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药品详细

Orciprenaline(奥西那林)

化学结构式图
中文名
奥西那林
英文名
Orciprenaline
分子式
C11H17NO3
化学名
5-{1-hydroxy-2-[(propan-2-yl)amino]ethyl}benzene-1,3-diol
分子量
Average: 211.2576
Monoisotopic: 211.120843415
CAS号
586-06-1
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

A beta-adrenergic agonist used in the treatment of asthma and bronchospasms. [PubChem]

生产厂家
  • American therapeutics inc
  • Astrazeneca lp
  • Boehringer ingelheim
  • Boehringer ingelheim pharmaceuticals inc
  • Dey lp
  • Morton grove pharmaceuticals inc
  • Muro pharmaceutical inc
  • Nephron pharmaceuticals corp
  • Novex pharma
  • Par pharmaceutical inc
  • Silarx pharmaceuticals inc
  • Teva pharmaceuticals usa
  • Teva pharmaceuticals usa inc
  • Usl pharma inc
  • 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
  • Resorcinols
Substructures
  • Hydroxy Compounds
  • Benzyl Alcohols and Derivatives
  • Aliphatic and Aryl Amines
  • Phenols and Derivatives
  • Benzene and Derivatives
  • Amino Alcohols
  • Phenethylamines
  • Aromatic compounds
  • Alcohols and Polyols
  • Phenyl Esters
  • Resorcinols
适应症
药理
Indication For the treatment of bronchospasm, chronic bronchitis, asthma, and emphysema.
Pharmacodynamics 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.
Mechanism of action 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.
Absorption 3% (oral bioavailability of 40%)
Volume of distribution Not Available
Protein binding Not Available
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.

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

Substrate Enzymes Product
Orciprenaline
    		Orciprenaline-3-O-sulfate Details
    Route of elimination Not Available
    Half life 6 hours
    Clearance Not Available
    Toxicity 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).
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 100 °C PhysProp
    water solubility 9.7mg/L Not Available
    logP 1 Not Available
    Predicted Properties
    Property Value Source
    water solubility 6.92e+00 g/l ALOGPS
    logP -0.32 ALOGPS
    logP 0.21 ChemAxon
    logS -1.5 ALOGPS
    pKa (strongest acidic) 8.84 ChemAxon
    pKa (strongest basic) 9.7 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 4 ChemAxon
    polar surface area 72.72 ChemAxon
    rotatable bond count 4 ChemAxon
    refractivity 58.4 ChemAxon
    polarizability 23.12 ChemAxon
    药物相互作用
    Drug Interaction
    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.
    食物相互作用
    • Avoid high doses of caffeine.
    • Take without regard to meals.

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