Tìm theo
Orciprenaline
Các tên gọi khác (4 ) :
  • Metaproterenol
  • Orciprenalina
  • Orciprenaline
  • Orciprenalinum
sympathomimetics, adrenergic beta 2 receptor agonists, bronchodilator agents, tocolytic agents
Thuốc Gốc
Small Molecule
CAS: 586-06-1
ATC: R03CB03, R03AB03
ĐG : Apotex Inc. , http://www.apotex.com
CTHH: C11H17NO3
PTK: 211.2576
A beta-adrenergic agonist used in the treatment of asthma and bronchospasms. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C11H17NO3
Phân tử khối
211.2576
Monoisotopic mass
211.120843415
InChI
InChI=1S/C11H17NO3/c1-7(2)12-6-11(15)8-3-9(13)5-10(14)4-8/h3-5,7,11-15H,6H2,1-2H3
InChI Key
InChIKey=LMOINURANNBYCM-UHFFFAOYSA-N
IUPAC Name
5-{1-hydroxy-2-[(propan-2-yl)amino]ethyl}benzene-1,3-diol
Traditional IUPAC Name
metaproterenol
SMILES
CC(C)NCC(O)C1=CC(O)=CC(O)=C1
Độ tan chảy
100 °C
Độ hòa tan
9.7mg/L
logP
1
logS
-1.5
pKa (strongest acidic)
8.84
pKa (Strongest Basic)
9.7
PSA
72.72 Å2
Refractivity
58.4 m3·mol-1
Polarizability
23.12 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
Dược Lực Học : Orciprenaline (also known as metaproterenol), a synthetic amine, is structurally and pharmacologically similar to isoproterenol. Orciprenaline is used exclusively as a bronchodilator. The pharmacologic effects of beta adrenergic agonist drugs, such as orciprenaline, are at least in part attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the enzyme which 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.
Cơ Chế Tác Dụng : A beta-adrenergic agonist used in the treatment of asthma and bronchospasms. [PubChem] Orciprenaline is a moderately selective beta(2)-adrenergic agonist that stimulates receptors of the smooth muscle in the lungs, uterus, and vasculature supplying skeletal muscle, with minimal or no effect on alpha-adrenergic receptors. Intracellularly, the actions of orciprenaline are mediated by cAMP, the production of which is augmented by beta stimulation. The drug is believed to work by activating adenylate cyclase, the enzyme responsible for producing the cellular mediator cAMP.
Dược Động Học :
▧ Absorption :
3% (oral bioavailability of 40%)
▧ Metabolism :
Hepatic and gastric. The major metabolite, orciprenaline-3-0-sulfate, is produced in the gastrointestinal tract. Orciprenaline is not metabolized by catechol-0-methyltransferase nor have glucuronide conjugates been isolated to date.
▧ Half Life :
6 hours
Độc Tính : Symptoms of overdose include angina, hypertension or hypotension, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise and insomnia. LD50=42 mg/kg (orally in rat).
Chỉ Định : For the treatment of bronchospasm, chronic bronchitis, asthma, and emphysema.
Tương Tác Thuốc :
  • Acebutolol Antagonism
  • Alseroxylon Increased arterial pressure
  • Amitriptyline The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of orciprenaline.
  • Amoxapine The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of orciprenaline.
  • Atenolol Antagonism
  • Betaxolol Beta-Blockers (Beta1 Selective) like betaxolol may diminish the bronchodilatory effect of Beta2-Agonists like orciprenaline. Therapy should be monitored.
  • Bevantolol Antagonism
  • Bisoprolol Antagonism
  • Carteolol Antagonism
  • Carvedilol Antagonism
  • Clomipramine The tricyclic antidepressant, clomipramine, increases the sympathomimetic effect of orciprenaline.
  • Deserpidine Increased arterial pressure
  • Desipramine The tricyclic antidepressant, desipramine, increases the sympathomimetic effect of orciprenaline.
  • Doxepin The tricyclic antidepressant, doxepin, increases the sympathomimetic effect of orciprenaline.
  • Esmolol Antagonism
  • Imipramine The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of orciprenaline.
  • 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 orciprenaline.
  • Nadolol Antagonism
  • Nortriptyline The tricyclic antidepressant, nortriptyline, increases the sympathomimetic effect of orciprenaline.
  • 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 orciprenaline.
  • 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 orciprenaline.
Liều Lượng & Cách Dùng : Syrup - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Alupent
  • Công ty :
    Sản phẩm biệt dược : Metaprel
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00816
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4086
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504464
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07144
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00685
ChemSpider
http://www.chemspider.com/Chemical-Structure.3944.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0597-0070-08
PharmGKB
http://www.pharmgkb.org/drug/PA450390
Wikipedia
http://en.wikipedia.org/wiki/Orciprenaline
RxList
http://www.rxlist.com/cgi/generic2/metaproterenol.htm
... loading
... loading