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药品详细

Salbutamol(沙丁胺醇)

化学结构式图
中文名
沙丁胺醇
英文名
Salbutamol
分子式
C13H21NO3
化学名
4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol
分子量
Average: 239.3107
Monoisotopic: 239.152143543
CAS号
18559-94-9
ATC分类
R03C 未知;R03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Salbutamol is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma and COPD. It is 29 times more selective for beta2 receptors than beta1 receptors giving it higher specificity for pulmonary beta receptors versus beta1-adrenergic receptors located in the heart. Salbutamol is formulated as a racemic mixture of the R- and S-isomers. The R-isomer has 150 times greater affinity for the beta2-receptor than the S-isomer and the S-isomer has been associated with toxicity. This lead to the development of levalbuterol, the single R-isomer of salbutamol. However, the high cost of levalbuterol compared to salbutamol has deterred wide-spread use of this enantiomerically pure version of the drug. Salbutamol is generally used for acute episodes of bronchospasm caused by bronchial asthma, chronic bronchitis and other chronic bronchopulmonary disorders such as chronic obstructive pulmonary disorder (COPD). It is also used prophylactically for exercise-induced asthma.

生产厂家
  • 3m pharmaceuticals inc
  • Actavis mid atlantic llc
  • American therapeutics inc
  • Amneal pharmaceuticals
  • Apotex inc
  • Apotex inc richmond hill
  • Armstrong pharmaceuticals inc
  • Bausch and lomb inc
  • Breath ltd
  • Cobalt laboratories inc
  • Copley pharmaceutical inc
  • Dava pharmaceuticals inc
  • Dey lp
  • Genpharm inc
  • Glaxosmithkline
  • Hi tech pharmacal co inc
  • Holopack international
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Landela pharmaceutical
  • Mova pharmaceuticals corp
  • Muro pharmaceutical inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Nephron corp
  • Nephron pharmaceuticals corp
  • Novex pharma
  • Pliva inc
  • Roxane laboratories inc
  • Sandoz inc
  • Schering corp sub schering plough corp
  • Sepracor inc
  • Teva global respiratory research llc
  • Teva parenteral medicines inc
  • Teva Pharmaceuticals
  • Teva pharmaceuticals usa inc
  • Ucb inc
  • Vintage pharmaceuticals llc
  • Vistapharm inc
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
  • Wockhardt eu operations (swiss) ag
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Benzyl Alcohols and Derivatives
  • Phenols and Derivatives
  • Phenethylamines
Substructures
  • Hydroxy Compounds
  • Benzyl Alcohols and Derivatives
  • Aliphatic and Aryl Amines
  • Phenols and Derivatives
  • Benzene and Derivatives
  • Alcohols and Polyols
  • Amino Alcohols
  • Phenethylamines
  • Aromatic compounds
  • Phenyl Esters
适应症
药理
Indication For symptomatic relief and prevention of bronchospasm due to bronchial asthma, chronic bronchitis, and other chronic bronchopulmonary disorders such as COPD.
Pharmacodynamics Salbutamol (INN) or albuterol (USAN), a moderately selective beta(2)-receptor agonist similar in structure to terbutaline, is widely used as a bronchodilator to manage asthma and other chronic obstructive airway diseases. The R-isomer, levalbuterol, is responsible for bronchodilation while the S-isomer increases bronchial reactivity. The R-enantiomer is sold in its pure form as Levalbuterol. The manufacturer of levalbuterol, Sepracor, has implied (although not directly claimed) that the presence of only the R-enantiomer produces fewer side-effects.
Mechanism of action Salbutamol is a beta(2)-adrenergic agonist and thus it stimulates beta(2)-adrenergic receptors. Binding of albuterol to beta(2)-receptors in the lungs results in relaxation of bronchial smooth muscles. It is believed that salbutamol increases cAMP production by activating adenylate cyclase, and the actions of salbutamol are mediated by cAMP. Increased intracellular cyclic AMP increases the activity of cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular calcium concentrations. A lowered intracellular calcium concentration leads to a smooth muscle relaxation and bronchodilation. In addition to bronchodilation, salbutamol inhibits the release of bronchoconstricting agents from mast cells, inhibits microvascular leakage, and enhances mucociliary clearance.
Absorption Systemic absorption is rapid following aerosol administration.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Hydrolyzed by esterases in tissue and blood to the active compound colterol. The drug is also conjugatively metabolized to salbutamol 4'-O-sulfate.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Salbutamol
    		Salbutamol 4-O-sulfate Details
    Route of elimination Approximately 72% of the inhaled dose is excreted in the urine within 24 hours, 28% as unchanged drug and 44% as metabolite.
    Half life 1.6 hours
    Clearance Not Available
    Toxicity LD50=1100 mg/kg (orally in mice)
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 151 °C PhysProp
    water solubility 1.41E+004 mg/L YALKOWSKY,SH & HE,Y (2003)
    logP 1.4 Not Available
    logS -1.22 ADME Research, USCD
    pKa 10.3 Not Available
    Predicted Properties
    Property Value Source
    water solubility 2.15e+00 g/l ALOGPS
    logP 0.44 ALOGPS
    logP 0.34 ChemAxon
    logS -2 ALOGPS
    pKa (strongest acidic) 10.12 ChemAxon
    pKa (strongest basic) 9.4 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 4 ChemAxon
    polar surface area 72.72 ChemAxon
    rotatable bond count 5 ChemAxon
    refractivity 67.87 ChemAxon
    polarizability 26.86 ChemAxon
    药物相互作用
    Drug Interaction
    Amitriptyline The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of salbutamol.
    Amoxapine The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of salbutamol.
    Atenolol Antagonism
    Bisoprolol Antagonism
    Carvedilol Antagonism
    Clomipramine The tricyclic antidepressant, clomipramine, increases the sympathomimetic effect of salbutamol.
    Desipramine The tricyclic antidepressant, desipramine, increases the sympathomimetic effect of salbutamol.
    Doxepin The tricyclic antidepressant, doxepin, increases the sympathomimetic effect of salbutamol.
    Esmolol Antagonism
    Imipramine The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of salbutamol.
    Isocarboxazid Increased arterial pressure
    Labetalol Antagonism
    Linezolid Possible increase of arterial pressure
    Methyldopa Increased arterial pressure
    Metoprolol Antagonism
    Midodrine Increased arterial pressure
    Moclobemide Moclobemide increases the sympathomimetic effect of salbutamol.
    Nadolol Antagonism
    Nortriptyline The tricyclic antidepressant, nortriptyline, increases the sympathomimetic effect of salbutamol.
    Oxprenolol Antagonism
    Phenelzine Increased arterial pressure
    Pindolol Antagonism
    Propranolol Antagonism
    Rasagiline Increased arterial pressure
    Reserpine Increased arterial pressure
    Timolol Antagonism
    食物相互作用
    Not Available

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