Colestipol

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Colestipol
Colestipol skeletal 2.svg
Names
Pronunciationkoe les' ti pol[1]
Trade namesColestid, Cholestabyl, others
Other namesColestipol hydrochloride
  • Copolymer of bis(2-aminoethyl)amine and 2-(chloromethyl)oxirane
Clinical data
Drug classBile acid sequestrant[2]
Main usesHigh cholesterol, biliary obstruction, liver disease[2][1]
Side effectsConstipation[2]
Pregnancy
category
  • US: B (No risk in non-human studies)
Routes of
use
By mouth (suspension or tablets)
Typical dose5 to 30 gram/day[3]
External links
AHFS/Drugs.comMonograph
US NLMColestipol
MedlinePlusa682157
Legal
Legal status
Pharmacokinetics
BioavailabilityNone
ExcretionFaeces, in complex with bile acids
Chemical and physical data
Formula(C4H10N3)m(C3H6O)n
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Colestipol, sold under the brand name Colestid among others, is a medication used to treat high cholesterol, biliary obstruction, and liver disease.[2][1] In liver disease it is used to decrease itchiness.[1] It is taken by mouth.[2]

Common side effects include constipation.[2] Other side effects may include fat soluble vitamin deficiency.[2] While there is no evidence of harm in pregnancy, such use has not been well studied.[4] It is a bile acid sequestrant.[2] It works by binding bile acids in the intestines and preventing them from being reabsorbed.[1] This decreases in bile results in less cholesterol being made by the liver.[1]

Colestipol was approved for medical use in the United States in 1977.[2] It is available as a generic medication.[1] In the United Kingdom 30 doses of 5 grams costs the NHS about £15 as of 2021.[3] This amount in the United States costs about 31 USD.[5]

Medical use

It is also used to treat certain types of chronic diarrhea.[6]

Dosage

It may be taken at a dose of 5 to 30 grams per day.[3]

Side effects

The following notable side effects may occur:[7]

Interactions

Colestipol can bind to a number of drugs and nutrients in the gut and inhibit or delay their absorption. Such substances include:[7]

Contraindications

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

Chemistry

Colestipol is a copolymer of diethylenetriamine (DETA) —or tetraethylenepentamine according to some sources[8][9]— and epichlorohydrin.[10][11] 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)

References

  1. 1.0 1.1 1.2 1.3 1.4 1.5 1.6 "Colestipol". LiverTox: Clinical and Research Information on Drug-Induced Liver Injury. National Institute of Diabetes and Digestive and Kidney Diseases. 2012. Retrieved 6 January 2022.
  2. 2.0 2.1 2.2 2.3 2.4 2.5 2.6 2.7 2.8 "Colestipol Monograph for Professionals". Drugs.com. Retrieved 6 January 2022.
  3. 3.0 3.1 3.2 BNF 81: March-September 2021. BMJ Group and the Pharmaceutical Press. 2021. p. 212. ISBN 978-0857114105.
  4. "Colestipol Use During Pregnancy". Drugs.com. Retrieved 6 January 2022.
  5. "Colestipol Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 6 January 2022.
  6. "colestipol (Colestid)". MedicineNet.
  7. 7.0 7.1 Drugs.com: Colestipol Hydrochloride
  8. Clinical Pharmacology: Colestipol structure
  9. Beth Israel Deaconess Medical Center & Care Group: Colestipol structure Archived 2010-12-29 at the Wayback Machine
  10. Haberfeld H, ed. (2009). Austria-Codex (in German) (2009/2010 ed.). Vienna: Österreichischer Apothekerverlag. ISBN 978-3-85200-196-8.CS1 maint: unrecognized language (link)
  11. Steinhilber D, Schubert-Zsilavecz M, Roth HJ (2005). Medizinische Chemie (in German). Stuttgart: Deutscher Apotheker Verlag. p. 433. ISBN 3-7692-3483-9.CS1 maint: unrecognized language (link)

External links

Identifiers: