colestipol hydrochloride
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.
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.