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Therapeutic Classification: lipid-lowering agents

Pharmacologic Classification: bile acid sequestrants

• Management of primary hypercholesterolemia.
• Pruritus associated with elevated levels of bile acids.

Unlabeled Uses:

• Diarrhea associated with excess bile acids.

• Bind bile acids in the GI tract, forming an insoluble complex. Result is increased clearance of cholesterol.

• Decreased plasma cholesterol and low-density lipoprotein (LDL) cholesterol.
• Decreased pruritus.

Absorption: Action takes place in the GI tract. No absorption occurs.

Distribution: No distribution.

Metabolism/Excretion: After binding bile acids, insoluble complex is eliminated in the feces.

Half-life: Unknown.

(hypocholesterolemic effects)

Contraindicated in:

• Hypersensitivity
• Complete biliary obstruction
• Some products contain aspartame and should be avoided in patients with phenylketonuria.

Use Cautiously in:

• History of constipation
• OB: Safety not established in pregnancy; not systemically absorbed, but may interfere with absorption of fat-soluble vitamins
• Lactation: May interfere with absorption of fat-soluble vitamins in infant.

Exercise Extreme Caution in:

• Pedi: Children (may cause intestinal obstruction; deaths have occurred).

Derm: irritation, rashes.

EENT: irritation of the tongue.

F and E: hyperchloremic acidosis.

GI: abdominal discomfort, constipation, nausea, fecal impaction, flatulence, hemorrhoids, perianal irritation, steatorrhea, vomiting.

Metab: vitamin A, D, and K deficiency.

Drug-Drug:

• May decrease absorption/effects of orally administered acetaminophen, amiodarone, clindamycin, digoxin, diuretics, gemfibrozil, glipizide, corticosteroids, imipramine, mycophenolate, methotrexate, niacin, NSAIDs, penicillin, phenytoin, phosphates, propranolol, tetracyclines, thyroid preparations, ursodiol, warfarin, and fat-soluble vitamins (A, D, E, and K).
• May decrease absorption of other orally administered medications.

• PO (Adults): 4 g 1–2 times daily (initially, may be increased as needed/tolerated up to 24 g/day in 6 divided doses).
• PO (Children): 240 mg/kg/day in 2–3 divided doses (not >8 g/day).

(Generic available)

• Powder for suspension with aspartame (unflavored [Olestyr Light, Prevalite]): 4 g cholestyramine/packet or scoop;
• Powder for suspension (unflavored [Olestyr, generic]): 4 g cholestyramine/packet or scoop;

• Hypercholesterolemia: Obtain a diet history, especially in regard to fat consumption.
• Pruritus: Assess severity of itching and skin integrity. Dose may be decreased when relief of pruritus occurs.
• Diarrhea: Assess frequency, amount, and consistency of stools.

• Serum cholesterol and triglyceride levels should be evaluated before initiating, frequently during first few mo and periodically throughout therapy. Discontinue medication if paradoxical increase in cholesterol level occurs.
  • May cause an increase in AST, ALT, phosphorus, chloride, and alkaline phosphatase and a decrease in serum calcium, sodium, and potassium levels.
  • May also cause prolonged prothrombin times.

• Parenteral or water-miscible forms of fat-soluble vitamins (A, D, and K) and folic acid may be ordered for patients on chronic therapy.
• PO: Administer before meals.
  • Scoops for powdered preparations may not be exchangeable between products.
  • Administer other medications 1 hr before or 4–6 hr after the administration of this medication.

• Instruct patient to take medication exactly as directed; do not skip doses or double up on missed doses.
• Instruct patient to take medication before meals. Mix cholestyramine with 4–6 oz water, milk, fruit juice, or other noncarbonated beverages. Shake vigorously. Slowly stir in a large glass. Rinse glass with small amount of additional beverage to ensure all medication is taken. May also mix with highly fluid soups, cereals, or pulpy fruits (applesauce, crushed pineapple). Allow powder to sit on fluid and hydrate for 1–2 min before mixing. Do not take dry. Variations in the color of cholestyramine do not alter stability.
• Advise patient that this medication should be used in conjunction with dietary restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking.
• Explain that constipation may occur. Increase in fluids and bulk in diet, exercise, stool softeners, and laxatives may be required to minimize the constipating effects. Instruct patient to notify health care professional if constipation, nausea, flatulence, and heartburn persist or if stools become frothy and foul smelling.
• Advise patient to notify health care professional if unusual bleeding or bruising; petechiae; or black, tarry stools occur. Treatment with vitamin K may be necessary.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. May interfere with absorption of fat-soluble vitamins in pregnant women and in infants of women breastfeeding.

• Decrease in serum low-density lipoprotein cholesterol levels. Therapy is usually discontinued if the clinical response remains poor after 3 mo of therapy.
• Decrease in severity of pruritus. Relief usually occurs 1–3 wk after therapy is initiated.
• Decrease in frequency and severity of diarrhea.

Prevalite, Questran, Questran Light

Olestyr, Olestyr Light