Colesevelam
- Atc Codes:C10AC04
- CAS Codes:182815-44-7#182815-43-6
- PHARMGKB ID:182815-44-7#182815-43-6
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Cholestagel; Bulgaria: Cholestagel; Cyprus: Cholestagel; Czech Republic: Cholestagel; Denmark: Cholestagel; Estonia: Cholestagel; Finland: Cholestagel; France: Cholestagel; Germany: Cholestagel; Greece: Cholestagel; Hungary: Cholestagel; Ireland: Cholestagel; Italy: Cholestagel; Latvia: Cholestagel; Lithuania: Cholestagel; Luxembourg: Cholestagel; Malta: Cholestagel; Netherlands: Cholestagel; Poland: Cholestagel; Portugal: Cholestagel; Romania: Cholestagel; Slovakia: Cholestagel; Slovenia: Cholestagel; Sweden: Cholestagel; UK: Cholestagel.
North America
USA: WelChol.
Drug combinations
Chemistry
Colesevelam Hydrochloride: (C~3~H~7~N)~m~(C~3~H~5~ClO)~n~(C~12~H~27~ClN~2~)~o~(C~13~H~27~N)~p~ xHCl. (1) 2-Propen-1-amine polymer with (chloromethyl)oxirane, N,N,N-trimethyl-6-(2-propenylamino)-1-hexanaminium chloride, and N-2-propenyl-1-decanamine, hydrochloride; (2) Allylamine polymer with 1-chloro-2,3-epoxypropane, [6-(allylamino)hexyl]trimethylammonium chloride and N-allyldecylamine, hydrochloride. CAS-182815-44-7; CAS-182815-43-6 (colesevelam)(1997).
Pharmacologic Category
Antilipemic Agents; Bile Acid Sequestrants. (ATC-Code: C10AC04).
Mechanism of action
Binds to bile acids in the intestine and forms a nonabsorbable complex. Thus, bile acids are partially removed from enterohepatic circulation and conversion of cholesterol to bile acids in the liver is increased. This enhanced demand for cholesterol in liver cells causes a compensatory increase in hepatic uptake (and thus systemic clearance) of circulating LDL-C. Serum total cholesterol, LDL-C, and APOB are reduced, and HDL-C concentrations increase. Serum triglyceride concentrations may remain unchanged or increase slightly (5-10%).
Therapeutic use
Elevated LDL in primary hypercholesterolemia (Fredrickson type IIa; alone or in combination with an HMG-CoA reductase inhibitor). Control of type 2 diabetes mellitus (non-insulin-dependent, in combination with insulin or oral antidiabetic agents).
Pregnancy and lactiation implications
There are no adequate studies in pregnant women. Use only in pregnancy if clearly needed. Excretion in breast milk unknown.
Unlabeled use
Contraindications
History of bowel obstruction. Serum triglyceride concentration >500 mg/dL. History of hypertriglyceridemia-induced pancreatitis.
Warnings and precautions
Use with caution in dysphagia, swallowing disorders, severe gastrointestinal motility disorders or major gastrointestinal tract surgery. Use with caution in treating patients with serum triglyceride concentrations >300 mg/dL (may cause increased concentrations). Minimal effects are seen on HDL-C and triglyceride concentrations. Use with caution in patients susceptible to fat-soluble vitamin deficiencies. Colesevelam is not indicated for the management of type 1 diabetes mellitus, particularly in acute management (it is also not indicated as monotherapy and must be used as an adjunct to insulin or oral antidiabetic agents).