Colestipol

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Colestipol
Colestipol skeletal 2.svg
Clinical data
Trade names Colestid, Cholestabyl
AHFS/Drugs.com Monograph
MedlinePlus a682157
Pregnancy
category
  • US: B (No risk in non-human studies)
Routes of
administration
Oral (suspension or tablets)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability None
Excretion Faeces, in complex with bile acids
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
  • none
UNII
KEGG
ChEMBL
Chemical and physical data
Formula (C4H10N3)m(C3H6O)n
 NYesY (what is this?)  (verify)

Colestipol (trade names Colestid, Cholestabyl) is a bile acid sequestrant used to lower blood cholesterol, specifically low-density lipoprotein (LDL).[1][2] It is also used to reduce stool volume and frequency, and in the treatment of chronic diarrhea.[3]

Like cholestyramine, colestipol works in the gut by trapping bile acids and preventing them from being reabsorbed. This leads to decreased enterohepatic recirculation of bile acids, increased synthesis of new bile acids by the liver from cholesterol, decreased liver cholesterol, increased LDL receptor expression, and decreasing LDL in blood.[4]

Side effects[edit]

The following notable side effects may occur:[2]

Interactions[edit]

Colestipol can bind to a number of drugs and nutrients in the gut and inhibit or delay their absorption. Such substances include:[2]

Contraindications[edit]

Colestipol is contraindicated in hypertriglyceridemia (high level of triglycerides in the blood).[citation needed]

Chemistry[edit]

Colestipol is a copolymer of diethylenetriamine (DETA) —or tetraethylenepentamine according to some sources[5][6]— and epichlorohydrin.[7][8] The structure drawing (top right) shows the DETA moieties in blue and the epichlorohydrin moieties in red.

Alternative chemical structure, with tetraethylenepentamine instead of diethylenetriamine; formula (C8H18N5)m(C3H6O)n
The constituent DETA

The constituents tetraethylenepentamine (top) and epichlorohydrin (bottom)

Notes and references[edit]

  1. ^ Handelsman, Y. (2011). "Role of Bile Acid Sequestrants in the Treatment of Type 2 Diabetes". Diabetes Care. 34: S244–S250. doi:10.2337/dc11-s237. PMID 21525463. 
  2. ^ a b c Drugs.com: Colestipol Hydrochloride
  3. ^ http://www.medicinenet.com/colestipol/article.htm
  4. ^ Mutschler, Ernst; Schäfer-Korting, Monika (2001). Arzneimittelwirkungen (in German) (8 ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. p. 523. ISBN 3-8047-1763-2. 
  5. ^ Clinical Pharmacology: Colestipol structure
  6. ^ Beth Israel Deaconess Medical Center & Care Group: Colestipol structure Archived 2010-12-29 at the Wayback Machine.
  7. ^ Haberfeld, H, ed. (2009). Austria-Codex (in German) (2009/2010 ed.). Vienna: Österreichischer Apothekerverlag. ISBN 3-85200-196-X. 
  8. ^ Steinhilber, D; Schubert-Zsilavecz, M; Roth, HJ (2005). Medizinische Chemie (in German). Stuttgart: Deutscher Apotheker Verlag. p. 433. ISBN 3-7692-3483-9.