Class: Bile Acid Sequestrants
VA Class: CV350
CAS Number: 37296-80-3
Medically reviewed on November 20, 2017
Antilipemic agent; bile acid sequestrant.
Uses for Colestipol Hydrochloride
Adjunct to dietary therapy to decrease elevated serum total and LDL-cholesterol concentrations in the management of primary hypercholesterolemia in patients who do not respond adequately to diet.166 167
Generally has no clinically relevant effect on serum triglyceride concentrations,100 167 but may increase triglyceride concentrations in some patients.167 (See Hypertriglyceridemia under Cautions.) Do not use in patients with primary dysbetalipoproteinemia (Fredrickson type III).350
ACC/AHA cholesterol management guideline states that nonstatin drugs (e.g., bile acid sequestrants) do not provide acceptable atherosclerotic cardiovascular disease (ASCVD) risk reduction benefits compared to their potential for adverse effects in the routine prevention of ASCVD.350 May be useful as adjuncts to statin therapy in high-risk patients (e.g., patients with ASCVD, LDL-cholesterol concentrations ≥190 mg/dL, or diabetes mellitus) who have a less-than-anticipated response to statins, are unable to tolerate even a less-than-recommended intensity of a statin, or are completely intolerant to statin therapy.350 Select nonstatin drug based on favorable benefit-risk ratio (i.e., demonstrated benefit of ASCVD risk reduction outweighs risks of adverse effects and drug interactions) and patient preferences.350
Colestipol Hydrochloride Dosage and Administration
Instruct patients to take other drugs at least 1 hour before or 4 hours after taking colestipol tablets or suspension to minimize possible interference with absorption.166 167 (See Effects on GI Absorption of Drugs under Interactions.)
Monitoring during Antilipemic Therapy
Determine serum cholesterol and triglyceride concentrations prior to and regularly (e.g., every 3–6 months) during colestipol therapy. ACC/AHA cholesterol management guideline recommends obtaining a fasting lipoprotein profile before initiating bile acid sequestrant therapy, after 3 months of therapy, and every 6–12 months thereafter.350
To avoid accidental inhalation or esophageal distress, do not administer colestipol hydrochloride for oral suspension in its dry form.166
To minimize excessive swallowing of air, advise patients to avoid rapid ingestion of suspensions of the drug.136 After the mixture is ingested, rinse the glass with a small amount of additional fluid and ingest the remaining liquid to ensure that the entire dose has been taken.166
Add the prescribed amount of colestipol hydrochloride granules to at least 90 mL of a liquid (e.g., fruit juice, water, milk, soft drink) and stir until completely mixed (colestipol will not dissolve in the liquid).166 Palatability and compliance may be increased if the entire next-day’s dose is mixed in one of these liquids in the evening and then refrigerated.121 Use of a heavy or pulpy fruit juice may minimize complaints about consistency of suspensions of the drug.135 136 166 If a carbonated beverage is used, mix the powder slowly in a large glass to minimize excessive foaming; however, use of a carbonated beverage as a vehicle may be associated with adverse GI effects.166
Alternatively, mix colestipol powder with milk in hot or regular breakfast cereals, a highly fluid soup, or pulpy fruit (e.g., crushed pineapple, pears, peaches, fruit cocktail).166
One dose (1 packet or 1 level teaspoon) of colestipol hydrochloride granules contains 5 g of colestipol hydrochloride.166 One dose (1 packet or 1 level scoop) of flavored colestipol hydrochloride granules contains 7.5 g of granules, which contains 5 g of colestipol hydrochloride.166
Pediatric dosage has not been established;100 166 167 however, dosages of 10–20 g or 500 mg/kg daily in 2–4 divided doses have been used.115 116 118 119 Lower dosages (e.g., 125–250 mg/kg daily) have also been used in some children when serum cholesterol concentrations were only 15–20% above normal after dietary management alone.117
If the desired therapeutic effect is not achieved with the usual dosage of 2–16 g daily with good compliance and acceptable adverse effects, consider combined therapy or alternative treatment.167
If triglyceride concentrations increase markedly, consider reducing dosage, discontinuing therapy, or using combined or alternative treatment.167
Oral (Granules for oral suspension)
Initially, 5 g (1 packet or 1 level scoop) once or twice daily.100 166 Titrate dose upward as necessary in 5-g increments at 1- or 2-month intervals.135 136 166 Usual daily dosage range is 5–30 g (1–6 packets or level scoops) taken once or in divided doses.100 166
If the desired therapeutic effect is not achieved with the usual dosage of 1–6 doses per day with good compliance and acceptable adverse effects, consider combined therapy or alternative treatment.166
If triglyceride concentrations increase markedly, consider reducing dosage, discontinuing therapy, or using combined or alternative treatment.166
Patients with preexisting constipation receiving granules for oral suspension: Initially, 5 g once daily for 5–7 days; then increase dosage to 5 g twice daily and monitor constipation and serum lipoprotein values, at least twice, 4–6 weeks apart.166 Thereafter, increase dosage as needed by 1 dose per day (at monthly intervals) with periodic monitoring of serum lipoprotein values;166 adjust dosage accordingly to achieve the desired effect while avoiding excessive dosage.135 136 If constipation worsens or the desired effect is not achieved with acceptable adverse effects with the usual dosage of 1–6 doses per day, consider combined therapy or alternative treatment.135 136 166
Cautions for Colestipol Hydrochloride
Known hypersensitivity to colestipol or any ingredient in the formulation.166
To avoid accidental inhalation or esophageal distress, do not administer colestipol hydrochloride for oral suspension in its dry form.166 Always mix colestipol hydrochloride granules with water or other fluids before ingesting.166 (See Administration under Dosage and Administration.)
