Skip to Content
Here’s what to ask a doctor about hereditary angioedema

Cholestyramine Resin

Pronunciation

Pronunciation

(koe LES teer a meen REZ in)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Packet, Oral:

Prevalite: 4 g (1 ea, 42 ea, 60 ea) [contains aspartame; orange flavor]

Questran: 4 g (1 ea, 60 ea) [orange flavor]

Questran Light: 4 g (1 ea [DSC], 60 ea [DSC]) [sugar free; contains aspartame; orange flavor]

Generic: 4 g (1 ea, 60 ea)

Powder, Oral:

Prevalite: 4 g/dose (231 g) [contains aspartame; orange flavor]

Questran: 4 g/dose (378 g) [orange flavor]

Questran Light: 4 g/dose (210 g) [sugar free; contains aspartame; orange flavor]

Generic: 4 g/dose (210 g, 239.4 g, 378 g)

Brand Names: U.S.

  • Prevalite
  • Questran
  • Questran Light

Pharmacologic Category

  • Antilipemic Agent, Bile Acid Sequestrant

Pharmacology

Forms a nonabsorbable complex with bile acids in the intestine, releasing chloride ions in the process; inhibits enterohepatic reuptake of intestinal bile salts and thereby increases the fecal loss of bile salt-bound low density lipoprotein cholesterol

Absorption

None

Excretion

Feces (as insoluble complex with bile acids)

Onset of Action

Peak effect: 21 days

Use: Labeled Indications

Adjunct in the management of primary hypercholesterolemia; pruritus associated with elevated levels of bile acids; regression of arteriolosclerosis

Use: Unlabeled

Diarrhea associated with excess fecal bile acids (Westergaard, 2007); may be used to enhance elimination of digoxin when non-life-threatening toxicity occurs (Henderson, 1988)

Contraindications

Hypersensitivity to bile acid sequestering resins or any component of the formulation; complete biliary obstruction

Dosing: Adult

Dosages are expressed in terms of anhydrous resin:

Dyslipidemia: Oral: Initial: 4 g 1-2 times/day; increase gradually over ≥1-month intervals; maintenance: 8-16 g/day divided in 2 doses; maximum: 24 g/day

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Dosages are expressed in terms of anhydrous resin:

Dyslipidemia (off-label use): Oral: 240 mg/kg/day in 2-3 divided doses; titrate dose to response and tolerance; maximum: 8 g/day

Dosing: Renal Impairment

No dosage adjustment provided in manufacturer's labeling; however, use with caution in renal impairment; may cause hyperchloremic acidosis.

Dosing: Hepatic Impairment

No dosage adjustment necessary; not absorbed from the gastrointestinal tract.

Reconstitution

Powder for suspension: Prior to administration, add powder to 60-180 mL water or other noncarbonated liquid and mix well. May also be mixed with highly fluid soups, applesauce or crushed pineapple.

Administration

Administer prepared suspension orally. Not to be taken in dry form. Suspension should not be sipped or held in mouth for prolonged periods (may cause tooth discoloration or enamel decay). Administration at mealtime is recommended. Twice-daily dosing is recommended, but may be administered in 1-6 doses daily.

Dietary Considerations

Supplementation of vitamins A, D, E, and K, folic acid, and iron may be required with high-dose, long-term therapy. Some products may contain phenylalanine.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Drug Interactions

Acetaminophen: Cholestyramine Resin may decrease the absorption of Acetaminophen. Effect is minimal if cholestyramine is administered 1 hour after acetaminophen. Consider therapy modification

Amiodarone: Bile Acid Sequestrants may decrease the bioavailability of Amiodarone. Consider therapy modification

AtorvaSTATin: Bile Acid Sequestrants may decrease the serum concentration of AtorvaSTATin. Monitor therapy

Cardiac Glycosides: Bile Acid Sequestrants may decrease the absorption of Cardiac Glycosides. Monitor therapy

