Tìm theo
Pirbuterol
Các tên gọi khác (3) :
  • Maxair autohaler
  • Pirbuterol
  • Pirbuterolum
adrenergic beta 2 receptor agonists, bronchodilator agents, cardiotonic agents
Thuốc Gốc
Small Molecule
CAS: 38677-81-5
ATC: R03AC08, R03CC07
ĐG : 3M Health Care , http://www.3m.com
CTHH: C12H20N2O3
PTK: 240.2988
Pirbuterol is a beta-2 adrenergic bronchodilator. In vitro studies and in vivo pharmacologic studies have demonstrated that pirbuterol has a preferential effect on beta-2 Adrenergic receptors compared with isoproterenol. While it is recognized that beta-2 adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta-2 receptors in the human heart, existing in a concentration between 10-50%. The precise function of these receptors has not been established. The pharmacologic effects of beta adrenergic agonist drugs, including pirbuterol, are at least in proof attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (AlP) to cyclic-3† ,5†-adenosine monophosphate (c-AMP). Increased c-AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H20N2O3
Phân tử khối
240.2988
Monoisotopic mass
240.147392516
InChI
InChI=1S/C12H20N2O3/c1-12(2,3)13-6-11(17)8-4-5-10(16)9(7-15)14-8/h4-5,11,13,15-17H,6-7H2,1-3H3
InChI Key
InChIKey=VQDBNKDJNJQRDG-UHFFFAOYSA-N
IUPAC Name
6-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)pyridin-3-ol
Traditional IUPAC Name
pirbuterol
SMILES
CC(C)(C)NCC(O)C1=NC(CO)=C(O)C=C1
Độ hòa tan
6.22e+00 g/l
logP
-0.66
logS
-1.6
pKa (strongest acidic)
8.79
pKa (Strongest Basic)
9.59
PSA
85.61 Å2
Refractivity
64.74 m3·mol-1
Polarizability
26.31 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
5
H Bond Donor Count
4
Physiological Charge
1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Pirbuterol is a beta-2 adrenergic bronchodilator. In vitro studies and in vivo pharmacologic studies have demonstrated that pirbuterol has a preferential effect on beta-2 adrenergic receptors compared with isoproterenol. While it is recognized that beta-2 adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta-2 receptors in the human heart, existing in a concentration between 10-50%. The precise function of these receptors has not been established.
Cơ Chế Tác Dụng : Pirbuterol is a beta-2 adrenergic bronchodilator. In vitro studies and in vivo pharmacologic studies have demonstrated that pirbuterol has a preferential effect on beta-2 Adrenergic receptors compared with isoproterenol. While it is recognized that beta-2 adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta-2 receptors in the human heart, existing in a concentration between 10-50%. The precise function of these receptors has not been established. The pharmacologic effects of beta adrenergic agonist drugs, including pirbuterol, are at least in proof attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (AlP) to cyclic-3† ,5†-adenosine monophosphate (c-AMP). Increased c-AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. The pharmacologic effects of beta adrenergic agonist drugs, including pirbuterol, are at least in proof attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (AlP) to cyclic-3† ,5†-adenosine monophosphate (c-AMP). Increased c-AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.
Dược Động Học :

▧ Half Life :
The plasma half-life measured after oral administration is about two hours.
Độc Tính : As with all sympathomimetic aerosol medication, cardiac arrest and even death may be associated with abuse of pirbuterol.
Chỉ Định : For the prevention and reversal of bronchospasm in patients 12 years of age and older with reversible bronchospasm including asthma.
Tương Tác Thuốc :
  • Acebutolol Antagonism
  • Amitriptyline The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of pirbuterol.
  • Amoxapine The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of pirbuterol.
  • Atenolol Antagonism
  • Bisoprolol Antagonism
  • Carvedilol Antagonism
  • Clomipramine The tricyclic antidepressant, clomipramine, increases the sympathomimetic effect of pirbuterol.
  • Desipramine The tricyclic antidepressant, desipramine, increases the sympathomimetic effect of pirbuterol.
  • Doxepin The tricyclic antidepressant, doxepin, increases the sympathomimetic effect of pirbuterol.
  • Esmolol Antagonism
  • Imipramine The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of pirbuterol.
  • 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 pirbuterol.
  • Nadolol Antagonism
  • Nortriptyline The tricyclic antidepressant, nortriptyline, increases the sympathomimetic effect of pirbuterol.
  • 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 - Respiratory (inhalation)
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Maxair
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01291
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4845
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506379
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07807
ChemSpider
http://www.chemspider.com/Chemical-Structure.4679.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0089-0815-21
PharmGKB
http://www.pharmgkb.org/drug/PA450983
RxList
http://www.rxlist.com/cgi/generic/pirbu.htm
Drugs.com
http://www.drugs.com/cdi/pirbuterol.html
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