From the Guidelines
Cholestyramine should be used to lower cholesterol levels at a dose 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. To use cholestyramine effectively, it is essential to take it before meals, mixed with 4-6 ounces of water, juice, or non-carbonated beverages, or mixed with applesauce or soup. The medication works by binding to bile acids in the intestines, preventing their reabsorption, which forces the liver to use cholesterol to make more bile acids, thereby reducing cholesterol levels in the blood 1. Some key considerations when using cholestyramine include:
- Taking other medications at least 1 hour before or 4-6 hours after cholestyramine to prevent interference with their absorption
- Drinking plenty of fluids while using this medication
- Monitoring for common side effects such as constipation, bloating, and gas
- Being aware of potential contraindications, including a history of serious hypersensitivity to this medication 1 It is also important to note that cholestyramine may increase triglyceride levels and cause acute pancreatitis, so it is essential to monitor triglyceride levels and discontinue the medication if signs and symptoms of acute pancreatitis occur 1. Overall, cholestyramine is a useful medication for lowering cholesterol levels, but it is crucial to use it correctly and be aware of its potential side effects and contraindications, as supported by the 2022 ACC expert consensus decision pathway on the role of nonstatin therapies for LDL-cholesterol lowering in the management of atherosclerotic cardiovascular disease risk 1.
From the FDA Drug Label
CLINICAL PHARMACOLOGY Cholesterol is probably the sole precursor of bile acids. During normal digestion, bile acids are secreted into the intestines. A major portion of the bile acids is absorbed from the intestinal tract and returned to the liver via the enterohepatic circulation. Only very small amounts of bile acids are found in normal serum Cholestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. The FDA drug label does not answer the question.
From the Research
Uses of Cholestyramine
- Cholestyramine is a bile acid sequestrant used to lower circulating low-density lipoprotein (LDL) cholesterol levels 2
- It is used mainly for the treatment of primary hypercholesterolemia and hypercholesterolemia associated with mild hypertriglyceridemia 3
- Cholestyramine is also used as a second-line treatment for pruritus associated with cholestatic disease, in patients with incomplete biliary obstruction 3
- It can be used to manage diabetes mellitus and diarrhea from bile acid malabsorption 3
- Cholestyramine is effective in treating chronic diarrhea due to bile acid malabsorption, with a success rate of 70% in 801 patients 4
Administration and Safety
- Cholestyramine is a non-digestible resin that binds to bile acids in the intestine to form an insoluble complex, which is excreted in the feces 3
- It is generally safe and well-tolerated, but may cause side effects such as constipation and decreased absorption of concomitant medications 5
- Cholestyramine may also cause modest increases in plasma triglyceride levels due to the alteration of hepatic lipid metabolism 5
- The dosage of cholestyramine may need to be adjusted to minimize side effects, and alternative therapies such as colesevelam and aluminium hydroxide may be considered 4