ALBUTEROL SULFATE HFA
  • ALBUTEROL SULFATE HFA

  • (Generic for PROAIR HFA)
  • QTY 18 • 90 MCG • HFA AER AD • Near 77381

ALBUTEROL (al BYOO ter ole) is a bronchodilator. It helps open up the airways in your lungs to make it easier to breathe. This medicine is used to treat and to prevent bronchospasm.

ALBUTEROL SULFATE HFA Pediatric Monographs
  • General Administration Information
    For storage information, see the specific product information within the How Supplied section.

    Route-Specific Administration

    Oral Administration
    -Administer with food to minimize gastric irritation.
    Oral Solid Formulations
    -Extended-release tablets: Swallow whole with the aid of liquids. Do not chew or crush.

    Oral Liquid Formulations
    -Administer using a calibrated measuring device.




    Inhalation Administration
    Aerosol Inhalation (metered-dose inhaler [MDI]; e.g., ProAir HFA, Ventolin HFA)
    -Instruct patient and/or caregiver on proper inhalation technique. Make sure the canister is firmly seated in the plastic mouthpiece actuator before each use. Shake the inhaler well. Prime the inhaler prior to the initial use by releasing 3 to 4 sprays into the air, away from the face and other people. If not used for more than 2 weeks or if the canister has been dropped, re-prime the inhaler.
    -For patients of any age unable to coordinate inhalation and actuation, a spacer or valved holding chamber (VHC) may be beneficial.
    -The choice of using a mouthpiece versus a face mask with a spacer/VHC device must be made based on the skills and understanding of each individual patient. However, in general, children younger than 4 years require administration with a tight fitting face mask and spacer/VHC device to achieve optimal delivery. If a face mask is used, allow 5 to 6 inhalations per actuation.
    -General administration instructions: Shake the inhaler well before each use. Take the cap off the mouthpiece. Hold the inhaler as directed for the inhaler type. Patient will breathe out through the mouth and push as much air from lungs as the patient can. Put the mouthpiece in the mouth and have patient close lips around it. Push the top of the canister all the way down while the patient breathes in deeply and slowly through the mouth. Right after the spray comes out, release the canister. After the patient has breathed in all the way, take the inhaler out of the mouth. The patient should hold breath as long as they can, up to 10 seconds, then breathe normally. If prescribed more sprays, wait 1 minute and shake the inhaler again. Repeat inhaler steps. Put the cap back on the mouthpiece after use.
    -After administration, instruct patient to rinse mouth with water to minimize dry mouth.
    -Clean the plastic mouthpiece of the inhaler at least once a week. After removing the medication canister wash the mouthpiece in warm running water. Do not allow the medication canister to get wet. Shake excess water from the mouthpiece and verify that all medication build-up has been rinsed away. Allow the mouthpiece to air-dry completely before next use (e.g., overnight).
    -Some products may have an actuation counter. Discard medication and inhaler after expiration date or once the labeled number of actuations have been expelled, whichever comes first. Ventolin HFA expires 12 months after medication removal from foil pouch.
    -To avoid the spread of infection, do not use the inhaler for more than one person.

    Powder for Inhalation (e.g., ProAir RespiClick, ProAir Digihaler)
    -Instruct patient on proper inhalation technique. The ProAir RespiClick inhaler does not require priming.
    -Do NOT use with a spacer or valved holding chamber (VHC).
    -Before first use, check the dose counter window to ensure the inhaler is full and displaying the number "200" in the window. The dose counter will count down each time the mouthpiece cap is opened and closed. The dose counter window only displays even numbers (e.g., 200, 198, 196).
    -Instruct the patient to hold the inhaler upright while opening the cap fully until a "click" sound is heard.
    -The cap should not be opened unless the patient is ready to take a dose; opening and closing the cap without inhaling a dose will waste the medicine and may damage the inhaler.
    -The patient should breathe out through the mouth and push as much air from the lungs as possible. Instruct the patient to be careful not to breathe out into the inhaler mouthpiece. Put the mouthpiece in the mouth and have patient close lips around it. The patient should breathe in deeply through the mouth, until their lungs feel completely full of air. Ensure that the vent above the mouthpiece is not blocked by the patient's lips or fingers. Instruct the patient to hold breath for about 10 seconds or as long as comfortable.
    -Remove the inhaler from the mouth.
    -Check the dose counter on the back of the inhaler to make sure the dose was received.
    -Close the cap over the mouthpiece after each use of the inhaler; make sure the cap closes firmly into place.
    -To inhale another dose, close the cap and then repeat inhaler steps.
    -When there are "20" doses left, the dose counter will change to red; refill the prescription or contact the doctor for another prescription.
    -Keep the inhaler clean and dry at all times. Do not wash or put any part of the inhaler in water. If the mouthpiece requires cleaning, gently wipe with a dry cloth or tissue as needed.
    -ProAir Digihaler contains a built-in electronic module which detects, records, and stores data on inhaler events, including peak inspiratory flow rate. A mobile app is required for data transmission, but is not required for the administration of albuterol to the patient.
    -Discard the inhaler 13 months after opening the foil pouch, when the dose counter displays "0", or after the product expiration date, whichever comes first.
    -To avoid the spread of infection, do not use the inhaler for more than one person.

