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Colestipol

Class: Bile Acid Sequestrants
VA Class: CV350
CAS Number: 37296-80-3
Brands: Colestid

Medically reviewed by Drugs.com on Jul 26, 2021. Written by ASHP.

Introduction

Antilipemic agent; bile acid sequestrant.

Uses for Colestipol

Dyslipidemias

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.

Generally has no clinically relevant effect on serum triglyceride concentrations, but may increase triglyceride concentrations in some patients. (See Hypertriglyceridemia under Cautions.)

As effective as cholestyramine in lowering serum cholesterol concentrations. Select bile acid sequestrant based on patient tolerance, including palatability and taste preference, and cost.

AHA/ACC cholesterol management guideline states that lifestyle modification is the foundation of cardiovascular risk reduction. If pharmacologic therapy is needed, statins are first-line drugs of choice because of their demonstrated benefits in reducing risk of atherosclerotic cardiovascular disease (ASCVD). The addition of a nonstatin drug (e.g., ezetimibe, bile acid sequestrants, PCSK9 inhibitor) may be considered in certain circumstances such as in patients with very severe elevations of LDL-cholesterol concentrations who are not achieving adequate LDL lowering with maximally tolerated statin therapy.

Colestipol Dosage and Administration

General

  • Patients should be placed on a standard lipid-lowering diet before initiation of colestipol therapy and should remain on this diet during treatment with the drug.

  • To optimize antilipemic effects while minimizing the risk of adverse GI effects, adjust dosage carefully and titrate slowly.

  • 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. (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.

Administration

Oral Administration

Administer tablets one at a time; promptly swallow whole, using plenty of water or other appropriate liquid. The tablets must not be cut, crushed, or chewed.

To avoid accidental inhalation or esophageal distress, do not administer colestipol hydrochloride for oral suspension in its dry form.

To minimize excessive swallowing of air, advise patients to avoid rapid ingestion of suspensions of the drug. 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.

Reconstitution

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). 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. Use of a heavy or pulpy fruit juice may minimize complaints about consistency of suspensions of the drug. 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.

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).

Dosage

Available as colestipol hydrochloride; expressed in terms of the salt.

One dose (1 packet or 1 level teaspoon) of colestipol hydrochloride granules contains 5 g of colestipol hydrochloride. 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.

Pediatric Patients

Dyslipidemias†
Oral

Pediatric dosage has not been established; however, dosages of 10–20 g or 500 mg/kg daily in 2–4 divided doses have been used. 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.

Adults

Dyslipidemias
Oral (Tablets)

Initially, 2 g once or twice daily. Increase dosage by 2 g once or twice daily at intervals of 1 or 2 months. Usual daily dosage range is 2–16 g taken once or in divided doses.

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.

If triglyceride concentrations increase markedly, consider reducing dosage, discontinuing therapy, or using combined or alternative treatment.

Oral (Granules for oral suspension)

Initially, 5 g (1 packet or 1 level scoop) once or twice daily. Titrate dose upward as necessary in 5-g increments at 1- or 2-month intervals. Usual daily dosage range is 5–30 g (1–6 packets or level scoops) taken once or in divided doses.

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.

If triglyceride concentrations increase markedly, consider reducing dosage, discontinuing therapy, or using combined or alternative treatment.

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. Thereafter, increase dosage as needed by 1 dose per day (at monthly intervals) with periodic monitoring of serum lipoprotein values; adjust dosage accordingly to achieve the desired effect while avoiding excessive dosage. 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.

30 g daily (as granules for oral suspension) has been used in combination with niacin in adults with heterozygous familial hypercholesterolemia.

Cautions for Colestipol

Contraindications

  • Known hypersensitivity to colestipol or any ingredient in the formulation.

Warnings/Precautions

Warnings

Administration

To avoid accidental inhalation or esophageal distress, do not administer colestipol hydrochloride for oral suspension in its dry form. Always mix colestipol hydrochloride granules with water or other fluids before ingesting. (See Administration under Dosage and Administration.)

Phenylketonuria

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.

General Precautions

Hypertriglyceridemia

Generally has no clinically relevant effect on serum triglyceride concentrations, but may increase triglyceride concentrations in some patients.

GI Effects

Mild and, occasionally, severe constipation has occurred. Exacerbation of preexisting constipation and aggravation of hemorrhoids secondary to constipation may occur. Encourage increased fluid and fiber intake to alleviate constipation; a stool softener can be added if necessary. In addition, adjust dosage carefully and titrate slowly to minimize adverse GI effects (e.g., fecal impaction). (See Dosage under Dosage and Administration.) Make particular effort to avoid constipation in patients with symptomatic CHD. Discontinuation of colestipol therapy may be required in some patients.

Difficulty swallowing and transient esophageal obstruction have been reported rarely. 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. If abdominal pressure or discomfort (secondary to esophageal obstruction) occurs, advise patients to consult a clinician prior to administering the next dose.

