ALBUTEROL SULFATE

Albuterol sulfate inhalation solution is a sterile, clear, colorless solution of the sulfate salt of racemic albuterol, albuterol sulfate. Albuterol sulfate is a relatively selective beta 2 -adrenergic bronchodilator (see CLINICAL PHARMACOLOGY ). The chemical name for albuterol sulfate is α 1 [(tert-butylamino) methyl]-4-hydroxy-m-xylene-α, α'-diol sulfate (2:1) (salt), and its established chemical structure is as follows: The molecular weight of albuterol sulfate is 576.7 and the empirical formula is (C 13 H 21 NO 3 ) 2 • H 2 SO 4 . Albuterol sulfate is a white crystalline powder, soluble in water and slightly soluble in ethanol. The World Health Organization recommended name for albuterol is salbutamol. Albuterol sulfate inhalation solution is supplied in two strengths in unit dose vials. Each unit dose vial contains either 0.63 mg of albuterol equivalent to 0.75 mg of albuterol sulfate or 1.25 mg of albuterol equivalent to 1.5 mg of albuterol sulfate with sodium chloride and sulfuric acid in a 3-mL isotonic, sterile, aqueous solution. Sodium chloride is added to adjust isotonicity of the solution and sulfuric acid is added to adjust pH of the solution to between 3.0 and 5.0 (see HOW SUPPLIED ). Albuterol sulfate inhalation solution does not require dilution prior to administration by nebulization. For albuterol sulfate inhalation solution, like all other nebulized treatments, the amount delivered to the lungs will depend on patient factors, the jet nebulizer utilized, and compressor performance. Using the Pari LC Plus™ nebulizer (with face mask or mouthpiece) connected to a Pari PRONEB™ compressor, under in vitro conditions, the mean delivered dose from the mouth piece (% nominal dose) was approximately 43% of albuterol (1.25 mg strength) and 39% of albuterol (0.63 mg strength) at a mean flow rate of 3.6 L/min. The mean nebulization time was 15 minutes or less. Albuterol sulfate inhalation solution should be administered from a jet nebulizer at an adequate flow rate, via a mouthpiece or face mask (see DOSAGE AND ADMINISTRATION ). structure

Albuterol sulfate inhalation solution is indicated for the relief of bronchospasm in patients 2 to 12 years of age with asthma (reversible obstructive airway disease).

The usual starting dosage for patients 2 to 12 years of age is 1.25 mg or 0.63 mg of albuterol sulfate inhalation solution administered 3 or 4 times daily, as needed, by nebulization. More frequent administration is not recommended. To administer 1.25 mg or 0.63 mg of albuterol, use the entire contents of one unit-dose vial (3 mL of 1.25 mg or 0.63 mg inhalation solution) by nebulization. Adjust nebulizer flow rate to deliver albuterol sulfate inhalation solution over 5 to 15 minutes. The use of albuterol sulfate inhalation solution can be continued as medically indicated to control recurring bouts of bronchospasm. During this time most patients gain optimum benefit from regular use of the inhalation solution. Patients 6 to 12 years of age with more severe asthma (baseline FEV 1 less than 60% predicted), weight > 40 kg, or patients 11 to 12 years of age may achieve a better initial response with the 1.25 mg dose. Albuterol sulfate inhalation solution has not been studied in the setting of acute attacks of bronchospasm. A 2.5 mg dose of albuterol provided by a higher concentration product (2.5 mg albuterol per 3 mL) may be more appropriate for treating acute exacerbations, particularly in children 6 years old and above. If a previously effective dosage regimen fails to provide the usual relief, medical advice should be sought immediately, as this is often a sign of seriously worsening asthma which would require reassessment of therapy. The drug compatibility (physical and chemical), clinical efficacy and safety of albuterol sulfate inhalation solution, when mixed with other drugs in a nebulizer have not been established. The safety and efficacy of albuterol sulfate inhalation solution have been established in clinical trials when administered using the Pari LC Plus™ nebulizer and Pari PRONEB™ compressor. The safety and efficacy of albuterol sulfate inhalation solution when administered with other nebulizer systems have not been established. Albuterol sulfate inhalation solution should be administered via jet nebulizer connected to an air compressor with adequate air flow, equipped with a mouthpiece or suitable face mask.

Albuterol sulfate inhalation solution is contraindicated in patients with a history of hypersensitivity to any of its components.

Clinical Trial Experience: Adverse events reported in >1% of patients receiving albuterol sulfate inhalation solution and more frequently than in patients receiving placebo in a four-week double-blind study are listed in the following table. Table 1: Adverse Events with an Incidence of >1% of Patients Receiving Albuterol Sulfate Inhalation Solution and Greater than Placebo (expressed as % of treatment group) 1.25 mg Albuterol Sulfate Inhalation Solution (N=115) 0.63 mg Albuterol Sulfate Inhalation Solution (N=117) Placebo (N=117) Asthma Exacerbation 13 11.1 8.5 Otitis Media 4.3 0.9 0 Allergic Reaction 0.9 3.4 1.7 Gastroenteritis 0.9 3.4 0.9 Cold Symptoms 0 3.4 1.7 Flu Syndrome 2.6 2.6 1.7 Lymphadenopathy 2.6 0.9 1.7 Skin/Appendage Infection 1.7 0 0 Urticaria 1.7 0.9 0 Migraine 0.9 1.7 0 Chest Pain 0.9 1.7 0 Bronchitis 0.9 1.7 0.9 Nausea 1.7 0.9 0.9 There was one case of ST segment depression in the 1.25 mg albuterol sulfate inhalation solution treatment group. No clinically relevant laboratory abnormalities related to albuterol sulfate inhalation solution administration were seen in this study. Postmarketing Experience: Metabolic acidosis has been reported after the use of albuterol sulfate inhalation solution. Because this reaction is reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate its frequency or establish a causal relationship to drug exposure. To report SUSPECTED ADVERSE REACTIONS, contact Ingenus Pharmaceuticals, LLC at 1-877-748-1970 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch

STORAGE Store between 2°C to 25°C (36°F to 77°F). Protect from light and excessive heat. Store unit-dose vials in protective foil pouch at all times. Once removed from the foil pouch, use vial(s) within one week. Discard the vial if the solution is not colorless. Keep out of the reach of children. Manufactured for: Ingenus Pharmaceuticals, LLC Orlando, FL 32811-7193 Made in China Revised: 08/2024 LXK0042/01 logo3