    Inhalation Solution for Nebulization
    -To administer a 0.63 mg dose of albuterol, use 3 mL of the commercially available (0.63mg/3mL) solution.
    -To administer a 1.25 mg dose of albuterol, dilute 0.25 mL of a 0.5% solution for nebulization to a final volume of 3 mL with sterile 0.9% Sodium Chloride Injection or use 3 mL of the commercially available (1.25mg/3mL) solution.
    -To administer a 2.5 mg dose of albuterol, dilute 0.5 mL of a 0.5% solution for nebulization to a final volume of 3 mL with sterile 0.9% Sodium Chloride Injection or use 3 mL of the commercially available 0.083% solution for nebulization.
    -Deliver solution by nebulization over 5 to 15 minutes.
    -The choice of using a mouthpiece versus a face mask must be made based on the skills and understanding of each individual patient.
    -Using the 'blow by' technique (i.e., holding the face mask or open tube near the patient's nose and mouth) is not recommended.
    -To avoid microbial contamination, aseptic technique should be used each time a multi-dose bottle is opened. Precautions should be taken to prevent contact of dropper tip with any surface, including nebulizer reservoir and ventilatory equipment. Each multi-dose bottle should be used for only 1 patient.
    -Unit-dose vials should be stored in protective foil pouch at all times. Specific products may be good for up to 1 week outside of the foil pouch, but should remain protected from light.
    -Discard the vial if the solution changes color or becomes cloudy.

    The most common adverse reactions associated with albuterol use are related to its sympathomimetic effects, although certain cardiovascular effects may be less common with albuterol than with sympathomimetics that have less selectivity for beta2-adrenergic receptors. In general, the sympathomimetic effects of albuterol are dose-related and are more frequent with oral dosage forms than with the inhalation aerosol or solution for inhalation.

    Central nervous system (CNS) stimulation is common with all forms of albuterol. Tremor (10 to 24%) and nervousness or anxiety (4 to 20%) are some of the most common adverse effects reported with albuterol use; these may occur early in treatment initiation and lessen with continued use. During clinical trials with extended-release albuterol tablets, tremor occurred less frequently in adolescents than in their adult counterparts; incidence increased with increasing patient age. The incidence of tremor in young children is unclear. Tremor development in children receiving inhaled albuterol may be more common when the drug is delivered via nebulization compared to valved holding chamber (VHC) (RR 0.64; 95% CI, 0.44-0.95). Excitability and nervousness appear to occur more frequently in young children (20% and 15%, respectively) than in older children and adolescents (2% and 9%, respectively) receiving oral albuterol. During clinical trials of albuterol syrup, tremor (10%), shakiness (9%), and hyperactivity (2%) occurred in older children and adolescents; in addition, hyperkinesis (4%) was reported in younger children. Restlessness (< 1%) and insomnia (1-3%) have also been reported with albuterol use. Other central nervous system (CNS) effects associated with albuterol use include headache (3-19%), migraine (1-2%), dizziness/lightheadedness (7% or less), vertigo, weakness (2% or less), drowsiness (< 1%), sleep disturbance, not specified (2% or less), and nightmares. Agitation (1%), irritability (< 1%), emotional lability (1%), and aggressive behavior (1%) have also been reported, specifically in pediatric patients.

