Cholestyramine Side Effects

Some side effects of cholestyramine may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

For the Consumer

Applies to cholestyramine: oral powder for reconstitution

Get emergency medical help if you have any of these signs of an allergic reaction while taking cholestyramine: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have a serious side effect such as:

• blood in your urine;

• severe stomach pain;

• ongoing constipation;

• feeling short of breath;

• black, bloody, or tarry stools; or

• easy bruising or bleeding.

Less serious side effects of cholestyramine may include:

• mild constipation, diarrhea;

• stomach pain, nausea, loss of appetite, weight changes;

• bloating or gas;

• hiccups or a sour taste in your mouth;

• skin rash or itching;

• irritation of your tongue;

• itching or irritation around your rectal area;

• muscle or joint pain; or

• dizziness, spinning sensation; ringing in your ears.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.

For Healthcare Professionals

Applies to cholestyramine: compounding powder, oral powder for reconstitution

Gastrointestinal

Gastrointestinal side effects include constipation (28%), heartburn (17%), belching or bloating (11%), nausea (9%), eructation, anorexia, steatorrhea, hemorrhoids, rectal pain and irritation, diverticulitis, and bleeding from a known duodenal ulcer. Intestinal obstruction and pancreatitis are also reported in the literature.

Gastrointestinal side effects occur in the majority of patients treated with cholestyramine. Constipation is most common and can be severe. Intestinal obstruction has been reported in pediatric patients. Elderly patients are probably at risk for this as well. In one large study, gastrointestinal side effects diminished with continued therapy. If gastrointestinal side effects are significant, dosage reductions, even if temporary, may be beneficial.

Metabolic

Metabolic side effects include hyperchloremic metabolic acidosis, weight loss, and weight gain. Cholestyramine has been reported to decrease the absorption of thyroxine (T4).

Hyperchloremic metabolic acidosis has been reported in pediatric as well as adult patients. Onset of clinical illness ranged from days to several weeks after beginning cholestyramine therapy. In three out of four adult cases in the literature, spironolactone was used as concomitant therapy. Several patients had moderate underlying renal disease. With appropriate supportive care, correction of the acidosis, and discontinuation of cholestyramine, the patients recovered.

The mechanism by which cholestyramine causes metabolic acidosis has not been completely resolved. However, it may involve the release of chloride ions by cholestyramine (a chloride salt form) in addition to binding of bicarbonate and carbonate ions to the resin, creating a metabolic imbalance. Patients with impaired renal function may be at increased risk due to impairment of chloride elimination.

Hematologic

Hematologic side effects include rare cases of elevated prothrombin time, ecchymoses, and anemia.

Hepatic

Hepatic side effects of cholestyramine include rare cases of abnormal liver function tests although causality is unknown. In addition, calcification in the right upper quadrant and of the biliary tree has been reported, as has biliary colic.

Respiratory

Respiratory side effects include asthma, wheezing, and shortness of breath although causality is unknown.

Nervous system

Nervous system side effects include headache, anxiety, vertigo, dizziness, syncope, drowsiness, femoral nerve pain, and paresthesia although causality is unknown.

Renal

Renal side effects include hematuria, dysuria, burnt odor to the urine, and diuresis, as well as a case report of urethral calculi composed of uric acid.

Hypersensitivity

Hypersensitivity in the form of urticaria has been reported.

Musculoskeletal

Musculoskeletal side effects include osteoporosis, muscle and joint pain, muscle weakness, arthritis, and osteomalacia.

Other

Loss of dental enamel has been reported when cholestyramine was mixed with a relatively acidic liquid (in the case-report Kool-Aid was used).

Ocular

Ocular side effects include uveitis although causality is unknown.

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