxycholic acid The resin decreases the effect of ursodiol
Warfarin The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of warfarin by decreasing its absorption.
Food Interactions
  • Take with food, do not mix with soft drinks.

Targets


Bile acids
Name Bile acids
Gene Name Not Available
Pharmacological action yes
Actions binder
References
  • Nichifor M, Cristea D, Mocanu G, Carpov A: Aminated polysaccharides as bile acid sorbents: in vitro study. J Biomater Sci Polym Ed. 1998;9(6):519-34. - Pubmed
  • Benson GM, Alston DR, Hickey DM, Jaxa-Chamiec AA, Whittaker CM, Haynes C, Glen A, Blanchard S, Cresswell SR, Suckling KE: SK&F 97426-A: a novel bile acid sequestrant with higher affinities and slower dissociation rates for bile acids in vitro than cholestyramine. J Pharm Sci. 1997 Jan;86(1):76-81. - Pubmed
DTHybrid score Not Available

Predictions


Id Partner name Gene Name Score
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