    Like other sympathomimetics, albuterol can cause various adverse cardiovascular effects including palpitations (5% or less), sinus tachycardia (1 to 5%), hypertension (3% or less), chest pain (unspecified) (< 3%), and angina. Increases in pulse rate may be less significant when albuterol is administered via valved holding chamber (VHC) compared to nebulization. Peripheral vasodilation (e.g., hypotension) may occur from beta-2 stimulation of the vasculature. Arrhythmia exacerbation or precipitation, such as atrial fibrillation, supraventricular tachycardia (SVT), and extrasystole have been reported with albuterol use. In addition, beta-agonists have been reported to produce ECG changes, ST-T wave changes (e.g., flattening of the T wave, ST segment depression), and QT prolongation. Cardiac effects may be related to sympathomimetic effects and/or beta-agonist-induced hypokalemia. Stimulation of beta-2 receptors results in gluconeogenesis and intracellular movement of potassium, which may cause hyperglycemia and hypokalemia. Significant metabolic effects occur most commonly with relatively large doses of nebulized albuterol or with enteral products. In general, cardiovascular reactions are transient and more common with systemic albuterol therapy. Clinically significant effects are uncommon after administration of albuterol at recommended doses; however, if they occur the drug should be discontinued.

    Metabolic acidosis has been reported in post-marketing experience with albuterol inhalation solution and aerosol. A causal relationship has not been established. Diabetic ketoacidosis has been reported after administration of large doses of intravenous albuterol; the potential for this adverse event after the use of other albuterol dosage forms is unknown.

    Anaphylactoid reactions, including rare cases of angioedema, difficulty breathing, oropharyngeal edema, urticaria, and rash (unspecified) have been reported with albuterol use. In clinical trials of albuterol inhalation, allergic reactions (1% to 3%) and urticaria (1% to 2%) were infrequently reported. Rarely, oral albuterol has been associated with cases of Stevens-Johnson syndrome and erythema multiforme in children.

    Paradoxical bronchospasm can occur after treatment with albuterol inhalations and can be life threatening. Patients who continue to have dyspnea, cough, and/or wheezing after albuterol administration with no relief of symptoms should stop using albuterol immediately and seek emergency medical attention. Paradoxical bronchospasm appears more likely to occur with the first few uses of a new canister of inhaled albuterol pressurized inhalation or MDI. Asthma exacerbation/lack of efficacy (11% to 13%), bronchospasm (8% to 15%), cough (2% or more), wheezing (1%), dyspnea (< 3%) have been reported during clinical trials of inhaled albuterol.

    Nausea (4% or less) and vomiting (3% to 4%) are sympathomimetic effects that may occur with any albuterol dosage form; these reactions are usually transient and may respond to temporary dose reduction. Though gastrointestinal symptoms such as appetite stimulation (3%), anorexia (1%), and abdominal pain (< 1%) are more common with systemic albuterol, dyspepsia (1% to 1.5%) and diarrhea (< 3%) have been reported with inhaled albuterol use. Flatulence (< 3%) and eructation (< 3%) have also been reported.

    Musculoskeletal pain (5% or less), muscle spasm (< 1%), leg pain, and muscle cramps (3%) have been reported with albuterol use. During clinical trials with extended-release albuterol tablets, muscle cramps occurred less frequently in adolescents than in their adult counterparts; incidence increased with increasing patient age. Muscle cramps may be related to beta-agonist-induced hypokalemia.

    Oropharyngeal/throat irritation is a sympathomimetic effects that may occur with any albuterol dosage form; however, local nose, and throat effects are more likely to occur with the inhaled formulations. Xerostomia and throat irritation (10% or less), oropharyngeal pain (2% or more), sinusitis (5% or more), sinus headache (1%), naso-pharyngitis (2% or more), pharyngitis (14% or less), rhinitis (4% to 5%), upper respiratory inflammation (5%), laryngitis, hoarseness, dysphonia (< 3%), glossitis (< 3%), nasal congestion (1%), epistaxis (1% to 3%), tongue oral ulceration, and gagging have been reported with inhaled albuterol use. Systemic sympathomimetic effects (e.g., oropharyngeal irritation) are usually transient and may respond to temporary dose reduction. Local effects due to oral inhalation may be limited by rinsing the mouth with water after drug administration. Infections have also been reported with all albuterol dosage forms. Viral respiratory tract infection (4-7%), upper respiratory tract infection (5% or more), bronchitis (5% or more), lung disorders (< 3%), and increased sputum (1.5%) have been reported as respiratory infectious adverse events of inhaled albuterol therapy. Miscellaneous infectious events such as cold symptoms (3%), flu-like syndrome (3%), fever (5% or more), lymphadenopathy (1% to 3%), gastroenteritis (1% to 3%), skin/appendage infection (2%), and urinary tract infection (< 3%) have also been reported.