Chenodiol: Bile Acid Sequestrants may decrease the serum concentration of Chenodiol. Management: Administration of chenodiol 5 hours or more after bile acid sequestrants may reduce chenodiol adsorption in the gastrointestinal tract. Monitor for decreased therapeutic effects of chenodiol in patients receiving bile acid sequestrants. Consider therapy modification

Cholic Acid: Bile Acid Sequestrants may decrease the absorption of Cholic Acid. Management: Administer cholic acid at least 1 hour before or 4 to 6 hours after administration of any bile acid-binding products to minimize the potential for a significant interaction. Consider therapy modification

Contraceptives (Estrogens): Bile Acid Sequestrants may decrease the serum concentration of Contraceptives (Estrogens). Management: Administer estrogen-based oral contraceptives at least 1-4 hours prior to or 4-6 hours after administration of a bile acid sequestrant. Consider therapy modification

Contraceptives (Progestins): Bile Acid Sequestrants may decrease the serum concentration of Contraceptives (Progestins). Management: Administer oral progestin-containing contraceptives at least 1-4 hours prior to or 4-6 hours after administration of a bile acid sequestrant. Consider therapy modification

Corticosteroids (Oral): Bile Acid Sequestrants may decrease the absorption of Corticosteroids (Oral). Monitor therapy

Deferasirox: Bile Acid Sequestrants may decrease the serum concentration of Deferasirox. Management: Avoid combination when possible; if the combination must be used, consider a 50% increase in initial deferasirox dose, with monitoring of serum ferritin concentrations and clinical responses to guide further dosing. Consider therapy modification

Ezetimibe: Bile Acid Sequestrants may decrease the absorption of Ezetimibe. Management: Administer ezetimibe at least 2 hours before or 4 hours after any bile acid sequestrant. Consider therapy modification

Fibric Acid Derivatives: Bile Acid Sequestrants may decrease the absorption of Fibric Acid Derivatives. Management: Separate doses by at least 2 hours to minimize this interaction; fenofibric acid labeling recommends administration one hour prior to or 4-6 hours after a bile acid sequestrant. Consider therapy modification

Fluvastatin: Cholestyramine Resin may decrease the serum concentration of Fluvastatin. Management: Administer fluvastatin at least 1 hour or greater (particularly with extended-release form) before, or at least 4 hours after cholestyramine to minimize the risk for any significant interaction. Consider therapy modification

Leflunomide: Bile Acid Sequestrants may decrease serum concentrations of the active metabolite(s) of Leflunomide. Management: Unless using this combination to intentionally enhance leflunomide elimination, consider an alternative to the bile acid sequestrants when possible. Separating drug administration is not likely to be effective at avoiding this interaction. Consider therapy modification

Lomitapide: Bile Acid Sequestrants may decrease the absorption of Lomitapide. Management: Administer lomitapide at least 4 hours before or after administration of a bile acid sequestrant. Consider therapy modification

Loop Diuretics: Bile Acid Sequestrants may decrease the absorption of Loop Diuretics. Consider therapy modification

Methotrexate: Bile Acid Sequestrants may decrease the absorption of Methotrexate. Monitor therapy

Methylfolate: Cholestyramine Resin may decrease the serum concentration of Methylfolate. Monitor therapy

Multivitamins/Fluoride (with ADE): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Fluoride (with ADE). Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (e.g., cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Consider therapy modification

Multivitamins/Minerals (with ADEK, Folate, Iron): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Minerals (with ADEK, Folate, Iron). Specifically, bile acid sequestrants may impair the absorption of fat-soluble vitamins. Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (e.g., cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Consider therapy modification

Multivitamins/Minerals (with AE, No Iron): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Minerals (with AE, No Iron). Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (e.g., cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Consider therapy modification

Mycophenolate: Cholestyramine Resin may decrease the serum concentration of Mycophenolate. Avoid combination

Niacin: Bile Acid Sequestrants may decrease the absorption of Niacin. Consider therapy modification

Nonsteroidal Anti-Inflammatory Agents: Bile Acid Sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Consider therapy modification

