Colestyramine

Colestyramine (INN) or cholestyramine (USAN) (trade names Questran, Questran Light, Cholybar, Olestyr) is a bile acid sequestrant, which binds bile in the gastrointestinal tract to prevent its reabsorption. It is a strong ion exchange resin, which means 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.

Colestyramine
Clinical data
Pronunciation/kˈlɛstərəmn/, /klɪˈstrəmn/
Trade namesQuestran, Cholybar, Olestyr, others
AHFS/Drugs.comMonograph
MedlinePlusa682672
Pregnancy
category
  • AU: B2
Routes of
administration
By mouth
ATC code
Legal status
Legal status
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailabilitylow
Protein bindingunknown
Metabolismbile acids
Elimination half-life1 hour
ExcretionFaecal
Identifiers
CAS Number
DrugBank
ChemSpider
  • none
UNII
KEGG
ChEMBL
ECHA InfoCard100.031.143
Chemical and physical data
Molar massIn average, exceeds 1×106 g/mol
 NY (what is this?)  (verify)

Colestyramine removes bile acids from the body by forming insoluble complexes with bile acids in the intestine, which are then excreted in the feces. As a result of this loss of bile acids, more plasma cholesterol is converted to bile acids in the liver to normalise levels. This conversion of cholesterol into bile acids lowers plasma cholesterol levels.

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