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Pronunciation
(koe LES teer a meen REZ in)
Generic Available (U.S.)
Yes
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
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)
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.
Lactation
Does not enter breast milk/use caution
Breast-Feeding Considerations
Due to lack of systemic absorption cholestyramine is not expected to be excreted into breast milk; however, the tendency of cholestyramine to interfere with vitamin absorption may have an effect on the nursing infant.
Contraindications
Hypersensitivity to bile acid sequestering resins or any component of the formulation; complete biliary obstruction
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:
• 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.
Adverse Reactions
Frequency not defined.
Cardiovascular: Edema, syncope
Central nervous system: Anxiety, dizziness, drowsiness, eructation, fatigue, headache, vertigo
Dermatologic: Bruising, rash, skin irritation, urticaria
Endocrine & metabolic: Hyperchloremic acidosis (children), libido increased
Gastrointestinal: Abdominal pain, anorexia, biliary colic, black stools, constipation, dental bleeding, dental caries, dental erosion, diarrhea, diverticulitis, duodenal ulcer bleeding, dysphagia, eructation, flatulence, gallbladder calcification, GI hemorrhage, intestinal obstruction (rare), hemorrhoidal bleeding, nausea, pancreatitis, perianal irritation, rectal bleeding, rectal pain, steatorrhea, taste disturbance, tongue irritation, tooth discoloration, ulcer, vomiting, weight gain/loss
Hepatic: Hypothrombinemia, liver function abnormalities, prothrombin time increased
Hematologic: Anemia, bleeding
Neuromuscular & skeletal: Arthritis, backache, joint/muscle/nerve pain, osteoporosis, paresthesia
Ocular: Night blindness (rare), uveitis
Otic: Tinnitus
Renal: Diuresis, dysuria, hematuria
Respiratory: Asthma, dyspnea, wheezing
Miscellaneous: Hiccups, swollen glands
Metabolism/Transport Effects
None known.
Drug Interactions
Acetaminophen: Cholestyramine Resin may decrease the absorption of Acetaminophen. Effect is minimal if cholestyramine is administered 1 hour after acetaminophen. Risk D: Consider therapy modification
Amiodarone: Bile Acid Sequestrants may decrease the bioavailability of Amiodarone. Risk D: Consider therapy modification
Antidiabetic Agents (Thiazolidinedione): Bile Acid Sequestrants may decrease the absorption of Antidiabetic Agents (Thiazolidinedione). Risk D: Consider therapy modification
Cardiac Glycosides: Bile Acid Sequestrants may decrease the absorption of Cardiac Glycosides. Risk C: 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. Risk D: 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. Risk D: 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. Risk D: Consider therapy modification
Corticosteroids (Oral): Bile Acid Sequestrants may decrease the absorption of Corticosteroids (Oral). Risk C: Monitor therapy
Deferasirox: Cholestyramine Resin may decrease the serum concentration of Deferasirox. Management: Avoid combination when possible; if the combination must be used, consider an increase in initial deferasirox dose to 30 mg/kg, and monitor serum ferritin concentrations/clinical responses to guide further dosing. Risk D: Consider therapy modification
Ezetimibe: Bile Acid Sequestrants may decrease the absorption of Ezetimibe. Risk C: Monitor therapy
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. Risk D: 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. Risk D: 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. Risk D: Consider therapy modification
Loop Diuretics: Bile Acid Sequestrants may decrease the absorption of Loop Diuretics. Risk D: Consider therapy modification
Methotrexate: Bile Acid Sequestrants may decrease the absorption of Methotrexate. Risk C: Monitor therapy
Methylfolate: Cholestyramine Resin may decrease the serum concentration of Methylfolate. Risk C: Monitor therapy
Mycophenolate: Cholestyramine Resin may decrease the serum concentration of Mycophenolate. Risk X: Avoid combination
Niacin: Bile Acid Sequestrants may decrease the absorption of Niacin. Risk D: Consider therapy modification
Nonsteroidal Anti-Inflammatory Agents: Bile Acid Sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Risk D: 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. Risk D: 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. Risk D: Consider therapy modification
Propranolol: Bile Acid Sequestrants may decrease the serum concentration of Propranolol. Risk C: Monitor therapy
Raloxifene: Bile Acid Sequestrants may decrease the absorption of Raloxifene. Risk D: Consider therapy modification
Tetracycline Derivatives: Bile Acid Sequestrants may decrease the absorption of Tetracycline Derivatives. Risk D: Consider therapy modification
Thiazide Diuretics: Bile Acid Sequestrants may decrease the absorption of Thiazide Diuretics. The diuretic response is likewise decreased. Risk D: Consider therapy modification
Thyroid Products: Bile Acid Sequestrants may decrease the absorption of Thyroid Products. Risk C: Monitor therapy
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. Risk D: 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. Risk D: 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. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Bile Acid Sequestrants may decrease the absorption of Vitamin K Antagonists. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Food: Cholestyramine (especially high doses or long-term therapy) may decrease the absorption of folic acid, calcium, and iron.
Herb/Nutraceutical: Cholestyramine (especially high doses or long-term therapy) may decrease the absorption of fat-soluble vitamins (vitamins A, D, E, and K).
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).
