Tìm theo
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
5
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
1
Bioavailability
1
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 (Sf 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
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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