Colestipol

Colestipol

Clinical data
Trade names	Colestid, Cholestabyl
AHFS/Drugs.com	Monograph
MedlinePlus	a682157
Routes of administration	Oral (suspension or tablets)
ATC code	C10AC02 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Bioavailability	None
Excretion	Faeces, in complex with bile acids
Identifiers
IUPAC name Copolymer of bis(2-aminoethyl)amine and 2-(chloromethyl)oxirane
CAS Number	26658-42-4 N 37296-80-3 (HCl)
PubChem CID	62816
DrugBank	DB00375 Y
ChemSpider	none
UNII	K50N755924
KEGG	C06925 Y
ChEMBL	ChEMBL1201678 Y
CompTox Dashboard (EPA)	DTXSID00965206 DTXSID901009549, DTXSID00965206
ECHA InfoCard	100.123.044
Chemical and physical 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). It is also used to reduce stool volume and frequency, and in the treatment of chronic diarrhea.

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.

Side effects

The following notable side effects may occur:

• 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:

• thiazide diuretics, furosemide
• gemfibrozil
• benzylpenicillin, tetracycline
• digoxin
• lipid-soluble vitamins (A, D, E, K)

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— and epichlorohydrin. 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)