Identification

Name
Cholestyramine
Accession Number
DB01432
Type
Small Molecule
Groups
Approved, Investigational
Description

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.

Synonyms
  • Cholestyramine resin
  • Colestyramine
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CholestyraminePowder, for suspension4 gOralSorres Pharma Inc1998-02-172010-10-19Canada
CholestyraminePowder, for suspension4 gOralSorres Pharma Inc1998-02-172010-10-06Canada
Cholestyramine-odanPowder, for suspension4 gOralOdan Laboratories Ltd2016-12-23Not applicableCanada
OlestyrPowder, for suspension4 gOralPharmascience Inc1996-03-15Not applicableCanada
OlestyrPowder, for suspension4 gOralPharmascience Inc1993-12-31Not applicableCanada
QuestranPowder, for suspension4 g/6.4gOralPar Pharmaceutical2009-06-012011-09-09Us
QuestranPowder, for suspension4 g/9gOralPar Pharmaceutical2009-06-012011-09-09Us
Questran Light Pws 4gm/pckPowder, for solution4 gOralBristol Labs Division Of Bristol Myers Squibb1991-12-312005-08-01Canada
Questran Pwr 378gm/canPowder, for solution4 gOralBristol Labs Division Of Bristol Myers Squibb1985-12-312005-08-01Canada
Questran Pwr 4gm/9gmPowder, for solution4 gOralBristol Labs Division Of Bristol Myers Squibb1979-12-312005-08-01Canada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alti-cholestyramine LightKit; Powder4 gOralAltimed Pharma Inc.1994-12-311999-09-17Canada
CholestyraminePowder, for suspension4 g/9gOralUpsher Smith Laboratories1996-08-15Not applicableUs
CholestyraminePowder, for suspension4 g/9gOralZydus Pharmaceuticals Usa, Inc.2018-08-01Not applicableUs
CholestyraminePowder, for suspension4 g/5gOralPhysicians Total Care, Inc.2006-02-08Not applicableUs
CholestyraminePowder, for suspension4 g/9gOralANI Pharmaceuticals, Inc.2018-06-26Not applicableUs
CholestyraminePowder, for suspension4 g/5.5gOralZydus Pharmaceuticals Usa, Inc.2017-06-08Not applicableUs
CholestyraminePowder, for suspension4 g/9gOralGolden State Medical Supply2005-09-152017-01-02Us
CholestyraminePowder, for suspension4 g/5gOralPar Pharmaceutical2005-09-15Not applicableUs
CholestyraminePowder, for suspension4 g/5.5gOralCadila Pharnmaceuticals2017-06-08Not applicableUs
CholestyraminePowder, for suspension4 g/9gOralEon Labs, Inc.1996-08-15Not applicableUs
International/Other Brands
Cholybar / Locholest / Locholest light / Questran Light
Categories
UNII
4B33BGI082
CAS number
11041-12-6
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

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.

Associated Conditions
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 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.

TargetActionsOrganism
ABile acids
binder
Human
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
Toxicity

Overdose may result in blockage of intestine or stomach.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(4R)-limoneneCholestyramine can cause a decrease in the absorption of (4R)-limonene resulting in a reduced serum concentration and potentially a decrease in efficacy.
16-BromoepiandrosteroneCholestyramine can cause a decrease in the absorption of 16-Bromoepiandrosterone resulting in a reduced serum concentration and potentially a decrease in efficacy.
19-norandrostenedioneCholestyramine can cause a decrease in the absorption of 19-norandrostenedione resulting in a reduced serum concentration and potentially a decrease in efficacy.
5-androstenedioneCholestyramine can cause a decrease in the absorption of 5-androstenedione resulting in a reduced serum concentration and potentially a decrease in efficacy.
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.
AcetyldigitoxinCholestyramine can cause a decrease in the absorption of Acetyldigitoxin resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcetyldigoxinCholestyramine can cause a decrease in the absorption of Acetyldigoxin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Food Interactions
  • Take with food, do not mix with soft drinks.

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
External Links
PubChem Substance
46506251
ChEMBL
CHEMBL1201625
PharmGKB
PA448974
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cholestyramine
ATC Codes
C10AC01 — Colestyramine
AHFS Codes
  • 24:06.04 — Bile Acid Sequestrants
MSDS
Download (74.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceDisseminated Sclerosis1
1CompletedBasic ScienceImpaired Renal Function1
1CompletedTreatmentAlagille Syndrome / Orphan Cholestatic Liver Diseases / Primary Biliary Cirrhosis (PBC) / Progressive Familial Intrahepatic Cholestasis (PFIC)1
2Active Not RecruitingTreatmentHigh Cholesterol1
2CompletedTreatmentCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia1
3CompletedPreventionCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Dyslipidemia (Fredrickson Type Ⅱa) / Heart Diseases / Myocardial Infarction / Myocardial Ischemia1
3CompletedPreventionCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia2
3CompletedTreatmentDisseminated Sclerosis1
3RecruitingTreatmentGraves Diseases / Hyperthyroidism1
3RecruitingTreatmentHigh Cholesterol2
4CompletedPreventionDiabetes Mellitus (DM) / Diabetic Neuropathies / Retinopathy, Diabetic1
4CompletedTreatmentHealthy Volunteers2
Not AvailableCompletedBasic ScienceHyperlipidemias1
Not AvailableCompletedTreatmentGraves Diseases1

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
Powder, for suspensionOral4 g/5.5g
Powder, for suspensionOral4 g/5g
Powder, for suspensionOral4 g
Powder, for suspensionOral4 g/9g
Powder, for suspensionOral4 g/5.7g
Powder; suspensionOral4 g
Powder, for suspensionOral400 g
Powder, for solutionOral400 g
PowderOral4 g
Powder, for suspensionOral4 g/6.4g
Powder, for solutionOral4 g
TabletOral1 g
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

Taxonomy

Classification
Not classified

Targets

1. Bile acids
Kind
Group
Organism
Human
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. [PubMed:9659597]
  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. [PubMed:9002463]

Drug created on July 24, 2007 12:41 / Updated on October 16, 2018 08:36