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PubChem Substance
Name: Cholestyramine Resin
PubChem Substance ID: 168195
Description: A strongly basic anion exchange resin whose main constituent is polystyrene trimethylbenzylammonium Cl(-) anion.
CHOLESTYRAMINE RESIN; Cuemid; Questran; Colestyraminum [INN-Latin]; Quantalan; Duolite AP-143 Resin; Questran Light; Cholestyramine resin [USAN]; 9007-26-5; Cholestyramine chloride.
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Name: Cholestyramine Resin
Name (isomeric): DB01432
Drug Type: small molecule
Description: A strongly basic anion exchange resin whose main constituent is polystyrene trimethylbenzylammonium Cl(-) anion.
Brand: Novo-Cholamine Light, Locholest, Cholybar, Prevalite, PMS Cholestyramine, Novo-Cholamine, Locholest light, Questran Light, Questran
Category: Cholesterol Absorption Inhibitors, Antihyperlipidemics, Anticholesteremic Agents
CAS number: 11041-12-6
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.
Cholesterol is probably the sole precursor of bile acids. During normal digestion, bile acids are secreted into the intestines. A major portion of the bile acids is absorbed from the intestinal tract and returned to the liver via the enterohepatic circulation. Only very small amounts of bile acids are found in normal serum. Cholestyramine resin ads...
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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 ammon...
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Absorption: Not absorbed from the gastrointestinal tract following oral administration.
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.
Half Life: 6 minutes
Toxicity: Overdose may result in blockage of intestine or stomach.
Affected organisms: Humans and other mammals
Food interaction:
Take with food, do not mix with soft drinks.
Drug interaction:
BezafibrateBile 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.
TenoxicamCholestyramine 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.
AcenocoumarolThe bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of acenocoumarol by decreasing its absorption.
FluvastatinIncreased/decreased effect according to spacing
CholecalciferolBile 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.
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