Cholestyramine

Cholestyramine is an oral medication that reduces the levels of cholesterol in the blood and improves the itching associated with liver disease. Cholesterol that is ingested or manufactured in the body is eliminated primarily by conversion to bile acids in the liver and excretion into the intestine with bile. The bile enters the intestine, and most of the bile acids are reabsorbed from the intestine. These reabsorbed bile acids are removed from the blood by the liver and excreted again into bile. Thus, bile acids re-circulate in the body. Cholestyramine binds to bile acids in the intestine. This prevents their absorption, and the cholestyramine/bile acid complexes are eliminated in the stool. As a result, the body loses bile acids. To compensate for this loss, the liver increases the conversion of cholesterol to bile acids. The conversion of cholesterol to bile acids reduces the cholesterol in the body, and the levels of cholesterol drop in the blood.

One of the most troubling symptoms in patients with liver and biliary disease is itching. The itching is believed in some cases to be the result of accumulation of bile acids in the skin due to the inability of the liver or bile ducts to eliminate bile acids normally. By binding bile acids in the intestines and preventing their absorption, cholestyramine hastens the elimination of bile acids from the body and skin, and the itching improves. Cholestyramine also binds some drugs in the intestine, preventing their absorption and hastening their elimination. Therefore, cholestyramine is useful in some situations in which there has been an overdose of drugs. The FDA approved cholestyramine in August 1973.

Tell your doctor about all prescription, non-prescription, illegal, recreational, herbal, nutritional, or dietary drugs you're taking before taking cholestyramine, especially:

• Antibiotics
• Anticoagulants (blood thinners) such as Coumadin (warfarin)
• Arava (leflunomide)
• CellCept or Myfortic (mycophenolate)
• Cordarone (amiodarone)
• Digitoxin
• Diuretics (water pills)
• Imodium (loperamide)
• Inderal (propranolol)
• Iron
• Lanoxin (digoxin)
• Oral diabetes medications
• Phenobarbital
• Phenylbutazone
• Thyroid medications
• Vitamins

Cholestyramine may interfere with the absorption of other drugs.

Try to take other medicines at least one hour before or four hours after you take cholestyramine.

Cholestyramine and Other Interactions

Cholestyramine may make you dizzy or drowsy.

Don't drive or perform any activity that requires alertness until you know how the medicine affects you.

Cholestyramine and Alcohol

Alcohol can worsen certain side effects of cholestyramine.

Talk to your doctor before you consume alcohol while taking this medicine.

The most common adverse reaction is constipation. When used as a cholesterol-lowering agent predisposing factors for most complaints of constipation are high dose and increased age (more than 60 years old). Most instances of constipation are mild, transient, and controlled with conventional therapy. Some patients require a temporary decrease in dosage or discontinuation of therapy.

Less Frequent Adverse Reactions: Abdominal discomfort and/or pain, flatulence, nausea, vomiting, diarrhea, eructation, anorexia, and steatorrhea, bleeding tendencies due to hypoprothrombinemia (Vitamin K deficiency) as well as Vitamin A (one case of night blindness reported) and D deficiencies, hyperchloremic acidosis in children, osteoporosis, rash and irritation of the skin, tongue and perianal area. Rare reports of intestinal obstruction, including two deaths, have been reported in pediatric patients.

Occasional calcified material has been observed in the biliary tree, including calcification of the gallbladder, in patients to whom QUESTRAN has been given. However, this may be a manifestation of the liver disease and not drug related.

One patient experienced biliary colic on each of three occasions on which he took QUESTRAN. One patient diagnosed as acute abdominal symptom complex was found to have a “pasty mass” in the transverse colon on x-ray.

Other events (not necessarily drug related) reported in patients taking QUESTRAN include:

Gastrointestinal - GI-rectal bleeding, black stools, hemorrhoidal bleeding, bleeding from known duodenal ulcer, dysphagia, hiccups, ulcer attack, sour taste, pancreatitis, rectal pain, diverticulitis.

