Class: Bile Acid Sequestrants
VA Class: CV350
CAS Number: 11041-12-6
Brands: Prevalite, Questran, Questran Light
Antilipemic agent; bile acid sequestrant.100
Uses for Cholestyramine Resin
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
Do not use in patients with primary dysbetalipoproteinemia (Frederickson type III).350 (See Hypertriglyceridemia under Cautions.)
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
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
Current recommendations from ACC/AHA regarding prevention of ASCVD and lifestyle modifications to reduce cardiovascular risk are available at or 352 .
Pruritus Associated with Partial Cholestasis
Relief of pruritus associated with partial cholestasis.100 Effects on serum cholesterol in these patients is variable.100
Cholestyramine Resin Dosage and Administration
Patients should be placed on a standard lipid-lowering diet before initiation of cholestyramine therapy and should remain on this diet during treatment with the drug.100
Monitoring during Antilipemic Therapy
Determine serum cholesterol and triglyceride concentrations prior to and regularly (e.g., every 3–6 months) during cholestyramine 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
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.)
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
240 mg/kg daily in 2–3 divided doses suggested by manufacturers and some clinicians.100 187 188 c
Dyslipidemias or Pruritus Associated with Partial Cholestasis
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
Maximum 8 g daily.100 187 188
Maximum 24 g (6 packets or 6 level scoops) daily.100 187 188
Cautions for Cholestyramine Resin
Complete biliary obstruction in which no bile products reach the intestine.100
Known hypersensitivity to cholestyramine or any ingredient in the formulation.100
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
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
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.)
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
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.)
Use with caution; possible lack of proper vitamin absorption associated with cholestyramine therapy may have an effect on nursing infants.100
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
Interactions for Cholestyramine Resin
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
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
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 Resin Pharmacokinetics
Not absorbed from the GI tract.100
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
Binds to bile acids in the intestine and forms a nonabsorbable complex that is excreted in feces.100
Powder for Oral Suspension
20–25°C (may be exposed to 15–30°C).100 187 188
Actions and Spectrum
Binds to bile acids in the intestine and forms a nonabsorbable complex that is excreted in feces.100 Partial removal of bile acids from the enterohepatic circulation results in increased conversion of cholesterol to bile acids in the liver.100 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.100
Reduces serum total and LDL-cholesterol concentrations.100
In patients with partial biliary obstruction, reduction of serum bile acid concentrations reduces excess bile acids deposited in dermal tissues, resulting in relief of pruritus.100
Advice to Patients
Importance of advising patients that sipping or holding cholestyramine suspension in the mouth for prolonged periods may lead to changes in the surface of the teeth, resulting in discoloration, erosion of enamel, or decay.100 187 188 Maintain good oral hygiene.100 187 188
Importance of adhering to nondrug therapies and measures, including dietary management, weight control, physical activity, and management of potentially contributory disease (e.g., diabetes mellitus).184 186
For phenylketonurics, importance of informing them that Questran Light, generic cholestyramine light, and Prevalite contain aspartame.100 187 188
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.100
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.100
Importance of informing patients of other important precautionary information.100 (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
4 g (of dried cholestyramine resin) per 9 g*
4 g (of dried cholestyramine resin) per 5.5 g
4 g (of dried cholestyramine resin) per 5 g*
AHFS DI Essentials. © Copyright 2017, Selected Revisions November 6, 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