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indicationFor the prevention and reversal of bronchospasm in patients 12 years of age and older with reversible bronchospasm including asthma.
pharmacologyPirbuterol 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 actionThe 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.
toxicityAs with all sympathomimetic aerosol medication, cardiac arrest and even death may be associated with abuse of pirbuterol.
half lifeThe plasma half-life measured after oral administration is about two hours.
drug interactionsAcebutolol: Antagonism
Amitriptyline: The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of pirbuterol.
Amoxapine: The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of pirbuterol.
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.
Imipramine: The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of pirbuterol.
Isocarboxazid: Increased arterial pressure
Linezolid: Possible increase of arterial pressure
Methyldopa: Increased arterial pressure
Midodrine: Increased arterial pressure
Moclobemide: Moclobemide increases the sympathomimetic effect of pirbuterol.
Nortriptyline: The tricyclic antidepressant, nortriptyline, increases the sympathomimetic effect of pirbuterol.
Phenelzine: Increased arterial pressure
Rasagiline: Increased arterial pressure
Reserpine: Increased arterial pressure