Individuals with phenylketonuria (i.e., homozygous genetic deficiency of phenylalanine hydroxylase) and other individuals who must restrict their intake of phenylalanine should be warned that Flavored Colestid granules for oral suspension contain aspartame (NutraSweet), which is metabolized in the GI tract following oral administration to provide 18.2 mg of phenylalanine per 7.5-g packet.166
Generally has no clinically relevant effect on serum triglyceride concentrations,100 167 but may increase triglyceride concentrations in some patients.167 Use with caution in patients with baseline triglyceride concentrations of 250–299 mg/dL; discontinue when triglyceride concentrations >400 mg/dL.350
Do not use in patients with baseline fasting triglyceride concentrations ≥300 mg/dL or in those with primary dysbetalipoproteinemia (Fredrickson type III).350
Mild and, occasionally, severe constipation has occurred.166 167 Exacerbation of preexisting constipation and aggravation of hemorrhoids secondary to constipation may occur.166 167 Encourage increased fluid and fiber intake to alleviate constipation;111 114 121 136 166 167 173 a stool softener can be added if necessary.135 136 166 167 In addition, adjust dosage carefully and titrate slowly to minimize adverse GI effects (e.g., fecal impaction).135 166 167 (See Dosage under Dosage and Administration.) Make particular effort to avoid constipation in patients with symptomatic CHD.166 167 Discontinuation of colestipol therapy may be required in some patients.166 167
Difficulty swallowing and transient esophageal obstruction have been reported rarely.166 167 Patients with a history of swallowing difficulties or choking with food, liquids, or other tablets or capsules should consult a clinician before initiating therapy with colestipol hydrochloride tablets.167 If abdominal pressure or discomfort (secondary to esophageal obstruction) occurs, advise patients to consult a clinician prior to administering the next dose.167
Abdominal discomfort (including pain and cramping), belching, flatulence, indigestion, heartburn, nausea, vomiting, and diarrhea or loose stools also have been reported.166 167 Bleeding hemorrhoids and blood in the stool have been reported infrequently.166 167 Peptic ulceration, cholecystitis, and cholelithiasis have been reported occasionally but are not necessarily drug-related.166 167
Fat-soluble Vitamin Deficiency
May interfere with the absorption of folic acid and fat-soluble vitamins (e.g., vitamins A, D, E, K).166 167 Prolonged use may be associated with an increased bleeding tendency as a result of hypoprothrombinemia secondary to vitamin K deficiency.166 167 (See Specific Drugs under Interactions.)
Common Adverse Effects
Interactions for Colestipol Hydrochloride
Effects on GI Absorption of Drugs
May bind to a number of drugs in the GI tract and may delay or reduce their absorption.166 167 Instruct patients to allow as long a time interval as possible between ingestion of other drugs and colestipol.166 167 The manufacturer recommends administering other drugs at least 1 hour before or 4 hours after colestipol.166 167
Consider the possibility that discontinuance of colestipol in patients stabilized on potentially toxic drugs that bind to the resin may lead to toxicity and that administration of colestipol to patients stabilized on other drugs may reduce the effect of these drugs.166 167
Antidiabetic agents (sulfonylureas)
Decreased antilipemic effects of colestipold
β-adrenergic blocking agents (propranolol)
Diuretics, thiazide (e.g., hydrochlorothiazide, chlorothiazide)
Fat-soluble Vitamins (i.e., vitamins A, D, E, K)
Consider supplemental administration of vitamins A and D if colestipol is to be given for a prolonged period.d
Phosphate supplements, oral
Colestipol Hydrochloride Pharmacokinetics
Granules for Suspension
Actions and Spectrum
Binds to bile acids in the intestine and forms a nonabsorbable complex that is excreted in feces.166 167 Partial removal of bile acids from the enterohepatic circulation via this mechanism results in increased conversion of cholesterol to bile acids in the liver.166 167 This causes an increased demand for cholesterol in liver cells, resulting in a compensatory increase in hepatic uptake (and thus systemic clearance) of circulating LDL-cholesterol.166 167
Advice to Patients
Inform patients that colestipol hydrochloride tablets may be larger than typical tablets or capsules.167 (See GI Effects under Cautions.)
For phenylketonurics, importance to inform them that Flavored Colestid granules for oral suspension contains aspartame.166
Importance of informing patients of other important precautionary information. (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
5 g/packet or calibrated scoop*
Colestipol Hydrochloride for Oral Suspension
5 g/7.5 g packet or calibrated scoop
Colestid Flavored Granules
AHFS DI Essentials. © Copyright 2018, Selected Revisions November 20, 2014. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
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- Drug class: bile acid sequestrants
Other brands: Colestid