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 beta2 - adrenergic bronchodilator (see CLINICAL PHARMACOLOGY). The chemical name for albuterol sulfate is α1 [(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 (C13H21NO3)2 • H2SO4. 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, edetate disodium (EDTA), and sulfuric acid in a 3-mL isotonic, sterile, aqueous solution. Sodium chloride is added to adjust isotonicity of the solution, EDTA is added as a stabilizer for the active pharmaceutical ingredient, and sulfuric acid is added to adjust pH of the solution to 3.5 (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).

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 beta2-adrenergic receptors compared with isoproterenol. While it is recognized that beta2-adrenergic receptors are the predominant receptors in bronchial smooth muscle, recent data indicate that 10% to 50% of the beta-receptors in the human heart may be beta2-receptors. The precise function of these receptors, however, is not yet established. 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.

Clinical Trials

The safety and efficacy of Albuterol Sulfate Inhalation Solution was evaluated in a 4-week, multicenter, randomized, double-blind, placebo-controlled, parallel group study in 349 children 6 to 12 years of age with mild-to-moderate asthma (mean baseline FEV1 60% to 70% of predicted). Approximately half of the patients were also receiving inhaled corticosteroids. Patients were randomized to receive Albuterol Sulfate Inhalation Solution 0.63 mg, Albuterol Sulfate Inhalation Solution 1.25 mg, or placebo three times a day administered via a Pari LC Plus™ nebulizer and a Pari PRONEB™ compressor. Racemic albuterol, delivered by a chlorofluorocarbon (CFC) metered dose inhaler (MDI) or nebulized, was used on an as-needed basis as the rescue medication.

Efficacy, as measured by the mean percent change from baseline in the area under the 6-hour curve for FEV1, was demonstrated for both active treatment regimens (n=112 [1.25 mg group] and n=110 [0.63 mg group]) compared with placebo (n=110) on day 1 and day 28. Figures 1 and 2 illustrate the mean percentage change from pre-dose FEV1 on day 1 and day 28, respectively. The mean baseline FEV1 for all patients was 1.49 L.

Figure 1 % Change from Pre-Dose FEV1 Intent-to-Treat Population Day 1

 

Figure 2 % Change from Pre-Dose FEV1 Intent-to-Treat Population Day 28

The onset of a 15% increase in FEV1 over baseline for both doses of Albuterol Sulfate Inhalation Solution was seen at 30 minutes (the first post-dose assessment). The mean time to peak effect was approximately 30 to 60 minutes for both doses on day 1 and after 4 weeks of treatment. The mean duration of effect, as measured by a >15% increase from baseline in FEV1, was approximately 2.5 hours for both doses on day 1 and approximately 2 hours for both doses after 4 weeks of treatment. In some patients, the duration of effect was as long as 6 hours.

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).

Albuterol Sulfate Inhalation Solution is contraindicated in patients with a history of hypersensitivity to any of its components.

The expected symptoms with overdosage are those of excessive beta-adrenergic stimulation and/or occurrence or exaggeration of symptoms such as 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, insomnia, and exaggeration of the pharmacological effects listed in ADVERSE REACTIONS. Hypokalemia may also occur. As with all sympathomimetic aerosol medications, cardiac arrest and even death may be associated with abuse of Albuterol Sulfate Inhalation Solution. Treatment consists of discontinuation of Albuterol Sulfate Inhalation 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 Inhalation Solution.

The oral median lethal dose of albuterol sulfate in mice is greater than 2000 mg/kg (approximately 580 times the maximum recommended daily inhalation dose of Albuterol Sulfate Inhalation Solution on a mg/m2 basis). The subcutaneous median lethal dose of albuterol sulfate in mature rats and small young rats is approximately 450 mg/kg and 2000 mg/kg, respectively (approximately 260 and 1200 times the maximum recommended daily inhalation dose of Albuterol Sulfate Inhalation Solution on a mg/m2 basis). The inhalation median lethal dose has not been determined in animals.

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 FEV1 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 supplied as a 3 mL, clear, colorless, sterile, preservative-free, aqueous solution in two different strengths, 0.63 mg/3 mL and 1.25 mg/3 mL, of albuterol (equivalent to 0.75 mg of albuterol sulfate or 1.5 mg of albuterol sulfate per 3 mL) in unit-dose low-density polyethylene (LDPE) vials. Each unit-dose LDPE vial is protected in a foil pouch, and each foil pouch contains 5 unit-dose LDPE vials. Each strength of Albuterol Sulfate Inhalation Solution is available in a shelf carton containing multiple foil pouches.

