Tìm theo
Terbutaline
Các tên gọi khác (6 ) :
  • Terbutalin
  • Terbutalina
  • Terbutaline (sulfate de)
  • Terbutalini sulfas
  • Terbutalinsulfat
  • Terbutalinum
Thuốc tác dụng trên đường hô hấp
Thuốc Gốc
Small Molecule
CAS: 23031-25-6
ATC: R03AC03, R03CC03
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C12H19NO3
PTK: 225.2842
A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H19NO3
Phân tử khối
225.2842
Monoisotopic mass
225.136493479
InChI
InChI=1S/C12H19NO3/c1-12(2,3)13-7-11(16)8-4-9(14)6-10(15)5-8/h4-6,11,13-16H,7H2,1-3H3
InChI Key
InChIKey=XWTYSIMOBUGWOL-UHFFFAOYSA-N
IUPAC Name
5-[2-(tert-butylamino)-1-hydroxyethyl]benzene-1,3-diol
Traditional IUPAC Name
terbutaline
SMILES
CC(C)(C)NCC(O)C1=CC(O)=CC(O)=C1
Độ tan chảy
119-122 °C
Độ hòa tan
213 mg/mL
logP
0.90
logS
-1.6
pKa (strongest acidic)
8.86
pKa (Strongest Basic)
9.76
PSA
72.72 Å2
Refractivity
63.04 m3·mol-1
Polarizability
24.78 Å3
Rotatable Bond Count
4
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
caco2 Permeability
-6.38
Dược Lực Học : Terbutaline is a relatively selective beta2-adrenergic bronchodilator that has little or no effect on alpha-adrenergic receptors. The drug has exerts a preferential effect on beta2-adrenergic receptors but stimulates beta-adrenergic receptors less selectively than relatively selective beta2-agonists. Terbutaline appears to have a greater stimulating effect on beta-receptors of the bronchial, vascular, and uterine smooth muscles (beta2 receptors) than on the beta-receptors of the heart (beta1 receptors). This drug relaxes smooth muscle and inhibits uterine contractions, but may also cause some cardiostimulatory effects and CNS stimulation.
Cơ Chế Tác Dụng : A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic. [PubChem] The pharmacologic effects of terbutaline are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) 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 :
▧ Absorption :
Approximately 30-50% if administered orally and well absorbed subcutaneously.
▧ Route of Elimination :
About 90% of the drug was excreted in the urine at 96 hours after subcutaneous administration, with about 60% of this being unchanged drug. It appears that the sulfate conjugate is a major metabolite of terbutaline and urinary excretion is the primary route of elimination
▧ Half Life :
5.5-5.9 hours
▧ Clearance :
* 311 +/- 112 mL/min
Độc Tính : Terbutaline Sulfate: Oral LD50(rat) = 8.7 g/kg; Oral LD50(mouse) = 205 mg/kg; Oral LD50(dog) = 1.5 g/kg; IP LD50(rat)= 220 mg/kg ; IP LD50(mouse) = 130 mg/kg; Oral LD50(rabbit) = >8 g/kg; IV LD50(mouse) = 36 mg/kg; IV LD50(dog) = 116 mg/kg; IV LD50(rabbit) = 110 mg/kg
Chỉ Định : For the prevention and reversal of bronchospasm in patients 12 years of age and older with reversible, obstructive airway disease, as well as symptomatic management of reversible bronchospasm associated with bronchitis and emphysema. Also used acute IV and sub-Q therapy in selected women to inhibit uterine contractions in preterm labor (tocolysis) and prolong gestation when beneficial.
Tương Tác Thuốc :
  • Acebutolol Antagonism
  • Alseroxylon Increased arterial pressure
  • Amitriptyline The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of terbutaline.
  • Amoxapine The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of terbutaline.
  • Atenolol Antagonism
  • Betaxolol Beta-Blockers (Beta1 Selective) like betaxolol may diminish the bronchodilatory effect of Beta2-Agonists like terbutaline. Therapy should be monitored.
  • Bevantolol Antagonism
  • Bisoprolol Antagonism
  • Carteolol Antagonism
  • Carvedilol Antagonism
  • Clomipramine The tricyclic antidepressant, clomipramine, increases the sympathomimetic effect of terbutaline.
  • Deserpidine Increased arterial pressure
  • Desipramine The tricyclic antidepressant, desipramine, increases the sympathomimetic effect of terbutaline.
  • Doxepin The tricyclic antidepressant, doxepin, increases the sympathomimetic effect of terbutaline.
  • Esmolol Antagonism
  • Imipramine The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of terbutaline.
  • 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 terbutaline.
  • Nadolol Antagonism
  • Nortriptyline The tricyclic antidepressant, nortriptyline, increases the sympathomimetic effect of terbutaline.
  • Oxprenolol Antagonism
  • Pargyline Increased arterial pressure
  • Penbutolol Antagonism
  • Phenelzine Increased arterial pressure
  • Pindolol Antagonism
  • Practolol Antagonism
  • Propranolol Antagonism
  • Protriptyline The tricyclic antidepressant, protriptyline, increases the sympathomimetic effect of terbutaline.
  • Rasagiline Increased arterial pressure
  • Reserpine Increased arterial pressure
  • Sotalol Antagonism
  • Timolol Antagonism
  • Tranylcypromine Increased arterial pressure
  • Trimipramine The tricyclic antidepressant, trimipramine, increases the sympathomimetic effect of terbutaline.
Liều Lượng & Cách Dùng : Aerosol, metered - Respiratory (inhalation)
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Novartis
    Sản phẩm biệt dược : Brethaire
  • Công ty :
    Sản phẩm biệt dược : Brethine
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Bricanyl
  • Công ty : Johnson
    Sản phẩm biệt dược : Bricardyl
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Bricasma
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Bricasol
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Dracanyl
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Terbasmin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00871
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5403
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506887
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07129
ChemSpider
http://www.chemspider.com/Chemical-Structure.5210.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25770
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0143-9746-10
PharmGKB
http://www.pharmgkb.org/drug/PA451616
Wikipedia
http://en.wikipedia.org/wiki/Terbutaline
RxList
http://www.rxlist.com/cgi/generic3/terbutaline.htm
Drugs.com
http://www.drugs.com/cdi/terbutaline.html
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