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Identification
Name Cholestyramine
Accession Number DB01432
Type small molecule
Groups approved
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.
Structure Thumb
Synonyms
  • Colestyramine
Brand names
  • Cholybar
  • Locholest
  • Locholest light
  • Novo-Cholamine
  • Novo-Cholamine Light
  • PMS Cholestyramine
  • Prevalite
  • Questran
  • Questran Light
Brand name mixtures Not Available
Categories
  • Anticholesteremic Agents
  • Antihyperlipidemics
  • Cholesterol Absorption Inhibitors
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
Mass Spec Not Available
Taxonomy
Kingdom Not Available
Classes Not Available
Substructures 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.
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.
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
Pharmacoeconomics
Manufacturers
  • Parke davis div warner lambert co
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Par pharmaceutical inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Teva pharmaceuticals usa
  • Upsher smith laboratories inc
  • Bristol myers co
  • Apothecon inc div bristol myers squibb
Packagers
Dosage forms
Form Route Strength
Powder Oral
Powder, for solution Oral
Powder, for suspension Oral
Prices
Unit description Cost Unit
Questran Light 4 gm/dose Powder 210 gm Can 116.3 USD can
Questran 4 gm/dose Powder 378 gm Can 115.62 USD can
Questran Light 4 gm/dose Powder 268 gm Can 102.35 USD can
Cholestyramine 4 gm/dose Powder 378 gm Can 57.99 USD can
Cholestyramine Light 4 gm/dose Powder 210 gm Can 57.99 USD can
Cholestyramine resin powder 16.83 USD g
Questran 4 gm Packets 4.4 USD packet
Questran light packet 4.25 USD each
Questran packet 4.23 USD each
Cholestyramine 4 gm Packets 3.5 USD packet
Cholestyramine Light 4 gm Packets 3.49 USD packet
Cholestyramine light packet 3.35 USD each
Prevalite packet 2.58 USD each
Pms-Cholestyramine Light 4 g Powder Packet 1.41 USD packet
Pms-Cholestyramine Regular 4 g Powder Packet 1.41 USD packet
Patents Not Available
Properties
State solid
Melting point Not Available
Experimental Properties
Property Value Source
water solubility Insoluble PhysProp
Predicted Properties Not Available
References
Synthesis Reference Not Available
General Reference Not Available
External Links
Resource Link
PharmGKB PA448974 Link_out
Drug Product Database 890960 Link_out
RxList http://www.rxlist.com/cgi/generic/cholestyramine.htm Link_out
Drugs.com http://www.drugs.com/cdi/cholestyramine-powder.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Cholestyramine Link_out
ATC Codes
  • C10AC01
AHFS Codes
  • 24:06.04
PDB Entries Not Available
FDA label Not Available
MSDS show (74.1 KB)
Interactions
Drug Interactions Not Available
Food Interactions
  • Take with food, do not mix with soft drinks.
Targets

1. Bile acids

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
  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
Comments
Drug created on July 24, 2007 12:41 / Updated on October 05, 2011 16:34

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