Albuterol Sulfate Inhalation Solution, 0.63 mg/3 mL (potency expressed as albuterol) contains 0.75 mg albuterol sulfate per 3 mL in unit-dose vials and is available in the following packaging configuration.

NDC 0378-7057-52 5 foil pouches, each containing 5 vials, total 25 vials per carton

Albuterol Sulfate Inhalation Solution, 1.25 mg/3 mL (potency expressed as albuterol) contains 1.5 mg albuterol sulfate per 3 mL in unit-dose vials and is available in the following packaging configuration.

NDC 0378-7058-52 5 foil pouches, each containing 5 vials, total 25 vials per carton

Rx only

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 two weeks. Discard the vial if the solution is not colorless.

Keep out of the reach of children.

The brands listed are trademarks of their respective owners.

Manufactured for:

Mylan Pharmaceuticals Inc.

Morgantown, WV 26505 U.S.A.

Manufactured by:

The Ritedose Corporation

Columbia, SC 29203 U.S.A.

TRC:ASISLD:R2

RPIN0178

Revised: 8/2022

Albuterol Sulfate Inhalation Solution

(al bue' ter ol sul' fate)

0.63 mg*/3 mL and 1.25 mg*/3 mL

(*Equivalent to 0.75 mg of albuterol sulfate or 1.5 mg of albuterol sulfate per 3 mL)

Read the patient information that comes with Albuterol Sulfate Inhalation Solution before using it and each time you get a refill for your child. There may be new information. This leaflet does not take the place of talking to your child’s doctor about your child’s medical condition or treatment.

What is Albuterol Sulfate Inhalation Solution?

Albuterol Sulfate Inhalation Solution is a medicine that is used for the relief of bronchospasms caused by asthma in children ages 2 to 12 years. Bronchospasm is the tightening and swelling of the muscles around the airways. Albuterol Sulfate Inhalation Solution can help relax these airway muscles for up to 6 hours so that your child may breathe more easily.

Who should not use Albuterol Sulfate Inhalation Solution?

Do not give your child Albuterol Sulfate Inhalation Solution if he or she is allergic to any of its ingredients. The active ingredient is albuterol sulfate. See the end of this leaflet for a complete list of ingredients.

What should I tell my child’s doctor before giving Albuterol Sulfate Inhalation Solution?

Tell your child’s doctor about all of your child’s medical conditions including if your child has:

•

Heart problems

•

High blood pressure

•

Seizures

•

A thyroid problem called hyperthyroidism

•

Diabetes

Tell your child’s doctor about all the medicines your child takes, including prescription and non-prescription medicines, vitamins and herbal supplements. Albuterol Sulfate Inhalation Solution and some other medicines can affect each other and may cause serious side effects. Especially tell your child’s doctor if your child is taking or using:

•

Any short-acting bronchodilator medicines (sometimes called rescue inhalers)

•

Epinephrine

•

Medicines called monoamine oxidase inhibitors (MAOIs) or tricyclic anti-depressants or has stopped taking them in the past 2 weeks. These medicines are usually used for mental problems.

•

Medicines called beta-blockers (used for heart problems and high blood pressure)

•

Certain diuretic medicines (water pills)

•

Digoxin

Know the medicines your child takes. Keep a list of them and show it to your child’s doctor and pharmacist each time your child gets a new medicine.

How should Albuterol Sulfate Inhalation Solution be given?

Read the Patient’s Instructions for Use that comes with Albuterol Sulfate Inhalation Solution. Ask your pharmacist for these instructions if they are not with your medicine. Keep the instructions with Albuterol Sulfate Inhalation Solution because you may want to read them again.

•

Give Albuterol Sulfate Inhalation Solution exactly as prescribed for your child. Do not change your child’s dose or how often it is used without talking to your child’s doctor first.

•

Albuterol Sulfate Inhalation Solution is breathed into the lungs. Albuterol Sulfate Inhalation Solution is used with a special breathing machine called a nebulizer. Do not mix other medicines with Albuterol Sulfate Inhalation Solution in the nebulizer. Do not use Albuterol Sulfate Inhalation Solution that is not clear and colorless.