    Taste disturbance (dysgeusia, < 3%) may occur with albuterol use, especially with inhaled formulations. Conjunctivitis has been reported in 1% of patients receiving albuterol oral solution ; conjunctivitis or ocular irritation may also occur if formulations for inhalation are inadvertently sprayed in the eyes. Unusual taste and mydriasis (1.5%) are sympathomimetic effects that may occur with any albuterol dosage form. Other sensory system effects are more likely to occur with the inhaled formulations. Otitis media (1% to 4%), ear pain or otalgia (< 3%), tinnitus, and tooth discoloration (1%) have been reported with inhaled albuterol use. Rinsing the mouth with water after inhaled albuterol administration helps to limit any localized effects.

    General adverse events reported in albuterol clinical trials include back pain (2%), pain (2%), edema (< 3%), ataxia (< 3%), increased sweating (hyperhidrosis, < 3%), flushing (< 1%), pallor (1%), and rigors or chills (< 3%). Urinary retention (< 1%) has also been rarely reported.

    Do not exceed recommended dosages of beta-agonists; fatalities have been reported in association with excessive use of inhaled sympathomimetic drugs in patients with asthma. The exact cause of death is unknown, but cardiac arrest after an unexpected development of a severe acute asthmatic crisis and subsequent hypoxia is suspected.

    Paradoxical bronchospasm can occur after treatment with albuterol and can be life-threatening. If this occurs, albuterol should be discontinued immediately and supportive care provided as necessary. In addition, increased albuterol use (more than 2 days/week, not including exercise-induced bronchospasm) may indicate asthma destabilization. Asthma may deteriorate acutely over a period of hours or chronically over several days or weeks. If deterioration of asthma occurs appropriate evaluation of the patient and the treatment strategy is warranted, giving special consideration to corticosteroid therapy. Albuterol has no anti-inflammatory activity and is not a substitute for inhaled or oral corticosteroid therapy. The use of beta-agonists alone may not be adequate to control asthma in many patients. Early consideration should be given to adding anti-inflammatory agents (e.g., corticosteroids) to the therapeutic regimen. Corticosteroids should not be stopped or reduced when albuterol therapy is instituted.

    Albuterol is contraindicated in patients with albuterol hypersensitivity, levalbuterol hypersensitivity, or hypersensitivity to any component of the specific dosage formulation. Albuterol inhalation powder (i.e., ProAir RespiClick and ProAir Digihaler), is contraindicated in patients with severe milk protein hypersensitivity because the formulation contains lactose, which contains milk proteins. Immediate hypersensitivity reactions may occur after administration of racemic albuterol, as demonstrated by rare cases of urticaria, angioedema, rash, bronchospasm, anaphylaxis, and oropharyngeal edema. Like other beta-agonists, albuterol can produce paradoxical bronchospasm, which may be life-threatening. If paradoxical bronchospasm occurs, albuterol should be discontinued immediately and alternative therapy instituted. It should be recognized that paradoxical bronchospasm, when associated with inhaled formulations, frequently occurs with the first use of a new canister or vial.

    Albuterol, like other sympathomimetic amines, should be used cautiously in patients with a history of seizures or seizure disorder, hyperthyroidism, pheochromocytoma, or unusual responsiveness to other sympathomimetic amines. Pheochromocytoma may increase the risk of prolonging the QT interval when using albuterol.

    Monitor heart rate and blood pressure in patients receiving high doses of albuterol for acute asthma exacerbations; cardiovascular adverse effects are more likely to occur when aggressive doses are used. Use albuterol with caution in patients with cardiovascular disorders including ischemic cardiac disease (coronary artery disease), hypertension, cardiac arrhythmias, tachycardia, or QT prolongation. Beta-agonists should be avoided in patients with congenital long QT syndrome due to the risk of torsade de pointes and QT prolongation. Use albuterol with caution in patients with conditions that may increase the risk of QT prolongation including bradycardia, AV block, heart failure, stress-related cardiomyopathy, myocardial infarction, stroke, hypomagnesemia, hypocalcemia, or in patients receiving medications known to prolong the QT interval or cause electrolyte imbalances. Females, patients with sleep deprivation, pheochromocytoma, sickle cell disease, hypothyroidism, hyperparathyroidism, hypothermia, systemic inflammation (e.g., human immunodeficiency virus (HIV) infection, fever, and some autoimmune diseases including rheumatoid arthritis, systemic lupus erythematosus (SLE), and celiac disease) and patients undergoing apheresis procedures (e.g., plasmapheresis [plasma exchange], cytapheresis) may also be at increased risk for QT prolongation. Significant changes in systolic and diastolic blood pressure and heart rate may occur in some patients after the use of any beta-adrenergic bronchodilator. As with other beta-agonist medications, albuterol may produce significant hypokalemia in some patients, which has the potential to produce adverse cardiovascular effects, including an increased risk of prolonging the QT interval. After repeated dosing of albuterol inhalation solution in normokalemic pediatric patients (5 to 17 years), an asymptomatic 20% to 25% decrease in serum potassium concentrations was noted. The decrease is usually transient, not requiring supplementation. Correct pre-existing hypokalemia prior to beta-agonist administration.

