colestipol

コレスチポール

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/08/04 01:01:39」(JST)

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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 Y 37296-80-3 (HCl)
ATC code	C10AC02
PubChem	CID: 62816
DrugBank	DB00375 Y
UNII	K50N755924 Y
KEGG	C06925 Y
ChEMBL	CHEMBL1201678 Y
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).

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)

References

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

• Systematic review: the management of chronic diarrhoea due to bile acid malabsorption.

• Wilcox C1, Turner J, Green J.Author information 1Cochrane Medical Education Centre, Cardiff University School of Medicine, Cardiff, UK.AbstractBACKGROUND: Bile acid malabsorption (BAM) is a common, yet under-recognised, cause of chronic diarrhoea, with limited guidance available on the appropriate management of patients with BAM.
• Alimentary pharmacology & therapeutics.Aliment Pharmacol Ther.2014 May;39(9):923-39. doi: 10.1111/apt.12684. Epub 2014 Mar 6.
• BACKGROUND: Bile acid malabsorption (BAM) is a common, yet under-recognised, cause of chronic diarrhoea, with limited guidance available on the appropriate management of patients with BAM.AIM: To summarise the evidence supporting different treatments available for patients with bile acid malabsorpti
• PMID 24602022

• Treatment of erythropoietic protoporphyria with the oral sorbent colestipol: a proof-of-concept clinical trial.

• Tishler PV1, Rosner B2.
• Journal of the American Academy of Dermatology.J Am Acad Dermatol.2014 Feb;70(2):391-2. doi: 10.1016/j.jaad.2013.10.011.
• PMID 24438965

• Bile acid malabsorption in chronic diarrhea: pathophysiology and treatment.

• Barkun AN, Love J, Gould M, Pluta H, Steinhart H.AbstractBACKGROUND: Bile acid malabsorption (BAM) is a common but frequently under-recognized cause of chronic diarrhea, with an estimated prevalence of 4% to 5%.
• Canadian journal of gastroenterology = Journal canadien de gastroenterologie.Can J Gastroenterol.2013 Nov;27(11):653-9.
• BACKGROUND: Bile acid malabsorption (BAM) is a common but frequently under-recognized cause of chronic diarrhea, with an estimated prevalence of 4% to 5%.METHODS: The published literature for the period 1965 to 2012 was examined for articles regarding the pathophysiology and treatment of BAM to prov
• PMID 24199211

Japanese Journal

• Beneficial effects of colestipol-niacin on coronary atherosclerosis : a 4-year follow-up

• CASHIN-HEMPHILL L.
• JAMA 264, 3013-3017, 1990
• NAID 30005350739

• Beneficial effects of comfined colestipol niacin therapy on coronary atherosclerosis and coronary venous bypass grafts

• BLANKENHORN DN
• JAMA 257, 3233-3240, 1987
• NAID 30005346240

• Effects of dietary factors and fecal bile acids on DMH induced colon cancer in rat.

• 清水 豊,中澤 三郎
• 日本消化器病学会雑誌 82(10), 2554-2561, 1985
• … factors and fecal bile acids on colon carcinogenesis, Donryu rats were maintained on one of the diets containing high fat, 1.5% of colestipol, high fiber, high fat plus high fiber or control and were given subcutaneous injection of DMH, and fecal bile acids were measured with high performance liquid chromatography.The number of colon tumors was increased in rats fed high fat diet and colestipol diet compared with control diet, and in these groups fecal bile acids were increased, too.However, in high fiber diet group the …
• NAID 130001064146

Related Links

• Colestipol: MedlinePlus Drug Information

Colestipol comes as granules to take by mouth. It usually is taken two to four times a day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take ...

• Colestipol - FDA prescribing information, side effects and uses

The active ingredient in micronized Colestipol hydrochloride tablets is micronized Colestipol hydrochloride, which is a lipid lowering agent for oral use. Colestipol is an insoluble, high molecular weight basic anion-exchange copolymer ...

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