From the Guidelines
Cholestyramine should be considered as an adjunct to diet and exercise to decrease LDL-C levels in patients with primary hyperlipidemia, with a typical dosage of 8-16 g/day orally divided into 2 doses, as it has been shown to reduce LDL-C levels by 10.4% compared to placebo 1. The mechanism of action of cholestyramine involves binding to bile acids in the intestine, impeding their reabsorption, and increasing the conversion of cholesterol to bile acids, ultimately leading to increased clearance of LDL-C from the blood 1. Key considerations when prescribing cholestyramine include:
- Pill burden and inconvenience in preparation of oral suspension preparations
- GI side effects such as constipation, dyspepsia, and nausea
- Exacerbation of hypertriglyceridemia
- Potential drug-drug interactions, which can be mitigated by taking other medications at least 1 hour before or 4 hours after cholestyramine
- CV outcomes data, which have shown a 19% reduction in risk of definite CHD death and/or definite nonfatal MI in the LRC-CPPT trial 1 It is essential to weigh these factors and consider individual patient needs and medical history when deciding to prescribe cholestyramine. Some notable points to consider are:
- Cholestyramine can increase the risk of constipation, and patients should be advised to maintain adequate fluid intake and consider using stool softeners if necessary
- The medication can also interfere with the absorption of other medications, and patients should be instructed to separate their medications by at least 4 hours
- Cholestyramine has been shown to be effective in reducing LDL-C levels, but its effects on cardiovascular morbidity and mortality have not been fully determined, except for the LRC-CPPT trial 1.
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 Therapy with lipid-altering agents should be a component of multiple risk factor intervention in those individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia. The main use of cholestyramine is as an adjunctive therapy to diet for reducing elevated serum cholesterol in patients with primary hypercholesterolemia who do not respond adequately to diet 2.
- Key points:
- Cholestyramine is used to reduce LDL cholesterol.
- It is used in patients who do not respond adequately to diet.
- It is also used in patients with hypertriglyceridemia, but not as the primary treatment for this condition.
From the Research
Cholestyramine Overview
- Cholestyramine is a bile acid sequestrant used to treat primary hypercholesterolemia and hypercholesterolemia associated with mild hypertriglyceridemia 3
- It works by binding to bile acids in the intestine, forming an insoluble complex that is excreted in the feces, thereby reducing cholesterol levels in the blood 3
Efficacy of Cholestyramine
- Studies have shown that cholestyramine is effective in reducing total plasma cholesterol and low-density lipoprotein (LDL) cholesterol levels, but may not be as effective as other treatments such as lovastatin or atorvastatin 4, 5
- Cholestyramine has been shown to increase high-density lipoprotein (HDL) cholesterol levels, but the effect is generally smaller compared to other treatments 4, 6
- Cholestyramine may also increase plasma triglyceride levels, which can be a concern for patients with hypertriglyceridemia 4, 6
Comparison with Other Treatments
- Cholestyramine has been compared to other treatments such as simvastatin, atorvastatin, and lovastatin, and has been found to be less effective in reducing LDL cholesterol levels 4, 5, 6
- However, cholestyramine can be used in combination with other treatments to enhance efficacy, and has been shown to be well-tolerated when used in combination with simvastatin 6