Pirbuterol(吡布特罗)
Monoisotopic: 240.147392516
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.
- Graceway pharmaceuticals llc
Synthesis Reference | Not Available |
General Reference | Not Available |
Type | small molecule |
Classes |
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Substructures |
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Indication | For the prevention and reversal of bronchospasm in patients 12 years of age and older with reversible bronchospasm including asthma. |
Pharmacodynamics | 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. |
Mechanism of action | 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. |
Absorption | Not Available |
Volume of distribution | Not Available |
Protein binding | Not Available |
Metabolism |
Not Available
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Route of elimination | Not Available |
Half life | The plasma half-life measured after oral administration is about two hours. |
Clearance | Not Available |
Toxicity | As with all sympathomimetic aerosol medication, cardiac arrest and even death may be associated with abuse of pirbuterol. |
Affected organisms |
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Pathways | Not Available |
Properties | |||||||||||||||||||||||||||||||||||||||||||
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State | solid | ||||||||||||||||||||||||||||||||||||||||||
Experimental Properties | Not Available | ||||||||||||||||||||||||||||||||||||||||||
Predicted Properties |
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Drug | Interaction |
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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 |