cholestyramine

Adult Dosing

Hypercholesterolemia

Initially 4 g mixed with water or other fluids PO qd-bid; gradually increase q4 wk after periodic assessments of lipid/lipoprotein levels
Maintenance dose: 8-16 g divided into 2 doses
Max: 24 g/day [6 pouches or scoops qd]

Pruritus due to partial biliary obstruction

Initially 4 g mixed with water or other fluids PO qd-bid; gradually increase q4 wk after periodic assessments of lipid/lipoprotein levels
Maintenance dose: 8-16 g divided into 2 doses
Max: 24 g/day [6 pouches or scoops qd]

Pediatric Dosing

Hypercholesterolemia [Non FDA approved]

Usually, 240 mg/kg daily PO divided bid-tid before meals, not to exceed 8 g/day; alternatively for children >6 yrs, 80 mg/kg or 2.35 g/m²tid; alternatively 2 or 4 g PO bid before meals, gradually increasing the dosage until a serum total cholesterol concentration of 250 mg/dL or less is achieved

[Outline]

Adult Dosing
Pediatric Dosing

Indications ⬆ ⬇

An adjunctive therapy to diet for the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia (elevated low density lipoprotein [LDL] cholesterol) who do not respond adequately to diet
Pruritus due to partial biliary obstruction

Contraindications ⬆ ⬇

Hypersensitivity to any of the ingredients of the product
Complete biliary obstruction

Black Box Warnings ⬆ ⬇

Dosing Adjustment ⬆ ⬇

Renal Dose Adjustment

Renal impairment: No dose adjustments

Hepatic Dose Adjustment

Hepatic impairment: Dose adjustments not defined

Warnings/Precautions ⬆ ⬇

See Supplemental Patient Information

Fat-soluble vitamin deficiency possible. Side effects may increase with >24 g/day
Chronic use of cholestyramine resin may be associated with increased bleeding tendency due to hypoprothrombinemia associated with vitamin K deficiency; usually responds promptly to parenteral vitamin K1 and recurrences can be prevented by oral administration of vitamin K1
Long-term administration of cholestyramine resin may reduce serum or red cell folate concentration; supplementation with folic acid should be considered
Prolonged use of cholestyramine resin may produce hyperchloremic acidosis
May produce or worsen preexisting constipation; dose should be increased gradually to minimize the risk of developing fecal impaction
Serum cholesterol levels should be determined frequently during the first few months of therapy and periodically thereafter to detect whether significant changes have occurred
If bleeding or bruising occurs, monitor prothrombin time. Drug may reduce vitamin K absorption

Cautions: Use cautiously in

Renal insufficiency/volume depletion
Patients receiving concomitant spironolactone
Coronary artery disease
Elderly patients >60 yrs
Phenylketonuria (phenylalanine-containing forms)

Supplemental Patient Information

Inform physician if pregnant or plan to become pregnant or are breast-feeding
Drink plenty of fluids and mix each 5 or 9 gram dose in at least 2 to 6 ounces of fluid before taking
Sipping or holding the resin suspension in the mouth for prolonged periods may lead to discoloration, erosion of enamel or decay; good oral hygiene should be maintained
Can be mixed with highly fluid soups or pulpy fruits with high moisture content such as applesauce or crushed pineapple
Increase fluid and fiber intake to alleviate constipation; use prophylactic stool softeners if indicated

Interactions ⬆ ⬇

Locholest, Locholest Light, Prevalite, Questran, Questran Light interacts with :

Pregnancy/Breast Feeding ⬆ ⬇

Pregnancy Category:C

Breastfeeding: Cholestyramine is a nonabsorbable resin. Does not enter mother's bloodstream, it will not reach the infant via breastmilk; acceptable for use during lactation. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT last accessed 28 December 2010). Manufacturer advises caution while administering cholestyramine to a nursing mother.

Adverse Reactions ⬆ ⬇

GI: Constipation, abdominal discomfort or pain, flatulence, nausea, vomiting, diarrhea, eructation, steatorrhea, intestinal obstruction, fecal impaction, dyspepsia
METABOLIC: Anorexia, vitamin A, D, K deficiency, hyperchloremic acidosis, decreased folate levels
DERM: Rash, irritation, urticaria
MISC: Bleeding, fatigue, osteoporosis

Clinical Pharmacology ⬆ ⬇

Anticholesteremic agents; binds with bile acids in GI tract to form an insoluble complex excreted in feces. Although the complex regulates and increases cholesterol synthesis, there is a decrease in serum cholesterol and low-density lipoprotein levels, possibly due to an increased rate of LDL clearance from the plasma
No systemic absorption
Metabolism: Bile acids
Excreted in the feces
Half-life: 6 mins

Brands and Availability ⬆ ⬇

US Trade Name(s)

Locholest (Discontinued)
Locholest Light (Discontinued)
Prevalite
Questran
Questran Light

US Availability

cholestyramine (generic)

PWDR for SUSP: 4 g resin/packet
PWDR for SUSP: 4 g resin/scoopful

cholestyramine light (generic)

PWDR for SUSP: 4 g resin/packet
PWDR for SUSP: 4 g resin/scoopful

Locholest, Locholest Light, Prevalite, Questran, Questran Light

PWDR for SUSP: 4 g resin/packet
PWDR for SUSP: 4 g resin/scoopful

Canadian Trade Name(s)

Novo-cholamine
Novo-cholamine Light
Olestyr
Olestyr Light

Canadian Availability

Novo-cholamine, Novo-cholamine Light

PWDR for SUSP: 4 g/dose

Olestyr Light

PWDR for SUSP: 4 g/5 g pouches

Olestyr

PWDR for SUSP: 4 g/9 g pouches

UK Trade Name(s)

Questran
Questran Light

UK Availability

colestyramine (generic)

PWDR: 4 g/sachet

Questran, Questran Light

PWDR: 4 g/sachet

Australian Trade Name(s)

Questran Lite

Australian Availability

Questran Lite

PWDR: 4 g/sachet
PWDR: 8 g/sachet

[Outline]

Classification ⬆ ⬇

Endocrine/Metabolic

Antihyperlipidemic Agents
Bile Acid Sequestrants

Cardiovascular