Tìm theo
Colestipol
Các tên gọi khác (3) :
  • Colestipolum
  • Copolymer of bis(2-aminoethyl)amine and 2-(chloromethyl)oxirane
  • Epichlorohydrin-tetraethylenepentamine polymer
anion exchange resins, hypolipidemic agents
Thuốc Gốc
Small Molecule
CAS: 50925-79-6
ATC: C10AC02
ĐG : Catalent Pharma Solutions , http://www.catalent.com
CTHH: C11H28ClN5O
PTK: 281.826
Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C11H28ClN5O
Phân tử khối
281.826
Monoisotopic mass
281.19823825
InChI
InChI=1S/C8H23N5.C3H5ClO/c9-1-3-11-5-7-13-8-6-12-4-2-10;4-1-3-2-5-3/h11-13H,1-10H2;3H,1-2H2
InChI Key
InChIKey=GMRWGQCZJGVHKL-UHFFFAOYSA-N
IUPAC Name
(2-aminoethyl)[2-({2-[(2-aminoethyl)amino]ethyl}amino)ethyl]amine; 2-(chloromethyl)oxirane
Traditional IUPAC Name
epichlorohydrin; tetraethylenepentamine
SMILES
ClCC1CO1.NCCNCCNCCNCCN
Độ hòa tan
Insoluble
logP
-2.206
pKa (Strongest Basic)
9.81
PSA
88.13 Å2
Refractivity
56.04 m3·mol-1
Polarizability
23.97 Å3
Rotatable Bond Count
11
H Bond Acceptor Count
5
H Bond Donor Count
5
Physiological Charge
3
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Cholesterol is the major, and probably the sole precursor of bile acids. During normal digestion, bile acids are secreted via the bile from the liver and gall bladder into the intestines. Bile acids emulsify the fat and lipid materials present in food, thus facilitating absorption. A major portion of the bile acids secreted is reabsorbed from the intestines and returned via the portal circulation to the liver, thus completing the enterohepatic cycle. Only very small amounts of bile acids are found in normal serum. Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces. This nonsystemic action results in a partial removal of the bile acids from the enterohepatic circulation, preventing their reabsorption. Since colestipol hydrochloride is an anion exchange resin, the chloride anions of the resin can be replaced by other anions, usually those with a greater affinity for the resin than the chloride ion.
Cơ Chế Tác Dụng : Highly crosslinked and insoluble basic anion exchange resin used as anticholesteremic. It may also may reduce triglyceride levels. [PubChem] Colestipol is a non-absorbed, lipid-lowering polymer that binds bile acids in the intestine, impeding their reabsorption. As the bile acid pool becomes depleted, the hepatic enzyme, cholesterol 7-(alpha)-hydroxylase, is upregulated, which increases the conversion of cholesterol to bile acids. This causes an increased demand for cholesterol in the liver cells, resulting in the dual effect of increasing transcription and activity of the cholesterol biosynthetic enzyme, hydroxymethyl-glutaryl-coenzyme A (HMG-CoA) reductase, and increasing the number of hepatic low-density lipoprotein (LDL) receptors. These compensatory effects result in increased clearance of LDL cholesterol (LDL-C) from the blood, resulting in decreased serum LDL-C levels. Serum triglyceride levels may increase or remain unchanged. The end result is increased clearance of LDL-cholesterol from the blood with decreased serum LDL-cholesterol.
Dược Động Học :
▧ Absorption :
Not absorbed from the gastrointestinal tract.
▧ Protein binding :
Not applicable (not hydrolyzed by digestive enzymes and not absorbed).
▧ Metabolism :
Not applicable (not hydrolyzed by digestive enzymes and not absorbed).
▧ Route of Elimination :
Colestipol hydrochloride binds bile acids in the intestine forming a complex that is excreted in the feces. In humans, less than 0.17% of a single 14C-labeled colestipol hydrochloride dose is excreted in the urine when given following 60 days of chronic dosing of 20 grams of colestipol hydrochloride per day. The increased fecal loss of bile acids due to colestipol hydrochloride administration leads to an increased oxidation of cholesterol to bile acids.
Độc Tính : Oral LD50 in rats is > 1000 mg/kg. Symptoms of overdose may include eye irritation, constipation, abdominal cramps, nausea, vomiting, diarrhea, and hypersensitivity. However, as colestipol is not absorbed, the risk of systemic toxicity is low.
