Colestyramine

A bile acid sequestrant used to lower cholesterol levels and treat certain conditions

Colestyramine
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Colestyramine (also known as cholestyramine) is a bile acid sequestrant, a type of medication used primarily to lower cholesterol levels in the blood and to treat certain conditions related to bile acid metabolism. It is a non-absorbable resin that binds bile acids in the gastrointestinal tract, preventing their reabsorption.

Mechanism of Action

Colestyramine works by binding to bile acids in the intestine. Bile acids are produced from cholesterol in the liver and are essential for the digestion and absorption of dietary fats. By binding to these acids, colestyramine prevents their reabsorption into the bloodstream. This process forces the liver to convert more cholesterol into bile acids to replace those lost, thereby reducing the level of cholesterol in the blood.

Medical Uses

Colestyramine is used in the treatment of several conditions:

• Hypercholesterolemia: It is used to lower high levels of cholesterol, particularly low-density lipoprotein (LDL) cholesterol, which is a risk factor for atherosclerosis and cardiovascular disease.

• Pruritus associated with partial biliary obstruction: Colestyramine can relieve itching caused by the accumulation of bile acids in the bloodstream due to liver disease or bile duct obstruction.

• Diarrhea due to bile acid malabsorption: It is effective in treating diarrhea caused by excess bile acids in the colon, which can occur after gallbladder removal or in certain diseases like Crohn's disease.

Administration and Dosage

Colestyramine is typically administered orally in the form of a powder that is mixed with water or other fluids. The dosage varies depending on the condition being treated and the patient's response to the medication. It is important to follow the prescribed dosage and administration instructions to achieve optimal results.

Side Effects

Common side effects of colestyramine include:

• Constipation
• Abdominal discomfort
• Bloating
• Nausea

Less common but more serious side effects can include:

• Severe constipation
• Intestinal obstruction
• Vitamin deficiencies (due to interference with the absorption of fat-soluble vitamins)

Interactions

Colestyramine can interfere with the absorption of other medications and nutrients. It is recommended to take other medications at least 1 hour before or 4 to 6 hours after taking colestyramine to avoid interactions. Patients should also be monitored for potential deficiencies in fat-soluble vitamins (A, D, E, and K).

Related Pages

• Bile acid sequestrant
• Hypercholesterolemia
• Cardiovascular disease
• Liver disease