Clofibrate

Các tên gọi khác (15 ) :

2-(4-Chlorophenoxy)-2-methylpropanoic acid ethyl ester
2-(p-Chlorophenoxy)-2-methylpropionic acid ethyl ester
alpha-(p-Chlorophenoxy)isobutyric acid, ethyl ester
alpha-p-Chlorophenoxyisobutyryl ethyl ester
Atromid-S
Clofibrate
Clofibrato
Clofibratum
ELPI
EPIB
Ethyl 2-(P-chlorophenoxy)isobutyrate
Ethyl chlorophenoxyisobutyrate
Ethyl clofibrate
Lipofacton
Liprin

anticholesteremic agents, hypolipidemic agents

Thuốc Gốc

Small Molecule

CAS: 637-07-0

ATC: C10AB01, C10AB03

ĐG : Banner Pharmacaps Inc. , http://www.banpharm.com

CTHH: C₁₂H₁₅ClO₃

PTK: 242.699

A fibric acid derivative used in the treatment of hyperlipoproteinemia type III and severe hypertriglyceridemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986)

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₁₂H₁₅ClO₃

Phân tử khối

242.699

Monoisotopic mass

242.070972053

InChI

InChI=1S/C12H15ClO3/c1-4-15-11(14)12(2,3)16-10-7-5-9(13)6-8-10/h5-8H,4H2,1-3H3

InChI Key

InChIKey=KNHUKKLJHYUCFP-UHFFFAOYSA-N

IUPAC Name

ethyl 2-(4-chlorophenoxy)-2-methylpropanoate

Traditional IUPAC Name

clofibrate

SMILES

CCOC(=O)C(C)(C)OC1=CC=C(Cl)C=C1

Độ tan chảy

118-119

Độ sôi

149 °C at 2.00E+01 mm Hg

Độ hòa tan

Insoluble

logP

3.3

logS

-3.9

pKa (Strongest Basic)

-4.9

PSA

35.53 Å²

Refractivity

62.14 m³·mol^-1

Polarizability

24.7 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Ghose Filter

true

Dược Lực Học : Clofibrate is an antilipidemic agent similar to gemfibrozil. It acts to lower elevated serum lipids by reducing the very low-density lipoprotein fraction (S_f 20-400) rich in triglycerides. Serum cholesterol may be decreased, particularly in those patients whose cholesterol elevation is due to the presence of IDL as a result of Type III hyperlipoproteinemia. Several investigators have observed in their studies that clofibrate may produce a decrease in cholesterol linoleate but an increase in palmitoleate and oleate, the latter being considered atherogenic in experimental animals. The significance of this finding is unknown at this time. Reduction of triglycerides in some patients treated with clofibrate or certain of its chemically and clinically similar analogs may be associated with an increase in LDL cholesterol. Increase in LDL cholesterol has been observed in patients whose cholesterol is initially normal. Animal studies suggest that clofibrate interrupts cholesterol biosynthesis prior to mevalonate formation.

Cơ Chế Tác Dụng : A fibric acid derivative used in the treatment of hyperlipoproteinemia type III and severe hypertriglyceridemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p986) Clofibrate increases the activity of extrahepatic lipoprotein lipase (LL), thereby increasing lipoprotein triglyceride lipolysis. Chylomicrons are degraded, VLDLs are converted to LDLs, and LDLs are converted to HDL. This is accompanied by a slight increase in secretion of lipids into the bile and ultimately the intestine. Clofibrate also inhibits the synthesis and increases the clearance of apolipoprotein B, a carrier molecule for VLDL. Also, as a fibrate, Clofibrate is an agonist of the PPAR-α receptor[4] in muscle, liver, and other tissues. This agonism ultimately leads to modification in gene expression resulting in increased beta-oxidation, decreased triglyceride secretion, increased HDL, increased lipoprotein lipase activity.

