Identification

Summary

Cholestyramine is a bile acid sequestrant used as an adjunct in the reduction of elevated serum cholesterol in patients with primary hypercholesterolemia, and for the relief of pruritus associated with partial biliary obstruction.

Brand Names
Prevalite, Questran
Generic Name
Cholestyramine
DrugBank Accession Number
DB01432
Background

Cholestyramine or colestyramine is a bile acid sequestrant. Bile acid sequestrants are polymeric compounds which serve as ion exchange resins. Cholestyramine resin is quite hydrophilic, but insoluble in water.

Type
Small Molecule
Groups
Approved, Investigational
Synonyms
  • Cholestyramine resin
  • Colestiramina
  • Colestyramine

Pharmacology

Indication

Indicated as 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. Also for the relief of pruritus associated with partial biliary obstruction.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

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.

Mechanism of action

Cholestyramine forms a resin that acts as a bile acid sequestrant to limit the reabsorption of bile acids in the gastrointestinal tract. Cholestyramine resin is a strong anion exchange resin, allowing it to exchange its chloride anions with anionic bile acids present in the gastrointestinal tract and form a strong resin matrix. Cholestyramine consists of a functional group, which is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer, in the anion exchange resin.

TargetActionsOrganism
ABile acids
binder
Humans
Absorption

Not absorbed from the gastrointestinal tract following oral administration.

Volume of distribution

Not Available

Protein binding

Not Available

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

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Overdose may result in blockage of intestine or stomach.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AcarboseThe therapeutic efficacy of Acarbose can be increased when used in combination with Cholestyramine.
AceclofenacCholestyramine can cause a decrease in the absorption of Aceclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcemetacinCholestyramine can cause a decrease in the absorption of Acemetacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcenocoumarolCholestyramine can cause a decrease in the absorption of Acenocoumarol resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcetaminophenCholestyramine can cause a decrease in the absorption of Acetaminophen resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcetazolamideCholestyramine can cause a decrease in the absorption of Acetazolamide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetyl sulfisoxazoleCholestyramine can cause a decrease in the absorption of Acetyl sulfisoxazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcetyldigitoxinCholestyramine can cause a decrease in the absorption of Acetyldigitoxin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetylsalicylic acidCholestyramine can cause a decrease in the absorption of Acetylsalicylic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
AlclofenacCholestyramine can cause a decrease in the absorption of Alclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy.
Interactions
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Food Interactions
  • Take with fluids. Do not take with carbonated fluids.
  • Take with food. Take with a meal unless this interferes with other medications.

Products

Products2
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International/Other Brands
Cholybar / Locholest / Locholest light / Questran Light
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CholestyraminePowder, for suspension4 g / 9 gOralSorres Pharma Inc1998-02-172010-10-06Canada flag
CholestyraminePowder, for suspension4 g / 5 gOralSorres Pharma Inc1998-02-172010-10-19Canada flag
Cholestyramine-odanPowder, for suspension4 g / sachetOralOdan Laboratories Ltd2016-12-23Not applicableCanada flag
OlestyrPowder, for suspension4 g / sachetOralPharmascience Inc1993-12-31Not applicableCanada flag
OlestyrPowder, for suspension4 g / sachetOralPharmascience Inc1996-03-15Not applicableCanada flag
QuestranPowder, for suspension4 g/6.4gOralPar Pharmaceutical2009-06-012011-09-09US flag
QuestranPowder, for suspension4 g/9gOralPar Pharmaceutical2009-06-012011-09-09US flag
Questran Light Pws 4gm/pckPowder, for solution4 g / pckOralBristol Labs Division Of Bristol Myers Squibb1991-12-312005-08-01Canada flag
Questran Pwr 378gm/canPowder, for solution4 g / pckOralBristol Labs Division Of Bristol Myers Squibb1985-12-312005-08-01Canada flag
Questran Pwr 4gm/9gmPowder, for solution4 g / 9 gOralBristol Labs Division Of Bristol Myers Squibb1979-12-312005-08-01Canada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Alti-cholestyramine LightKit; Powder4 g / pckOralAltimed Pharma Inc.1994-12-311999-09-17Canada flag
CholestyraminePowder, for suspension4 g/5gOralbryant ranch prepack2005-09-15Not applicableUS flag
CholestyraminePowder, for suspension4 g/9gOralANI Pharmaceuticals, Inc.2018-06-26Not applicableUS flag
CholestyraminePowder, for suspension4 g/5gOralPhysicians Total Care, Inc.2006-02-08Not applicableUS flag
CholestyraminePowder, for suspension4 g/5gOralbryant ranch prepack2005-09-15Not applicableUS flag
CholestyraminePowder, for suspension4 g/9gOralZydus Pharmaceuticals (USA) Inc.2018-08-01Not applicableUS flag
CholestyraminePowder, for suspension4 g/5gOralPar Pharmaceutical, Inc.2005-09-15Not applicableUS flag
CholestyraminePowder, for suspension4 g/9gOralGolden State Medical Supply2005-09-152017-01-02US flag
CholestyraminePowder, for suspension4 g/9gOralbryant ranch prepack2005-09-15Not applicableUS flag
CholestyraminePowder, for suspension4 g/5.5gOralA-S Medication Solutions2017-06-08Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
KOLESTRAN 9 GR 30 POSETCholestyramine (4 g)PowderOralSANDOZ İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag

Categories

ATC Codes
C10AC01 — Colestyramine
Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
4B33BGI082
CAS number
11041-12-6
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

Synthesis Reference

Moh. S. Amer, Jack C. Gray, "Cholestyramine compositions and method for preparation thereof." U.S. Patent US4895723, issued March, 1967.