•

Call your child’s doctor or get emergency help right away if your child’s breathing is not helped or gets worse during treatment with Albuterol Sulfate Inhalation Solution.

•

Call your child’s doctor right away if your child needs to use Albuterol Sulfate Inhalation Solution more often than prescribed.

•

Albuterol Sulfate Inhalation Solution has not been studied for treating acute attacks of bronchospasm (rescue use). Your child may need a different medicine for rescue use.

•

If you give your child too much Albuterol Sulfate Inhalation Solution call your child’s doctor right away.

What are the side effects with Albuterol Sulfate Inhalation Solution?

Albuterol Sulfate Inhalation Solution may cause the following serious side effects:

•

Worsening of the tightening and swelling of the muscles around your child’s airways (bronchospasm). This side effect can be life threatening. Call your child’s doctor or get emergency help right away if your child’s breathing is not helped or gets worse during treatment with Albuterol Sulfate Inhalation Solution.

•

Serious and life threatening allergic reactions.

 

Symptoms of a serious allergic reaction include:

•

Hives, rash

•

Swelling of your child’s face, eyelids, lips, tongue, or throat, and trouble swallowing

•

Worsening of your child’s breathing problems such as wheezing, chest tightness or shortness of breath

•

Shock (loss of blood pressure and consciousness).

The most common side effects with Albuterol Sulfate Inhalation Solution include a fast or irregular heartbeat, chest pain, shakiness, or nervousness.

How should Albuterol Sulfate Inhalation Solution be stored?

•

Store Albuterol Sulfate Inhalation Solution at room temperature, 2°C to 25°C (36°F to 77°F) in its tightly closed container.

•

Protect vials from light before use. Therefore, keep unused vials in the foil pouch or carton. Once removed from the foil pouch, use vial(s) within two weeks.

•

Do not use Albuterol Sulfate Inhalation Solution after the expiration (EXP) date printed on the vial.

•

Do not use Albuterol Sulfate Inhalation Solution that is not clear and colorless.

•

Safely, discard Albuterol Sulfate Inhalation Solution that is out-of-date or no longer needed.

•

Keep Albuterol Sulfate Inhalation Solution and all medicines out of the reach of children.

General Information about Albuterol Sulfate Inhalation Solution

Medicines are sometimes prescribed for conditions that are not mentioned in the patient information leaflets. Do not use Albuterol Sulfate Inhalation Solution for a condition for which it was not prescribed. Do not give Albuterol Sulfate Inhalation Solution to other people, even if they have the same symptoms your child has. It may harm them.

This leaflet summarizes the most important information about Albuterol Sulfate Inhalation Solution. If you would like more information, talk with your child’s doctor. You can ask your child’s doctor or pharmacist for information about Albuterol Sulfate Inhalation Solution that is written for health professionals.

To report SUSPECTED ADVERSE REACTIONS, contact Ritedose Pharmaceuticals, LLC at 1-855-806-3300 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

What are the ingredients in Albuterol Sulfate Inhalation Solution?

Active Ingredient: albuterol sulfate

Inactive Ingredients: sodium chloride, edetate disodium (EDTA), and sulfuric acid

Rx only

Manufactured for:

Mylan Pharmaceuticals Inc.

Morgantown, WV 26505 U.S.A.

Manufactured by:

The Ritedose Corporation

Columbia, SC 29203 U.S.A.

Albuterol Sulfate Inhalation Solution

0.63 mg*/3 mL and 1.25 mg*/3 mL

(*Equivalent to 0.75 mg of albuterol sulfate or 1.5 mg of albuterol sulfate per 3 mL)

PATIENT’S INSTRUCTIONS FOR USE

Read this patient information completely every time your prescription is filled as information may have changed. Keep these instructions with your medication, as you may want to read them again.

Albuterol Sulfate Inhalation Solution should only be used under the direction of a physician. Your physician and pharmacist have more information about Albuterol Sulfate Inhalation Solution and the condition for which it has been prescribed. Contact them if you have additional questions.

Storing your Medicine

Store Albuterol Sulfate Inhalation Solution between 2°C to 25°C (36°F to 77°F). Vials should be protected from light before use, therefore, keep unused vials in the foil pouch. Do not use after the expiration (EXP) date printed on the vial.