Dược Động Học :

▧ Absorption :
Completely but slowly absorbed from the intestine. Between 95% and 99% of an oral dose of clofibrate is excreted in the urine as free and conjugated clofibric acid; thus, the absorption of clofibrate is virtually complete.
▧ Protein binding :
Highly protein-bound (95% to 97%).
▧ Metabolism :
Hepatic and gastrointestinal: rapid de-esterification occurs in the gastrointestinal tract and/or on first-pass metabolism to produce the active form, clofibric acid (chlorophenoxy isobutyric acid [CPIB]).
▧ Half Life :
Half-life in normal volunteers averages 18 to 22 hours (range 14 to 35 hours) but can vary by up to 7 hours in the same subject at different times.

Độc Tính : Oral, mouse: LD₅₀ = 1220 mg/kg; Oral, rabbit: LD₅₀ = 1370 mg/kg; Oral, rat: LD₅₀ = 940 mg/kg. No reported case of overdosage in humans.

Chỉ Định : For Primary Dysbetalipoproteinemia (Type III hyperlipidemia) that does not respond adequately to diet. This helps control high cholesterol and high triglyceride levels.

Tương Tác Thuốc :

Acenocoumarol The fibrate increases the anticoagulant effect
Acetohexamide Clofibrate may increase the effect of sulfonylurea, acetohexamide.
Anisindione The fibrate increases the anticoagulant effect
Chlorpropamide Clofibrate may increase the effect of sulfonylurea, chlorpropamide.
Dicoumarol The fibrate increases the anticoagulant effect
Gliclazide Clofibrate may increase the effect of sulfonylurea, gliclazide.
Glipizide Clofibrate may increase the effect of sulfonylurea, glipizide.
Glisoxepide Clofibrate may increase the effect of sulfonylurea, glisoxepide.
Glyburide Clofibrate may increase the effect of sulfonylurea, glibenclamide.
Glycodiazine Clofibrate may increase the effect of sulfonylurea, glycodiazine.
Insulin Aspart Increases the effect of insulin
Insulin Detemir Increases the effect of insulin
Insulin Glulisine Increases the effect of insulin
Tolazamide Clofibrate may increase the effect of sulfonylurea, tolazamide.
Tolbutamide Clofibrate may increase the effect of sulfonylurea, tolbutamide.
Ursodeoxycholic acid The fibric acid derivative decreases the effect of ursodiol
Warfarin The fibrate increases the anticoagulant effect

Liều Lượng & Cách Dùng : Capsule - Oral

Dữ Kiện Thương Mại

Nhà Sản Xuất

Công ty : The Central

Sản phẩm biệt dược : Alufibrate
Công ty :

Sản phẩm biệt dược : Atromid-S
Công ty : Kotobuki Seiyaku

Sản phẩm biệt dược : Binograc
Công ty : Johnson

Sản phẩm biệt dược : Clobrate
Công ty : Banner

Sản phẩm biệt dược : Clofibrate
Công ty : Newai Chem

Sản phẩm biệt dược : Hisunsero
Công ty : Golden Horse

Sản phẩm biệt dược : Koliva
Công ty : Sinton

Sản phẩm biệt dược : Myanlin

Đóng gói

Công ty : Banner Pharmacaps Inc.

Website : http://www.banpharm.com
Công ty : Major Pharmaceuticals

Website : http://www.majorpharmaceuticals.com
Công ty : Novopharm Ltd.

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB00636

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2796

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504748

KEGG Compound

http://www.genome.jp/dbget-bin/www_bget?cpd:C06916

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D00279

ChemSpider

http://www.chemspider.com/Chemical-Structure.2694.html

PharmGKB

http://www.pharmgkb.org/drug/PA449045

Wikipedia

http://en.wikipedia.org/wiki/Clofibrate

RxList

http://www.rxlist.com/cgi/generic2/clofibrate.htm

Drugs.com

http://www.drugs.com/mtm/clofibrate.html

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