Colestipol

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]

Colestipol
Clinical data
Trade namesColestid, Cholestabyl
AHFS/Drugs.comMonograph
MedlinePlusa682157
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
    BioavailabilityNone
    ExcretionFaeces, in complex with bile acids
    Identifiers
    CAS Number
    PubChem CID
    DrugBank
    ChemSpider
    • none
    UNII
    KEGG
    ChEMBL
    ECHA InfoCard100.123.044
    Chemical and physical data
    Formula(C4H10N3)m(C3H6O)n
     NY (what is this?)  (verify)

    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

    The following notable side effects may occur:[2]

    • gastrointestinal tract disturbances, especially (mild, occasionally severe) constipation
    • sometimes increase in VLDL and triglyceride synthesis

    Interactions

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

    Contraindications

    Colestipol is contraindicated in hypertriglyceridemia (high level of triglycerides in the blood).

    Chemistry

    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

    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. PMC 3632187. PMID 21525463.
    2. 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.
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