ALBUTEROL SULFATE- albuterol sulfate solution
Ritedose Pharmaceuticals, LLC
Albuterol Sulfate Inhalation Solution 0.083% 1
1
(Potency expressed as albuterol, equivalent to 3 mg albuterol sulfate)
PRESCRIBING INFORMATION
FOR INHALATION USE ONLY-NOT FOR INJECTION
Albuterol sulfate inhalation solution is a relatively selective beta 2 -adrenergic bronchodilator (see CLINICAL PHARMACOLOGY section below). Albuterol sulfate, the racemic form of albuterol, has the chemical name ? 1 -[( tert -Butylamino)methyl]-4-hydroxy- m -xylene-?,?'-diol sulfate (2:1) (salt)
Albuterol sulfate has a molecular weight of 576.70 and the molecular formula (C 13 H 21 NO 3 ) 2 � H 2 SO 4 . Albuterol sulfate is a white or practically white powder, freely soluble in water and slightly soluble in alcohol.
The World Health Organization recommended name for albuterol base is salbutamol.
Albuterol sulfate inhalation solution 0.083% requires no dilution before administration.
Each milliliter of albuterol sulfate inhalation solution 0.083% contains 0.83 mg of albuterol (as 1 mg of albuterol sulfate) in an isotonic, sterile, aqueous solution containing sodium chloride; sulfuric acid is used to adjust the pH to between 3 and 5. Albuterol sulfate inhalation solution 0.083% contains no sulfiting agents or preservatives.
Albuterol sulfate inhalation solution is a clear, colorless to light yellow solution.
CLINICAL PHARMACOLOGY
The prime action of beta-adrenergic drugs is to stimulate adenyl cyclase, the enzyme which catalyzes the formation of cyclic-3?,5?-adenosine monophosphate (cyclic AMP) from adenosine triphosphate (ATP). The cyclic AMP thus formed mediates the cellular responses. In vitro studies and in vivo pharmacologic studies have demonstrated that albuterol 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, 10% to 50% of the beta-receptors in the human heart may be beta 2 -receptors. The precise function of these receptors, however, is not yet established. Albuterol has been shown in most controlled clinical trials to have more effect on the respiratory tract in the form of bronchial smooth muscle relaxation than isoproterenol at comparable doses while producing fewer cardiovascular effects. Controlled clinical studies and other clinical experience have shown that inhaled albuterol, like other beta-adrenergic agonist drugs, can produce a significant cardiovascular effect in some patients, as measured by pulse rate, blood pressure, symptoms, and/or electrocardiographic changes.
Albuterol is longer acting than isoproterenol in most patients by any route of administration because it is not a substrate for the cellular uptake processes for catecholamines nor for catechol-O-methyl transferase.