Dose

Albuterol Sulfate Inhalation Solution is supplied as a single-dose, ready-to-use vial containing 3 mL of solution. No mixing or dilution is needed. Use one new vial with each nebulizer treatment.

1.

Remove one vial from the foil pouch. Place remaining vials back into foil pouch for storage.

2.

Twist the cap completely off the vial and squeeze the contents into the nebulizer reservoir (Figure 1).

3.

Connect the nebulizer to the mouthpiece or face mask (Figure 2).

4.

Connect the nebulizer to the compressor.

5.

Sit in a comfortable, upright position; place the mouthpiece in your mouth (Figure 3) or put on the face mask (Figure 4); and turn on the compressor.

6.

Breathe as calmly, deeply and evenly as possible through your mouth until no more mist is formed in the nebulizer chamber (about 5-15 minutes). At this point, the treatment is finished.

7.

Clean the nebulizer (see manufacturer’s instructions).

Manufactured for:

Mylan Pharmaceuticals Inc.

Morgantown, WV 26505 U.S.A.

Manufactured by:

The Ritedose Corporation

Columbia, SC 29203 U.S.A.

TRC:PIL:ASISLD:R2

RPIN0178

Revised: 8/2022

NDC 0378-7057-52

Albuterol

Sulfate

Inhalation Solution

0.63 mg*/3 mL

*Each unit dose vial contains 0.63 mg of albuterol

equivalent to 0.75 mg of albuterol sulfate.

For Inhalation Only

Sterile Unit-Dose Vials

ATTENTION PHARMACIST:

Detach “Patient’s Instructions

for Use” from package insert

and dispense with solution.

Rx only

Carton contains:

5 pouches of 5 x 3 mL vials each

INGREDIENTS:

Active: Albuterol sulfate (0.75 mg/3 mL).

Inactive: Sodium chloride, edetate disodium, sulfuric

acid (to adjust to pH 3.5) and water for injection.

STORAGE CONDITIONS: Protect from light. Store

between 2°C to 25°C (36°F to 77°F). Store the

unit-dose vials in the protective foil pouch at all times.

Once removed from the foil pouch, use the vial(s)

within two weeks. Discard the vial if the solution is not

colorless.

Keep out of reach of children.

USUAL DOSAGE: FOR USE IN CHILDREN AGES 2 TO 12.

See accompanying prescribing information. USE ONLY

AS DIRECTED BY YOUR PHYSICIAN. DO NOT EXCEED

RECOMMENDED DOSAGE.

Manufactured for:

Mylan Pharmaceuticals Inc.

Morgantown, WV 26505 U.S.A.

Manufactured by:

The Ritedose Corporation

Columbia, SC 29203 U.S.A.

TRC: 7057:25C:R1     RPSC0453

Mylan.com

NDC 0378-7058-52

Albuterol

Sulfate

Inhalation Solution

1.25 mg*/3 mL

*Each unit dose vial contains 1.25 mg of albuterol

equivalent to 1.5 mg of albuterol sulfate.

For Inhalation Only

Sterile Unit-Dose Vials

ATTENTION PHARMACIST:

Detach “Patient’s Instructions

for Use” from package insert

and dispense with solution.

Rx only

Carton contains:

5 pouches of 5 x 3 mL vials each

INGREDIENTS:

Active: Albuterol sulfate (1.5 mg/3 mL).

Inactive: Sodium chloride, edetate disodium, sulfuric

acid (to adjust to pH 3.5) and water for injection.

STORAGE CONDITIONS: Protect from light. Store

between 2°C to 25°C (36°F to 77°F). Store the

unit-dose vials in the protective foil pouch at all times.

Once removed from the foil pouch, use the vial(s)

within two weeks. Discard the vial if the solution is not

colorless.

Keep out of reach of children.

USUAL DOSAGE: FOR USE IN CHILDREN AGES 2 TO 12.

See accompanying prescribing information. USE ONLY

AS DIRECTED BY YOUR PHYSICIAN. DO NOT EXCEED

RECOMMENDED DOSAGE.

Manufactured for:

Mylan Pharmaceuticals Inc.

Morgantown, WV 26505 U.S.A.

Manufactured by:

The Ritedose Corporation

Columbia, SC 29203 U.S.A.

TRC: 7058:25C:R1     RPSC0454

Mylan.com