Chỉ Định : For use, as adjunctive therapy to diet, for the reduction of elevated serum total and LDL-C in patients with primary hypercholesterolemia (elevated LDL-C) who do not respond adequately to diet.
Tương Tác Thuốc :
  • Acenocoumarol The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of acenocoumarol by decreasing its absorption.
  • Anisindione The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of anisindione by decreasing its absorption.
  • Chlorothiazide Bile acid sequestrants may decrease the absorption of thiazide diuretics such as chlorothiazide. The diuretic response is likewise decreased. Monitor for decreased therapeutic effects of thiazide diuretics if coadministered with a bile acid sequestrant. If these agents are used concomitantly, separate doses 2 or more hours to minimize the interaction.
  • Cholecalciferol Bile acid sequestrants such as colestipol may decrease the serum concentration of Vitamin D analogs such as cholecalciferol. More specifically, bile acid sequestrants may impair absorption of Vitamin D analogs. Avoid concomitant administration of vitamin D analogs and bile acid sequestrants. Monitor plasma calcium concentrations in patients receiving combined therapy with these agents. This is particularly important in patients receiving higher doses of a bile acid sequestant (i.e., 30 g/day or more of cholestyramine or equivalent) or in patients experiencing bile acid sequestrant-induced steatorrhea. Specific recommendations regarding the separation of administration of these agents are not defined; however, it would seem prudent to separate the administration of these agents by several hours to minimize the potential risk of interaction. Similar precautions do not apply to parenterally administered vitamin D analogs.
  • Dicoumarol The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of dicumarol by decreasing its absorption.
  • Digoxin The resin decreases the effect of digoxin
  • Fluvastatin Increased/decreased effect according to spacing
  • Hydrocortisone Cholestyramine decreases the effect of hydrocortisone
  • Levothyroxine The resin, colestipol, decreases the absorption of the thyroid hormone, levothyroxine.
  • Liothyronine The resin, colestipol, decreases the absorption of the thyroid hormone, liothyronine.
  • Liotrix The resin, colestipol, decreases the absorption of the thyroid hormone, liotrix.
  • Lomitapide Bile acid sequestrants also used for treating high cholesterol may interfere with the absorption of oral medications, thus separate administration by 4 hours.
  • Raloxifene The resin decreases the effect of raloxifene
  • Sulindac The bile acid sequestrant, colestipol, may decrease the absorption of the NSAID, sulindac. Monitor for changes in the therapeutic and adverse effects of sulindac if colestipol is initiated, discontinued or dose changed. Administering the two agents 2 or more hours apart may reduce, but not eliminate, the risk of this interactions.
  • Thyroglobulin The resin, colestipol, decreases the absorption of the thyroid hormone, thyroglobulin.
  • Tiaprofenic acid The bile acid sequestrant, Colestipol, may reduce Tiaprofenic acid absorption and therapeutic effect.
  • Tolmetin Colestipol may decrease the absorption of Tolmetin. Monitor for changes in the therapeutic and adverse effects of Tolmetin if Colestipol is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction.
  • Torasemide Colestipol may decrease the bioavailability of Torasemide by inhibiting Torasemide absorption. Monitor for changes in the therapeutic and adverse effects of Torasemide if Colestipol is initiated, discontinued or dose changed. Spacing administration by at least 2 hours may reduce the risk of interaction.
  • Trichlormethiazide The bile acid sequestrant, Colestipol, may inhibit the absorption of Trichlormethiazide.
  • Ursodeoxycholic acid The resin decreases the effect of ursodiol
  • Warfarin The bile acid sequestrant, colestipol, may decrease the anticoagulant effect of warfarin by decreasing its absorption.
Liều Lượng & Cách Dùng : Granule - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Cholestabyl
  • Công ty : Pfizer
    Sản phẩm biệt dược : Colestid
  • Công ty : Global
    Sản phẩm biệt dược : Colestipol Hydrochloride
  • Công ty : Pfizer
    Sản phẩm biệt dược : Lestid
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00375
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=62816
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505777
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06925
ChemSpider
http://www.chemspider.com/Chemical-Structure.56550.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/59762-0260-1
PharmGKB
http://www.pharmgkb.org/drug/PA449096
Wikipedia
http://en.wikipedia.org/wiki/Colestipol
RxList
http://www.rxlist.com/cgi/generic/colestipol.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/col1094.shtml
Drugs.com
http://www.drugs.com/cdi/colestipol.html
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