コレスチポール
Wikipedia preview
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)
[Wiki en表示]
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 |
|
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).[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]
Contents
- 1 Side effects
- 2 Interactions
- 3 Contraindications
- 4 Chemistry
- 5 References
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 (C 8H 18N 5) m(C 3H 6O) n
|
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.
Lipid modifying agents (C10)
|
|
GI tract |
Cholesterol absorption inhibitors, NPC1L1 |
|
|
Bile acid sequestrants/resins (LDL) |
- Cholestyramine
- Colestipol
- Colestilan
- Colextran
- Colesevelam
|
|
|
Liver |
Statins (HMG-CoA reductase, LDL) |
- Simvastatin#
- Atorvastatin
- Fluvastatin
- Lovastatin
- Mevastatin
- Pitavastatin
- Pravastatin
- Rosuvastatin
- Cerivastatin‡
|
|
Niacin and derivatives (HDL and LDL) |
- Niceritrol
- Niacin
- Nicofuranose
- Aluminium nicotinate
- Nicotinyl alcohol
- Acipimox
|
|
MTTP inhibitors (VLDL) |
- Dirlotapide
- Lomitapide
- Mitratapide
|
|
|
Blood vessels |
Fibrates (PPAR) |
- Clofibrate‡
- Bezafibrate
- Aluminium clofibrate
- Gemfibrozil
- Fenofibrate
- Simfibrate
- Ronifibrate
- Ciprofibrate
- Etofibrate
- Clofibride
- Clinofibrate
|
|
CETP inhibitors (HDL) |
- Anacetrapib†
- Dalcetrapib§
- Evacetrapib†
- Torcetrapib§
|
|
|
Combinations |
- Niacin/lovastatin
- Niacin/simvastatin
- Ezetimibe/simvastatin
- Ezetimibe/atorvastatin
- Niacin/laropiprant
|
|
Other |
- Dextrothyroxine‡
- Probucol
- Tiadenol
- Benfluorex
- Meglutol
- Omega-3-triglycerides
- Magnesium pyridoxal 5-phosphate glutamate
- Policosanol
- Lapaquistat§
- Mipomersen
- Alipogene tiparvovec
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
Index of nutrition
|
|
Description |
- Vitamins
- Cofactors
- Metal metabolism
- Fats
- metabolism
- intermediates
- lipoproteins
- Sugars
- Glycolysis
- Glycogenesis and glycogenolysis
- Fructose and galactose
|
|
Disease |
- Vitamins
- Carbohydrate
- Lipid
- Metals
- Other
- Symptoms and signs
|
|
Treatment |
- Drugs
- Vitamins
- Mineral supplements
|
|
|
UpToDate Contents
全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.
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
- Beneficial effects of comfined colestipol niacin therapy on coronary atherosclerosis and coronary venous bypass grafts
- 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 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 ...
- 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 ...
Related Pictures
★リンクテーブル★
[★]
- 英
- colestipol
- 化
- 塩酸コレスチポール colestipol hydrochloride
[★]
コレスチポール。塩酸コレスチポール