Cholestyramine (cholestyramine (with sugar))
Last reviewed · Source: First Databank (FDB) drug data
Overview
Cholestyramine resin is a bile acid sequestrant antilipemic agent.
USES: Cholestyramine is used along with a proper diet to lower cholesterol in the blood. Lowering cholesterol helps decrease the risk for strokes and heart attacks. In addition to a proper diet (such as a low-cholesterol/low-fat diet), other lifestyle changes that may help this medication work better include exercising, losing weight if overweight, and stopping smoking.
Consult your doctor for more details. Cholestyramine may also be used to treat itching in people with too much bile acid caused by a certain type of liver/bile duct disease (partial biliary obstruction). This medication is known as a bile acid-binding resin.
It works by removing bile acid from the body. In people with high cholesterol, this causes the liver to make more bile acid by using cholesterol in the blood. This helps to lower the cholesterol levels.
Generic name: cholestyramine (with sugar)
Pronunciation: (KOE-le-STYE-ra-meen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Cholestyramine
Indications
The following indications are listed for Cholestyramine:
- Biliary Obstruction With Pruritus
- Hypercholesterolemia
Also known as: Elevated Blood Cholesterol Level, Pruritus Associated With Biliary Obstruction.
Dosing
Dosage of cholestyramine is expressed in terms of the anhydrous (i.e., dried) resin. Each 9 g of Questran(R) or generic (nonproprietary) cholestyramine, 5.5 g of Prevalite(R), or 5 g of Questran Light(R) or generic cholestyramine light powder contains about 4 g of anhydrous cholestyramine resin. In calculating pediatric dosages, each 100 mg of Questran(R), generic cholestyramine, Prevalite(R), Questran(R) Light, or generic cholestyramine light powder contains 44.4, 44.4, 72.7, 80, or 80 mg, respectively, of anhydrous cholestyramine resin. Dosage must be carefully adjusted according to the condition being treated and the patient's response and tolerance.
For the management of primary hypercholesterolemia, the usual adult dosage of anhydrous cholestyramine resin is 4-24 g (1-6 packets or level scoops) daily taken once or in divided doses. To optimize antilipemic effects while minimizing the risk of adverse GI effects (e.g., fecal impaction), dosage should be adjusted carefully and titrated slowly. Cholestyramine therapy generally is initiated in adults with 4 g (1 packet or level scoop) once or twice daily; if the initial dosage is well tolerated, the dosage may be titrated upward as necessary at intervals of no less than 4 weeks. In patients with preexisting constipation, the initial dosage of anhydrous cholestyramine resin should be 4 g (1 packet or level scoop) daily for 5-7 days, increasing to 4 g twice daily with monitoring of constipation and of serum lipoprotein values, at least twice, 4-6 weeks apart; if the initial dosage is well tolerated, the dosage may be increased as needed by one dose (i.e., 4 g) per day at monthly intervals. Serum lipoprotein concentrations should be determined periodically and dosage adjusted accordingly to achieve the desired effect while avoiding excessive dosage. The usual maintenance dosage recommended by the manufacturers is 8-16 g (2-4 packets or level scoops) daily, given in 2 divided doses; the usual dosage range suggested by the Third Report of the National Cholesterol Education Program (NCEP) (Adult Treatment Panel (ATP) III) is 4-16 g daily. The maximum recommended dosage is 24 g (6 packets or level scoops) daily. If constipation worsens or the desired effect is not achieved with acceptable adverse effects within the usual dosage range of 1-6 doses (i.e., 4-24 g) per day, substitution or addition of another antilipemic agent should be considered.
The manufacturers state that the optimal dosage of cholestyramine resin for pediatric patients has not been established. Pediatric dosages of anhydrous cholestyramine resin generally have ranged from 8-16 g daily in 2 or 3 divided doses before meals. The usual pediatric dosage suggested by the manufacturers and some clinicians is 240 mg/kg daily, given in 2 or 3 divided doses, not to exceed 8 g daily. Some clinicians suggest that children older than 6 years of age be given 80 mg/kg or 2.35 g/m2 3 times daily. Alternatively, some clinicians suggest initiating cholestyramine at a pediatric dosage of 2 or 4 g twice daily before meals, and then gradually increasing the dosage until a serum total cholesterol concentration of 250 mg/dL or less is achieved or intolerable adverse effects occur.
Cholestyramine resin is administered orally as a suspension prepared from the powder. Cholestyramine suspension should be administered at mealtime. Patients should be instructed to take other drugs at least 1 hour before or 4-6 hours (or as long an interval as possible) after taking cholestyramine suspension to minimize possible interference with absorption. Although the recommended dosing schedule is twice daily, cholestyramine may be administered in 1-6 doses per day.
Cholestyramine powder should not be taken in its dry form; the resin should always be mixed with water or other fluids before ingesting. Just prior to administration, each packet or level scoop of cholestyramine powder (containing 4 g of dried cholestyramine resin) should be mixed with 60-180 mL of water or another noncarbonated beverage (e.g., fruit juice). Some clinicians suggest that 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. To minimize excessive swallowing of air, patients should be advised to avoid rapid ingestion of suspensions of the drug. If a carbonated beverage is used, excessive foaming can be minimized by mixing the powder slowly in a large glass. Alternatively, cholestyramine resin may be mixed with a highly fluid soup or a pulpy fruit with a high moisture content such as applesauce or crushed pineapple.
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Drug interactions
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There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
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There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
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There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Since cholestyramine resin is not absorbed systemically, the drug is not expected to cause fetal harm when administered in usual dosages to pregnant women. However, there are no adequate and controlled studies to date using cholestyramine resin in pregnant women, and the known interference with absorption of fat-soluble vitamins may cause fetal harm even in the presence of supplementation. Currently, most experts recommend that dyslipidemias in pregnant women be managed with dietary measures; consultation with a lipid specialist may be indicated for pregnant women with severe forms of dyslipidemia.
Cholestyramine resin should be used with caution in nursing women, and the potential effect on the nursing infant of cholestyramine-induced interference with maternal absorption of fat-soluble vitamins should be considered.
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ICD codes
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Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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