Tìm theo
Salbutamol
Các tên gọi khác (4 ) :
  • Albuterol
  • Levalbuterol
  • Proventil
  • Salbutamol
Thuốc tác dụng trên đường hô hấp
Thuốc Gốc
Small Molecule
CAS: 18559-94-9
ATC: R03CC02, R03AC02
ĐG : 3M Health Care , http://www.3m.com
CTHH: C13H21NO3
PTK: 239.3107
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C13H21NO3
Phân tử khối
239.3107
Monoisotopic mass
239.152143543
InChI
InChI=1S/C13H21NO3/c1-13(2,3)14-7-12(17)9-4-5-11(16)10(6-9)8-15/h4-6,12,14-17H,7-8H2,1-3H3
InChI Key
InChIKey=NDAUXUAQIAJITI-UHFFFAOYSA-N
IUPAC Name
4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol
Traditional IUPAC Name
albuterol
SMILES
CC(C)(C)NCC(O)C1=CC(CO)=C(O)C=C1
Độ tan chảy
147-149
Độ hòa tan
1.41E+004 mg/L
logP
1.4
logS
-1.22
pKa (strongest acidic)
10.12
pKa (Strongest Basic)
9.4
PSA
72.72 Å2
Refractivity
67.87 m3·mol-1
Polarizability
26.86 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
4
H Bond Donor Count
4
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
10.3
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. 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.
Dược Động Học :
▧ Absorption :
Systemic absorption is rapid following aerosol administration.
▧ Metabolism :
Hydrolyzed by esterases in tissue and blood to the active compound colterol. The drug is also conjugatively metabolized to salbutamol 4'-O-sulfate.
▧ 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
Độc Tính : LD50=1100 mg/kg (orally in mice)
Chỉ Định : For symptomatic relief and prevention of bronchospasm due to bronchial asthma, chronic bronchitis, and other chronic bronchopulmonary disorders such as COPD.
Tương Tác Thuốc :
  • 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
Liều Lượng & Cách Dùng : Aerosol, metered - Respiratory (inhalation)
Liquid - Oral
Powder - Respiratory (inhalation)
Solution - Intramuscular
Solution - Intravenous
Solution - Oral
Solution - Respiratory (inhalation)
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : AccuNeb
  • Công ty :
    Sản phẩm biệt dược : Aerolin
  • Công ty :
    Sản phẩm biệt dược : Airomir
  • Công ty :
    Sản phẩm biệt dược : Asmol
  • Công ty :
    Sản phẩm biệt dược : Asthalin
  • Công ty :
    Sản phẩm biệt dược : Asthavent
  • Công ty : Teva
    Sản phẩm biệt dược : ProAir
  • Công ty :
    Sản phẩm biệt dược : PROAIRHFA
  • Công ty :
    Sản phẩm biệt dược : Proventil
  • Công ty :
    Sản phẩm biệt dược : Salamol
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Ventilan
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Ventolin
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Ventoline
  • Công ty :
    Sản phẩm biệt dược : VENTOLINHFA
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Ventorlin
  • Công ty :
    Sản phẩm biệt dược : VoSpire
  • Công ty :
    Sản phẩm biệt dược : Xopenex
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01001
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2083
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505312
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02147
ChemSpider
http://www.chemspider.com/Chemical-Structure.1999.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25769
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0085-0614-02
PharmGKB
http://www.pharmgkb.org/drug/PA448068
Wikipedia
http://en.wikipedia.org/wiki/Salbutamol
RxList
http://www.rxlist.com/cgi/generic/duoneb.htm
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