Pronunciation

(koe LES ti pole)

Index Terms

• Colestipol HCl
• Colestipol Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Granules, Oral, as hydrochloride:

Colestid: 5 g/5 g scoop (300 g, 500 g) [contains aspartame; unflavored flavor]

Colestid Flavored: 5 g/7.5 g scoop (450 g) [contains aspartame; orange flavor]

Generic: 5 g/5 g scoop (500 g)

Packet, Oral, as hydrochloride:

Colestid: 5 g (30 ea, 90 ea) [unflavored flavor]

Colestid Flavored: 5 g (60 ea) [contains aspartame; orange flavor]

Generic: 5 g (30 ea, 90 ea)

Tablet, Oral, as hydrochloride:

Colestid: 1 g

Generic: 1 g

Brand Names: U.S.

• Colestid
• Colestid Flavored

Pharmacologic Category

• Antilipemic Agent, Bile Acid Sequestrant

Pharmacology

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

Absorption

None

Excretion

Feces

Onset of Action

Lowering of serum cholesterol: ~1 month; LDL-C reduction: ~19%

Use: Labeled Indications

Primary hypercholesterolemia: Adjunctive therapy to diet in patients with primary hypercholesterolemia

Off Label Uses

Diarrhea associated with excess fecal bile acids

Data from a double-blind, placebo-controlled trial in critically-ill patients receiving enteral feeding with diarrhea associated with excess luminal bile acids supports the use of colestipol in the treatment of this condition ^{[DeMoe 1998]}. Additionally, data from a retrospective study in patients with collagenous colitis and bile acid malabsorption associated diarrhea suggests that colestipol is beneficial for treatment of this condition ^{[Ung 2000]}. Clinical experience also suggests the utility of colestipol in managing diarrhea associated with excess fecal bile acids ^{[Walter 2010]}. Additional trials may be necessary to further define the role of cholestyramine resin in this condition.

Pruritus with primary biliary obstruction

Data from a limited number of patients studied (case series) suggests that cholestyramine may be beneficial for the treatment of patients who are experiencing pruritus due to elevated serum bile acid concentrations ^{[Datta 1963]}. When cholestyramine is not tolerated well due to gastrointestinal side effects (eg, bloating, constipation) or unpleasant taste, colestipol may be used although clinical trial data are lacking ^{[Schlichting 2001]}. Clinical experience also suggests the utility of colestipol in providing relief of pruritus associated with elevated serum levels of bile acids ^{[Scaldaferri 2011]}. Additional data may be necessary to further define the role of colestipol in this condition.

American Association for the Study of Liver Diseases practice guidelines for primary biliary cirrhosis recommend bile acid sequestrants as first-line drug therapy for pruritus associated with liver disease, noting that the benefits of cholestyramine (which is approved for relief of pruritus associated with partial biliary obstruction) are supported by consensus based on older data. The guidelines also note that at the time of guideline development, there were no controlled trials evaluating colesevelam or colestipol for treatment of pruritus.

Contraindications

Hypersensitivity to colestipol or any component of the formulation

Canadian labeling: Additional contraindications (not in US labeling): Complete biliary obstruction; phenylketonurics (Colestid Orange Granules only)

Dosing: Adult

Primary hypercholesterolemia: Oral:

Granules: Initial: 5 g once or twice daily; increase by 5 g per day at 1- to 2-month intervals. In patients with preexisting constipation, initiate at 5 g once daily for 5 to 7 days, then increase to 5 g twice daily. Maintenance: 5 to 30 g per day, once daily or in divided doses.

Tablets: Initial: 2 g once or twice daily; increase by 2 g once or twice daily at 1- to 2-month intervals. Maintenance: 2 to 16 g per day, once daily or in divided doses.

Pruritus with primary biliary obstruction (off-label use): Oral: Initial: 5 g once daily; increase as needed, up to 30 g/day (Schlichting 2001). Additional data may be necessary to further define the role of colestipol in this condition.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling; however, dosage adjustment is unlikely because not absorbed from the gastrointestinal tract.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling; however, dosage adjustment is unlikely because not absorbed from the gastrointestinal tract.

Administration

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 or respiratory distress). Add granules to ≥90 mL of liquid and stir until completely mixed; may be mixed with any beverage or added to soups, cereal, or pulpy fruits (eg, fruit cocktail, crushed pineapple, peaches, or pears), yogurt, pudding, or cottage cheese. After administration, rinse glass with a small amount of liquid and ingest to ensure all medication is taken.

