Tìm theo
Fenofibrate
Các tên gọi khác (12 ) :
  • 2-(4-(4-Chlorobenzoyl)phenoxy)-2-methylpropanoic acid 1-methylethyl ester
  • Fenofibrate
  • Fenofibrato
  • Fenofibratum
  • Fenofibric acid
  • Finofibrate
  • FNF
  • Isopropyl (4'-(P-chlorobenzoyl)-2-phenoxy-2-methyl)propionate
  • Isopropyl 2-(4-(4-chlorobenzoyl)phenoxy)-2-methylpropionate
  • Lipantil (tn)
  • Procetofen
  • Tricor (tn)
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 49562-28-9
ATC: C10AB05
ĐG : Abbott Laboratories Ltd. , http://www.abbott.com
CTHH: C20H21ClO4
PTK: 360.831
An antilipemic agent which reduces both cholesterol and triglycerides in the blood. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C20H21ClO4
Phân tử khối
360.831
Monoisotopic mass
360.112836867
InChI
InChI=1S/C20H21ClO4/c1-13(2)24-19(23)20(3,4)25-17-11-7-15(8-12-17)18(22)14-5-9-16(21)10-6-14/h5-13H,1-4H3
InChI Key
InChIKey=YMTINGFKWWXKFG-UHFFFAOYSA-N
IUPAC Name
propan-2-yl 2-{4-[(4-chlorophenyl)carbonyl]phenoxy}-2-methylpropanoate
Traditional IUPAC Name
fenofibrate
SMILES
CC(C)OC(=O)C(C)(C)OC1=CC=C(C=C1)C(=O)C1=CC=C(Cl)C=C1
Độ tan chảy
80.5 °C
Độ hòa tan
0.25mg/ml at 25 °C
logP
5.3
logS
-5.7
pKa (Strongest Basic)
-4.9
PSA
52.6 Å2
Refractivity
97.13 m3·mol-1
Polarizability
38.15 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Ghose Filter
true
Dược Lực Học : Fenofibrate is a lipid regulating agent indicated as adjunctive therapy to diet to reduce elevated LDL-C, Total-C,Triglycerides and Apo B, and to increase HDL-C in adult patients with primary hypercholesterolemia or mixed dyslipidemia (Fredrickson Types IIa and IIb). Fenofibrate is also indicated as adjunctive therapy to diet for treatment of adult patients with hypertriglyceridemia (Fredrickson Types IV and V hyperlipidemia). Fenofibric acid, the active metabolite of Fenofibrate, produces reductions in total cholesterol, LDL cholesterol, apolipoprotein B, total triglycerides and triglyceride rich lipoprotein (VLDL) in treated patients. In addition, treatment with fenofibrate results in increases in high density lipoprotein (HDL) and apoproteins apoAI and apoAII.
Cơ Chế Tác Dụng : An antilipemic agent which reduces both cholesterol and triglycerides in the blood. [PubChem] Fenofibrate exerts its therapeutic effects through activation of peroxisome proliferator activated receptor a (PPARa). This increases lipolysis and elimination of triglyceride-rich particles from plasma by activating lipoprotein lipase and reducing production of apoprotein C-III. The resulting fall in triglycerides produces an alteration in the size and composition of LDL from small, dense particles, to large buoyant particles. These larger particles have a greater affinity for cholesterol receptors and are catabolized rapidly.
Dược Động Học :
▧ Absorption :
Fenofibrate is well absorbed from the gastrointestinal tract. After absorption, fenofibrate is mainly excreted in the urine in the form of metabolites, primarily fenofibric acid and fenofibric acid glucuronide
▧ Volume of Distribution :
* 95 L [moderate renal impairment (creatinine clearance of 50 to 90 mL/min)] * 30 L [healthy adults]
▧ Protein binding :
~99% (Serum protein binding)
▧ Route of Elimination :
Fenofibric acid is primarily conjugated with glucuronic acid and then excreted in urine. Following oral administration in healthy volunteers, approximately 60% of a single dose of radiolabelled fenofibrate appeared in urine, primarily as fenofibric acid and its glucuronate conjugate and 25% was excreted in the feces.
▧ Half Life :
20 hours
▧ Clearance :
* 1.2 L/h [Eldery]
Độc Tính : LD50=1600 mg/kg (Oral, in mice); Investigated as a teratogen and reproductive hazard.
Chỉ Định : For use as adjunctive therapy to diet to reduce elevated LDL-C, Total-C,Triglycerides and Apo B, and to increase HDL-C in adult patients with primary hypercholesterolemia or mixed dyslipidemia (Fredrickson Types IIa and IIb)
Tương Tác Thuốc :
  • Acenocoumarol Fenofibrate may increase the anticoagulant effect of acenocoumarol.
  • Anisindione Fenofibrate may increase the anticoagulant effect of anisindione.
  • Atorvastatin Increased risk of myopathy/rhabdomyolysis
  • Cerivastatin Increased risk of myopathy/rhabdomyolysis
  • Dicoumarol Fenofibrate may increase the anticoagulant effect of dicumarol.
  • Fluvastatin Increased risk of myopathy/rhabdomyolysis
  • Insulin Lispro Concomitant therapy with drugs that may increase the blood-glucose-lowering effect of insulin lispro and thus the chance of hypoglycemia should be monitored closely.
  • Lovastatin Increased risk of myopathy/rhabdomyolysis
  • Pitavastatin Increased incidence of adverse drug reactions (ie. rhabdomyolysis) of both fenofibrate and pitavastatin via pharmacodynamic synergism. Use alternative therapy.
  • Pravastatin Increased risk of myopathy/rhabdomyolysis
  • Rosuvastatin May cause additive myotoxicity. Monitor for symptoms of muscle toxicity during concomitant therapy.
  • Simvastatin Increased risk of myopathy/rhabdomyolysis
  • Ursodeoxycholic acid The fibric acid derivative decreases the effect of ursodiol
  • Warfarin Fenofibrate may increase the anticoagulant effect of warfarin. Monitor prothrombin time and therapeutic and adverse effects of warfarin if fenofibrate is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Capsule - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Sản phẩm biệt dược : Antara
  • Công ty : SMB Laboratories
    Sản phẩm biệt dược : Fenogal
  • Công ty :
    Sản phẩm biệt dược : Fenoglide
  • Công ty :
    Sản phẩm biệt dược : FIBRICOR
  • Công ty : Abbott
    Sản phẩm biệt dược : Lipanthyl
  • Công ty : lbirn
    Sản phẩm biệt dược : Lipidil
  • Công ty :
    Sản phẩm biệt dược : Lipofen
  • Công ty : Teva
    Sản phẩm biệt dược : Lofibra
  • Công ty : Abbott
    Sản phẩm biệt dược : TriCor
  • Công ty :
    Sản phẩm biệt dược : Triglide
  • Công ty :
    Sản phẩm biệt dược : Trilipix
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01039
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3339
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507371
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07586
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00565
ChemSpider
http://www.chemspider.com/Chemical-Structure.3222.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-7100-77
PharmGKB
http://www.pharmgkb.org/drug/PA449594
Wikipedia
http://en.wikipedia.org/wiki/Fenofibrate
RxList
http://www.rxlist.com/cgi/generic3/fenofibrate.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/cx1550.shtml
Drugs.com
http://www.drugs.com/fenofibrate.html
... loading
... loading