colestipol hydrochloride

colestipol hydrochloride

[kōles′tipol]

an antihyperlipidemic that acts by sequestering bile acids in the intestine for excretion, thus reducing plasma levels of cholesterol when the liver removes cholesterol to synthesize new bile.

indications It is prescribed in the treatment of hypercholesterolemia and xanthoma.

contraindications Biliary obstruction or known hypersensitivity to this drug prohibits its use.

adverse effects Among the more serious adverse reactions are skin rash; fecal impaction; and a deficiency of vitamins A, D, and K.

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colestipol hydrochloride

Colestid

Pharmacologic class: Bile acid sequestrant

Therapeutic class: Antihyperlipidemic

Pregnancy risk category NR

Action

Binds bile acids in GI tract and forms insoluble complex, impeding bile acid reabsorption and promoting its excretion. As a result, cholesterol and low-density lipoprotein levels decrease.

Availability

Granules for suspension: 5 g/packet or scoop

Tablets: 1 g

⊘Indications and dosages

➣ Primary hypercholesterolemia

Adults: Granules - 5 g P.O. once or twice daily; may increase q 1 to 2 months up to 30 g/day P.O. given in one or two divided doses. Tablets - 2 g P.O. once or twice daily; may increase q 1 to 2 months up to 16 g/day P.O. given in one or two divided doses.

Off-label uses

• Digoxin toxicity

Contraindications

• Hypersensitivity to drug

Precautions

Use cautiously in:
• history of constipation
• breastfeeding patients
• children (safety and efficacy not established).

Administration

• Mix granules with at least 90 ml of liquid, and stir until completely mixed.
• Give tablets with large amount of water.
• Administer other drugs 1 hour before or 4 hours after colestipol.

Route	Onset	Peak	Duration
P.O.	24-48 hr	1 mo	1 mo

Adverse reactions

CNS: dizziness, headache, vertigo, anxiety, syncope, fatigue

CV: chest pain

GI: nausea, vomiting, constipation, abdominal discomfort, fecal impaction, flatulence, fatty stools, hemorrhoids, perianal irritation, tongue irritation

Metabolic: deficiency of vitamins A, D, E, and K and folic acid, hyperchloremic acidosis

Musculoskeletal: osteoporosis, backache, muscle and joint pain, arthritis

Skin: irritation, rashes

Interactions

Drug-drug. Amiodarone, corticosteroids, digoxin, diuretics, fat-soluble vitamins (A, D, E, K), folic acid, gemfibrozil, imipramine, methotrexate, mycophenolate, nonsteroidal anti-inflammatory drugs, penicillin G, phosphates, propranolol, tetracyclines, thyroid preparations, ursodiol: decreased absorption of these drugs (when given orally)

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, phosphorus: increased levels

Prothrombin time: prolonged

Patient monitoring

• Monitor lipid levels frequently during first few months of therapy and periodically thereafter.
• Evaluate patient for signs and symptoms of abnormal bleeding.
• Be aware that prolonged use may increase bleeding tendency (from hypoprothrombinemia resulting from vitamin K deficiency). As prescribed and needed, give oral or parenteral vitamin K to reverse this effect.

Patient teaching

• Instruct patient to take granules with 3 to 4 oz of water, fruit juice, soup with high fluid content, cereal, or pulpy fruits (crushed).
• Tell patient to swallow tablets whole, one at a time, and not to crush, cut, or chew them.
• Inform patient that drug may interfere with absorption of many other drugs. Advise him to take other drugs 1 hour before or 4 hours after colestipol.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.