Colestipol

Title: Colestipol
CAS Registry Number: 26658-42-4
CAS Name: N-(2-Aminoethyl)-N¢-[2-[(2-aminoethyl)amino]ethyl]-1,2-ethanediamine polymer with (chloromethyl)oxirane
Literature References: A basic anion exchange resin described as a high molecular wt copolymer of diethylenetriamine and 1-chloro-2,3-epoxypropane (hydrochloride), with approx 1 out of 5 amine nitrogens protonated, for which no structural formula has been assigned and for which no specific mol wt information is available, due to the highly cross-linked and insoluble nature of the material. Prepn: Nelson, Van den Berg, DE 1927336; eidem, US 3692895 (1969, 1971 to Upjohn); Lednicer, Peery, DE 2053585; eidem, US 3803237 (1971, 1974 to Upjohn). Activity studies: Parkinson et al., Atherosclerosis 11, 531 (1970); 17, 167 (1973); Marmo et al., G. Arterioscler. 8, 229 (1970); Goodman et al., J. Clin. Invest. 52, 2646 (1973). Toxicology: Webster, Bollert, Toxicol. Appl. Pharmacol. 28, 57 (1974). Review of pharmacology and therapeutic efficacy: R. C. Heel et al., Drugs 19, 161-180 (1980).
Derivative Type: Hydrochloride
CAS Registry Number: 37296-80-3
Manufacturers' Codes: U-26597A
Trademarks: Cholestabyl (Fournier); Colestid (Pfizer); Lestid (Pfizer)
Properties: Light yellow, hygroscopic resin. Insol in water. Swells when suspended in water or aqueous fluids. LD50 in rats (mg/kg): >4000 i.p.; >1000 orally (Webster, Bollert).
Toxicity data: LD50 in rats (mg/kg): >4000 i.p.; >1000 orally (Webster, Bollert)
Therap-Cat: Antilipemic.
Keywords: Antilipemic; Bile Acid Sequesterants; Ion-exchange Resin.
Colforsin Colfosceril Palmitate Colicins Colistin Collagenase

Colestipol
Colestipol skeletal 2.svg
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 YesY
37296-80-3 (HCl)
ATC code C10AC02
PubChem CID 62816
DrugBank DB00375
UNII K50N755924 YesY
KEGG C06925 YesY
ChEMBL CHEMBL1201678 YesY
Chemical data
Formula (C4H10N3)m(C3H6O)n
 N (what is this?)  (verify)

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]