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DESCRIPTION
Cholestyramine is a medication used to reduce cholesterol levels by binding bile acids. It also binds other chemicals.
FORMS AND USES
- Cholestyramine (Questran, Questran Light) is provided as a 4-g packet of powder for dissolution in liquid.
- It is also available as bars (cholybar) containing 4 g of cholestyramine and in cans (Questran)
MECHANISM OF ACTION
- Cholestyramine adsorbs bile acids in the intestine to form an insoluble complex that is excreted in the feces.
- Increased fecal loss of bile acids leads to an increased oxidation of cholesterol to bile acids, a decrease in beta-lipoprotein or low-density lipoprotein plasma levels, and a decrease in serum cholesterol levels.
- Cholestyramine is used occasionally in toxicology to interfere with the absorption of ingested drugs.
DRUG AND DISEASE INTERACTIONS
Cholestyramine interferes with the absorption of many drugs, including acetaminophen, amiodarone, bezafibrate, cephalexin, chloroquine, chlorothiazide, cholecalciferol, dicumarol, digitoxin, digoxin, doxepin, fluvastatin, folic acid, furosemide, glipizide, hydrochlorothiazide, hydrocortisone, iron, levothyroxin, liothyronine, methotrexate, metronidazole, mofentil, mycophenolate, penicillin G, phenobarbital, phenprocoumon, phenylbutazone, piroxicam, pova-statin, sulindac, temoxicam, tetracycline, trimethoprim, ursodiol, vitamin A, vitamin E, vitamin K, and warfarin.
PREGNANCY AND LACTATION
- US FDA Pregnancy Category C. The drug exerts animal or embryocidal effects, but there are no controlled studies in women, or no studies are available in either animals or women.
- Cholestyramine is not excreted in breast milk, but it does bind fat soluble vitamins; therefore, its use is not recommended in nursing mothers.
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There are no widely accepted indications for the use of cholestyramine in the treatment of poisoning. The following proposed uses are considered investigational.
ORGANOCHLORINE PESTICIDE POISONING
- Cholestyramine enhances fecal elimination but has not been shown to affect outcome.
- Routine use is not recommended.
CARDIAC GLYCOSIDE TOXICITY
- Cholestyramine enhances elimination of digoxin and digitoxin but has not been shown to affect outcome.
- Routine use is not recommended.
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The adult dose for hypercholesterolemia is 4 to 16 g/day orally in two to four divided doses. However, the dose for potential use in poisoning is unknown.
PEDIATRIC
- Experience is limited.
- In children 6 to 12 years of age, a dose of 80 mg/kg three times a day has been used.
- A dose of 2 g twice daily for 3 days, has been used for outpatient treatment of acute diarrhea in infants 4 to 36 months of age.
Section Outline:
Although cholestryamine may increase excretion of some compounds, the time course is not likely to be clinically meaningful.
Author: Katherine M. Hurlbut
Reviewer: Richard C. Dart