Tablets: Administer tablets 1 at a time, swallowed whole, with plenty of liquid. Canadian labeling recommends administration with meals. Do not cut, crush, or chew tablets.

Dietary Considerations

Some products may contain phenylalanine.

Storage

Store at 20°C to 25°C (68°F to 77°F).

Drug Interactions

Amiodarone: Bile Acid Sequestrants may decrease the bioavailability of Amiodarone. Consider therapy modification

AtorvaSTATin: Bile Acid Sequestrants may decrease the serum concentration of AtorvaSTATin. Monitor therapy

Cardiac Glycosides: Bile Acid Sequestrants may decrease the absorption of Cardiac Glycosides. 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. Consider therapy modification

Cholic Acid: Bile Acid Sequestrants may decrease the absorption of Cholic Acid. Management: Administer cholic acid at least 1 to 4 hours before or 4 to 6 hours after administration of any bile acid-binding products to minimize the potential for a significant interaction. Consider therapy modification

Corticosteroids (Oral): Bile Acid Sequestrants may decrease the absorption of Corticosteroids (Oral). Monitor therapy

Deferasirox: Bile Acid Sequestrants may decrease the serum concentration of Deferasirox. Management: Avoid combination when possible; if the combination must be used, consider a 50% increase in initial deferasirox dose, with monitoring of serum ferritin concentrations and clinical responses to guide further dosing. Consider therapy modification

DilTIAZem: Colestipol may decrease the absorption of DilTIAZem. Monitor therapy

Estrogen Derivatives (Contraceptive): Bile Acid Sequestrants may decrease the serum concentration of Estrogen Derivatives (Contraceptive). Management: Administer estrogen-based oral contraceptives at least 1 to 4 hours prior to or 4 to 6 hours after administration of a bile acid sequestrant. Consider therapy modification

Ezetimibe: Bile Acid Sequestrants may decrease the absorption of Ezetimibe. Management: Administer ezetimibe at least 2 hours before or 4 hours after any bile acid sequestrant. Consider therapy modification

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. 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. Consider therapy modification

Lomitapide: Bile Acid Sequestrants may decrease the absorption of Lomitapide. Management: Administer lomitapide at least 4 hours before or after administration of a bile acid sequestrant. Consider therapy modification

Loop Diuretics: Bile Acid Sequestrants may decrease the absorption of Loop Diuretics. Consider therapy modification

Methotrexate: Bile Acid Sequestrants may decrease the absorption of Methotrexate. Monitor therapy

Methylfolate: Colestipol may decrease the serum concentration of Methylfolate. Monitor therapy

Multivitamins/Fluoride (with ADE): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Fluoride (with ADE). Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (eg, cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Consider therapy modification

Multivitamins/Minerals (with ADEK, Folate, Iron): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Minerals (with ADEK, Folate, Iron). Specifically, bile acid sequestrants may impair the absorption of fat-soluble vitamins. Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (eg, cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Consider therapy modification

Multivitamins/Minerals (with AE, No Iron): Bile Acid Sequestrants may decrease the serum concentration of Multivitamins/Minerals (with AE, No Iron). Management: Avoid concomitant administration of multivitamins and bile acid sequestrants (e.g., cholestyramine). Separate administration of these agents by several hours to minimize the risk of an interaction. Consider therapy modification

Mycophenolate: Bile Acid Sequestrants may decrease the serum concentration of Mycophenolate. Avoid combination

Niacin: Bile Acid Sequestrants may decrease the absorption of Niacin. Consider therapy modification

Nonsteroidal Anti-Inflammatory Agents: Bile Acid Sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Consider therapy modification

Obeticholic Acid: Bile Acid Sequestrants may decrease the serum concentration of Obeticholic Acid. Management: Administer obeticholic acid at least 4 hours before or at least 4 hours after the administration of bile acid sequestrants. 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. Consider therapy modification

Progestins (Contraceptive): Bile Acid Sequestrants may decrease the serum concentration of Progestins (Contraceptive). Management: Administer oral progestin-containing contraceptives at least 1 to 4 hours prior to or 4 to 6 hours after administration of a bile acid sequestrant. Consider therapy modification

Propranolol: Bile Acid Sequestrants may decrease the serum concentration of Propranolol. Monitor therapy

Raloxifene: Bile Acid Sequestrants may decrease the absorption of Raloxifene. Consider therapy modification

