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Cholestyramine (Monograph)

Brand names: Prevalite, Questran, Questran Light
Drug class: Bile Acid Sequestrants
VA class: CV350
CAS number: 11041-12-6

Medically reviewed by Drugs.com on Jul 17, 2023. Written by ASHP.

Introduction

Antilipemic agent; bile acid sequestrant.100

Uses for Cholestyramine

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.100

As effective as colestipol in lowering serum cholesterol concentrations.b Select bile acid sequestrant based on patient tolerance, including palatability and taste preference, and cost.148 181

AHA/ACC cholesterol management guideline states that lifestyle modification is the foundation of cardiovascular risk reduction.400 If pharmacologic therapy is needed, statins are first-line drugs of choice because of their demonstrated benefits in reducing risk of ASCVD.400 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.400

Pruritus Associated with Partial Cholestasis

Relief of pruritus associated with partial cholestasis.100 Effects on serum cholesterol in these patients is variable.100

Cholestyramine Dosage and Administration

General

Monitoring during Antilipemic Therapy

Administration

Oral Administration

Administer orally at mealtime.100

Do not administer the powder in its dry form; always mix with water or other fluids before ingesting.100 187 188

Mix cholestyramine powder for oral suspension with an adequate amount (60–180 mL for 1 packet or level scoop of powder) of a liquid (e.g., water, fruit juice, other noncarbonated beverage) and stir to uniform consistency.100 186 187 188

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.127

Use of a heavy or pulpy fruit juice may minimize complaints about consistency of suspensions of the drug.148

If a carbonated beverage is used, mix the powder slowly in a large glass to minimize excessive foaming.b To minimize excessive swallowing of air, advise patients to avoid rapid ingestion of suspensions of the drug.148

Alternatively, mix cholestyramine powder with a highly fluid soup or a pulpy fruit with a high moisture content such as applesauce or crushed pineapple.100 157 173

Instruct patients to take other drugs at least 1 hour before or 4–6 hours after taking cholestyramine to minimize possible interference with absorption.100 157 173 187 188 (See Effects on GI Absorption of Drugs under Interactions.)

Dosage

Available as cholestyramine resin; dosage expressed in terms of anhydrous (i.e., dried) cholestyramine resin.100

Each 9 g of Questran100 or generic cholestyramine (1 dose, 1 packet, or 1 level scoop),188 5.5 g of Prevalite (1 dose, 1 packet, or 1 level scoop),187 or 5 g of Questran Light100 or generic cholestyramine light (1 dose, 1 packet, or 1 level scoop)188 contains about 4 g of anhydrous cholestyramine resin.100 187 188

In calculating pediatric dosages, each 100 mg of the commercially available powders contains either 44.4 mg (e.g., Questran, generic cholestyramine), 72.7 mg (e.g., Prevalite), or 80 mg (e.g., Questran Light, generic cholestyramine light) of anhydrous cholestyramine resin.100 187 188

Pediatric Patients

Dyslipidemias† [off-label]
Oral

240 mg/kg daily in 2–3 divided doses suggested by manufacturers and some clinicians.100 187 188 c

Adults

Dyslipidemias or Pruritus Associated with Partial Cholestasis
Oral

Initially, 4 g of anhydrous resin (1 packet or 1 level scoop) once or twice daily at mealtime.100 187 188

Increase dosage gradually to minimize adverse GI effects (e.g., fecal impaction).100 187 188

Usual maintenance dosage recommended by manufacturers is 8–16 g daily, given in 2 divided doses.100 187 188 Usual dosage range suggested by Third Report of the National Cholesterol Education Program (NCEP) (Adult Treatment Panel [ATP] III) is 4–16 g daily.186

Although the recommended dosing schedule is twice daily, may be administered in 1–6 doses per day.100 187 188

In patients with preexisting constipation: Initially, 4 g of anhydrous resin (1 packet or 1 level scoop) once daily for 5–7 days; then increase dosage to 4 g twice daily and monitor constipation and serum lipoprotein values, at least twice, 4–6 weeks apart.100 187 188 Thereafter, increase dosage as needed by 1 dose (i.e., 4 g) per day (at monthly intervals) with periodic monitoring of serum lipoprotein values.100 187 188

If constipation worsens or the desired effect is not achieved with acceptable adverse effects with the usual dosage of 1–6 doses (i.e., 4–24 g) per day, consider combined therapy or alternative treatment.100 187 188

Prescribing Limits

Pediatric Patients

Oral

Maximum 8 g daily.100 187 188

Adults

Oral

Maximum 24 g (6 packets or 6 level scoops) daily.100 187 188

Detailed Cholestyramine dosage information

Cautions for Cholestyramine

Contraindications

Warnings/Precautions

Warnings

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 each 5-g dose of Questran Light, 5-g dose of generic cholestyramine light, or 5.5-g dose of Prevalite contains aspartame (NutraSweet), which is metabolized in the GI tract to provide about 14, 14, or 14.1 mg, respectively, of phenylalanine following oral administration.100 187 188

Major Toxicities

GI Effects

Mild constipation has occurred, especially after high doses and in patients >60 years of age.100 Exacerbation of preexisting constipation and aggravation of hemorrhoids secondary to constipation may occur.100

Encourage increased fluid and fiber intake to alleviate constipation;100 a stool softener can be added if necessary.100 In addition, adjust dosage carefully and titrate slowly to minimize adverse GI effects (e.g., fecal impaction).100 (See Dosage under Dosage and Administration.)

