| Version |
2.5 |
| Creation Date |
2007-07-24 18:41:58 |
| Update Date |
2009-06-23 18:08:00 |
| Primary Accession Number |
DB01432 |
| Secondary Accession Number |
Not Available |
| Name |
Cholestyramine |
| Drug Type |
|
| 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 |
- Colestyramine
|
| Brand Names |
- Cholybar
- Locholest
- Locholest light
- Novo-Cholamine
- Novo-Cholamine Light
- PMS Cholestyramine
- Prevalite
- Questran
- Questran Light
|
| Brand Mixtures |
Not Available |
| Chemical IUPAC Name |
Not Available |
| Chemical Formula |
Not Available |
| Chemical Structure |
 |
| CAS Registry Number |
11041-12-6 |
| InChI Identifier |
Not Available |
| InChI Key |
Not Available |
| KEGG Drug |
Not Available |
| KEGG Compound |
Not Available |
| PubChem Compound |
Not Available |
| PubChem Substance |
Not Available |
| ChEBI ID |
Not Available |
| PharmGKB ID |
PA448974  |
| HET ID |
Not Available |
| GenBank ID |
Not Available |
| Drug ID Number [DIN] |
00890960 |
| RxList Link |
http://www.rxlist.com/cgi/generic/cholestyramine.htm |
| PDRhealth Link |
Not Available |
| Wikipedia Link |
http://en.wikipedia.org/wiki/Cholestyramine |
| FDA Label |
Not Available |
| Material Safety Data Sheet (MSDS) |
|
| Synthesis Reference |
Not Available |
| Average Molecular Weight |
Not Available |
| Monoisotopic Molecular Weight |
Not Available |
| State |
Solid |
| Melting Point |
Not Available |
| Experimental Water Solubility |
Insoluble
Source: PhysProp
|
| Predicted Water Solubility |
Not Available
Calculated using ALOGPS
|
| Experimental LogP/Hydrophobicity |
Not Available
Source: PhysProp
|
| Predicted LogP |
Not Available
Calculated using ALOGPS
|
| Experimental LogS |
Not Available |
| Predicted LogS |
Not Available
Calculated using ALOGPS
|
| Experimental Caco2 Permeability |
Not Available |
| pKa/Isoelectric Point |
Not Available |
| Mass Spectrum |
Not Available
|
| MOL File |
Not Available |
| SDF File |
Not Available |
| PDB File |
Not Available |
| Experimental PDB ID |
Not Available |
| Isomeric SMILES |
Not Available |
| Canonical SMILES |
Not Available |
| Drug Category |
- Anticholesteremic Agents
- Antihyperlipidemics
- Cholesterol Absorption Inhibitors
|
| ATC Codes |
|
| AHFS Codes |
|
| 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. |
| Pharmacology |
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. |
| Toxicity |
Overdose may result in blockage of intestine or stomach. |
| Protein Binding |
Not Available |
| Biotransformation |
Bile acids |
| Half Life |
6 minutes |
| Dosage Forms |
| Form |
Route |
| Powder |
Oral |
| Powder, for solution |
Oral |
| Powder, for suspension |
Oral |
|
| Patient Information |
Show |
| Contraindications |
Show |
| Interactions |
Show |
| Drug Interactions |
| Drug |
Interaction |
| Acenocoumarol |
The gastro-intestinal binding agent decreases the anticoagulant effect |
| Acenocoumarol |
The gastro-intestinal binding agent decreases the anticoagulant effect |
| Anisindione |
The gastro-intestinal binding agent decreases the anticoagulant effect |
| Dicumarol |
The gastro-intestinal binding agent decreases the anticoagulant effect |
| Digoxin |
The resin decreases the effect of digoxin |
| Ezetimibe |
Decreases the levels of ezetimibe |
| Fluvastatin |
Increased/decreased effect according to spacing |
| Hydrocortisone |
Decreases the effect of hydrocortisone |
| Levothyroxine |
The resin decreases the absorption of thyroid hormones |
| Liothyronine |
The resin decreases the absorption of thyroid hormones |
| Liotrix |
The resin decreases the absorption of thyroid hormones |
| Methotrexate |
Decreased levels of methotrexate |
| Raloxifene |
The resin decreases the effect of raloxifene |
| Spironolactone |
Increased risk of acidosis and hyperkaliemia |
| Thyroglobulin |
The resin decreases the absorption of thyroid hormones |
| Troglitazone |
Decreases the effect of troglitazone |
| Ursodeoxycholic acid |
The resin decreases the effect of ursodiol |
| Warfarin |
The gastro-intestinal binding agent decreases the anticoagulant effect |
|
| Food Interactions |
- Take with food, do not mix with soft drinks.
|
| Pathways |
Not Available
|
| General References |
- Wikipedia
- RxList
|
| Organisms Affected |
|
| Phase 1 Metabolizing Enzymes |
- Liver carboxylesterase
|
