物质信息
ID:915
名称和标识
商标名
AnkebinAntaraFenobrateFenogalLipanthylLipantilSecalipElasterinLipositLofibraLuxacorProctofeneFenotardLipidexLipidil MicroLipofeneNolipaxTricorTrilipixElasterateTriglideLipirexLipoclarLipsinLipidilLipidil SupraLipifenProcetofenProtolipanSedufen
别名
Fenofibratum [INN-Latin]FenofibrateFenofibrato [INN-Spanish]Fenofibric acidFinofibrateFNF
IUPAC标准名
propan-2-yl 2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoate
IUPAC传统名
isopropyl 2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoate
化合物性质
理化性质
溶解度
0.25mg/ml at 25 oC
疏水性(logP)
5.3
描述信息
Drug Groups
approved
Description
An antilipemic agent which reduces both cholesterol and triglycerides in the blood. [PubChem]
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)
Pharmacology
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.
Toxicity
LD50=1600 mg/kg (Oral, in mice); Investigated as a teratogen and reproductive hazard.
Affected Organisms
Humans and other mammals
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
Half Life
20 hours
Protein Binding
~99% (Serum protein binding)
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.
Distribution
* 95 L [moderate renal impairment (creatinine clearance of 50 to 90 mL/min)]
* 30 L [healthy adults]
* 30 L [healthy adults]
Clearance
* 1.2 L/h [Eldery]
References
•
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]
•
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]
External Links
分子图谱
暂无数据
点击上传数据
参考文献
• 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
• 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