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QuickView for Colesevelam (compound)


PubChem
Name: colesevelam
PubChem Compound ID: 160051
Molecular formula: C31H67Cl3N4O
Molecular weight: 618.248 g/mol
Synonyms:
LS-74936; 1-Hexaminium, N,N,N-trimethyl-6-(2-propenylamino)-, chloride, polymer with (chloromethyl)oxirane, 2-propen-4-amine and N-2-propenyl-1-decanamine, hydrochloride; GT 31-104HB; Welchol; GT 31-104; 182815-44-7; GT31-104; CholestaGel; Colesevelam hydrochloride
DrugBank
Identification
Name: colesevelam
Name (isomeric): DB00930
Drug Type: small molecule
Synonyms:
Colesevelam hydrochloride
Brand: Welchol, CholestaGel
Category: Bile acid sequestrants, Anticholesteremic Agents
CAS number: 182815-44-7
Pharmacology
Indication: For use, alone or in combination with an HMG-CoA reductase inhibitor, as adjunctive therapy to diet and exercise for the reduction of elevated LDL cholesterol in patients with primary hypercholesterolemia (Fredrickson Type IIa).
Pharmacology:
Colesevelam is a high capacity bile-acid binding molecule. Colesevelam binds to bile acids in the intestine which reduces the amount of bile acids that are returned to the liver via enterohepatic circulation. Clinical studies have demonstrated that elevated levels of total cholesterol (total-C), LDL-C, and apolipoprotein B (Apo B, a protein associa...
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Mechanism of Action:
Colesevelam 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 ...
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Absorption: Not hydrolyzed by digestive enzymes and is not absorbed.
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: Excretion: In 16 healthy volunteers, an average of 0.05% of administered radioactivity from a single 14C-labeled colesevelam hydrochloride dose was excreted in the urine.
Toxicity: Symptoms of overdose may include eye irritation, constipation, abdominal cramps, nausea, vomiting, diarrhea, and hypersensitivity. However, as colesevelam is not absorbed, the risk of systemic toxicity is low. Doses in excess of 4.5 g per day have not been tested.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Drink liberally.
Take with a meal.
Drug interaction:
Chenodeoxycholic acidBile Acid Sequestrants may decrease the serum concentration of Chenodiol. Consider administration of chenodiol 5 hours or more after bile acid sequestrants to reduce chenodiol adsorption in the gastrointestinal tract. Monitor for decreased therapeutic effects of chenodiol in patients receiving bile acid sequestrants.
KetorolacBile acid sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Monitor for decreased serum concentrations/therapeutic effects of nonsteroidal anti-inflammatory agents (NSAID) if coadministered with bile acid sequestrants. Separating the administration of doses by 2 or more hours may reduce (but not eliminate) the risk of interaction. The manufacturer of colesevelam recommends that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
PhenytoinColesevelam may decrease the serum concentration of Phenytoin. Phenytoin should be administered at least 4 hours prior to colesevelam.
CalcitriolBile acid sequestrants such as colesevelam may decrease the serum concentration of Vitamin D Analogs. More specifically, bile acid sequestrants may impair absorption of Vitamin D Analogs. Avoid concomitant administration of vitamin D analogs and bile acid sequestrants (e.g., cholestyramine). 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.
DemeclocyclineBile acid sequestrants such as colesevelam may decrease the absorption of Tetracycline Derivatives. Monitor for decreased therapeutic effects of tetracycline derivatives if coadministered with a bile acid sequestrant. If these agents are used concomitantly, separate doses 2 or more hours to minimize the interaction. The manufacturer of colesevelam suggests that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
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Targets