Colestipol
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| Systematic (IUPAC) name | |
| Copolymer of bis(2-aminoethyl)amine and 2-(chloromethyl)oxirane | |
| Clinical data | |
| Trade names | Colestid, Cholestabyl |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a682157 |
| Pregnancy cat. | B (US) |
| Legal status | ℞-only (US) |
| Routes | Oral (suspension or tablets) |
| Pharmacokinetic data | |
| Bioavailability | None |
| Excretion | Faeces, in complex with bile acids |
| Identifiers | |
| CAS number | 50925-79-6  37296-80-3 (HCl) |
| ATC code | C10AC02 |
| PubChem | CID 62816 |
| DrugBank | DB00375 |
| UNII | K50N755924 |
| KEGG | C06925 |
| ChEMBL | CHEMBL1201678 |
| Chemical data | |
| Formula | (C4H10N3)m(C3H6O)n |
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Colestipol (trade names Colestid, Cholestabyl) is a bile acid sequestrant used to lower blood cholesterol, specifically low-density lipoprotein (LDL).[1][2]
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.[3]
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[edit] Side effects
The following notable side effects may occur:[2]
- gastrointestinal tract disturbances, especially (mild, occasionally severe) constipation
- sometimes increase in VLDL[citation needed] and triglyceride synthesis
[edit] Interactions
Colestipol can bind to a number of drugs and nutrients in the gut and inhibit or delay their absorption. Such substances include:[2]
- thiazide diuretics, furosemide
- gemfibrozil
- benzylpenicillin, tetracycline
- digoxin
- lipid soluble vitamins (A, D, E, K)
[edit] Contraindications
Colestipol is contraindicated in hypotriglyceridemia (low level of triglycerides in the blood).[citation needed]
[edit] Chemistry
Colestipol is a copolymer of diethylenetriamine (DETA) —or tetraethylenepentamine according to some sources[4][5]— and epichlorohydrin.[6][7] The structure drawing (top right) shows the DETA moieties in blue and the epichlorohydrin moieties in red.
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[edit] References
- ^ 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.
- ^ a b c Drugs.com: Colestipol Hydrochloride
- ^ Mutschler, Ernst; Schäfer-Korting, Monika (2001) (in German). Arzneimittelwirkungen (8 ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. p. 523. ISBN 3-8047-1763-2.
- ^ Clinical Pharmacology: Colestipol structure
- ^ Beth Israel Deaconess Medical Center & Care Group: Colestipol structure
- ^ Haberfeld, H, ed. (2009) (in German). Austria-Codex (2009/2010 ed.). Vienna: Österreichischer Apothekerverlag. ISBN 3-85200-196-X.
- ^ Steinhilber, D; Schubert-Zsilavecz, M; Roth, HJ (2005) (in German). Medizinische Chemie. Stuttgart: Deutscher Apotheker Verlag. p. 433. ISBN 3-7692-3483-9.
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