Obeticholic Acid: Bile Acid Sequestrants may decrease the serum concentration of Obeticholic Acid. Management: Administer obeticholic acid at least 4 hours before or at least 4 hours after the administration of bile acid sequestrants. Consider therapy modification

PHENobarbital: Cholestyramine Resin may decrease the serum concentration of PHENobarbital. Management: Administer phenobarbital at least 1 hour before or 4-6 hours after administration of cholestyramine in order to minimize the risk for any significant interaction. Consider therapy modification

Pravastatin: Bile Acid Sequestrants may decrease the serum concentration of Pravastatin. Management: Administer pravastatin at least 1 hour before or 4 hours after administration of bile-acid resins (eg, cholestyramine, colestipol, colesevelam) to minimize the risk for any significant interaction. Consider therapy modification

Propranolol: Bile Acid Sequestrants may decrease the serum concentration of Propranolol. Monitor therapy

Raloxifene: Bile Acid Sequestrants may decrease the absorption of Raloxifene. Consider therapy modification

Rosiglitazone: Cholestyramine Resin may decrease the serum concentration of Rosiglitazone. Management: Administer rosiglitazone at least 2 hours prior to cholestyramine in order to minimize the likelihood of an interaction, and monitor patients closely for evidence of reduced rosiglitazone effectiveness. Consider therapy modification

Spironolactone: Cholestyramine Resin may enhance the adverse/toxic effect of Spironolactone. Specifically, the risks of developing metabolic acidosis and hyperkalemia may be elevated with this combination. Monitor therapy

Teriflunomide: Bile Acid Sequestrants may decrease the serum concentration of Teriflunomide. Management: Unless using this combination to intentionally enhance teriflunomide elimination, consider an alternative to the bile acid sequestrants when possible. Separating drug administration is unlikely to be effective at avoiding the interaction. Consider therapy modification

Tetracycline Derivatives: Bile Acid Sequestrants may decrease the absorption of Tetracycline Derivatives. Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Bile Acid Sequestrants may decrease the absorption of Thiazide and Thiazide-Like Diuretics. The diuretic response is likewise decreased. Consider therapy modification

Thyroid Products: Bile Acid Sequestrants may decrease the serum concentration of Thyroid Products. Management: Administer oral thyroid products at least 4 h prior to colesevelam, and at least 1 h before or 4-6 h after cholestyramine. Specific recommendations for colestipol are not available. Monitor for decreased concentrations/effects of the thyroid product. Consider therapy modification

Ursodiol: Bile Acid Sequestrants may decrease the serum concentration of Ursodiol. Management: Administer ursodiol 5 hours or more after bile acid sequestrants to minimize ursodiol adsorption in the gastrointestinal tract. Monitor for decreased therapeutic effects of ursodiol in patients receiving bile acid sequestrants. Consider therapy modification

Valproic Acid and Derivatives: Cholestyramine Resin may decrease the serum concentration of Valproic Acid and Derivatives. Management: Separate administration of valproic acid and cholestyramine by at least 3 hours whenever possible in order to minimize the potential for a significant interaction. Consider therapy modification

Vancomycin: Bile Acid Sequestrants may diminish the therapeutic effect of Vancomycin. Management: Avoid concurrent administration of oral vancomycin and bile acid sequestrants when possible. If use of both agents is necessary, consider separating doses by at least 2 hours to minimize the significance of the interaction. Consider therapy modification

Vitamin D Analogs: Bile Acid Sequestrants may decrease the serum concentration of Vitamin D Analogs. More specifically, bile acid sequestrants may impair absorption of Vitamin D Analogs. Management: Avoid concomitant administration of vitamin D analogs and bile acid sequestrants (e.g., cholestyramine). Separate administration of these agents by several hours to minimize the potential risk of interaction. Monitor plasma calcium concentrations. Exceptions: Calcipotriene. Consider therapy modification

Vitamin K Antagonists (eg, warfarin): Bile Acid Sequestrants may decrease the absorption of Vitamin K Antagonists. Monitor therapy

Test Interactions

Increased prothrombin time

Adverse Reactions

Frequency not defined.

Cardiovascular: Edema, syncope

Central nervous system: Anxiety, dizziness, drowsiness, fatigue, headache, neuralgia, paresthesia, vertigo

Dermatologic: Perianal skin irritation, skin irritation, skin rash, urticaria

Endocrine & metabolic: Hyperchloremic metabolic acidosis (children), increased libido, weight gain, weight loss

Gastrointestinal: Abdominal pain, anorexia, biliary colic, constipation, dental bleeding, dental caries, dental discoloration, diarrhea, diverticulitis, duodenal ulcer with hemorrhage, dysgeusia, dysphagia, eructation, flatulence, gallbladder calcification, gastric ulcer, gastrointestinal hemorrhage, hemorrhoidal bleeding, hiccups, intestinal obstruction (rare), melena, nausea, pancreatitis, rectal pain, steatorrhea, tongue irritation, tooth enamel damage (dental erosion), vomiting

Genitourinary: Diuresis, dysuria, hematuria

Hematologic & oncologic: Adenopathy, anemia, bruise, hemorrhage, hypoprothrombinemia, prolonged prothrombin time, rectal hemorrhage

Hepatic: Abnormal hepatic function tests

Neuromuscular & skeletal: Arthralgia, arthritis, back pain, myalgia, osteoporosis

Ophthalmic: Nocturnal amblyopia (rare), uveitis

Otic: Tinnitus

Respiratory: Asthma, dyspnea, wheezing

Warnings/Precautions

Concerns related to adverse effects:

• Bleeding: Chronic use may be associated with bleeding problems (especially in high doses); may be prevented with use of oral vitamin K therapy.

• Constipation: May produce or exacerbate constipation problems; initiate therapy at a reduced dose in patients with a history of constipation. Hemorrhoids may be worsened.

Disease-related concerns:

• Hypertriglyceridemia: Bile acid sequestrants should not be used in patients with baseline fasting triglyceride levels ≥300 mg/dL or type III hyperlipoproteinemia since severe triglyceride elevations may occur. Use bile acid sequestrants with caution in patients with triglyceride levels 250-299 mg/dL and evaluate a fasting lipid panel in 4-6 weeks after initiation; discontinue use if triglycerides are >400 mg/dL (Stone, 2013).

• Renal impairment: Use caution in patients with renal impairment.

Concurrent drug therapy issues:

• Decreased absorption (orally administered drugs): Not to be taken simultaneously with many other medicines (decreased absorption).

• Patients susceptible to fat-soluble vitamin deficiencies: Use with caution in patients susceptible to fat-soluble vitamin deficiencies. Absorption of fat soluble vitamins A, D, E, and K and folic acid may be decreased; patients should take vitamins ≥4 hours before cholestyramine.

Dosage form specific issues:

• Phenylalanine: Some products may contain phenylalanine.

Other warnings/precautions:

• Hyperlipidemia: Secondary causes of hyperlipidemia should be ruled out prior to therapy.

Monitoring Parameters

Fasting lipid profile before initiating treatment, 3 months after initiation (within 4-6 weeks if baseline fasting triglycerides of 250-299 mg/dL), and every 6-12 months thereafter (Stone, 2013)

Pregnancy Risk Factor

C

Pregnancy Considerations

Cholestyramine is not absorbed systemically, but may interfere with vitamin absorption; therefore, regular prenatal supplementation may not be adequate. There are no studies in pregnant women; use with caution.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience nausea, vomiting, flatulence, burping, bloating, or lack of appetite. Have patient report immediately to prescriber signs of bleeding (vomiting blood or vomit that looks like coffee grounds; coughing up blood; blood in the urine; black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a reason or that get bigger; or any bleeding that is very bad or that will not stop); severe abdominal pain, severe constipation, or severe diarrhea (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

Hide