Cholestyramine
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
- Colestiramina
- Colestyramine
- Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Cholestyramine Powder, for suspension 4 g Oral Sorres Pharma Inc 1998-02-17 2010-10-19 Canada 
Cholestyramine Powder, for suspension 4 g Oral Sorres Pharma Inc 1998-02-17 2010-10-06 Canada Cholestyramine-odan Powder, for suspension 4 g Oral Odan Laboratories Ltd 2016-12-23 Not applicable Canada Olestyr Powder, for suspension 4 g Oral Pharmascience Inc 1993-12-31 Not applicable Canada Olestyr Powder, for suspension 4 g Oral Pharmascience Inc 1996-03-15 Not applicable Canada Questran Powder, for suspension 4 g/6.4g Oral Par Pharmaceutical 2009-06-01 2011-09-09 US 
Questran Powder, for suspension 4 g/9g Oral Par Pharmaceutical 2009-06-01 2011-09-09 US Questran Light Pws 4gm/pck Powder, for solution 4 g Oral Bristol Labs Division Of Bristol Myers Squibb 1991-12-31 2005-08-01 Canada Questran Pwr 378gm/can Powder, for solution 4 g Oral Bristol Labs Division Of Bristol Myers Squibb 1985-12-31 2005-08-01 Canada Questran Pwr 4gm/9gm Powder, for solution 4 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 Alti-cholestyramine Light Kit; Powder 4 g Oral Altimed Pharma Inc. 1994-12-31 1999-09-17 Canada Cholestyramine Powder, for suspension 4 g/9g Oral Upsher Smith Laboratories 1996-08-15 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral Cadila Pharnmaceuticals 2018-08-01 Not applicable US Cholestyramine Powder, for suspension 4 g/5.5g Oral Cadila Pharnmaceuticals 2017-06-08 Not applicable US Cholestyramine Powder, for suspension 4 g/5g Oral Physicians Total Care, Inc. 2006-02-08 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral ANI Pharmaceuticals, Inc. 2018-06-26 Not applicable US Cholestyramine Powder, for suspension 4 g/5g Oral Par Pharmaceutical, Inc. 2005-09-15 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral Eon Labs, Inc. 1996-08-15 Not applicable US Cholestyramine Powder, for suspension 4 g/5.5g Oral A-S Medication Solutions 2017-06-08 Not applicable US Cholestyramine Powder, for suspension 4 g/9g Oral Physicians Total Care, Inc. 2010-03-22 Not applicable US - International/Other Brands
- Cholybar / Locholest / Locholest light / Questran Light
- Categories
- Anion Exchange Resins
- Anticholesteremic Agents
- Benzene Derivatives
- Benzylidene Compounds
- Bile Acid Sequestrants
- Bile-acid Binding Activity
- Biomedical and Dental Materials
- Hypolipidemic Agents
- Ion Exchange Resins
- Laboratory Chemicals
- Lipid Modifying Agents
- Lipid Modifying Agents, Plain
- Lipid Regulating Agents
- Macromolecular Substances
- Noxae
- Plastics
- Polymers
- Polystyrenes
- Styrene
- Styrenes
- Toxic Actions
- 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.
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
- 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
Drug Interaction (R)-warfarin Cholestyramine can cause a decrease in the absorption of (R)-warfarin resulting in a reduced serum concentration and potentially a decrease in efficacy. (S)-Warfarin Cholestyramine can cause a decrease in the absorption of (S)-Warfarin resulting in a reduced serum concentration and potentially a decrease in efficacy. 1alpha-Hydroxyvitamin D5 The serum concentration of 1alpha-Hydroxyvitamin D5 can be decreased when it is combined with Cholestyramine. 3,5-diiodothyropropionic acid Cholestyramine can cause a decrease in the absorption of 3,5-diiodothyropropionic acid resulting in a reduced serum concentration and potentially a decrease in efficacy. 4-hydroxycoumarin Cholestyramine can cause a decrease in the absorption of 4-hydroxycoumarin resulting in a reduced serum concentration and potentially a decrease in efficacy. 5-(2-methylpiperazine-1-sulfonyl)isoquinoline Cholestyramine can cause a decrease in the absorption of 5-(2-methylpiperazine-1-sulfonyl)isoquinoline resulting in a reduced serum concentration and potentially a decrease in efficacy. Abaloparatide Cholestyramine can cause a decrease in the absorption of Abaloparatide resulting in a reduced serum concentration and potentially a decrease in efficacy. 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. - 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
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 Powder, for suspension Oral 4 g/5.5g Powder, for suspension Oral 4 g/5g Powder, for suspension Oral 4 g Powder, for suspension Oral 4 g/9g Powder, for suspension Oral 4 g/5.7g Powder; suspension Oral 4 g Powder, for suspension Oral 400 g Powder, for solution Oral 400 g Powder Oral 4 g Powder, for suspension Oral 4 g/6.4g Powder, for solution Oral 4 g Tablet Oral 1 g - 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
Taxonomy
- Classification
- Not classified
Targets
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. [PubMed:9659597]
- 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 February 16, 2019 05:57