ゲムフィブロジル 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
効能
脂質異常症治療薬, トリグリセリド合成阻害薬, ペルオキシソーム増殖因子活性化受容体(PPAR)α作動薬
説明
Gemfibrozil is a peroxisome proliferator-activated receptor α (PPARα) and PPARγ agonist (EC
50s = 193.3 and 147.8 μM, respectively, in transactivation assays).
In vivo, gemfibrozil (50 mg/kg, p.o.) reduces serum total cholesterol, triglyceride, and LDL levels in a rat model of high-cholesterol diet-induced hyperlipidemia. Gemfibrozil (100 mg/kg per day) reduces atherosclerotic plaque area, superoxide production, and expression of the genes encoding the NF-κB subunit p65 and chemokine (C-C) motif ligand 2 (CCL2) in
ApoE-/- mice. Formulations containing gemfibrozil have been used in the treatment of high cholesterol.
化学的特性
White Crystalline Powder
使用
Gemfibrozil has been used to to study its effects on cell cycle progression in yeast. It has been used to study the effects of fibrates on cell proliferation and gene expression in human cell lines.
世界保健機関（WHO）
Gemfibrozil, an antihyperlipidaemic derivative of clofibrate, was
introduced in the early 1980's. It is registered in several countries for the treatment
of hyperlipidaemia unresponsive to dietary measures. (See also the WHO comment
for clofibrate).
一般的な説明
Gemfibrozil, 5-(2,5-dimethylphenoxy)-2,2-dimethylpentanoic acid (Lopid), is a congener of clofibratethat was used first in the treatment of hyperlipoproteinemia inthe mid-1970s. Its mechanism of action and use are similar tothose of clofibrate. Gemfibrozil reduces plasma levels ofVLDL triglycerides and stimulates clearance of VLDL fromplasma. The drug has little effect on cholesterol plasma levelsbut does cause an increase of HDL.
Gemfibrozil is absorbed quickly from the gut and excretedunchanged in the urine. The drug has a plasma half-life of1.5 hours, but reduction of plasma VLDL concentration takesbetween 2 and 5 days to become evident. The peak effect of its hypolipidemic action may take up to 4 weeks to becomemanifest.
作用機序
From the chemical point of view, gemfibrozil is somewhat related to clofibrate and has
analogous pharmacological use. The primary action of gemibrozil as well as clofibrate
consists of a significant reduction in the level of very low-density proteins in the plasma
and an increase in high-density protein formation.
ゲムフィブロジル 上流と下流の製品情報
原材料
準備製品