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Pronunciation
(koe LES teer a meen REZ in)
Generic Available (U.S.)
Yes
U.S. Brand Names
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Adjunct in the management of primary hypercholesterolemia; pruritus associated with elevated levels of bile acids; diarrhea associated with excess fecal bile acids; binding toxicologic agents; pseudomembraneous colitis
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
Contraindications
Hypersensitivity to bile acid sequestering resins or any component of the formulation; complete biliary obstruction; bowel obstruction
Warnings/Precautions
Concerns related to adverse effects:
• Bleeding: Chronic use may be associated with bleeding problems (especially in high doses).
• Constipation: May produce or exacerbate constipation problems; fecal impaction may occur. Hemorrhoids may be worsened.
Concurrent drug therapy issues:
• Decreased absorption (orally administered drugs): Not to be taken simultaneously with many other medicines (decreased absorption).
• Fat-soluble vitamins/folic acid: May interfere with fat-soluble vitamins (A, D, E, K) and folic acid.
Dosage form specific issues:
• Phenylalanine: Questran® Light contains phenylalanine.
Other warnings/precautions:
• Hyperlipidemia: Secondary causes of hyperlipidemia should be ruled out prior to therapy.
Adverse Reactions
>10%: Gastrointestinal: Constipation, heartburn, nausea, vomiting, stomach pain
1% to 10%:
Central nervous system: Headache
Gastrointestinal: Belching, bloating, diarrhea
<1% (Limited to important or life-threatening): Hyperchloremic acidosis, gallstones or pancreatitis, GI bleeding, peptic ulcer, steatorrhea or malabsorption syndrome, hypoprothrombinemia (secondary to vitamin K deficiency)
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
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 powder at controlled room temperature of 15°C to 30°C (59°F to 86°F). Suspension may be used for up to 48 hours after refrigeration.
Reconstitution
Mix contents of 1 packet or 1 level scoop of powder with 4-6 oz of beverage. Allow to stand 1-2 minutes prior to mixing. May also be mixed with highly-fluid soups, cereals, applesauce, etc.
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: 240 mg/kg/day in 3 divided doses; need to titrate dose depending on indication
Adults: 4 g 1-2 times/day to a maximum of 24 g/day and 6 doses/day
Dialysis: Not removed by hemo- or peritoneal dialysis; supplemental doses not necessary with dialysis or continuous arteriovenous or venovenous hemofiltration
Administration: Oral
Mix powder with water or other fluid prior to administration; 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).
Test Interactions
Increased prothrombin time; decreased cholesterol (S), iron (B)
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.
Anesthesia and Critical Care Concerns/Other Considerations
Cholestyramine alone or when combined with a statin 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 space other medications at least 1 hour before or 4 hours after cholestyramine administration.
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
Powder (Cholestyramine)
4 g/dose (378): $36.99
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.
International Brand Names
Lexi-Comp.com
Last full review/revision May 2011
Content last modified May 2011
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