Name: | colesevelam |
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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
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Name: | colesevelam |
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Name (isomeric): | DB00930 |
Drug Type: | small molecule |
Synonyms: |
Colesevelam hydrochloride
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Brand: | Welchol, CholestaGel |
Category: | Bile acid sequestrants, Anticholesteremic Agents |
CAS number: | 182815-44-7 |
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). |
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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 |
Food interaction: |
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Drug interaction: |
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