Drug intelligence / Profile preview

cholestyramine

Development stage
Approved
Lead developer
Bristol Myers Squibb
Modality
Device-based Delivery → Drug Delivery Systems, Small Molecules
Administration
Oral
01

Overview

Cholestyramine is a non-absorbable, quaternary ammonium anion-exchange resin used as a lipid-lowering agent and for the management of pruritus associated with partial biliary obstruction. By binding bile acids in the gastrointestinal tract to form an insoluble complex, it prevents their reabsorption and interrupts enterohepatic circulation. This results in an increased fecal loss of bile acids, prompting the liver to compensate by upregulating the conversion of endogenous cholesterol into new bile acids. This process increases the expression of hepatic LDL receptors, leading to a significant reduction in serum low-density lipoprotein (LDL) cholesterol levels. Beyond its primary use in hyperlipidemia, it is frequently employed to treat diarrhea caused by bile acid malabsorption and as an adjunct in the management of digitalis toxicity.

Brand names
QuestranQuestran LightPrevaliteLocholestOlestyrCholestat
Other names
colestyraminecholestyramine resin

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