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.
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- Contraindications & Blackbox Warnings
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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.
Target Actions Organism ABile acids binderHumans - 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
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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.
Drug Interaction Integrate drug-drug
interactions in your softwareAcarbose The therapeutic efficacy of Acarbose can be increased when used in combination with Cholestyramine. Aceclofenac Cholestyramine can cause a decrease in the absorption of Aceclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy. Acemetacin Cholestyramine can cause a decrease in the absorption of Acemetacin resulting in a reduced serum concentration and potentially a decrease in efficacy. Acenocoumarol Cholestyramine can cause a decrease in the absorption of Acenocoumarol resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetaminophen Cholestyramine can cause a decrease in the absorption of Acetaminophen resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetazolamide Cholestyramine can cause a decrease in the absorption of Acetazolamide resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetyl sulfisoxazole Cholestyramine can cause a decrease in the absorption of Acetyl sulfisoxazole resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetyldigitoxin Cholestyramine can cause a decrease in the absorption of Acetyldigitoxin resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetylsalicylic acid Cholestyramine can cause a decrease in the absorption of Acetylsalicylic acid resulting in a reduced serum concentration and potentially a decrease in efficacy. Alclofenac Cholestyramine can cause a decrease in the absorption of Alclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy. 
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- Take with fluids. Do not take with carbonated fluids.
- Take with food. Take with a meal unless this interferes with other medications.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Cholybar / Locholest / Locholest light / Questran Light
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Cholestyramine Powder, for suspension 4 g / 9 g Oral Sorres Pharma Inc 1998-02-17 2010-10-06 Canada 
Cholestyramine Powder, for suspension 4 g / 5 g Oral Sorres Pharma Inc 1998-02-17 2010-10-19 Canada Cholestyramine-odan Powder, for suspension 4 g / sachet Oral Odan Laboratories Ltd 2016-12-23 Not applicable Canada Olestyr Powder, for suspension 4 g / sachet Oral Pharmascience Inc 1993-12-31 Not applicable Canada Olestyr Powder, for suspension 4 g / sachet Oral Pharmascience Inc 1996-03-15 Not applicable Canada Questran Powder, for suspension 4 g/9g Oral Par Pharmaceutical 2009-06-01 2011-09-09 US 
Questran Powder, for suspension 4 g/6.4g Oral Par Pharmaceutical 2009-06-01 2011-09-09 US Questran Light Pws 4gm/pck Powder, for solution 4 g / pck Oral Bristol Labs Division Of Bristol Myers Squibb 1991-12-31 2005-08-01 Canada Questran Pwr 378gm/can Powder, for solution 4 g / pck Oral Bristol Labs Division Of Bristol Myers Squibb 1985-12-31 2005-08-01 Canada Questran Pwr 4gm/9gm Powder, for solution 4 g / 9 g Oral Bristol Labs Division Of Bristol Myers Squibb 1979-12-31 2005-08-01 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Alti-cholestyramine Light Kit; Powder 4 g / pck Oral Altimed Pharma Inc. 1994-12-31 1999-09-17 Canada Cholestyramine Powder, for suspension 4 g/9g Oral Upsher-Smith Laboratories, Inc. 1996-08-15 2023-09-30 US Cholestyramine Powder, for suspension 4 g/9g Oral Par Pharmaceutical, Inc. 2005-09-15 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral PuraCap Laboratories LLC dba Blu Pharmaceuticals 2023-03-14 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral Epic Pharma, LLC 2021-12-15 Not applicable US Cholestyramine Powder, for suspension 4 g/5.5g Oral Zydus Pharmaceuticals (USA) Inc. 2017-06-08 Not applicable US Cholestyramine Powder, for suspension 4 g/5.5g Oral Zydus Lifesciences Limited 2017-06-08 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral bryant ranch prepack 2005-09-15 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral Physicians Total Care, Inc. 2010-03-22 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral A-S Medication Solutions 2005-09-15 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image KOLESTRAN 9 GR 30 POSET Cholestyramine (4 g) Powder Oral SANDOZ İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey 