US4895723
General References
Not Available
PubChem Substance
46506251
RxNav
2447
ChEMBL
CHEMBL1201625
PharmGKB
PA448974
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cholestyramine
MSDS
Download (74.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionDiabetes / Diabetic Neuropathies / Diabetic Retinopathy (DR)1
4CompletedTreatmentHealthy Subjects (HS)2
3Active Not RecruitingTreatmentHigh Cholesterol1
3CompletedPreventionCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Myocardial Infarction / Myocardial Ischemia / Primary Hypercholesterolemia1
3CompletedPreventionCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Myocardial Ischemia2
3CompletedTreatmentHigh Cholesterol1
3CompletedTreatmentMultiple Sclerosis1
3Unknown StatusTreatmentGraves' Disease / Hyperthyroidism1
2CompletedTreatmentCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Myocardial Ischemia1
2CompletedTreatmentHigh Cholesterol1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • A-S Medication Solutions LLC
  • Bristol-Myers Squibb Co.
  • Catalent Pharma Solutions
  • Eon Labs
  • Major Pharmaceuticals
  • Mead Johnson and Co.
  • Medisca Inc.
  • Novopharm Ltd.
  • Par Pharmaceuticals
  • Physicians Total Care Inc.
  • Upsher Smith Laboratories
Dosage Forms
FormRouteStrength
Kit; powderOral4 g / pck
GranuleOral4 g
Powder, for suspensionOral4 g/5.5g
Powder, for suspensionOral4 g / 9 g
Powder, for suspensionOral4 g/8.3g
Powder, for suspensionOral4 g / 5 g
Powder, for suspensionOral4 g/5g
Powder, for suspensionOral4 g/9g
PowderNot applicable1 kg/1kg
Powder, for suspensionOral4 g/5.7g
Powder, for suspensionOral4 g/4.8g
Powder, for suspensionOral4 g/8.780g
Powder, for suspensionOral4 g / sachet
Powder, for suspensionOral4 g/5.718g
Powder, for suspensionOral4 g
TabletOral
PowderParenteral4 G
PowderParenteral4 g/9.5g
PowderOral
Powder; suspensionOral4 g / dose
Powder, for suspensionOral400 g / can
PowderOral4.00 g
Powder, for solutionOral4 g / 5 g
Powder, for solutionOral400 g / pck
PowderOral4 g / 9 g
Powder, for suspensionOral
Powder, for suspensionOral4 g/6.4g
Powder, for suspensionOral9 g
Powder, for solutionOral4 g / pck
Powder, for solutionOral4 g / 9 g
TabletOral1 g / tab
PowderOral4 g
Powder
GranuleOral0.7382 g/g
GranuleOral4 g/5.4g
Prices
Unit descriptionCostUnit
Questran Light 4 gm/dose Powder 210 gm Can116.3USD can
Questran 4 gm/dose Powder 378 gm Can115.62USD can
Questran Light 4 gm/dose Powder 268 gm Can102.35USD can
Cholestyramine 4 gm/dose Powder 378 gm Can57.99USD can
Cholestyramine Light 4 gm/dose Powder 210 gm Can57.99USD can
Cholestyramine resin powder16.83USD g
Questran 4 gm Packets4.4USD packet
Questran light packet4.25USD each
Questran packet4.23USD each
Cholestyramine 4 gm Packets3.5USD packet
Cholestyramine Light 4 gm Packets3.49USD packet
Cholestyramine light packet3.35USD each
Prevalite packet2.58USD each
Pms-Cholestyramine Light 4 g Powder Packet1.41USD packet
Pms-Cholestyramine Regular 4 g Powder Packet1.41USD packet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityInsolubleNot Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets2
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insights and accelerate drug research.
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1. Bile acids
Kind
Group
Organism
Humans
Pharmacological action
Yes
Actions
Binder
References
  1. Nichifor M, Cristea D, Mocanu G, Carpov A: Aminated polysaccharides as bile acid sorbents: in vitro study. J Biomater Sci Polym Ed. 1998;9(6):519-34. [Article]
  2. Benson GM, Alston DR, Hickey DM, Jaxa-Chamiec AA, Whittaker CM, Haynes C, Glen A, Blanchard S, Cresswell SR, Suckling KE: SK&F 97426-A: a novel bile acid sequestrant with higher affinities and slower dissociation rates for bile acids in vitro than cholestyramine. J Pharm Sci. 1997 Jan;86(1):76-81. [Article]

Drug created at July 24, 2007 18:41 / Updated at November 28, 2021 11:56