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Colestipol

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Colestipol
Clinical data
Trade namesColestid, Cholestabyl
AHFS/Drugs.comMonograph
MedlinePlusa682157
Routes of
administration
Oral (suspension or tablets)
ATC code
Legal status
Legal status
Pharmacokinetic data
BioavailabilityNone
ExcretionFaeces, in complex withbile acids
Identifiers
  • Copolymer of bis(2-aminoethyl)amine and 2-(chloromethyl)oxirane
CAS Number
PubChemCID
DrugBank
ChemSpider
  • none
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.123.044Edit this at Wikidata
Chemical and physical data
Formula(C4H10N3)m(C3H6O)n
 ☒NcheckY (what is this?)  (verify)

Colestipol (trade namesColestid,Cholestabyl) is abile acid sequestrant used to lower bloodcholesterol, specificallylow-density lipoprotein (LDL).[1][2] It is also used to reduce stool volume and frequency, and in the treatment of chronic diarrhea.[3]

Likecholestyramine, colestipol works in the gut by trappingbile acids and preventing them from being reabsorbed. This leads to decreasedenterohepatic recirculation of bile acids, increased synthesis of new bile acids by the liver from cholesterol, decreased liver cholesterol, increasedLDL 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 inhypertriglyceridemia (high level oftriglycerides in the blood).[citation needed]

Chemistry

[edit]

Colestipol is acopolymer ofdiethylenetriamine (DETA) —ortetraethylenepentamine according to some sources[5][6]— andepichlorohydrin.[7][8] The structure drawing (top right) shows the DETA moieties in blue and the epichlorohydrin moieties in red.

Alternative chemical structure, withtetraethylenepentamine instead ofdiethylenetriamine; formula (C8H18N5)m(C3H6O)n
The constituent DETA

The constituentstetraethylenepentamine (top) andepichlorohydrin (bottom)

Notes and references

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  1. ^Handelsman Y (May 2011)."Role of bile acid sequestrants in the treatment of type 2 diabetes".Diabetes Care.34 (Suppl 2): S244-50.doi:10.2337/dc11-s237.PMC 3632187.PMID 21525463.
  2. ^abc"Colestipol Hydrochloride".Drugs.com.
  3. ^"colestipol (Colestid)".MedicineNet.
  4. ^Mutschler E, Schäfer-Korting M (2001).Arzneimittelwirkungen (in German) (8th ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. p. 523.ISBN 3-8047-1763-2.
  5. ^"Colestipol structure".Clinical Pharmacology. Archived fromthe original on 2016-03-04. Retrieved2012-01-28.
  6. ^"Colestipol structure".Beth Israel Deaconess Medical Center & Care Group. Archived fromthe original on 2010-12-29.
  7. ^Haberfeld H, ed. (2009).Austria-Codex (in German) (2009/2010 ed.). Vienna: Österreichischer Apothekerverlag.ISBN 978-3-85200-196-8.
  8. ^Steinhilber D, Schubert-Zsilavecz M, Roth HJ (2005).Medizinische Chemie (in German). Stuttgart: Deutscher Apotheker Verlag. p. 433.ISBN 3-7692-3483-9.
GI tract
Cholesterol absorption inhibitors,NPC1L1
Bile acid sequestrants/resins (LDL)
Liver
Statins (HMG-CoA reductase,LDL)
Niacin and derivatives (HDL andLDL)
MTTP inhibitors (VLDL)
ATP citrate lyase inhibitors (LDL)
Thyromimetics (VLDL)
Blood vessels
PPAR agonists (LDL)
Fibrates
Others
CETP inhibitors (HDL)
PCSK9 inhibitors (LDL)
ANGPTL3 inhibitors (LDL/HDL)
Combinations
Other
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