From the Guidelines
Bile acid sequestrants should be taken with meals or immediately before meals, not without food. Medications in this class, including cholestyramine (Questran), colestipol (Colestid), and colesevelam (Welchol), work by binding to bile acids in the intestine, which requires the presence of food to be most effective, as stated in the 2022 ACC expert consensus decision pathway on the role of nonstatin therapies for LDL-cholesterol lowering 1. Taking these medications with meals also helps minimize gastrointestinal side effects like bloating, constipation, and nausea that commonly occur with these drugs. The typical dosing schedule involves taking them with breakfast and dinner, or 30 minutes before these meals. For example, cholestyramine powder is usually mixed with 4-6 ounces of water or other non-carbonated beverage and taken with meals. The timing with food is important because these medications work by interrupting the enterohepatic circulation of bile acids during digestion, which ultimately leads to lower cholesterol levels as the body uses more cholesterol to produce new bile acids. If you must take other medications, take them at least 1 hour before or 4-6 hours after the bile acid sequestrant to prevent interference with absorption, as noted in the 2017 focused update of the 2016 ACC expert consensus decision pathway on the role of non-statin therapies for LDL-cholesterol lowering 1. Additionally, the 2015 statement from the ATVB council also supports the use of bile acid sequestrants with meals to reduce cardiovascular risk 1. Some key points to consider when taking bile acid sequestrants include:
- Take with meals to minimize gastrointestinal side effects
- Take at least 1 hour before or 4-6 hours after other medications to prevent interference with absorption
- Follow the typical dosing schedule, which involves taking with breakfast and dinner, or 30 minutes before these meals
- Be aware of potential drug interactions and contraindications, such as history of hypertriglyceridemia-induced pancreatitis or bowel obstruction, as stated in the 2022 ACC expert consensus decision pathway 1.
From the FDA Drug Label
The suggested time of administration is at mealtime but may be modified to avoid interference with absorption of other medications The answer is no, bile acid sequestrants like cholestyramine should be taken at mealtime. However, the administration time may be modified if necessary, to avoid interference with absorption of other medications 2.
- Key points:
- Take at mealtime
- May be modified if necessary
- Always mix with water or other fluids before ingesting
From the Research
Bile Acid Sequestrants and Food Intake
- Bile acid sequestrants are typically taken with food to minimize gastrointestinal side effects 3, 4.
- The mechanism of action of bile acid sequestrants involves binding to bile acids in the intestine, which can be affected by the presence of food 5, 6.
- However, there is no clear evidence to suggest that bile acid sequestrants cannot be taken without food, but it may increase the risk of gastrointestinal side effects 4, 7.
Administration and Efficacy
- Bile acid sequestrants can be effective in reducing LDL-C and improving glycemic control when taken as directed 3, 4.
- The efficacy of bile acid sequestrants in treating bile acid diarrhea has been demonstrated in several studies, with significant improvements in cessation or improvement in diarrhea and fecal consistency 7.
- Different types of bile acid sequestrants have different levels of ability to bind to bile acids, stability, and in-vivo activity, which can affect their efficacy and safety profiles 6.
Potential Interactions and Side Effects
- Bile acid sequestrants can interfere with the absorption of lipid-soluble drugs and may have adverse effects on gut function, particularly in patients with gastrointestinal disease or high triglycerides 4.
- The use of bile acid sequestrants may be limited in certain patient populations due to potential interactions and side effects, and should be carefully considered and monitored by a healthcare professional 3, 7.