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药品详细

Terbutaline(特布他林)

化学结构式图
中文名
特布他林
英文名
Terbutaline
分子式
C12H19NO3
化学名
5-[2-(tert-butylamino)-1-hydroxyethyl]benzene-1,3-diol
分子量
Average: 225.2842
Monoisotopic: 225.136493479
CAS号
23031-25-6
ATC分类
R03A 未知;R03C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic. [PubChem]

生产厂家
  • Aaipharma llc
  • Akorn inc
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Hikma farmaceutica (portugal) sa
  • Impax laboratories inc
  • Lannett holdings inc
  • Novartis pharmaceuticals corp
  • Sanofi aventis us llc
  • Teva parenteral medicines inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Rhodes MC, Seidler FJ, Abdel-Rahman A, Tate CA, Nyska A, Rincavage HL, Slotkin TA: Terbutaline is a developmental neurotoxicant: effects on neuroproteins and morphology in cerebellum, hippocampus, and somatosensory cortex. J Pharmacol Exp Ther. 2004 Feb;308(2):529-37. Epub 2003 Nov 10. Pubmed
  2. Hochhaus G, Mollmann H: Pharmacokinetic/pharmacodynamic characteristics of the beta-2-agonists terbutaline, salbutamol and fenoterol. Int J Clin Pharmacol Ther Toxicol. 1992 Sep;30(9):342-62. Pubmed
  3. Haahtela T, Jarvinen M, Kava T, Kiviranta K, Koskinen S, Lehtonen K, Nikander K, Persson T, Reinikainen K, Selroos O, et al.: Comparison of a beta 2-agonist, terbutaline, with an inhaled corticosteroid, budesonide, in newly detected asthma. N Engl J Med. 1991 Aug 8;325(6):388-92. Pubmed
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 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.
Pharmacodynamics 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.
Mechanism of action 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.
Absorption Approximately 30-50% if administered orally and well absorbed subcutaneously.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Not Available
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
Toxicity 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
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 119-122 °C Not Available
water solubility 213 mg/mL Not Available
logP 0.90 TACAKS-NOVAK,K ET AL. (1995)
Caco2 permeability -6.38 ADME Research, USCD
Predicted Properties
Property Value Source
water solubility 5.84e+00 g/l ALOGPS
logP 0.55 ALOGPS
logP 0.44 ChemAxon
logS -1.6 ALOGPS
pKa (strongest acidic) 8.86 ChemAxon
pKa (strongest basic) 9.76 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 63.04 ChemAxon
polarizability 24.78 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 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.
食物相互作用
Not Available

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