QuickView for Cholestyramine (compound)

Summary
General Info

PubChem Substance

Name:	Cholestyramine Resin
PubChem Substance ID:	168195
Description:	A strongly basic anion exchange resin whose main constituent is polystyrene trimethylbenzylammonium Cl(-) anion.
Synonyms:	CHOLESTYRAMINE RESIN; Cuemid; Questran; Colestyraminum [INN-Latin]; Quantalan; Duolite AP-143 Resin; Questran Light; Cholestyramine resin [USAN]; 9007-26-5; Cholestyramine chloride. show more » CHOLESTYRAMINE RESIN; Cuemid; Questran; Colestyraminum [INN-Latin]; Quantalan; Duolite AP-143 Resin; Questran Light; Cholestyramine resin [USAN]; 9007-26-5; Cholestyramine chloride; Cholybar; 11041-12-6; Polystyrene benzyltrimethylaminonium chloride; Cholestyramine; Colestyramin; Colestiramina [INN-Spanish]; EINECS 234-270-8; CCRIS 725; HSDB 7219 show less «

DrugBank

Identification

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.
Synonyms:	Colestyramine
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

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.
Pharmacology:	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... show more » 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 adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. This results in a partial removal of bile acids from the enterohepatic circulation by preventing their absorption. show less «
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... show more » 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. show less «
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

Interactions

Food interaction:

Take with food, do not mix with soft drinks.

Drug interaction:

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.
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.
Acenocoumarol	The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of acenocoumarol by decreasing its absorption.
Fluvastatin	Increased/decreased effect according to spacing
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.

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.
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.
Acenocoumarol	The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of acenocoumarol by decreasing its absorption.
Fluvastatin	Increased/decreased effect according to spacing
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.
Thyroglobulin	The resin, cholestyramine, decreases the absorption of the thyroid hormone, thyroglobulin.
Ursodeoxycholic acid	The resin decreases the effect of ursodiol
Liotrix	The resin, cholestyramine, decreases the absorption of the thyroid hormone, liotrix.
Levothyroxine	The resin, cholestyramine, decreases the absorption of the thyroid hormone, levothyroxine.
Hydrocortisone	Cholestyramine may decrease the effect of hydrocortisone.
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.
Liothyronine	The resin, cholestyramine, decreases the absorption of the thyroid hormones, liothyronine.
Trichlormethiazide	The bile acid sequestrant, Cholestyramine resin, may inhibit the absorption of Trichlormethiazide.
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.
Methotrexate	Decreased levels of methotrexate
Tiaprofenic acid	The bile acid sequestrant, Cholestyramine resin, may reduce Tiaprofenic acid absorption and therapeutic effect.
Digoxin	The resin decreases the effect of digoxin
Spironolactone	Increased risk of acidosis and hyperkalemia
Warfarin	The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of warfarin by decreasing its absorption.
Troglitazone	Decreases the effect of troglitazone
Divalproex sodium	Cholestyramine decreases the levels of valproate
Dicumarol	The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of dicumarol by decreasing its absorption.
Ezetimibe	Cholestyramine may decrease the levels of ezetimibe.
Anisindione	The bile acid sequestrant, cholestyramine, may decrease the anticoagulant effect of anisindione by decreasing its absorption.
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.
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.
Raloxifene	The resin decreases the effect of raloxifene

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Targets

Bile acids