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Pronunciation
(koe LES ti pole)
Generic Available (U.S.)
Yes
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Adjunct in management of primary hypercholesterolemia
Use: Unlabeled
Diarrhea associated with excess fecal bile acids (Westergaard, 2007); relief of pruritus associated with elevated levels of bile acids (Datta, 1963; Scaldaferri, 2011)
Pregnancy Considerations
Colestipol is not absorbed systemically (<0.17%), but may interfere with vitamin absorption; therefore, regular prenatal supplementation may not be adequate. There are no studies in pregnant women; use with caution.
Lactation
Does not enter breast milk/use caution
Breast-Feeding Considerations
Due to lack of systemic absorption (<0.17%), colestipol is not expected to be excreted into breast milk; however, the tendency of colestipol to interfere with vitamin absorption may have an effect on the nursing infant.
Contraindications
Hypersensitivity to bile acid sequestering resins or any component of the formulation
Warnings/Precautions
Concerns related to adverse effects:
• Bleeding: Chronic use may be associated with bleeding problems; may be prevented with use of oral vitamin K therapy.
• Constipation: May produce or exacerbate constipation problems; fecal impaction may occur; initiate therapy at a reduced dose in patients with a history of constipation. Hemorrhoids may be worsened.
Concurrent drug therapy issues:
• Decreased absorption (orally administered drugs): Not to be taken simultaneously with many other medicines (decreased absorption).
• Patients susceptible to fat-soluble vitamin and folic acid deficiencies: Use with caution in patients susceptible to fat-soluble vitamin deficiencies. Absorption of fat soluble vitamins A, D, E, and K and folic acid may be decreased; patients should take vitamins ≥4 hours before colestipol.
Dosage form specific issues:
• Phenylalanine: Some products may contain phenylalanine.
Other warnings/precautions:
• Hyperlipidemia: Secondary causes of hyperlipidemia should be ruled out prior to therapy.
Adverse Reactions
Frequency not defined.
Cardiovascular: Angina, chest pain, edema of hands or feet, tachycardia
Central nervous system: Dizziness, fatigue, headache (including migraine and sinus), lightheadedness, insomnia
Dermatologic: Dermatitis, rash, urticaria
Gastrointestinal: Abdominal pain and cramping, anorexia, bloating, constipation, cholecystitis, cholelithiasis, diarrhea, dysphagia, esophageal obstruction, flatulence, indigestion, heartburn, hemorrhoids (bleeding), nausea, peptic ulceration, vomiting
Hepatic: Alkaline phosphatase increased, ALT increased, AST increased
Neuromuscular & skeletal: Arthritis, backache, joint/muscle pain, weakness
Respiratory: Dyspnea
Metabolism/Transport Effects
None known.
Drug Interactions
Amiodarone: Bile Acid Sequestrants may decrease the bioavailability of Amiodarone. Risk D: Consider therapy modification
Antidiabetic Agents (Thiazolidinedione): Bile Acid Sequestrants may decrease the absorption of Antidiabetic Agents (Thiazolidinedione). Risk D: Consider therapy modification
Cardiac Glycosides: Bile Acid Sequestrants may decrease the absorption of Cardiac Glycosides. Risk C: Monitor therapy
Chenodiol: Bile Acid Sequestrants may decrease the serum concentration of Chenodiol. Management: Administration of chenodiol 5 hours or more after bile acid sequestrants may reduce chenodiol adsorption in the gastrointestinal tract. Monitor for decreased therapeutic effects of chenodiol in patients receiving bile acid sequestrants. Risk D: Consider therapy modification
Contraceptives (Estrogens): Bile Acid Sequestrants may decrease the serum concentration of Contraceptives (Estrogens). Management: Administer estrogen-based oral contraceptives at least 1-4 hours prior to or 4-6 hours after administration of a bile acid sequestrant. Risk D: Consider therapy modification
Contraceptives (Progestins): Bile Acid Sequestrants may decrease the serum concentration of Contraceptives (Progestins). Management: Administer oral progestin-containing contraceptives at least 1-4 hours prior to or 4-6 hours after administration of a bile acid sequestrant. Risk D: Consider therapy modification
Corticosteroids (Oral): Bile Acid Sequestrants may decrease the absorption of Corticosteroids (Oral). Risk C: Monitor therapy
Diltiazem: Colestipol may decrease the absorption of Diltiazem. Risk C: Monitor therapy
Ezetimibe: Bile Acid Sequestrants may decrease the absorption of Ezetimibe. Risk C: Monitor therapy
