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Therapeutic Classification: lipid-lowering agents

Pharmacologic Classification: bile acid sequestrants

• Primary hypercholesterolemia.
• Pruritus associated with elevated levels of bile acids.

Unlabeled Uses:

• Diarrhea associated with excess bile acids.

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

• Decreased plasma cholesterol and LDL-C.
• 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.

Exercise Extreme Caution in:

• Pedi: May cause potentially fatal intestinal obstruction in children.

Derm: irritation, rash.

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

• PO (Adults): Granules: 5 g 1–2 times daily; may be ↑ every 1–2 mo up to 30 g/day in 1–2 doses. Tablets: 2 g 1–2 times daily, may be ↑ every 1–2 mo up to 16 g/day in 1–2 doses.

(Generic available)

• Granules for suspension (unflavored [with aspartame]): 5 g/packet or scoop;
• Tablets: 1 g;

• Hypercholesterolemia: Obtain a diet history, especially regarding 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.
• Assess for signs and symptoms of fecal impaction or obstruction (abdominal pain and tenderness, abdominal distention, severe constipation, watery diarrhea, nausea, and vomiting).

• 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 PT.

• Parenteral or water-miscible forms of fat-soluble vitamins (A, D, E, K) and folic acid may be ordered for patients on chronic therapy.
• PO: Administer before meals.
  • DNC: Swallow tablets whole; do not crush, break, or chew.
  • 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.

• Explain reason for and side effects of colestipol to patient.
• Instruct patient to take medication exactly as directed; do not skip doses or double up on missed doses. Supplementation of fat-soluble vitamins may be needed (A, D, E, K).
• Instruct patient to take medication before meals. Tablets should be taken with a full glass of water to avoid esophageal obstruction. Granules can be mixed with water, juice, or carbonated beverages. 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.
• Advise patient that this medication should be used in conjunction with diet 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 severe constipation, abdominal pain, bloating, cramps, nausea, vomiting, 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.

• Decrease in serum LDL 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.

Colestid