Class: Hypolipidemic, Bile Acid Sequestrant
Dosage Forms. Tablet: 625 mg; Granules for Suspension: 3.75 g/packet
Common FDA Label Indication, Dosing, and Titration.
1. Primary hyperlipidemia: 1875 mg (3 tablets or 1.875 g powder packet) po bid or 3750 mg (6 tablets or 3.75 g powder packet) po daily
1. Familial hypercholesterolemia: 1875 mg (3 tablets or 1.875 g powder packet) po bid or 3750 mg (6 tablets or 3.75 g powder packet) po daily
MOA. Colesevelam is a nonabsorbed, polymeric, lipid-lowering agent that binds intestinal bile acids, resulting in the increased clearance of LDL-cholesterol and a reduction of total cholesterol. Unlike cholestyramine and colestipol, colesevelam is not an anion exchange resin but binds bile acids and impedes their reabsorption.
Drug Characteristics: Colesevelam
Medication Safety Issues: Colesevelam
Drug Interactions: Colesevelam
Adverse Reactions: Colesevelam
Efficacy Monitoring Parameters. Reduction in total cholesterol, LDL-cholesterol, and triglycerides levels; increase in HDL-cholesterol levels.
Toxicity Monitoring Parameters. Signs/symptoms of gastrointestinal side effects, vitamin A, D, E, or K deficiencies.
Key Patient Counseling Points. Should be used together with diet and exercise to lower cholesterol levels. Empty contents of powder packet into a glass and mix with 4-8 ounces of water; stir well and drink. Oral suspension should not be taken in its dry form. Take with a meal. Tablet should be swallowed with liquid (water, milk, or juice). May be dosed concomitantly with an HMG-CoA reductase inhibitor.
Clinical Pearls. Safety and efficacy not established in pediatric patients younger than 10 y of age or in premenarcheal girls. Patients with difficulty swallowing should use oral suspension instead of tablets.