用户名： 密   码：
注册 | 忘记密码？
药品详细

Bezafibrate(苯扎贝特)

化学结构式图
中文名
苯扎贝特
英文名
Bezafibrate
分子式
C19H20ClNO4
化学名
2-(4-{2-[(4-chlorophenyl)formamido]ethyl}phenoxy)-2-methylpropanoic acid
分子量
Average: 361.819
Monoisotopic: 361.10808584
CAS号
41859-67-0
ATC分类
C10A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Antilipemic agent that lowers cholesterol and triglycerides. It decreases low density lipoproteins and increases high density lipoproteins. [PubChem]

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Link
    2. : Secondary prevention by raising HDL cholesterol and reducing triglycerides in patients with coronary artery disease: the Bezafibrate Infarction Prevention (BIP) study. Circulation. 2000 Jul 4;102(1):21-7. Pubmed
    3. Tenenbaum A, Motro M, Fisman EZ, Tanne D, Boyko V, Behar S: Bezafibrate for the secondary prevention of myocardial infarction in patients with metabolic syndrome. Arch Intern Med. 2005 May 23;165(10):1154-60. Pubmed
    4. Tenenbaum A, Motro M, Fisman EZ, Schwammenthal E, Adler Y, Goldenberg I, Leor J, Boyko V, Mandelzweig L, Behar S: Peroxisome proliferator-activated receptor ligand bezafibrate for prevention of type 2 diabetes mellitus in patients with coronary artery disease. Circulation. 2004 May 11;109(18):2197-202. Epub 2004 May 3. Pubmed
    5. Tenenbaum A, Fisman EZ, Boyko V, Benderly M, Tanne D, Haim M, Matas Z, Motro M, Behar S: Attenuation of progression of insulin resistance in patients with coronary artery disease by bezafibrate. Arch Intern Med. 2006 Apr 10;166(7):737-41. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Phenoxyacetates
    Substructures
    • Hydroxy Compounds
    • Acetates
    • Phenols and Derivatives
    • Amino Ketones
    • Phenoxyacetates
    • Short-chain Hydroxy Acids
    • Ethers
    • Benzene and Derivatives
    • Aryl Halides
    • Carboxylic Acids and Derivatives
    • Halobenzenes
    • Phenethylamines
    • Aromatic compounds
    • Anisoles
    • Carboxamides and Derivatives
    • Benzoyl Derivatives
    • Phenyl Esters
    • Benzamides
    适应症
    药理
    Indication For the treatment of primary hyperlipidaemia types IIa, IIb, III, IV and V (Fredrickson classification) corresponding to groups I, II and III of the European Atherosclerosis Society guidelines - when diet alone or improvements in lifestyle such as increased exercise or weight reduction do not lead to an adequate response. Also for the treatment of secondary hyperlipidaemias, e.g. severe hypertriglyceridemias, when sufficient improvement does not occur after correction of the underlying disorder (e.g. diabetes mellitus).
    Pharmacodynamics Bezafibrate is an antilipemic agent that lowers cholesterol and triglycerides. It decreases low density lipoproteins and increases high density lipoproteins. Bezafibrate lowers elevated blood lipids (triglycerides and cholesterol). Elevated VLDL and LDL are reduced by treatment with bezafibrate, whilst HDL-levels are increased. The activity of triglyceride lipases (lipoprotein lipase and hepatic lipoproteinlipase) involved in the catabolism of triglyceride-rich lipoproteins is increased by bezafibrate. In the course of the intensified degradation of triglyceride-rich lipoproteins (chylomicrons, VLDL) precursors for the formation of HDL are formed which explains an increase in HDL. Furthermore, cholesterol biosynthesis is reduced by bezafibrate, which is accompanied by a stimulation of the LDL-receptor-mediated lipoprotein catabolism. Elevated fibrinogen appears to be an important risk-factor, alongside the lipids, smoking and hypertension, in the development of atheroma. Fibrinogen plays an important role in viscosity, and therefore blood flow, and also appears to play an important role in thrombus development and lysability. Bezafibrate exerts an effect on thrombogenic factors. A significant decrease in elevated plasma fibrinogen levels can be achieved. This may lead, amongst other things, to a reduction in both blood and plasma viscosity. Inhibition of platelet aggregation has also been observed. A reduction in blood glucose concentration due to an increase in glucose tolerance has been reported in diabetic patients. In the same patients, the concentration of fasting and postprandial free fatty acids was reduced by bezafibrate.
    Mechanism of action Like the other fibrates, bezafibrate is an agonist of PPARα; some studies suggest it may have some activity on PPARγ and PPARδ as well.
    Absorption Bezafibrate is almost completely absorbed after oral administration. The relative bioavailability of bezafibrate retard compared to the standard form is about 70%.
    Volume of distribution Not Available
    Protein binding 94-96% of bezafibrate is bound to protein in human serum.
    Metabolism
    Hepatic.
    Route of elimination Not Available
    Half life 1-2 hours
    Clearance Not Available
    Toxicity Not Available
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 186 °C PhysProp
    Predicted Properties
    Property Value Source
    water solubility 1.55e-03 g/l ALOGPS
    logP 3.97 ALOGPS
    logP 3.99 ChemAxon
    logS -5.4 ALOGPS
    pKa (strongest acidic) 3.83 ChemAxon
    pKa (strongest basic) -0.84 ChemAxon
    physiological charge -1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 75.63 ChemAxon
    rotatable bond count 7 ChemAxon
    refractivity 95.96 ChemAxon
    polarizability 37.53 ChemAxon
    药物相互作用
    Drug Interaction
    Atorvastatin Increased risk of myopathy/rhabdomyolysis
    Cerivastatin Increased risk of myopathy/rhabdomyolysis
    Cholestyramine Bile acid sequestrants like cholestyramine may decrease the absorption of fibric acid derivatives like bezafibrate. Therapy modification should be considered. If concomitant therapy is used, separate doses by at least 2 hours to minimize this interaction. Fenofibric acid labeling recommends administration one hour prior to or 4-6 hours after a bile acid sequestrant.
    Conivaptan Conivaptan may increase the serum concentration of CYP3A4 substrates like bezafibrates. Consider therapy modification. Conivaptan may increase the serum concentration of CYP3A4 substrates.
    Cyclosporine Cyclosporine may enhance the nephrotoxic effect of fibric acid derivatives like bezafibrate. Fibric acid derivatives may decrease the serum concentration of cyclosporine. Extra monitoring of renal function and cyclosporine concentrations will likely be required. Adjustment of cyclosporine dose may be necessary.
    Fluvastatin Increased risk of myopathy/rhabdomyolysis
    Isocarboxazid MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like isocarboxazid.
    Linezolid MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like linezolid.
    Lovastatin Increased risk of myopathy/rhabdomyolysis
    Moclobemide MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like moclobemide.
    Phenelzine MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like phenelzine.
    Pravastatin Increased risk of myopathy/rhabdomyolysis
    Procarbazine MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like procarbazine.
    Rasagiline MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) rasagiline.
    Selegiline MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like selegiline.
    Tranylcypromine MAO Inhibitors may enhance the adverse/toxic effect of Bezafibrate. Avoid concomitant use of bezafibrate with monoamine oxidase inhibitors (MAOIs) like tranylcypromine.
    Warfarin Bezafibrate may increase the anticoagulant effect of warfarin. Monitor prothrombin time and therapeutic and adverse effects of warfarin if bezafibrate is initiated, discontinued or dose changed.
    食物相互作用
    Not Available

    返回 | 收藏