QuickView for Colestipol (compound)

Summary
General Info

PubChem

PubChem Compound 3084661

Name:	Colestipol
PubChem Compound ID:	3084661
Description:	Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels.
Molecular formula:	C₈H₂₄ClN₅
Molecular weight:	225.763 g/mol
Synonyms:	Lestid; Copolymer of diethylenetriamine and 1-chloro-2,3-epoxypropane, hydrochloride (with approximately 1 out of 5 amine nitrogens protonated); Colestid; Cholestabyl; Colestipol hydrochloride [USAN]; U-26597A; Colestipol hydrochloride; 37296-80-3

DrugBank

Identification

Name:	Colestipol
Name (isomeric):	DB00375
Drug Type:	small molecule
Description:	Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels.
Synonyms:	Colestipolum [INN-Latin]
Brand:	Colestid, Cholestabyl
Category:	Antilipemic Agents, Anion Exchange Resins
CAS number:	50925-79-6

Pharmacology

Indication:	For use, as adjunctive therapy to diet, for the reduction of elevated serum total and LDL-C in patients with primary hypercholesterolemia (elevated LDL-C) who do not respond adequately to diet.
Pharmacology:	Cholesterol is the major, and probably the sole precursor of bile acids. During normal digestion, bile acids are secreted via the bile from the liver and gall bladder into the intestines. Bile acids emulsify the fat and lipid materials present in food, thus facilitating absorption. A major portion of the bile acids secreted is reabsorbed from the i... show more » Cholesterol is the major, and probably the sole precursor of bile acids. During normal digestion, bile acids are secreted via the bile from the liver and gall bladder into the intestines. Bile acids emulsify the fat and lipid materials present in food, thus facilitating absorption. A major portion of the bile acids secreted is reabsorbed from the intestines and returned via the portal circulation to the liver, thus completing the enterohepatic cycle. Only very small amounts of bile acids are found in normal serum. Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces. This nonsystemic action results in a partial removal of the bile acids from the enterohepatic circulation, preventing their reabsorption. Since colestipol hydrochloride is an anion exchange resin, the chloride anions of the resin can be replaced by other anions, usually those with a greater affinity for the resin than the chloride ion. show less «
Mechanism of Action:	Colestipol is a non-absorbed, lipid-lowering polymer that binds bile acids in the intestine, impeding their reabsorption. As the bile acid pool becomes depleted, the hepatic enzyme, cholesterol 7-(alpha)-hydroxylase, is upregulated, which increases the conversion of cholesterol to bile acids. This causes an increased demand for cholesterol in the l... show more » Colestipol is a non-absorbed, lipid-lowering polymer that binds bile acids in the intestine, impeding their reabsorption. As the bile acid pool becomes depleted, the hepatic enzyme, cholesterol 7-(alpha)-hydroxylase, is upregulated, which increases the conversion of cholesterol to bile acids. This causes an increased demand for cholesterol in the liver cells, resulting in the dual effect of increasing transcription and activity of the cholesterol biosynthetic enzyme, hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase, and increasing the number of hepatic low-density lipoprotein (LDL) receptors. These compensatory effects result in increased clearance of LDL cholesterol (LDL-C) from the blood, resulting in decreased serum LDL-C levels. Serum triglyceride levels may increase or remain unchanged. The end result is increased clearance of LDL-cholesterol from the blood with decreased serum LDL-cholesterol. show less «
Absorption:	Not absorbed from the gastrointestinal tract.
Protein binding:	Not applicable (not hydrolyzed by digestive enzymes and not absorbed).
Biotransformation:	Not applicable (not hydrolyzed by digestive enzymes and not absorbed).
Route of elimination:	Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces. In humans, less than 0.17% of a single 14C-labeled colestipol hydrochloride dose is excreted in the urine when given following 60 days of chronic dosing of 20 grams of colestipol hydrochloride per day. The increased fecal loss of bile acids due to colestipol hydrochloride administration leads to an increased oxidation of cholesterol to bile acids.
Toxicity:	Oral LD₅₀ in rats is > 1000 mg/kg. Symptoms of overdose may include eye irritation, constipation, abdominal cramps, nausea, vomiting, diarrhea, and hypersensitivity. However, as colestipol is not absorbed, the risk of systemic toxicity is low.
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Take with food.

Drug interaction:

Thyroglobulin	The resin, colestipol, decreases the absorption of the thyroid hormone, thyroglobulin.
Liothyronine	The resin, colestipol, decreases the absorption of the thyroid hormone, liothyronine.
Warfarin	The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of warfarin by decreasing its absorption.
Torasemide	Colestipol may decrease the bioavailability of Torasemide by inhibiting Torasemide absorption. Monitor for changes in the therapeutic and adverse effects of Torasemide if Colestipol is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction.
Cholecalciferol	Bile acid sequestrants such as colestipol 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, colestipol, decreases the absorption of the thyroid hormone, thyroglobulin.
Liothyronine	The resin, colestipol, decreases the absorption of the thyroid hormone, liothyronine.
Warfarin	The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of warfarin by decreasing its absorption.
Torasemide	Colestipol may decrease the bioavailability of Torasemide by inhibiting Torasemide absorption. Monitor for changes in the therapeutic and adverse effects of Torasemide if Colestipol is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction.
Cholecalciferol	Bile acid sequestrants such as colestipol 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.
Liotrix	The resin, colestipol, decreases the absorption of the thyroid hormone, liotrix.
Fluvastatin	Increased/decreased effect according to spacing
Tolmetin	Colestipol may decrease the absorption of Tolmetin. Monitor for changes in the therapeutic and adverse effects of Tolmetin if Colestipol is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction.
Ursodeoxycholic acid	The resin decreases the effect of ursodiol
Anisindione	The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of anisindione by decreasing its absorption.
Tiaprofenic acid	The bile acid sequestrant, Colestipol, may reduce Tiaprofenic acid absorption and therapeutic effect.
Trichlormethiazide	The bile acid sequestrant, Colestipol, may inhibit the absorption of Trichlormethiazide.
Sulindac	The bile acid sequestrant, colestipol, may decrease the absorption of the NSAID, sulindac. Monitor for changes in the therapeutic and adverse effects of sulindac if colestipol 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.
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.
Hydrocortisone	Cholestyramine decreases the effect of hydrocortisone
Dicumarol	The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of dicumarol by decreasing its absorption.
Raloxifene	The resin decreases the effect of raloxifene
Acenocoumarol	The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of acenocoumarol by decreasing its absorption.
Levothyroxine	The resin, colestipol, decreases the absorption of the thyroid hormone, levothyroxine.
Digoxin	The resin decreases the effect of digoxin

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Targets

Bile acids