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	2010-10-06
Cholestyramine	Powder, for suspension	4 g	Oral	Sorres Pharma Inc	1998-02-17	2010-10-19
Cholestyramine-odan	Powder, for suspension	4 g	Oral	Odan Laboratories Ltd	2016-12-23	Not applicable
Olestyr	Powder, for suspension	4 g	Oral	Pharmascience Inc	1996-03-15	Not applicable
Olestyr	Powder, for suspension	4 g	Oral	Pharmascience Inc	1993-12-31	Not applicable
Questran	Powder, for suspension	4 g/6.4g	Oral	Par Pharmaceutical	2009-06-01	2011-09-09
Questran	Powder, for suspension	4 g/9g	Oral	Par Pharmaceutical	2009-06-01	2011-09-09
Questran Light Pws 4gm/pck	Powder, for solution	4 g	Oral	Bristol Labs Division Of Bristol Myers Squibb	1991-12-31	2005-08-01
Questran Pwr 378gm/can	Powder, for solution	4 g	Oral	Bristol Labs Division Of Bristol Myers Squibb	1985-12-31	2005-08-01
Questran Pwr 4gm/9gm	Powder, for solution	4 g	Oral	Bristol Labs Division Of Bristol Myers Squibb	1979-12-31	2005-08-01

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
Cholestyramine	Powder, for suspension	4 g/9g	Oral	Zydus Pharmaceuticals Usa, Inc.	2018-08-01	Not applicable
Cholestyramine	Powder, for suspension	4 g/5.5g	Oral	Zydus Pharmaceuticals Usa, Inc.	2017-06-08	Not applicable
Cholestyramine	Powder, for suspension	4 g/9g	Oral	Par Pharmaceutical, Inc.	2005-09-15	Not applicable
Cholestyramine	Powder, for suspension	4 g/5.5g	Oral	A-S Medication Solutions	2017-06-08	Not applicable
Cholestyramine	Powder, for suspension	4 g/5g	Oral	Physicians Total Care, Inc.	2006-02-08	Not applicable
Cholestyramine	Powder, for suspension	4 g/5.5g	Oral	Cadila Pharnmaceuticals	2017-06-08	Not applicable
Cholestyramine	Powder, for suspension	4 g/9g	Oral	Cadila Pharnmaceuticals	2018-08-01	Not applicable
Cholestyramine	Powder, for suspension	4 g/9g	Oral	Upsher Smith Laboratories	1996-08-15	Not applicable
Cholestyramine	Powder, for suspension	4 g/9g	Oral	Physicians Total Care, Inc.	2010-03-22	Not applicable

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.

Target	Actions	Organism
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

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

Phase	Status	Purpose	Conditions	Count
1	Completed	Basic Science	Disseminated Sclerosis	1
1	Completed	Basic Science	Impaired Renal Function	1
1	Completed	Treatment	Alagille Syndrome / Orphan Cholestatic Liver Diseases / Primary Biliary Cholangitis / Progressive Familial Intrahepatic Cholestasis (PFIC)	1
2	Completed	Treatment	Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia	1
2	Completed	Treatment	High Cholesterol	1
3	Completed	Prevention	Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Dyslipidemia (Fredrickson Type Ⅱa) / Heart Diseases / Myocardial Infarction / Myocardial Ischemia	1
3	Completed	Prevention	Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia	2
3	Completed	Treatment	Disseminated Sclerosis	1
3	Recruiting	Treatment	Graves Diseases / Hyperthyroidism	1
3	Recruiting	Treatment	High Cholesterol	2
4	Completed	Prevention	Diabetes Mellitus (DM) / Diabetic Neuropathies / Retinopathy, Diabetic	1
4	Completed	Treatment	Healthy Volunteers	2
Not Available	Completed	Basic Science	Hyperlipidemias	1
Not Available	Completed	Treatment	Graves Diseases	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
Powder, for suspension	Oral	4 g/9g
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/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

1. Bile acids

Kind

Group

Organism

Humans

Pharmacological action

Yes

Actions

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. [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 April 19, 2019 16:00