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Pharmacologic class: Bile acid sequestrant
Therapeutic class: Lipid-lowering agent
Pregnancy risk category C
Combines with bile acid in GI tract to form insoluble complex excreted in feces. Complex regulates and increases cholesterol synthesis, thereby decreasing serum cholesterol and low-density lipoprotein levels.
Powder for suspension; powder for suspension with aspartame: 4 g cholestyramine/packet or scoop
Indications and dosages
➣ Primary hypercholesterolemia and pruritus caused by biliary obstruction; primary hyperlipidemia
Adults: Initially, 4 g P.O. once or twice daily. May increase as needed and tolerated, up to 24 g/day in six divided doses.
• Antibiotic-induced pseudomembranous colitis
• Adjunct in infantile diarrhea
• Digoxin toxicity
• Hypersensitivity to drug, its components, or other bile-acid sequestering resins
• Complete biliary obstruction
• Phenylketonuria (suspension containing aspartame)
Use cautiously in:
• history of constipation or abnormal intestinal function
• pregnant patients
• Mix powder with soup, cereal, pulpy fruit, juice, milk, or water.
• Administer 1 hour before or 4 to 6 hours after other drugs.
• Be aware that fat-soluble vitamin supplements may be necessary with long-term drug use.
CNS: headache, anxiety, vertigo, dizziness, insomnia, fatigue, syncope
GI: nausea, vomiting, constipation, abdominal discomfort, fecal impaction, flatulence, hemorrhoids, perianal irritation, steatorrhea
GU: hematuria, dysuria, diuresis, burnt odor to urine
Hematologic: anemia, ecchymosis
Hepatic: hepatic dysfunction
Metabolic: vitamin A, D, E, and K deficiencies; hyperchloremic acidosis
Musculoskeletal: joint pain, arthritis, back pain, muscle pain
Respiratory: wheezing, asthma
Skin: hypersensitivity reaction (irritation, rash, urticaria)
Other: tongue irritation
Drug-drug. Acetaminophen, amiodarone, clindamycin, clofibrate, corticosteroids, digoxin, diuretics, fat-soluble vitamins (A, D, E, and K), gemfibrozil, glipizide, imipramine, methotrexate, methyldopa, mycophenolate, niacin, nonsteroidal anti-inflammatory drugs, penicillin, phenytoin, phosphates, propranolol, tetracyclines, tolbutamide, thyroid preparations, ursodiol, warfarin: decreased absorption and effects of these drugs
Drug-diagnostic tests. Alkaline phosphatase: increased level
Hemoglobin: decreased value
Prothrombin time: increased
• Monitor CBC with white cell differential and liver function test results.
• If bleeding or bruising occurs, monitor prothrombin time. Drug may reduce vitamin K absorption.
• Watch for constipation, especially in patients with coronary artery disease. Take appropriate steps to prevent this problem.
☞ Instruct patient to immediately report yellowing of skin or eyes or easy bruising or bleeding.
• Tell patient to take drug 1 hour before or 4 to 6 hours after other drugs.
• Teach patient about role of diet in controlling cholesterol level and preventing constipation.
• Instruct patient to avoid inhaling or ingesting raw powder. Tell him to mix powder with food, juice, or milk before consuming.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.