Mechanism of Action
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
Pharmacodynamics/Kinetics
Onset of action: Peak effect: 21 days
Absorption: None
Excretion: Feces (as insoluble complex with bile acids)
Dosage
Oral (dosages are expressed in terms of anhydrous resin):
Children (unlabeled use): 240 mg/kg/day in 2-3 divided doses; need to titrate dose depending on indication, response and tolerance; maximum: 8 g/day
Adults: 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
Dosage adjustment in renal impairment: No dosage adjustment provided in manufacturer's labeling; however, use with caution in renal impairment; may cause hyperchloremic acidosis.
Dosage adjustment in hepatic impairment: No dosage adjustment necessary; not absorbed from the gastrointestinal tract.
Administration: Oral
Mix powder with 60-180 mL water or other noncarbonated liquid prior to administration and mix well; may also be taken with highly fluid soups, applesauce or crushed pineapple; 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/day.
Monitoring Parameters
Serum cholesterol and triglyceride levels before initiating treatment and periodically throughout treatment (in accordance with NCEP guidelines)
Test Interactions
Increased prothrombin time
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.
Patient Education
Take once or twice a day as directed. Do not take the powder in its dry form; mix with fluid. Cholestyramine may lower absorption of many medications; check proper administration times. Ongoing medical follow-up and laboratory tests may be required. You may experience GI effects (these should resolve after continued use), nausea and vomiting, or constipation. Report unusual stomach cramping, pain or blood in stool, or unresolved nausea, vomiting, or constipation.
Geriatric Considerations
The definition of and, therefore, when to treat hyperlipidemia in the elderly is a controversial issue. The National Cholesterol Education Program recommends that all adults maintain a plasma cholesterol <160 mg/dL. Elderly with one additional risk factor, goal LDL would be <130 mg/dL. It is the authors' belief that pharmacologic treatment be reserved for those who are unable to obtain a desirable plasma cholesterol concentration by diet alone and for whom the benefits of treatment are believed to outweigh the potential adverse effects, drug interactions, and cost of treatment.
Cardiovascular Considerations
Cholestyramine alone or when combined with an HMG-CoA reductase inhibitor is effective in lowering cholesterol. Cholestyramine may increase triglycerides, therefore, it should be avoided in patients with triglyceride levels ≥200 mg/dL. Potential factors that may limit patient compliance include GI side effects and the need to separate administration of other medications from cholestyramine.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
None reported
Mental Health: Effects on Psychiatric Treatment
May decrease the absorption of psychotropics including TCAs, beta-blockers, valproic acid, barbiturates
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Powder for suspension, oral: Cholestyramine resin 4 g/5 g of powder (210 g); Cholestyramine resin 4 g/5.7 g of powder (239.4 g); Cholestyramine resin 4 g/9 g of powder (378 g); Cholestyramine resin 4 g/5 g packet (60s); Cholestyramine resin 4 g/5.7 g packet (60s); Cholestyramine resin 4 g/9 g packet (60s)
Prevalite®: Cholestyramine resin 4 g/5.5 g of powder (231 g); Cholestyramine resin 4 g/5.5 g packet (42s, 60s) [contains phenylalanine 14.1 mg/5.5 g; orange flavor]
Questran®: Cholestyramine resin 4 g/9 g of powder (378 g); Cholestyramine resin 4 g/9 g packet (60s) [orange flavor]
Questran® Light: Cholestyramine resin 4 g/5 g of powder (210 g); Cholestyramine resin 4 g/5 g packet (60s) [contains phenylalanine 14 mg/5 g; orange flavor]
Pricing: U.S. (www.drugstore.com)
Pack (Cholestyramine)
4 g (60): $122.99
Pack (Cholestyramine Light)
4 g (60): $102.00
Pack (Prevalite)
4 g (60): $144.76
Pack (Questran)
4 g (60): $215.96
Pack (Questran Light)
4 g (60): $230.00
Powder (Cholestyramine)
4 g/dose (378): $36.99
Powder (Cholestyramine Light)
4 g/dose (239.4): $59.99
Powder (Prevalite)
4 g/dose (231): $67.99
Powder (Questran)
4 g/dose (378): $109.99
References
“Executive Summary of The Third Report of The National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel III),” JAMA, 2001, 285(19):2486-97.
Henderson RP and Solomon CP, “Use of Cholestyramine in the Treatment of Digoxin Intoxication,” Arch Intern Med, 1988,148(3):745-6.
McPherson R, Frohlich J, Fodor G, et al, “Canadian Cardiovascular Society Position Statement--Recommendations for the Diagnosis and Treatment of Dyslipidemia and Prevention of Cardiovascular Disease,” Can J Cardiol, 2006, 22(11):913-27; published erratum appears in Can J Cardiol, 2006, 22(12):1077.
Smith SC Jr, Benjamin EJ, Bonow RO, et al, “AHA/ACCF Secondary Prevention and Risk Reduction Therapy for Patients With Coronary and Other Atherosclerotic Vascular Disease: 2011 Update: A Guideline From the American Heart Association and American College of Cardiology Foundation,” Circulation, 2011, 124(22):2458-73.
Westergaard H, “Bile Acid Malabsorption,” Curr Treat Options Gastroenterol, 2007, 10(1):28-33.
International Brand Names
Lexi-Comp.com
Last full review/revision January 2012
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