What are bile acid sequestrants?
Bile acid sequestrants such as cholestyramine (Questran, Prevalite), colestipol (Colestid, Flavored Colestid ), and colesevelam (Welchol) are medications for lowering LDL cholesterol in conjunction with diet modification.
How do bile acid sequestrants work?
Bile acid sequestrants bind bile acids in the intestine and increase the excretion of bile acids in the stool. This reduces the amount of bile acids returning to the liver and forces the liver to produce more bile acids to replace the bile acids lost in the stool. In order to produce more bile acids, the liver converts more cholesterol into bile acids, which lowers the level of cholesterol in the blood.
Bile acid sequestrants have modest LDL cholesterol lowering effects. Low doses (for example 8 gram/day of Cholestyramine) can lower LDL cholesterol by 10%-15%. But even high doses (24 gram/day of cholestyramine) can only lower LDL cholesterol by approximately 25%. Therefore, bile acid sequestrants used alone are not as effective as statins in lowering LDL cholesterol.
Bile acid sequestrants are most useful in combination with a statin or niacin to aggressively lower LDL cholesterol levels. The combination of a statin and bile acid sequestrant can lower LDL cholesterol levels by approximately 50%. The combination of a statin and niacin can substantially reduce LDL cholesterol and elevate HDL cholesterol.
What are the side effects of bile acid sequestrants?
Bile acid sequestrants are not absorbed into the body, and therefore they do not have systemic side effects (affecting other organs). Their most common side effects are gastrointestinal and these include:
Which drugs interact with bile acid sequestrants?
Bile acid sequestrants can bind to and decrease the absorption (and hence the effectiveness) of other drugs, such as warfarin (Coumadin), thyroid hormones (Synthroid, Levoxyl), digoxin (Lanoxin), thiazide diuretics (Hydrodiuril, Oretic, Dyazide, Maxzide), and many others. Therefore, these medications should be taken 1 hour before or 4-6 hours after the administration of a bile acid sequestrant.
Bile acid sequestrants reduces the absorption of vitamin A, D, E, and K. Long-term use may thus cause a deficiency of vitamin A, D, E, and K.
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Related Disease Conditions
High Cholesterol: Frequently Asked Questions
Cholesterol occurs naturally in the body. High blood cholesterol levels increase a person's risk of developing heart disease, heart attacks, strokes, TIAs, and more. In addition to medication (fibrates, statins, bile acid sequestrants, and niacin), lifestyle changes can be made to lower blood cholesterol levels
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Cholesterol (Lowering Your Cholesterol)
High cholesterol and triglyceride levels increase the risk of cardiovascular disease. Getting your cholesterol and triglyceride levels in an optimal range will help protect your heart and blood vessels. Cholesterol management may include lifestyle interventions (diet and exercise) as well as medications to get your total cholesterol, LDL, HDL, and triglycerides in an optimal range.
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Primary Biliary Cirrhosis (PBC)
Primary Biliary Cirrhosis (PBS) is a liver disease in which bile building up in the organ damages bile ducts. Ultimately, this can cause liver failure. A number of drugs are available to treat this disease of unknown cause, but the only ultimate cure is a liver transplant.
Heart Attack Prevention
Heart disease and heart attacks can be prevented by leading a healthy lifestyle with diet, exercise, and stress management. Symptoms of heart attack in men and women include chest discomfort and pain in the shoulder, neck, jaw, stomach, or back. Women experience the same symptoms as men; however, they also may experience: Extreme fatigue Pain in the upper abdomen Dizziness Fainting Leading a healthy lifestyle with a heart healthy low-fat diet, and exercise can help prevent heart disease and heart attack.
Crohn's Disease vs. Ulcerative Colitis (UC)
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