Categories
- ATC Codes
- C10AC01 — Colestyramine
- Drug Categories
- Anion Exchange Resins
- Anticholesteremic Agents
- Bile Acid Sequestrants
- Bile-acid Binding Activity
- Compounds used in a research, industrial, or household setting
- Hypolipidemic Agents
- Hypolipidemic Agents Indicated for Hyperlipidemia
- Ion Exchange Resins
- Laboratory Chemicals
- Lipid Modifying Agents
- Lipid Modifying Agents, Plain
- Lipid Regulating Agents
- Macromolecular Substances
- Non-statin Hypolipidemic Agents Indicated for Hyperlipidemia
- Plastics
- Polymers
- Polystyrenes
- 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
- External Links
- PubChem Substance
- 46506251
- 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
Phase Status Purpose Conditions Count 4 Completed Prevention Diabetes / Diabetic Neuropathies / Diabetic Retinopathy (DR) 1 4 Completed Treatment Healthy Subjects (HS) 2 4 Enrolling by Invitation Treatment Chronic Kidney Disease (CKD) / Complication of Hemodialysis / Hyperphosphataemia 1 3 Completed Prevention Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Myocardial Infarction / Myocardial Ischemia / Primary Hypercholesterolemia 1 3 Completed Prevention Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Myocardial Ischemia 2 3 Completed Treatment High Cholesterol 2 3 Completed Treatment Multiple Sclerosis 1 3 Not Yet Recruiting Treatment Multiple Sclerosis 1 3 Unknown Status Treatment Graves' Disease / Hyperthyroidism 1 2 Completed Treatment Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Myocardial Ischemia 1
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
Form Route Strength Kit; powder Oral 4 g / pck Granule Oral 4 g Powder, for suspension Oral 4 g/5.5g Powder, for suspension Oral 4 g / 9 g Powder, for suspension Oral 4 g/5g Powder, for suspension Oral 4 g/8.3g Powder, for suspension Oral 4 g / 5 g Powder, for suspension Oral 4 g/9g Powder Not applicable 1 kg/1kg Powder Oral 4 g/9g Powder Oral 4 g/5.7g Powder, for suspension Oral 4 g/5.7g Powder, for suspension Oral 4 g/4.8g Powder, for suspension Oral 4 g/8.780g Powder, for suspension Oral 4 g / sachet Powder, for suspension Oral 4 g/5.718g Powder, for suspension Oral 4 g Tablet Oral Powder Parenteral 4 G Powder Parenteral 4 g/9.5g Powder Oral Drug delivery system Oral 4.000 g Powder Oral 4 g Powder; suspension Oral 4 g / dose Powder Oral 4.000 g Powder, for suspension Oral 400 g / can Powder Oral 4.00 g Powder, for solution Oral 4 g / 5 g Powder, for solution Oral 400 g / pck Powder Oral 4 g / 9 g Powder Oral 4000.000 mg Powder, for suspension Oral 4 g/6.4g Powder, for suspension Oral 9 g Powder, for solution Oral 4 g / pck Powder, for solution Oral 4 g / 9 g Tablet Oral 1 g / tab Powder Granule Oral 0.7382 g/g Granule Oral 4 g/5.4g - Prices
Unit description Cost Unit Questran Light 4 gm/dose Powder 210 gm Can 116.3USD can Questran 4 gm/dose Powder 378 gm Can 115.62USD can Questran Light 4 gm/dose Powder 268 gm Can 102.35USD can Cholestyramine 4 gm/dose Powder 378 gm Can 57.99USD can Cholestyramine Light 4 gm/dose Powder 210 gm Can 57.99USD can Cholestyramine resin powder 16.83USD g Questran 4 gm Packets 4.4USD packet Questran light packet 4.25USD each Questran packet 4.23USD each Cholestyramine 4 gm Packets 3.5USD packet Cholestyramine Light 4 gm Packets 3.49USD packet Cholestyramine light packet 3.35USD each Prevalite packet 2.58USD each Pms-Cholestyramine Light 4 g Powder Packet 1.41USD packet Pms-Cholestyramine Regular 4 g Powder Packet 1.41USD packet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Insoluble Not Available - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
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1. Bile acids
Yes
Binder
References
- 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]
- 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 December 03, 2023 06:20