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All about: Cholestyramine

Big Image Pronouncation: (koe-less-TIE-ruh-meen)
Class: Antihyperlipidemic, Bile acid sequestrant

Trade Names:
Prevalite
- Powder 4 g (as anhydrous cholestyramine resin) per 5.5 g powder

Trade Names:
Questran
- Powder for suspension 4 g anhydrous cholestyramine resin per 9 g powder

Trade Names:
Questran Light
- Powder 4 g (as anhydrous cholestyramine resin) per 6.4 g powder

Novo-Cholamine (Canada)
Novo-Cholamine Light (Canada)

Mechanism of Action

Pharmacology

Adsorbs and combines with bile acids in the intestine to form an insoluble complex that is excreted in the feces, resulting in partial removal of bile acids from the enterohepatic circulation. The increased fecal loss of bile acids leads to an increased oxidation of cholesterol to bile acids, which results in a decrease in LDL cholesterol plasma levels and serum cholesterol levels.

Pharmacokinetics

Absorption

Not absorbed.

Indications and Usage

Adjunctive therapy to diet for reduction of elevated serum cholesterol in patients with primary hypercholesterolemia; relief of pruritus associated with partial biliary obstruction.

Unlabeled Uses

Binds the toxin produced by Clostridium difficile ; bile salt-mediated and postvagotomy diarrhea; digitalis toxicity; adjunctive treatment of hyperthyroidism; hyperoxaluria.

Contraindications

Hypersensitivity to bile acid sequestering resins; complete biliary obstruction.

Dosage and Administration

Adults

PO Initial: 1 scoop or single-use packet (4 g anhydrous cholestyramine) daily to twice daily. Maintenance: 2 to 4 packets or scoops daily, divided into 2 doses. Increase dose gradually with periodic assessment of lipid/lipoprotein levels at intervals of at least 4 wk; (max, 6 scoops or packets/day). Although recommended dosing schedule is twice daily, may be administered in 1 to 6 doses/day.

Children

PO Although optimal dosage schedule has not been established, usual dose is 240 mg/kg/day of anhydrous cholestyramine resin in 2 to 3 divided doses (max, 8 g/day).

General Advice

  • Instruct patients to never administer dry powder without liquid.
  • Instruct patients to place contents of 1 single-use packet or level scoopful in glass or cup and add 2 to 6 oz (4 to 6 oz for cholestyramine light, 2 to 3 oz for Prevalite ) of any noncarbonated liquid. Stir to uniform consistency and then have patient drink suspension. Also may mix with highly fluid soups or pulpy fruits with high moisture content (eg, applesauce, crushed pineapple).
  • Advise patients to administer with meals unless dosing interval needs to be modified to avoid interference with absorption of other medications.
  • Cholestyramine administration should be separate from other drugs. Advise patients to take other drugs at least 1 h before or 4 to 6 h after cholestyramine.
  • The color of the powder may vary somewhat from batch to batch, but this variation does not affect the efficacy of the product.

Storage/Stability

Store powder and single-use packets at controlled room temperature (59° to 86°F).

Drug Interactions

Acetaminophen, amiodarone, corticosteroids, digitalis glycosides, estrogens, furosemide, glipizide, HMG-CoA reductase inhibitors (eg, fluvastatin), methotrexate, certain NSAIDs (eg, piroxicam), penicillin G, phenobarbital, progestins, propranolol, tetracycline, thiazide diuretics, thyroid and thyroxine preparations, troglitazone, ursodiol, valproic acid, warfarin, and other drugs

Cholestyramine may interfere with the absorption of many drugs, especially those listed.

Fats and fat-soluble vitamins A, D, E, and K

Cholestyramine may interfere with normal fat absorption and digestion; consider supplementation with these vitamins and with folic acid.

Iopanoic acid

Coadministration may result in abnormal cholecystography.

Laboratory Test Interactions

None known.

Adverse Reactions

Dermatologic

Irritation of skin, tongue, and perianal area; rash.

GI

Abdominal pain, discomfort, and distention; aggravation of hemorrhoids; anorexia; bleeding; constipation (can be severe and at times accompanied by fecal impaction); diarrhea; eructation; flatulence; nausea; steatorrhea; vomiting; intestinal obstruction (rare).

Hematologic-Lymphatic

Bleeding tendencies related to vitamin K deficiency, folic acid deficiency.

Metabolic-Nutritional

Fat-soluble vitamin deficiencies, hyperchloremic acidosis, osteoporosis.

Precautions

Monitor

Determine serum lipids frequently during first few months of therapy and periodically thereafter.


Pregnancy

Category C .

Lactation

Undetermined.

Constipation

Cholestyramine may worsen pre-existing constipation. Start with low dose (eg, 1 packet or scoop/day for 5 to 7 days) and increase gradually. Increased fluid and fiber intake may be beneficial.

Diet

Before instituting therapy, attempt to control serum cholesterol with an appropriate dietary regimen and weight reduction.

Folate deficiency

Reduction of serum or red cell folate has been reported with long term administration. Consider supplementation with folic acid in such cases.

Hyperchloremic acidosis

There is a possibility for producing hyperchloremic acidosis during prolonged use. Use with caution in younger and smaller patients, patients with renal function impairment or volume depletion, or with concomitant spironolactone administration.

Phenylketonuria

These products contain phenylalanine. Do not administer to patient with phenylketonuria without discussing with health care provider.

Secondary causes of hypercholesterolemia

Ensure secondary causes of hyperlipidemia (eg, alcoholism, dysproteinemias, hypothyroidism, nephritic syndrome, obstructive liver disease, other drug therapy, poorly controlled diabetes) have been excluded before starting therapy.

Vitamin K deficiency

Chronic use may be associated with increased bleeding tendency because of hypoprothrombinemia associated with vitamin K deficiency.

Overdosage

Symptoms

GI obstruction.

Patient Information

  • Advise patient to read patient information leaflet before using the first time and to reread and check for new information with each refill.
  • Advise patient to drink plenty of fluids and maintain a high fiber intake to minimize risk of constipation.
  • Advise patient to try to take each dose with a meal unless the dosing interval needs to be modified to avoid interference with absorption of other medications.
  • Advise patient that the color of the powder may vary from batch to batch but that this does not alter the effectiveness of the medication.
  • Advise patient to place contents of 1 level scoop or single-dose packet in a glass or cup and add at least 2 to 6 oz of any noncarbonated fluid (4 to 6 oz for cholestyramine light, 2 to 3 oz for Prevalite ), stir to uniform consistency and drink.
  • Advise patient that powder also can be mixed with highly fluid soups or pulpy fruits with high moisture content (eg, applesauce, crushed pineapple).
  • Caution patient that sipping or holding the resin suspension in the mouth for prolonged periods may lead to changes in the surface of teeth, resulting in discoloration, erosion of enamel, or decay. Advise patient to maintain good oral hygiene.
  • Inform patient that constipation, gas, nausea, and heartburn may occur but usually go away with continued therapy. Advise patient to notify health care provider if these effects become bothersome or if bleeding or unusual bruising occurs.
  • Instruct patient to take all other medications at least 1 h before or 4 to 6 h after taking cholestyramine.
  • Inform patient that drug helps control, but not does cure, lipid abnormality and to continue taking drug as prescribed when lipid levels are lowered.
  • Caution patient not to change the dose or stop taking unless advised by health care provider.
  • Instruct patient to continue taking other cholesterol-lowering medications as prescribed by health care provider.
  • Emphasize to patient importance of other modalities on cholesterol control, such as dietary changes (eg, reduced saturated fat intake, increased soluble fiber intake), weight control, regular exercise, smoking cessation.

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