From the Guidelines
Cholestyramine should be started at a low dose of 2 to 4 g/d and titrated based on response, with a maximum dose of 4-24 g/d, as it is effective in treating bile acid diarrhea and has a favorable benefit-risk profile compared to other bile acid sequestrants 1, 2.
Key Points
- Cholestyramine is a bile acid sequestrant medication that works by binding to bile acids in the intestines, preventing their reabsorption and promoting their elimination through stool.
- The typical dosage ranges from 4 to 8 grams taken 1-2 times daily, usually mixed with water or other non-carbonated beverages.
- When taking cholestyramine, it's essential to consume it before meals and separate it from other medications by at least 4 hours, as it can interfere with their absorption.
- Common side effects include constipation, bloating, gas, and nausea.
- Cholestyramine is particularly effective for treating bile acid diarrhea and can also help manage pruritus (itching) associated with partial biliary obstruction.
- Patients should maintain adequate fluid intake while taking this medication to minimize constipation risk.
Dosage and Administration
- The dosage of cholestyramine should be titrated gradually to maximize symptom relief and minimize side effects, with a starting dose of 2 to 4 g/d and a maximum dose of 4-24 g/d 1.
- Colesevelam, an alternative bile acid sequestrant, can be used as second-line therapy in patients who are unable to tolerate cholestyramine, with a dosage of 3.75 g/d as three 625-mg tablets twice daily, 6 tablets once daily, or one 3.75-g powder packet once daily 3.
Safety and Efficacy
- Cholestyramine has been shown to be effective in reducing LDL cholesterol levels and cardiovascular risk, with a 19% reduction in risk of definite CHD death and/or definite nonfatal MI in the LRC-CPPT trial 4.
- The medication has a favorable benefit-risk profile compared to other bile acid sequestrants, with common side effects including constipation, bloating, gas, and nausea.
- Patients should be monitored for potential drug interactions, including decreased absorption of other medications, and exacerbation of hypertriglyceridemia 4.
From the FDA Drug Label
Cholestyramine for Oral Suspension, USP powder is indicated as adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet Cholestyramine for Oral Suspension, USP powder may be useful to lower LDL cholesterol in patients who also have hypertriglyceridemia, but it is not indicated where hypertriglyceridemia is the abnormality of most concern
- Indications for cholestyramine:
- Reduction of elevated serum cholesterol in patients with primary hypercholesterolemia
- Lowering LDL cholesterol in patients with hypertriglyceridemia
- Key points:
- Cholestyramine is used as adjunctive therapy to diet
- It is not indicated where hypertriglyceridemia is the primary concern
- Therapy should begin and continue with dietary therapy specific for the type of hyperlipoproteinemia determined prior to initiation of drug therapy 5
- Cholestyramine resin may interfere with the absorption of fat soluble vitamins such as A, D, E and K 6
From the Research
Cholestyramine Overview
- Cholestyramine is a bile acid sequestrant used to treat hypercholesterolemia and other conditions 7, 8
- It works by binding to bile acids in the intestine and forming an insoluble complex that is excreted in the feces 8
Efficacy in Hypercholesterolemia
- Cholestyramine has been shown to reduce total cholesterol, LDL cholesterol, and Apo B lipoprotein levels in patients with severe hypercholesterolemia 7
- In a short-term study, cholestyramine reduced total cholesterol by 18% and LDL cholesterol by 28% in patients with non-insulin-dependent diabetes mellitus (NIDDM) 9
- Cholestyramine has also been shown to slow the progression of coronary arteriosclerosis in patients with Type II hyperlipoproteinemia 10
Combination Therapy
- Cholestyramine can be used in combination with other lipid-lowering agents, such as simvastatin, to achieve greater reductions in LDL cholesterol 11
- Combination therapy with cholestyramine and simvastatin has been shown to reduce LDL cholesterol by 60% in patients with type II hyperlipoproteinaemia 11