Fibric Acid Derivatives: Bile Acid Sequestrants may decrease the absorption of Fibric Acid Derivatives. Management: Separate doses by at least 2 hours to minimize this interaction; fenofibric acid labeling recommends administration one hour prior to or 4-6 hours after a bile acid sequestrant. Risk D: Consider therapy modification
Leflunomide: Bile Acid Sequestrants may decrease serum concentrations of the active metabolite(s) of Leflunomide. Management: Unless using this combination to intentionally enhance leflunomide elimination, consider an alternative to the bile acid sequestrants when possible. Separating drug administration is not likely to be effective at avoiding this interaction. Risk D: Consider therapy modification
Loop Diuretics: Bile Acid Sequestrants may decrease the absorption of Loop Diuretics. Risk D: Consider therapy modification
Methotrexate: Bile Acid Sequestrants may decrease the absorption of Methotrexate. Risk C: Monitor therapy
Methylfolate: Colestipol may decrease the serum concentration of Methylfolate. Risk C: Monitor therapy
Niacin: Bile Acid Sequestrants may decrease the absorption of Niacin. Risk D: Consider therapy modification
Nonsteroidal Anti-Inflammatory Agents: Bile Acid Sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Risk D: Consider therapy modification
Pravastatin: Bile Acid Sequestrants may decrease the serum concentration of Pravastatin. Management: Administer pravastatin at least 1 hour before or 4 hours after administration of bile-acid resins (eg, cholestyramine, colestipol, colesevelam) to minimize the risk for any significant interaction. Risk D: Consider therapy modification
Propranolol: Bile Acid Sequestrants may decrease the serum concentration of Propranolol. Risk C: Monitor therapy
Raloxifene: Bile Acid Sequestrants may decrease the absorption of Raloxifene. Risk D: Consider therapy modification
Tetracycline Derivatives: Bile Acid Sequestrants may decrease the absorption of Tetracycline Derivatives. Risk D: Consider therapy modification
Thiazide Diuretics: Bile Acid Sequestrants may decrease the absorption of Thiazide Diuretics. The diuretic response is likewise decreased. Risk D: Consider therapy modification
Thyroid Products: Bile Acid Sequestrants may decrease the absorption of Thyroid Products. Risk C: Monitor therapy
Ursodiol: Bile Acid Sequestrants may decrease the serum concentration of Ursodiol. Management: Administer ursodiol 5 hours or more after bile acid sequestrants to minimize ursodiol adsorption in the gastrointestinal tract. Monitor for decreased therapeutic effects of ursodiol in patients receiving bile acid sequestrants. Risk D: Consider therapy modification
Vancomycin: Bile Acid Sequestrants may diminish the therapeutic effect of Vancomycin. Management: Avoid concurrent administration of oral vancomycin and bile acid sequestrants when possible. If use of both agents is necessary, consider separating doses by at least 2 hours to minimize the significance of the interaction. Risk D: Consider therapy modification
Vitamin D Analogs: Bile Acid Sequestrants may decrease the serum concentration of Vitamin D Analogs. More specifically, bile acid sequestrants may impair absorption of Vitamin D Analogs. Management: Avoid concomitant administration of vitamin D analogs and bile acid sequestrants (e.g., cholestyramine). Separate administration of these agents by several hours to minimize the potential risk of interaction. Monitor plasma calcium concentrations. Exceptions: Calcipotriene. Risk D: Consider therapy modification
Vitamin K Antagonists (eg, warfarin): Bile Acid Sequestrants may decrease the absorption of Vitamin K Antagonists. Risk C: Monitor therapy
Storage
Store at 20°C to 25°C (68°F to 77°F).
Mechanism of Action
Binds with bile acids to form an insoluble complex that is eliminated in feces; it thereby increases the fecal loss of bile acid-bound low density lipoprotein cholesterol
Pharmacodynamics/Kinetics
Absorption: None
Excretion: Feces
Dosage
Adults: Oral:
Granules: Initial: 5 g 1-2 times/day; maintenance: 5-30 g/day given once or in divided doses; increase by 5 g/day at 1- to 2-month intervals
Tablets: Initial: 2 g 1-2 times/day; maintenance: 2-16 g/day given once or in divided doses; increase by 2 g once or twice daily at 1- to 2-month intervals
Dosage adjustment in renal impairment: No dosage adjustment necessary; not absorbed from the gastrointestinal tract.
Dosage adjustment in hepatic impairment: No dosage adjustment necessary; not absorbed from the gastrointestinal tract.
Administration: Oral
Other drugs should be administered at least 1 hour before or 4 hours after colestipol.