Teriflunomide: Bile Acid Sequestrants may decrease the serum concentration of Teriflunomide. Management: Unless using this combination to intentionally enhance teriflunomide elimination, consider an alternative to the bile acid sequestrants when possible. Separating drug administration is unlikely to be effective at avoiding the interaction. Consider therapy modification

Tetracyclines: Bile Acid Sequestrants may decrease the absorption of Tetracyclines. Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Bile Acid Sequestrants may decrease the absorption of Thiazide and Thiazide-Like Diuretics. The diuretic response is likewise decreased. Consider therapy modification

Thyroid Products: Bile Acid Sequestrants may decrease the serum concentration of Thyroid Products. Management: Administer oral thyroid products at least 4 h prior to colesevelam, and at least 1 h before or 4-6 h after cholestyramine. Specific recommendations for colestipol are not available. Monitor for decreased concentrations/effects of the thyroid product. Consider therapy modification

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. 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. 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 (eg, cholestyramine). Separate administration of these agents by several hours to minimize the potential risk of interaction. Monitor plasma calcium concentrations. Exceptions: Calcipotriene; Calcitriol (Topical); Tacalcitol. Consider therapy modification

Vitamin K Antagonists (eg, warfarin): Bile Acid Sequestrants may decrease the absorption of Vitamin K Antagonists. Monitor therapy

Adverse Reactions

Frequency not defined.

Cardiovascular: Angina, chest pain, peripheral edema, tachycardia

Central nervous system: Dizziness, fatigue, headache (including migraine and sinus headache), insomnia

Dermatologic: Dermatitis, skin rash, urticaria

Gastrointestinal: Abdominal cramps, abdominal pain, anorexia, bloating, constipation, cholecystitis, cholelithiasis, diarrhea, dyspepsia, dysphagia, esophageal obstruction, flatulence, heartburn, hemorrhoidal bleeding, nausea, peptic ulcer, vomiting

Hepatic: Increased serum alkaline phosphatase, increased serum ALT, increased serum AST

Neuromuscular & skeletal: Arthralgia, arthritis, back pain, myalgia, weakness

Respiratory: Dyspnea

Warnings/Precautions

Concerns related to adverse effects:

• Acidosis: Chronic use may lead to development of hyperchloremic acidosis.

• Bleeding: Chronic use may be associated with bleeding problems due to hypoprothrombinemia from vitamin K deficiency; may be prevented with use of vitamin K therapy.

• Constipation: May produce or exacerbate constipation; fecal impaction may occur; initiate therapy at a reduced dose and increase gradually in patients with a history of constipation. Encourage increased fluid and fiber intake; a stool softener may also be indicated. Hemorrhoids may be worsened.

• Hypothyroidism: There is a theoretical risk of developing hypothyroidism, particularly in patients with limited thyroid reserve. Use with caution.

Disease-related concerns:

• Hypertriglyceridemia: Bile acid sequestrants should not be used in patients with baseline fasting triglyceride levels ≥300 mg/dL or type III hyperlipoproteinemia because severe triglyceride elevations may occur. Use bile acid sequestrants with caution in patients with triglyceride levels 250 to 299 mg/dL; evaluate a fasting lipid panel in 4 to 6 weeks after initiation; discontinue use if triglycerides are >400 mg/dL (ACC/AHA [Stone, 2013]).

Concurrent drug therapy issues:

• Decreased absorption (orally administered drugs): Not to be taken simultaneously with many other medicines, including vitamin supplements.

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Dosage form specific issues:

• Granules: Colestipol granules should never be taken in dry form; may cause esophageal spasm and/or respiratory distress.

• Phenylalanine: Some products may contain phenylalanine.

Other warnings/precautions:

• Hyperlipidemia: Secondary causes of hyperlipidemia should be ruled out prior to therapy initiation.

• 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.

Monitoring Parameters

Fasting lipid profile before initiating treatment, 3 months after initiation, and every 6-12 months thereafter (Stone, 2013)

Pregnancy Considerations

Lipid concentrations increase during pregnancy as required for normal fetal development. When increases are greater than expected, supervised dietary intervention should be initiated. Bile acid sequestrants are recommended when treatment is needed (Avis 2009; Jacobson 2015).

Colestipol is not absorbed systemically (<0.17%), but may interfere with maternal vitamin absorption; therefore, regular prenatal supplementation may not be adequate.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience heartburn, abdominal cramps, flatulence, diarrhea, nausea, or vomiting. Have patient report immediately to prescriber severe abdominal pain, severe constipation, or difficulty swallowing (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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