Uses

Colesevelam is indicated as an adjunct to diet and exercise to reduce elevated LDL cholesterol in adults and children (10–17 years) with primary hyperlipidemia or heterozygous familial hypercholesterolemia. It is also used to improve glycemic control in adults with type 2 diabetes mellitus.

Do not use if

Contraindicated in patients with serum triglycerides above 500 mg/dL, a history of hypertriglyceridemia-induced pancreatitis, or a history of bowel obstruction.

Side effects

Common adverse reactions include constipation, dyspepsia, nausea, and flatulence. Hypertriglyceridemia may occur or worsen, potentially leading to acute pancreatitis. Fat-soluble vitamin deficiencies (A, D, E, K) may develop with prolonged use.

Warnings

Monitor triglyceride levels before and during therapy; discontinue if levels exceed 500 mg/dL. May reduce absorption of fat-soluble vitamins and certain oral medications including thyroid hormones and oral contraceptives; administer these at least 4 hours before colesevelam.

How it works

Colesevelam is a non-absorbed polymer that binds bile acids in the intestinal lumen, reducing their reabsorption. This depletes the hepatic bile acid pool, upregulating cholesterol 7-alpha-hydroxylase and LDL receptors, thereby lowering plasma LDL-C. Its mechanism for glycemic improvement in type 2 diabetes is not fully elucidated.

Storage

Store at controlled room temperature (20–25°C). Keep in original container, tightly closed, away from moisture.