Granules: Do not administer in dry form (to avoid GI distress). Dry granules should be added to at least 90 mL of liquid and stirred until completely mixed; may be mixed with any beverage or added to soups, cereal, or pulpy fruits. Rinse glass with a small amount of liquid to ensure all medication is taken.
Tablets: Administer tablets 1 at a time, swallowed whole, with plenty of liquid. Do not cut, crush, or chew tablets.
Monitoring Parameters
Serum cholesterol, LDL, and triglyceride levels should be obtained before initiating treatment and periodically thereafter (in accordance with NCEP guidelines)
Test Interactions
Increased prothrombin time
Dietary Considerations
Some products may contain phenylalanine.
Patient Education
Take granules with 3-4 oz of water or fruit juice. Rinse glass with small amount of water to ensure full dose is taken. Take tablets one at a time. Other medications should be taken 1 hour before or 4 hours after colestipol. You may experience constipation, drowsiness, or dizziness. Report acute gastric pain, tarry stools, or respiratory difficulty.
Geriatric Considerations
The definition of and, therefore, when to treat hyperlipidemia in the elderly is a controversial issue. The National Cholesterol Education Program recommends that all adults maintain a plasma cholesterol <160 mg/dL. Elderly with one additional risk factor, goal LDL would be <130 mg/dL. It is the authors' belief that pharmacologic treatment be reserved for those who are unable to obtain a desirable plasma cholesterol concentration by diet alone and for whom the benefits of treatment are believed to outweigh the potential adverse effects, drug interactions, and cost of treatment.
Cardiovascular Considerations
Colestipol alone or when combined with an HMG-CoA reductase inhibitor is effective in lowering cholesterol. Colestipol may increase triglycerides, therefore, it should be avoided in patients with triglyceride levels ≥200 mg/dL. Potential factors that may limit patient compliance include GI side effects and the need to separate administration of other medications from colestipol.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause drowsiness or anxiety
Mental Health: Effects on Psychiatric Treatment
Constipation is common; may be exacerbated by concurrent psychotropic use; may decrease the absorption of TCAs
Nursing: Physical Assessment/Monitoring
Monitor bowel function. Be alert to potential for constipation or hemorrhoid problems.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Granules for suspension, oral, as hydrochloride: 5 g/scoop (500 g); 5 g/packet (30s, 90s)
Colestid®: 5 g/scoop (300 g, 500 g); 5 g/packet (30s, 90s) [unflavored]
Colestid® Flavored: 5 g/scoop (450 g) [contains phenylalanine 18.2 mg/scoop; orange flavor]
Colestid® Flavored: 5 g/packet (60s) [contains phenylalanine 18.2 mg/packet; orange flavor]
Tablet, oral, as hydrochloride: 1 g
Tablet, oral, as hydrochloride [micronized]: 1 g
Colestid®: 1 g
Pricing: U.S. (www.drugstore.com)
Granules (Colestid)
5 g (500): $158.55
Granules (Colestid Flavored)
5 g (450): $136.50
Pack (Colestid)
5 g (30): $90.30
5 g (90): $225.99
Pack (Colestid Flavored)
5 g/7.5 g (60): $210.00
Tablets (Colestid)
1 g (120): $111.29
Tablets (Micronized Colestipol HCl)
1 g (30): $26.99
References
“Executive Summary of The Third Report of The National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel III),” JAMA, 2001, 285(19):2486-97.
Datta DV and Sherlock S, “Treatment of Pruritus of Obstructive Jaundice With Cholestyramine,” B Med J, 1963, 1(5325):216-9.
McPherson R, Frohlich J, Fodor G, et al, “Canadian Cardiovascular Society Position Statement--Recommendations for the Diagnosis and Treatment of Dyslipidemia and Prevention of Cardiovascular Disease,” Can J Cardiol, 2006, 22(11):913-27; published erratum appears in Can J Cardiol, 2006, 22(12):1077.
Scaldaferri F, Pizzoferrato M, Ponziani FR, et al, “Use and Indications of Cholestyramine and Bile Acid Sequestrants,” Intern Emerg Med, 2011 [pub ahead of print].
Smith SC Jr, Benjamin EJ, Bonow RO, et al, “AHA/ACCF Secondary Prevention and Risk Reduction Therapy for Patients With Coronary and Other Atherosclerotic Vascular Disease: 2011 Update: A Guideline From the American Heart Association and American College of Cardiology Foundation,” Circulation, 2011, 124(22):2458-73.
Westergaard H, “Bile Acid Malabsorption,” Curr Treat Options Gastroenterol, 2007, 10(1):28-33.
International Brand Names
Lexi-Comp.com
Last full review/revision January 2012
Content last modified January 2012
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