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药品详细

Bevantolol(贝凡洛尔)

化学结构式图
中文名
贝凡洛尔
英文名
Bevantolol
分子式
C20H27NO4
化学名
[2-(3,4-dimethoxyphenyl)ethyl][2-hydroxy-3-(3-methylphenoxy)propyl]amine
分子量
Average: 345.4327
Monoisotopic: 345.194008357
CAS号
59170-23-9
ATC分类
C07A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Bevantolol is a beta-1 adrenoceptor antagonist that has been shown to be as effective as other beta blockers for the treatment of angina pectoris and hypertension. Mechanism of Action Animal experiments confirm both agonist and antagonist effects on alpha-receptors, in addition to antagonist activity at beta-1 receptors.

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    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Vaughan Williams EM: Bevantolol: a beta-1 adrenoceptor antagonist with unique additional actions. J Clin Pharmacol. 1987 Jul;27(7):450-60. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Catecholamines and Derivatives
    Substructures
    • Hydroxy Compounds
    • Aliphatic and Aryl Amines
    • Phenols and Derivatives
    • Ethers
    • Benzene and Derivatives
    • Amino Alcohols
    • Catechols
    • Phenethylamines
    • Aromatic compounds
    • Anisoles
    • Alcohols and Polyols
    • Phenyl Esters
    • Catecholamines and Derivatives
    适应症
    药理
    Indication For the treatment of angina pectoris and hypertension.
    Pharmacodynamics Bevantolol is a beta-1 adrenoceptor antagonist that has been shown to be as effective as other beta blockers for the treatment of angina pectoris and hypertension.
    Mechanism of action Animal experiments confirm both agonist and antagonist effects on alpha-receptors, in addition to antagonist activity at beta-1 receptors. By binding and antagonizing beta-1 receptors Bevantolol inhibits the normal normal epinephrine-mediated sympathetic actions such as increased heart rate. This has the effect of decreasing preload and blood pressure.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    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 137-138 °C PhysProp
    logP 3.00 HANSCH,C ET AL. (1995)
    Predicted Properties
    Property Value Source
    water solubility 1.37e-02 g/l ALOGPS
    logP 2.83 ALOGPS
    logP 3.03 ChemAxon
    logS -4.4 ALOGPS
    pKa (strongest acidic) 14.09 ChemAxon
    pKa (strongest basic) 9.31 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 5 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 59.95 ChemAxon
    rotatable bond count 10 ChemAxon
    refractivity 98.54 ChemAxon
    polarizability 39.75 ChemAxon
    药物相互作用
    Drug Interaction
    Chlorpropamide The beta-blocker, bevantolol, may decrease symptoms of hypoglycemia.
    Clonidine Increased hypertension when clonidine stopped
    Dihydroergotamine Ischemia with risk of gangrene
    Disopyramide The beta-blocker, bevantolol, may increase the toxicity of disopyramide.
    Epinephrine Hypertension, then bradycardia
    Ergotamine Ischemia with risk of gangrene
    Fenoterol Antagonism
    Formoterol Antagonism
    Gliclazide The beta-blocker, bevantolol, may decrease symptoms of hypoglycemia.
    Glyburide The beta-blocker, bevantolol, may decrease symptoms of hypoglycemia.
    Ibuprofen Risk of inhibition of renal prostaglandins
    Indomethacin Risk of inhibition of renal prostaglandins
    Insulin Glargine The beta-blocker, bevantolol, may decrease symptoms of hypoglycemia.
    Methysergide Ischemia with risk of gangrene
    Orciprenaline Antagonism
    Pipobroman Antagonism
    Piroxicam Risk of inhibition of renal prostaglandins
    Prazosin Risk of hypotension at the beginning of therapy
    Repaglinide The beta-blocker, bevantolol, may decrease symptoms of hypoglycemia.
    Terbutaline Antagonism
    食物相互作用
    Not Available

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