Colestipol

Colestipol is a bile acid sequestrant used to reduce low-density lipoprotein (LDL) cholesterol in adults and children with hypercholesterolemia. It is an insoluble anion-exchange resin that binds bile acids in the intestinal lumen, forming complexes that are excreted in feces. By interrupting bile acid reabsorption, colestipol lowers the hepatic bile acid pool and promotes upregulation of hepatic LDL receptors, producing a decline in circulating LDL cholesterol.

Indications include primary hypercholesterolemia or mixed dyslipidemia in patients who require additional LDL reduction beyond diet and lifestyle, or who cannot tolerate or respond adequately to statins. It is used as adjunctive therapy and is not a first-line monotherapy for most patients.

Dosing and administration: colestipol is available as tablets (commonly 5 g) and as a powder for suspension. Typical starting dose is 5 g daily, gradually titrating to 10–20 g daily in divided doses with meals; maximum dosing is generally around 30 g per day in divided doses. Tablets should be taken with plenty of water to prevent choking or GI discomfort and to aid bowel movement.

Pharmacology and interactions: colestipol is not absorbed. It can interfere with the absorption of other drugs and fat-soluble vitamins; separate administration by at least 1 hour before or 4–6 hours after colestipol. Monitoring includes lipid panels and vitamin status when appropriate.

Contraindications and safety: contraindicated in complete biliary obstruction or intestinal obstruction. Use with caution in significant hypertriglyceridemia. Common adverse effects include constipation, flatulence, abdominal fullness, and a bitter taste; rarer hypersensitivity reactions can occur.