Make particular effort to avoid constipation in patients with symptomatic CHD.100 167

Discontinuance of cholestyramine therapy may be required in some patients.100

Abdominal discomfort and/or pain, flatulence, nausea, vomiting, diarrhea, eructation, anorexia, biliary colic, and steatorrhea also reported.100 Intestinal obstruction, which rarely has been fatal, reported in pediatric patients.100

General Precautions

Hypertriglyceridemia

Use with caution in patients with baseline triglyceride concentrations of 250-299 mg/dL; discontinue when triglyceride concentrations <400 mg/dL.

Do not use in patients with baseline fasting triglyceride concentrations ≤300 mg/dL or in those with primary dysbetalipoproteinemia (Frederickson type III).

Fat-soluble Vitamin Deficiency

May interfere with the absorption of fat-soluble vitamins (e.g., vitamins A, D, E, K).100 Bleeding tendency due to hypoprothrombinemia secondary to vitamin K deficiency, night blindness secondary to vitamin A deficiency, and vitamin D deficiency have been reported.100 (See Specific Drugs under Interactions.)

Hyperchloremic Acidosis

Because cholestyramine is the chloride form of an anion-exchange resin, there is a possibility that prolonged use may lead to the development of hyperchloremic acidosis.100 Hyperchloremic acidosis reported in children.100

Caution during long-term therapy in patients with renal impairment or volume depletion and in patients receiving concomitant spironolactone.100 187 188

Specific Populations

Pregnancy

Category C.100 187 188

Interferes with absorption of fat-soluble vitamins, and regular prenatal supplementation may not be adequate.100 187 188 (See Specific Drugs under Interactions.)

Lactation

Use with caution; possible lack of proper vitamin absorption associated with cholestyramine therapy may have an effect on nursing infants.100

Pediatric Use

Safety and efficacy of long-term administration not established.100 The potential effect of cholestyramine on vitamin absorption and on electrolytes should be considered.100 116 117 118 119 120 121 122 123 124 125 157 173 181

Common Adverse Effects

Constipation, osteoporosis, rash, irritation of the skin/tongue/perianal area.100

Drug Interactions

Effects on GI Absorption of Drugs

May bind to a number of drugs (e.g., phenylbutazone, warfarin, propranolol, tetracycline, penicillin G, phenobarbital, thyroid and thyroxine preparations, estrogens and progestins, digoxin, iron salts, loperamide) in the GI tract and may delay or reduce their absorption.100 Instruct patients to administer other drugs at least 1 hour before or 4–6 hours after cholestyramine (or allow as long a time interval as possible between ingestion of other drugs and cholestyramine).100

May interfere with the pharmacokinetics of drugs that undergo enterohepatic circulation.100

Consider the possibility that discontinuance of cholestyramine in patients stabilized on potentially toxic drugs that bind to the resin may lead to toxicity and that administration of cholestyramine to patients stabilized on other drugs may reduce the effect of these drugs.100

Specific Drugs

Drug

Interaction

Comments

Amiodarone

Decreased elimination half-life and plasma concentrations of amiodarone139 147

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

Decreased absorption of fat-soluble vitamins100

Consider supplemental administration of water-miscible (or parenteral) forms of fat-soluble vitamins if cholestyramine is to be given for a prolonged period.100

Bleeding secondary to vitamin K deficiency usually responds promptly to parenteral administration of phytonadione; recurrences can be prevented by oral administration of phytonadione100

Phosphate supplements, oral

Other bile acid binding resins reported to interfere with the absorption of oral phosphate supplements100

Propranolol

May decrease GI absorption of propranolol100 144 157 173 180

When cholestyramine therapy is initiated or discontinued in patients receiving oral propranolol, dosage adjustment of the β-adrenergic blocking agent may be necessary144 146

Thiazide diuretics (e.g., chlorothiazide, hydrochlorothiazide)

May decrease GI absorption of diuretic100 140 141 142 143
Cholestyramine drug interactions (more detail)

Cholestyramine Pharmacokinetics

Absorption

Bioavailability

Not absorbed from the GI tract.100

Onset

Antilipemic response usually occurs within 1 month.100 In patients with pruritus associated with partial cholestasis, relief of pruritus usually occurs within 1–3 weeks after initiation of therapy.b

Elimination

Elimination Route

Binds to bile acids in the intestine and forms a nonabsorbable complex that is excreted in feces.100

Stability

Storage

Oral

Powder for Oral Suspension

20–25°C (may be exposed to 15–30°C).100 187 188

Actions and Spectrum

Advice to Patients

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

Cholestyramine Resin

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

For suspension

4 g (of dried cholestyramine resin) per 9 g*

Cholestyramine

Questran

Par

4 g (of dried cholestyramine resin) per 5.5 g

Prevalite

Upsher-Smith

4 g (of dried cholestyramine resin) per 5 g*

Cholestyramine Light

Questran Light

Par

AHFS DI Essentials™. © Copyright 2024, Selected Revisions July 26, 2021. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

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

References

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