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药品详细

Fenofibrate (非诺贝特 )

化学结构式图
中文名
非诺贝特
英文名
Fenofibrate
分子式
Not Available
化学名
propan-2-yl 2-{4-[(4-chlorophenyl)carbonyl]phenoxy}-2-methylpropanoate
分子量
Average: 360.831
Monoisotopic: 360.112836867
CAS号
49562-28-9
ATC分类
C10A 未知
药物类型
small molecule
阶段
商品名
Ankebin;Antara;Elasterate;Elasterin;Fenobrate;Fenogal;Fenotard;Lipanthyl;Lipantil;Lipidex;Lipidil;Lipidil Micro;Lipidil Supra;Lipifen;Lipirex;Lipoclar;Lipofene;Liposit;Lipsin;Lofibra;Luxacor;Nolipax;Procetofen;Proctofene;Protolipan;Secalip;Sedufen;Tricor;Triglide;Trilipix (Abbott Laboratories);
同义名
Fenofibrato [INN-Spanish];Fenofibratum [INN-Latin];Fenofibric acid;Finofibrate;FNF;
基本介绍

An antilipemic agent which reduces both cholesterol and triglycerides in the blood. [PubChem]

生产厂家
  • Abbott laboratories
  • Abbott laboratories pharmaceutical products div
  • Ar holding co inc
  • Cipher pharmaceuticals inc
  • Impax laboratories inc
  • Lupin atlantis holdings sa
  • Mylan pharmaceuticals inc
  • Ranbaxy laboratories ltd
  • Shionogi pharma inc
  • Skyepharma ag
  • Teva pharmaceuticals usa inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Wysocki J, Belowski D, Kalina M, Kochanski L, Okopien B, Kalina Z: Effects of micronized fenofibrate on insulin resistance in patients with metabolic syndrome. Int J Clin Pharmacol Ther. 2004 Apr;42(4):212-7. Pubmed
  2. Keech A, Simes RJ, Barter P, Best J, Scott R, Taskinen MR, Forder P, Pillai A, Davis T, Glasziou P, Drury P, Kesaniemi YA, Sullivan D, Hunt D, Colman P, d’Emden M, Whiting M, Ehnholm C, Laakso M: Effects of long-term fenofibrate therapy on cardiovascular events in 9795 people with type 2 diabetes mellitus (the FIELD study): randomised controlled trial. Lancet. 2005 Nov 26;366(9500):1849-61. Pubmed
剂型
Form Route Strength
Capsule Oral
Tablet Oral
规格
Unit description Cost Unit
Triglide 160 mg tablet 6.39 USD tablet
Fenoglide 120 mg tablet 5.17 USD tablet
Antara 130 mg capsule 5.13 USD capsule
Tricor 145 mg tablet 4.69 USD tablet
Lipofen 150 mg capsule 3.55 USD capsule
Lofibra 200 mg capsule 3.25 USD capsule
Lofibra 160 mg tablet 3.11 USD tablet
Fenofibrate Micronized 200 mg capsule 2.77 USD capsule
Fenofibrate 160 mg 2.47 USD tablet
Fenofibrate 160 mg tablet 2.38 USD tablet
Lofibra 134 mg capsule 2.03 USD capsule
Antara 43 mg capsule 1.8 USD capsule
Fenofibrate Micronized 134 mg capsule 1.79 USD capsule
Fenoglide 40 mg tablet 1.72 USD tablet
Tricor 48 mg tablet 1.63 USD tablet
Triglide 50 mg tablet 1.49 USD tablet
Lipidil Supra 160 mg Tablet 1.4 USD tablet
Lofibra 67 mg capsule 1.26 USD capsule
Lipidil Micro 200 mg Capsule 1.23 USD capsule
Lipidil Supra 100 mg Tablet 1.22 USD tablet
Apo-Feno-Micro 200 mg Capsule 1.14 USD capsule
Fenofibrate Micro 200 mg Capsule 1.14 USD capsule
Mylan-Fenofibrate Micro 200 mg Capsule 1.14 USD capsule
Novo-Fenofibrate Micronized 200 mg Capsule 1.14 USD capsule
Pms-Fenofibrate Micro 200 mg Capsule 1.14 USD capsule
Ratio-Fenofibrate Mc 200 mg Capsule 1.14 USD capsule
Fenofibrate Micronized 67 mg capsule 1.0 USD capsule
Lofibra 54 mg tablet 0.99 USD tablet
Fenofibrate 54 mg tablet 0.81 USD tablet
Apo-Feno-Super 160 mg Tablet 0.79 USD tablet
Novo-Fenofibrate-S 160 mg Tablet 0.79 USD tablet
Sandoz Fenofibrate S 160 mg Tablet 0.79 USD tablet
Apo-Feno-Super 100 mg Tablet 0.68 USD tablet
Novo-Fenofibrate-S 100 mg Tablet 0.68 USD tablet
Sandoz Fenofibrate S 100 mg Tablet 0.68 USD tablet
Apo-Fenofibrate 100 mg Capsule 0.64 USD capsule
Apo-Feno-Micro 67 mg Capsule 0.45 USD capsule
Novo-Fenofibrate Micronized 67 mg Capsule 0.45 USD capsule
化合物类型
Type small molecule
Classes
  • Benzophenones
Substructures
  • Carboxylic Acids and Derivatives
  • Acetates
  • Phenols and Derivatives
  • Phenoxyacetates
  • Short-chain Hydroxy Acids
  • Ethers
  • Benzene and Derivatives
  • Aryl Halides
  • Halobenzenes
  • Aromatic compounds
  • Anisoles
  • Benzophenones
  • Benzoyl Derivatives
  • Phenyl Esters
  • Ketones
适应症
hyperlipidemi 高血脂;
药理
Indication 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)
Pharmacodynamics 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.
Mechanism of action 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.
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)
Metabolism
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]
Toxicity LD50=1600 mg/kg (Oral, in mice); Investigated as a teratogen and reproductive hazard.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Melting point 80.5 oC
Experimental Properties
Property Value Source
water solubility 0.25mg/ml at 25 oC PhysProp
logP 5.3 PhysProp
Predicted Properties
Property Value Source
water solubility 7.07e-04 g/l ALOGPS
logP 4.86 ALOGPS
logP 5.28 ChemAxon Molconvert
logS -5.71 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 3 ChemAxon Molconvert
hydrogen donor count 0 ChemAxon Molconvert
polar surface area 52.60 ChemAxon Molconvert
rotatable bond count 7 ChemAxon Molconvert
refractivity 97.13 ChemAxon Molconvert
polarizability 38.15 ChemAxon Molconvert
药物相互作用
Drug Interaction
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
Dicumarol Fenofibrate may increase the anticoagulant effect of dicumarol.
Fluvastatin Increased risk of myopathy/rhabdomyolysis
Lovastatin Increased risk of myopathy/rhabdomyolysis
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.
食物相互作用
  • Increased absorption- take with meals.

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