Drug information of Cholestyramine

Cholestyramine

Drug group:

Cholestyramine helps reduce cholesterol (fatty acids) in the blood. High cholesterol is associated with an increased risk of heart disease and atherosclerosis (clogged arteries).
Cholestyramine is used to lower high levels of cholesterol in the blood, especially low-density lipoprotein (LDL) ("bad" cholesterol). Cholestyramine powder is also used to treat itching caused by a blockage in the bile ducts of the gallbladder.

Mechanism of effect

Cholestyramine binds bile in the gastrointestinal tract to prevent its reabsorption. The resin is a strong anion exchange resin, which means that it can exchange its chloride anions with anionic bile acids in the gastrointestinal tract and bind them strongly in the resin matrix.
The functional group of the anion exchange resin is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer.

Pharmacodynamic

Cholesterol is probably the sole precursor of bile acids. During normal digestion, bile acids are secreted into the intestines. A major portion of the bile acids is absorbed from the intestinal tract and returned to the liver via the enterohepatic circulation. Only very small amounts of bile acids are found in normal serum.
Cholestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces. This results in a partial removal of bile acids from the enterohepatic circulation by preventing their absorption.

Pharmacokinetics

Absorption : Not absorbed from the gastrointestinal tract following oral administration.
Metabolism : Bile acids
Route of elimination : Cholestyramine resin adsorbs and combines with the bile acids in the intestine to form an insoluble complex which is excreted in the feces.
Half life : 6 minutes

Dosage

• The recommended starting adult dose for Cholestyramine for oral suspension USP light powder is one pouch or one level scoopful once or twice a day.
• The recommended maintenance dose for Cholestyramine for oral suspension USP light powder is 2 to 4 pouches or scoopfuls daily (8 to 16 grams anhydrous Cholestyramine resin) divided into two doses.
• Four grams of anhydrous Cholestyramine resin is contained in each measured dose of Cholestyramine for oral suspension USP light powder as follows: Cholestyramine for oral suspension USP light powder 5.5 grams
• The maximum recommended daily dose is six pouches or scoopfuls of Cholestyramine for oral suspension USP light powder (24 grams of anhydrous Cholestyramine resin).
• The suggested time of administration is at mealtime but may be modified to avoid interference with absorption of other medications.
• Although the recommended dosing schedule is twice daily, Cholestyramine for oral suspension USP light powder may be administered in 1 to 6 doses per day.

Alerts

Phenylketonurics : Cholestyramine FOR ORAL SUSPENSION USP LIGHT POWDER CONTAINS 28 MG PHENYLALANINE PER 5.5 GRAM DOSE.

Points of recommendation

• Inform your physician if you are pregnant or plan to become pregnant or are breastfeeding.
• Drink plenty of fluids and mix each 5.5 gram dose of Cholestyramine for oral suspension USP light powder 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 changes in the surface of the teeth resulting in discoloration, erosion of enamel or decay; good oral hygiene should be maintained.

Pregnancy level

C

Related drugs

Colestipol , Colesevelam


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