Albuterol Oral Solution

Name: Albuterol Oral Solution

ALBUTEROL SULFATE SYRUP (ORAL SOLUTION) 2 mg/5 mL

Rx only

Albuterol Oral Solution - Clinical Pharmacology

In vitro studies and in vivo pharmacologic studies have demonstrated that albuterol has a preferential effect on beta2-adrenergic receptors compared with isoproterenol. While it is recognized that beta2-adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta2-receptors in the human heart existing in a concentration between 10% and 50%. The precise function of these receptors has not been established (see WARNINGS).

The pharmacologic effects of beta-adrenergic agonist drugs, including albuterol, 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 (cyclic AMP). Increased cyclic 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.

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.

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.

Preclinical:

Intravenous studies in rats with albuterol sulfate have demonstrated that albuterol crosses the blood brain barrier and reaches brain concentrations amounting to approximately 5% of the plasma concentrations. In structures outside the brain barrier (pineal and pituitary glands), albuterol concentrations were found to be 100 times those in the whole brain.

Studies in laboratory animals (minipigs, rodents, and dogs) have demonstrated the occurrence of cardiac arrhythmias and sudden death (with histologic evidence of myocardial necrosis) when beta-agonists and methylxanthines are administered concurrently. The clinical significance of these findings is unknown.

Pharmacokinetics:

Albuterol is rapidly absorbed after oral administration of 10 mL of albuterol sulfate syrup (oral solution) (4 mg of albuterol) in normal volunteers. Maximum plasma concentrations of about 18 ng/mL of albuterol are achieved within 2 hours, and the drug is eliminated with a half-life of about 5 hours.

In other studies, the analysis of urine samples of patients given 8 mg of tritiated albuterol orally showed that 76% of the dose was excreted over three days, with the majority of the dose being excreted within the first 24 hours. Sixty percent of this radioactivity was shown to be the metabolite. Feces collected over this period contained 4% of the administered dose.

Clinical Trials:

In controlled clinical trials in patients with asthma, the onset of improvement in pulmonary function, as measured by maximum midexpiratory flow rate (MMEF) and forced expiratory volume in 1 second (FEV1), was within 30 minutes after a dose of albuterol sulfate syrup (oral solution), with peak improvement occurring between 2 and 3 hours. In a controlled clinical trial involving 55 children, clinically significant improvement (defined as maintaining a 15% or more increase in FEV1 and a 20% or more increase in MMEF over baseline values) continued to be recorded up to 6 hours. No decrease in the effectiveness was reported in one uncontrolled study of 32 children who took albuterol sulfate syrup (oral solution) for a 3-month period.

Contraindications

Albuterol sulfate syrup (oral solution) is contraindicated in patients with a history of hypersensitivity to albuterol or any of its components.

Overdosage

The expected symptoms with overdosage are those of excessive beta-adrenergic stimulation and/or occurrence or exaggeration of any of the symptoms listed under ADVERSE REACTIONS, e.g., seizures, angina, hypertension or hypotension, tachycardia with rates up to 200 beats per minute, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, and sleeplessness. Hypokalemia may also occur. As with all sympathomimetic medications, cardiac arrest and even death may be associated with abuse of albuterol sulfate syrup (oral solution). Treatment consists of discontinuation of albuterol sulfate syrup (oral solution) together with appropriate symptomatic therapy. The judicious use of a cardioselective beta-receptor blocker may be considered, bearing in mind that such medication can produce bronchospasm. There is insufficient evidence to determine if dialysis is beneficial for overdosage of albuterol sulfate syrup (oral solution).

The oral median lethal dose of albuterol sulfate in mice is greater than 2000 mg/kg (approximately 240 times the maximum recommended daily oral dose for adults and children on a mg/m2 basis). In mature rats the subcutaneous (sc) median lethal dose of albuterol sulfate is approximately 450 mg/kg (approximately 110 times the maximum recommended daily oral dose for adults and children on a mg/m2 basis). In small young rats the oral median lethal dose is approximately 2000 mg/kg (approximately 480 times the maximum recommended daily oral dose for adults and children on a mg/m2 basis).

How is Albuterol Oral Solution Supplied

Albuterol Sulfate Syrup (Oral Solution), a clear, orange liquid with a strawberry flavor, contains 2 mg of albuterol (present as the sulfate) per 5 mL in bottles of 16 fluid ounces (one pint).

Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].

Dispense contents with a child-resistant closure (as required) and in a tight, light-resistant container as defined in the USP/NF.

Manufactured for:
QUALITEST PHARMACEUTICALS
Huntsville, AL 35811

8182035
Rev 4/13
R2

Principal display panel

ALBUTEROL SULFATE 
albuterol sulfate solution
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:0603-1008
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
ALBUTEROL SULFATE (ALBUTEROL) ALBUTEROL 2 mg  in 5 mL
Inactive Ingredients
Ingredient Name Strength
CITRIC ACID MONOHYDRATE  
FD&C YELLOW NO. 6  
HYPROMELLOSES  
WATER  
SACCHARIN SODIUM  
SODIUM BENZOATE  
SODIUM CITRATE  
Product Characteristics
Color ORANGE (clear, orange) Score     
Shape Size
Flavor STRAWBERRY Imprint Code
Contains     
Packaging
# Item Code Package Description
1 NDC:0603-1008-58 473 mL in 1 BOTTLE
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA078105 12/27/2006
Labeler - Qualitest Pharmaceuticals (011103059)
Establishment
Name Address ID/FEI Operations
Vintage Pharmaceuticals-Huntsville 825839835 MANUFACTURE(0603-1008)
Revised: 03/2015   Qualitest Pharmaceuticals
(web3)