Colesevelam
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|
| Clinical data | |
|---|---|
| Trade names | Welchol, Cholestagel |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a699050 |
| Pregnancy category |
|
| Routes of administration |
Oral |
| ATC code | C10AC04 (WHO) |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Bioavailability | N/A |
| Metabolism | Colesevelam is not absorbed and not metabolised. |
| Biological half-life | N/A (non-systemic drug) |
| Excretion | By intestines only, colesevelam is non-systemic. |
| Identifiers | |
|
|
| CAS Number |
182815-43-6 
|
| PubChem (CID) | 160051 |
| DrugBank |
DB00930 
|
| ChemSpider | none |
| UNII |
1XU104G55N
|
| KEGG |
D03582
|
| ChEMBL |
CHEMBL1201677
|
| ECHA InfoCard | 100.234.276 |
| Chemical and physical data | |
| Formula | C31H67Cl3N4O |
| Molar mass | 618.24888 g/mol |
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Colesevelam is a bile acid sequestrant administered orally. It was developed by GelTex Pharmaceuticals and later acquired by Genzyme. It is marketed in the US by Daiichi Sankyo under the brand name Welchol and elsewhere by Genzyme as Cholestagel. In Canada it is marketed by Valeant as Lodalis.
Colesevelam is indicated as an adjunct to diet and exercise to reduce elevated low-density lipoprotein cholesterol (LDL-C) in patients with primary hyperlipidemia as monotherapy and to improve glycemic control in adults with type 2 diabetes mellitus, including in combination with a statin. The expanded use of colesevelam in adults with type 2 diabetes mellitus is an example of drug repositioning.
Colesevelam is one of the bile-acid sequestrants, which along with niacin and the statins, are the three main types of cholesterol-lowering agents. The statins are considered the first-line agents. This is because of the larger body of evidence supporting statins' ability to prevent cardiovascular disease, as well as the prominent side effects from the other two types, including bloating and constipation (bile-acid sequestrants) and skin flushing (niacin). These side effects often lead to low patient compliance.
Colesevelam can be used instead of cholestyramine in symptomatic chronic diarrhea due to bile salt malabsorption (bile acid diarrhea), which can be a primary condition, or secondary to Crohn's disease or the postcholecystectomy syndrome.
Colesevelam is a modified polyallylamine. It is made by crosslinking polyallylamine with epichlorohydrin, and then modifying it with bromodecane and (6-bromohexyl)trimethylammonium bromide. The bromide ions are then replaced with chloride ions when the material is washed.
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Wikipedia