Abdominal discomfort (including pain and cramping), belching, flatulence, indigestion, heartburn, nausea, vomiting, and diarrhea or loose stools also have been reported. Bleeding hemorrhoids and blood in the stool have been reported infrequently. Peptic ulceration, cholecystitis, and cholelithiasis have been reported occasionally but are not necessarily drug-related.

Fat-soluble Vitamin Deficiency

May interfere with the absorption of folic acid and fat-soluble vitamins (e.g., vitamins A, D, E, K). Prolonged use may be associated with an increased bleeding tendency as a result of hypoprothrombinemia secondary to vitamin K deficiency. (See Specific Drugs under Interactions.)

Hypothyroidism

Theoretical risk for the development of hypothyroidism, especially in patients with limited thyroid reserve.

Hyperchloremic Acidosis

Because colestipol is the chloride form of an anion-exchange resin, there is a possibility that prolonged use may lead to the development of hyperchloremic acidosis.

Specific Populations

Pregnancy

Category B.

Interferes with absorption of fat-soluble vitamins, which may be detrimental even in the presence of supplementation.

Lactation

Use with caution; possible lack of proper vitamin absorption associated with colestipol therapy may have an effect on nursing infants.

Pediatric Use

Safety and efficacy not established.

Common Adverse Effects

Constipation.

Interactions for Colestipol

Effects on GI Absorption of Drugs

May bind to a number of drugs in the GI tract and may delay or reduce their absorption. Instruct patients to allow as long a time interval as possible between ingestion of other drugs and colestipol. The manufacturer recommends administering other drugs at least 1 hour before or 4 hours after colestipol.

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.

Specific Drugs

Drug

Interaction

Comments

Antidiabetic agents (sulfonylureas)

Decreased antilipemic effects of colestipol

β-adrenergic blocking agents (propranolol)

Decreases and/or delays GI absorption of propranolol; effect on absorption of other β-adrenergic blocking agents not fully determined

Monitor closely whenever colestipol therapy is initiated or discontinued in patients receiving propranolol; adjust propranolol dosage as necessary

Digoxin

Colestipol may bind digoxin in the GI tract and impair its absorption

Diuretics, thiazide (e.g., hydrochlorothiazide, chlorothiazide)

Substantially decreased absorption of diuretic

Decreases absorption of chlorothiazide even when administered 1 hour before colestipol hydrochloride

Fat-soluble vitamins (i.e., vitamins A, D, E, K)

Decreased absorption of fat-soluble vitamins

Consider supplemental administration of vitamins A and D if colestipol is to be given for a prolonged period

Bleeding secondary to vitamin K deficiency usually responds promptly to parenteral administration of phytonadione; recurrences can be prevented by oral administration of phytonadione

Furosemide

Substantially decreased absorption of furosemide

Gemfibrozil

Substantially decreased absorption of gemfibrozil

Hydrocortisone

Possible interference with absorption of hydrocortisone

Lovastatin

Possible additive antilipemic effects

Niacin

Additive antilipemic effects

Penicillin G

Substantially decreased absorption of penicillin G

Phosphate supplements, oral

Possible interference with absorption of oral phosphate supplements

Tetracycline

Substantially decreased absorption of tetracycline

Colestipol Pharmacokinetics

Absorption

Bioavailability

Not absorbed from the GI tract.

Onset

Therapeutic response usually occurs within 1 month.

Elimination

Elimination Route

Binds to bile acids in the intestine and forms a nonabsorbable complex that is excreted in feces.

Stability

Storage

Oral

Tablets

20–25°C.

Granules for Suspension

20–25°C.

Actions and Spectrum

  • Binds to bile acids in the intestine and forms a nonabsorbable complex that is excreted in feces. Partial removal of bile acids from the enterohepatic circulation via this mechanism results in increased conversion of cholesterol to bile acids in the liver. 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.

  • Reduces serum total and LDL-cholesterol concentrations. Serum triglyceride concentrations may increase or remain unchanged.

  • Antilipemic effects are additive when used with lovastatin or niacin.

Advice to Patients

  • Importance of adherence to prescribed directions for use. (See Oral Administration Under Dosage and Administration.)

  • Importance of adherence to standard lipid-lowering diet.

  • Inform patients that colestipol hydrochloride tablets may be larger than typical tablets or capsules. (See GI Effects under Cautions.)

  • Importance of administering other medications at least 1 hour before or 4 hours after colestipol.

  • For phenylketonurics, importance to inform them that Flavored Colestid granules for oral suspension contains aspartame.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

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

Colestipol Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

For suspension

5 g/packet or calibrated scoop*

Colestid Granules

Pfizer

Colestipol Hydrochloride for Oral Suspension

5 g/7.5 g packet or calibrated scoop

Colestid Flavored Granules

Pfizer

Tablets (micronized)

1 g

Colestid

Pfizer

AHFS DI Essentials™. © Copyright 2022, Selected Revisions July 26, 2021. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

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