Laboratory test changes - Liver function abnormalities.

Hematologic - Prolonged prothrombin time, ecchymosis, anemia

Hypersensitivity - Urticaria, asthma, wheezing, shortness of breath.

Musculoskeletal - Backache, muscle and joint pains, arthritis.

Neurologic - Headache, anxiety, vertigo, dizziness, fatigue, tinnitus, syncope, drowsiness, femoral nerve pain, paresthesia.

Eye - Uveitis.

Renal - Hematuria, dysuria, burnt odor to urine, diuresis.

Miscellaneous - Weight loss, weight gain, increased libido, swollen glands, edema, dental bleeding, dental caries, erosion of tooth enamel, tooth discoloration.

Overdosage with QUESTRAN has been reported in a patient taking 150% of the maximum recommended daily dosage for a period of several weeks. No ill effects were reported. Should an overdosage occur, the chief potential harm would be obstruction of the gastrointestinal tract. The location of such potential obstruction, the degree of obstruction, and the presence or absence of normal gut motility would determine treatment.

You should not take this medication if you are allergic to cholestyramine, or if you have a blockage in your stomach or intestines.

Before taking cholestyramine, tell your doctor if you have a thyroid disorder, diabetes, kidney or liver disease, or chronic constipation.

Avoid taking other medications at the same time you take cholestyramine. Wait at least 4 to 6 hours after taking cholestyramine before you take any other medications.

You should not take this medication if you are allergic to cholestyramine, or if you have a blockage in your stomach or intestines.

To make sure you can safely take cholestyramine, tell your doctor if you have any of these other conditions:

• a thyroid disorder;
• diabetes,
• kidney disease,
• liver disease, or
• chronic constipation.

FDA pregnancy category C. It is not known whether cholestyramine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

Taking cholestyramine can make it harder for your body to absorb certain vitamins your body needs while you are nursing a baby. Do not take cholestyramine without telling your doctor if you are breast-feeding.

This medicine may contain phenylalanine. Talk to your doctor before using cholestyramine if you have phenylketonuria (PKU).

It is very important that your doctor check your progress at regular visits. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to take it.

Do not take any other medicine unless prescribed by your doctor since cholestyramine may change the effect of other medicines.

Do not stop taking cholestyramine without first checking with your doctor. When you stop taking cholestyramine, your blood cholesterol levels may increase again. Your doctor may want you to follow a special diet to help prevent this from happening.

PHENYLKETONURICS: Cholestyramine FOR ORAL SUSPENSION USP LIGHT POWDER CONTAINS 28 MG PHENYLALANINE PER 5.5 GRAM DOSE.

Safety has not been established during pregnancy; benefit should outweigh risk. AU TGA pregnancy category: B2 US FDA pregnancy category: C Comments: This drug is known to interfere with absorption of fat-soluble vitamins even in the presence of vitamin supplementation and therefore, regular prenatal supplementation may not be adequate.

Animal studies have not been reported. There are no controlled data in human pregnancy. AU TGA pregnancy category B2: Drugs which have been taken by only a limited number of pregnant women and women of childbearing age, without an increase in the frequency of malformation or other direct or indirect harmful effects on the human fetus having been observed. Studies in animals are inadequate or may be lacking, but available data show no evidence of an increased occurrence of fetal damage. US FDA pregnancy category C: Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Summary of Use during Lactation

Cholestyramine is a nonabsorbable resin. Because it does not enter the mother's bloodstream, it will not reach the infant via breastmilk. It is acceptable for use during lactation.

Drug Levels

Maternal Levels. Relevant published information was not found as of the revision date.

Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

Relevant published information was not found as of the revision date.

Effects on Lactation and Breastmilk

Relevant published information was not found as of the revision date.

Alternate Drugs to Consider

Colesevelam, Colestipol

References

LactMed Record Number

515

Last Revision Date

20130907

Disclaimer

Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.