コレスチポール。塩酸コレスチポール
WordNet
- a complex consisting of an organic base in association with hydrogen chloride
Wikipedia preview
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
|
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
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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
Related Links
- Prior to initiating therapy with colestipol hydrochloride for oral suspension, secondary causes of hypercholesterolemia (e.g., poorly controlled diabetes mellitus, hypothyroidism, nephrotic syndrome, dysproteinemias, obstructive liver ...
- Contraindications Micronized Colestipol hydrochloride tablets are contraindicated in those individuals who have shown hypersensitivity to any of their components. Precautions Prior to initiating therapy with micronized Colestipol ...
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