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a complex consisting of an organic base in association with hydrogen chloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/05/13 13:13:54」(JST)

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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]

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

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)

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^[4]^[5]— and epichlorohydrin.^[6]^[7] 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

^ 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. edit
^ ^a ^b ^c Drugs.com: Colestipol Hydrochloride
^ Mutschler, Ernst; Schäfer-Korting, Monika (2001). Arzneimittelwirkungen (in German) (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). Austria-Codex (in German) (2009/2010 ed.). Vienna: Österreichischer Apothekerverlag. ISBN 3-85200-196-X.
^ Steinhilber, D; Schubert-Zsilavecz, M; Roth, HJ (2005). Medizinische Chemie (in German). Stuttgart: Deutscher Apotheker Verlag. p. 433. ISBN 3-7692-3483-9.

UpToDate Contents

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1. スタチン系およびフィブラート系以外の薬剤による脂質低下 lipid lowering with drugs other than statins and fibrates
2. 成人におけるクロストリジウム・ディフィシル：治療 clostridium difficile in adults treatment
3. 成人における過敏性腸症候群の治療 treatment of irritable bowel syndrome in adults
4. 胆汁うっ滞関連そう痒症 pruritus associated with cholestasis
5. ネフローゼ症候群における脂質異常 lipid abnormalities in nephrotic syndrome

English Journal

Bile Acid diarrhea: prevalence, pathogenesis, and therapy.

Camilleri M1.
Gut and liver.Gut Liver.2015 May 23;9(3):332-9. doi: 10.5009/gnl14397.
Bile acid diarrhea (BAD) is usually seen in patients with ileal Crohn's disease or ileal resection. However, 25% to 50% of patients with functional diarrhea or diarrhea-predominant irritable bowel syndrome (IBS-D) also have evidence of BAD. It is estimated that 1% of the population may have BAD. The
PMID 25918262

Feasibility study of colestipol as an oral phosphate binder in hemodialysis patients.

Hood CJ1, Wolley MJ, Kam AL, Kendrik-Jones JC, Marshall MR.
Nephrology (Carlton, Vic.).Nephrology (Carlton).2015 Apr;20(4):250-6. doi: 10.1111/nep.12388.
BACKGROUND: Currently available calcium- and aluminium-based phosphate binders are dose limited because of potential toxicity, and newer proprietary phosphate binders are expensive. We examined phosphate-binding effects of the bile acid sequestrant colestipol, a non-proprietary drug that is in the s
PMID 25557531

Luminal Toxin-Binding Agents for Clostridium difficile Infection.

McCoy RM1, Klick A2, Hill S3, Dull RB2.
Journal of pharmacy practice.J Pharm Pract.2015 Jan 22. pii: 0897190014566315. [Epub ahead of print]
OBJECTIVE: To systematically search the literature for trials evaluating luminal toxin-binding agents (LTBAs) for Clostridium difficile infection (CDI).METHODS: A systematic search was conducted utilizing PubMed and International Pharmaceutical Abstracts with the following terms: anion-exchange resi
PMID 25613056

Japanese Journal

EFFECTS OF COLESTIPOL HYDROCHLORIDE ON CHOLESTEROL AND BILE ACIDS ABSORPTION IN THE RAT INTESTINAL TRACT

FUJIHASHI TOSHIAKI,MUNEKIYO KATSUNORI,MESHI TERUHIKO
Journal of pharmacobio-dynamics 4(8), 552-558, 1981-08-00
… It was clearly shown that colestipol hydrochloride inhibits lymphatic absorption of not only endogenous but also exogenous cholesterol and triglyceride in thoracic duct cannulated rats. … Inhibition of cholesterol absorption by colestipol hydrochloride was effectively blocked by administration of cholic acid. …
NAID 110003636182

Colestipol hydrochloride in hypercholesterolemic patients-Effect on serum cholesterol and mortality

DORR AE
J Chron Dis 31, 5-14, 1978
NAID 30011797918

「コレスチポール」

Colestipol
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; category	US: B (No risk in non-human studies);
Legal status	US: ℞-only;
Routes of; administration	Oral (suspension or tablets)
Pharmacokinetic data
Bioavailability	None
Excretion	Faeces, in complex with bile acids
Identifiers
CAS Registry 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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