What is the use of Colestipol (Bile Acid Sequestrant)?

From the Guidelines

Colestipol is a recommended bile acid sequestrant for lowering LDL cholesterol levels in patients with hyperlipidemia, particularly for those who cannot tolerate statins or require additional cholesterol-lowering therapy, as supported by the 2022 ACC expert consensus decision pathway 1.

Mechanism of Action and Dosage

Colestipol works by binding to bile acids in the intestines, preventing their reabsorption, and causing the body to use cholesterol to make more bile acids, which ultimately reduces cholesterol levels in the bloodstream. The typical dosage ranges from 5 to 30 grams daily, usually divided into two doses and taken before meals with plenty of fluid.

Efficacy and Safety

Colestipol has been shown to reduce LDL cholesterol levels by 18-25% when used as monotherapy, and it can also augment the LDL-lowering effects of other drugs, such as statins 1. However, it may cause gastrointestinal side effects, such as constipation, bloating, and gas, and can also reduce the absorption of certain medications and fat-soluble vitamins.

Clinical Use

Colestipol is particularly useful for patients who cannot tolerate statins or need additional cholesterol-lowering therapy. It primarily reduces LDL (bad) cholesterol while having minimal effect on HDL (good) cholesterol or triglycerides. This medication is not recommended for patients with complete biliary obstruction and requires regular monitoring of lipid levels to assess effectiveness, as stated in the 2018 AHA/ACC/AACVPR/AAPA/ABC/ACPM/ADA/AGS/APhA/ASPC/NLA/PCNA guideline on the management of blood cholesterol 1.

Key Considerations

• Colestipol can be used in combination with other cholesterol-lowering medications, such as statins, to achieve greater reductions in LDL cholesterol levels.
• Patients should be monitored regularly for potential side effects, such as gastrointestinal symptoms and reduced absorption of other medications.
• Colestipol is not recommended for patients with complete biliary obstruction or those who have had a history of serious hypersensitivity to this medication.

From the FDA Drug Label

The possible lack of proper vitamin absorption described in the “pregnancy” section may have an effect on nursing infants. Pediatric Use Safety and effectiveness in the pediatric population have not been established. Drug Interactions Since colestipol hydrochloride is an anion exchange resin, it may have a strong affinity for anions other than the bile acids In vitro studies have indicated that colestipol hydrochloride binds a number of drugs. Therefore, colestipol hydrochloride for oral suspension resin may delay or reduce the absorption of concomitant oral medication.

Colestipol is a medication that may have various drug interactions and effects on the body.

• The medication may bind to other drugs, reducing their absorption.
• It is not recommended for use in pediatric populations, as safety and effectiveness have not been established.
• Nursing mothers should exercise caution when taking colestipol, as it may affect vitamin absorption in infants.
• Patients should take other drugs at least one hour before or four hours after colestipol to avoid impeding their absorption 2, 2, 2.

From the Research

Colestipol Overview

• Colestipol is a bile acid sequestrant used to lower cholesterol levels in patients with hypercholesterolemia 3
• It works by binding to bile acids in the gut, which are then excreted, leading to a reduction in cholesterol production in the liver 3

Efficacy of Colestipol

• Studies have shown that colestipol is effective in reducing low-density lipoprotein (LDL) cholesterol levels in patients with primary hypercholesterolemia 4, 5, 6
• Colestipol has been shown to reduce LDL cholesterol levels by 12-27% in patients with moderate hypercholesterolemia 5
• Combination therapy with colestipol and lovastatin has been shown to be more effective than monotherapy with lovastatin in reducing LDL cholesterol levels 6

Safety and Tolerability of Colestipol

• Colestipol is generally well-tolerated, with gastrointestinal side effects being the most common 4, 3
• Patients have reported a preference for colestipol tablets over granules due to ease of use and tolerability 4
• Colestipol may interact with other medications, reducing their absorption or enterohepatic recirculation, and dosage intervals of other concurrent medications should be adjusted to minimize this potential interaction 3

Dosage and Administration of Colestipol

• The recommended dose of colestipol varies from 5-30g per day, depending on the patient's response and tolerance 5, 3
• Low-dose colestipol therapy (5g per day) has been shown to be effective in reducing LDL cholesterol levels in patients with moderate hypercholesterolemia 5
• Combination therapy with low-dose colestipol and lovastatin has been shown to be cost-effective and produce significant reductions in LDL cholesterol levels 6