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Drug Profile

The information on this site is intended to supplement and enhance, not replace, the advice of a physician who is familiar with your medical history. Decisions about your health should always be made ONLY after detailed conversation with your doctor.

Limited Use [what does this mean?]
Generic drug name: cholestyramine (coal es TIRE am ene)
Brand name(s): CHOLESTYRAMINE LIGHT, LOCHOLEST, PREVALITE, QUESTRAN, QUESTRAN LIGHT
GENERIC: not available FAMILY: Other Drugs for High Cholesterol
Find the drug label by searching at DailyMed.

Pregnancy and Breast-feeding Warnings [top]

Pregnancy Warning

Cholestyramine is known to interfere with the absorption of fat-soluble vitamins, and even vitamin supplementation may not be adequate. Because of the potential for serious adverse effects to the fetus, this drug should not be used by pregnant women.

Breast-feeding Warning

Because the lack of proper vitamin absorption by the mother could have a harmful effect on a nursing infant, you should not take cholestyramine while nursing.

Facts About This Drug [top]

Cholestyramine was first marketed in the U.S. in 1973. It is used primarily to lower cholesterol, specifically low-density lipoprotein (LDL). It works by binding bile acid in the intestines and therefore increasing the breakdown of cholesterol in the body. In middle-aged people it is clear that lowering cholesterol lessens the risk of coronary artery disease, but no cholesterol-lowering drug has been shown to lower overall death rates in this age group. In older adults the extent to which...

Cholestyramine was first marketed in the U.S. in 1973. It is used primarily to lower cholesterol, specifically low-density lipoprotein (LDL). It works by binding bile acid in the intestines and therefore increasing the breakdown of cholesterol in the body. In middle-aged people it is clear that lowering cholesterol lessens the risk of coronary artery disease, but no cholesterol-lowering drug has been shown to lower overall death rates in this age group. In older adults the extent to which higher cholesterol levels contribute to heart disease and should be treated with drugs is much less clear. Cholestyramine helps control high cholesterol, but does not cure the condition. Besides removing cholesterol, cholestyramine may remove needed nutrients and medicines from your body, and actually increase triglycerides.[1] People over age 60 and those who take high doses are more likely to experience harmful effects from cholestyramine.  

The first, safer, and less costly measure to lower cholesterol for people under 70 is to eat a low-fat diet, using mostly polyunsaturated fats (such as canola, corn, safflower, and sunflower oils) or monounsaturated fats (such as olive oil). A change from animal to vegetable proteins often corrects high cholesterol. However, it is inadvisable to go on a very low-fat diet. The main focus on cholesterol-lowering diets has been on saturated fat and cholesterol content, not soluble fiber. (When added to the diet, psyllium or oat bran is a safe, effective way of lowering cholesterol.) Exercise and weight reduction are also recommended. Conditions that aggravate high cholesterol, such as dependence on alcohol or tobacco, diabetes, high blood pressure, low magnesium or potassium, and thyroid disease should be corrected before adding a cholesterol-reducing drug. If cholesterol remains high despite diet, add 10 grams of  psyllium (METAMUCIL, PERDIEM) a day.

Before You Use This Drug [top]

Do not use if you have or have had:

  • complete biliary obstruction
  • constipation

Tell your doctor if you have or have had:

  •   allergies to drugs
  •   bleeding disorders
  •   chronic constipation or other gastrointestinal problems
  •   diabetes
  •   gallbladder problems
  •   heart, kidney, or liver problems
  •   hemorrhoids
  •   osteoporosis
  •   phenylketonuria (PKU)
  •   thyroid disorder
  •   gastrointestinal ulcers
  •   pregnancy or are breast-feeding (impaired absorption of vitamins and nutrients)

Tell your doctor about any other drugs you take, including aspirin, herbs, vitamins, and other nonprescription products. When taking cholestyramine it is important that your doctor knows all the drugs you take.

When You Use This Drug [top]

  • Tell any other doctor, dentist, nurse practitioner, or surgeon you see that you take cholestyramine.
  • Tell your doctor whenever you start any new medication.
  • If you take other medications, check with your doctor.
  • Continue to follow a low-fat diet.
  • Avoid constipation. Increase your fiber with more bran, fluids, fruits, or psyllium. If constipation persists, try a stool softener.

How to Use This Drug [top]

  • If you miss a dose, take it as soon as you remember but skip it if it is almost time for the next dose. Do not take double doses.
  • Do not share your medication with others.
  • Take the drug at the same time(s) each day.
  • Take cholestyramine within half an hour of meals,[2] preferably before meals.[3]
  • If you take the bar form of cholestyramine, chew thoroughly before swallowing. Drink plenty of fluids.
  • If you take the powder form of cholestyramine, measure the dose, unless you use premeasured packets. The color of the powder varies from batch to batch. Never swallow the dry form, but mix the powder in two or more ounces of water, milk, or apple or orange juice. Stir vigorously, then shake. However, the mixture will not dissolve. To further improve flavor, try stirring in a heavy fruit juice or pulpy fruits (applesauce, fruit cocktail, crushed pineapple), thin soups, or mix it with milk in cold or hot cereal. Chilling the mixture may aid the flavor. If you use a carbonated beverage, stir slowly to reduce foaming. Avoid taking with highly acidic drinks, such as Kool-Aid.[4] Swallow immediately. Do not hold or swish the mixture in your mouth.[4] To be sure all the medication is taken, rinse the container thoroughly and drink the remaining contents.
  • If you take any other medications, separate the times as far apart from cholestyramine as possible, but at least one hour before you take the cholestyramine, or four to eight hours after you take the cholestyramine.
  • Store at room temperature with the lid of bulk powder closed tightly.
  • Do not store in the bathroom. Do not expose to heat, moisture, or strong light. Keep out of reach of children.

Interactions with Other Drugs [top]

The following drugs, biologics (e.g., vaccines, therapeutic antibodies), or foods are listed in Evaluations of Drug Interactions 2003 as causing “highly clinically significant” or “clinically significant” interactions when used together with any of the drugs in this section. In some sections with multiple drugs, the interaction may have been reported for one but not all drugs in this section, but we include the interaction because the drugs in this section are similar to one another. We have also included potentially serious interactions listed in the drug’s FDA-approved professional package insert or in published medical journal articles. There may be other drugs, especially those in the families of drugs listed below, that also will react with this drug to cause severe adverse effects. Make sure to tell your doctor and pharmacist the drugs you are taking and tell them if you are taking any of these interacting drugs:

ARAVA, CELLCEPT, COUMADIN, CRYSTODIGIN, digitoxin, EVISTA, furosemide, glipizide, GLUCOTROL, LASIX, leflunomide, mycophenolate, raloxifene, THYROID STRONG, warfarin.

If you stop taking cholestyramine, your doctor will again review doses of your other drugs. Serious harm may occur if you stop taking cholestyramine while taking other medicines.

Adverse Effects [top]

Call your doctor immediately if you experience:

  • unusual bleeding or bruising
  • black, tarry stools
  • constipation
  • severe stomach pain with nausea and vomiting
  • sudden weight loss

Call your doctor if these symptoms continue:

  • belching or hiccups
  • bloating
  • diarrhea
  • dizziness
  • headache
  • heartburn, indigestion, stomach pain
  • irritation of skin, tongue, or anal area
  • nausea or vomiting

Periodic Tests[top]

Ask your doctor which of these tests should be done periodically while you are taking this drug:

  • blood calcium, cholesterol, and triglyceride levels
  • prothrombin time
  • blood pressure

 

last reviewed April 30, 2021