    Use albuterol with caution in patients with diabetes mellitus. Large doses of intravenous racemic albuterol have been reported to aggravate preexisting diabetes mellitus and diabetic ketoacidosis. Also, patients with diabetic ketoacidosis (DKA) typically have a severe electrolyte imbalance. Serum potassium concentrations must be closely monitored during the treatment of DKA and albuterol may contribute to changes in serum potassium concentrations.

    Description: Albuterol is a moderately selective short-acting beta2-agonist. It is a racemic mixture of R- and S-isomers and is widely used as a bronchodilator. Albuterol is indicated for the management of acute bronchospasm in asthma and other chronic obstructive airway diseases. It is also used off-label as an adjuvant treatment for hyperkalemia in certain clinical situations. Albuterol is similar in structure to terbutaline, and when compared to non-selective beta-agonists, produces equivalent bronchodilation with less cardiac stimulation. Asthma guidelines recommend orally inhaled short-acting beta2-agonists (SABAs) as the preferred pharmacologic treatment to relieve acute bronchospasm. Quick-relief medication such as SABAs should be made available to all patients with persistent asthma for acute symptom control. Although, historically, a trial of albuterol was an option for infants and young children presenting with bronchiolitis, the American Academy of Pediatrics (AAP) no longer recommends this practice, citing a lack of clinical benefit. Outside the United States albuterol is referred to as salbutamol. Albuterol sulfate inhalation solution is FDA-approved in children 2 years and older; other formulations are approved for use in patients of varying ages depending on the specific product.

    General dosing information:
    -Short-acting beta2-agonists (SABAs), such as albuterol, are the treatment of choice for relief of acute reactive airway symptoms and prevention of bronchospasm associated with exercise. Increasing use of SABA treatment or use >= 2 days/week for symptom relief (not prevention) generally indicates inadequate disease state control and may indicate the need for the initiation or intensification of anti-inflammatory therapy.
    -For mild to moderate reactive airway exacerbations, the use of a metered-dose inhaler (MDI) plus valved holding chamber (VHC) is as effective as nebulized therapy when appropriate administration technique is used.-In a Cochrane review of 39 randomized trials that included 1897 children and 729 adults with acute asthma, the method of delivery did not result in a significant difference in hospital admission rates. The risk ratio of hospital admission for VHC vs. nebulizer administration was 0.71 (95% CI, 0.47 to 1.08) in children seen in the emergency department or equivalent community setting. Length of stay in the emergency department was significantly shorter when a VHC was used; mean duration was 103 minutes for children receiving a nebulized SABA and 33 minutes less for those receiving drug via VHC (95% CI, -43 to -24 minutes). Peak flow and forced expiratory volume were similar between the 2 delivery methods. Pulse rate and risk of developing tremor were lower in the VHC group.


    For the treatment of acute bronchospasm (e.g., asthma) and bronchospasm prophylaxis:
    Oral inhalation dosage (metered-dose inhaler [MDI]; e.g., ProAir HFA, Ventolin HFA):
    Neonates*: 1 to 2 puffs/dose administered via inspiratory limb of the mechanical ventilator circuit appear to improve pulmonary mechanics in ventilator-dependent neonates. In a survey of 68 academic medical center neonatal intensive care units (NICUs), 95% reported 1 to 2 puffs as the average dose used. Frequency of administration has not been clearly defined in the neonatal population; albuterol administration is recommended every 1 to 4 hours as needed in other pediatric populations. Of note, MDIs with inline spacers have demonstrated superior drug delivery when compared to jet nebulizers in simulated neonatal lung models.
    Infants* and Children younger than 4 years*: 2 puffs using a valved holding chamber (VHC) and face mask every 4 to 6 hours as needed for symptoms of bronchospasm is recommended by the National Asthma Education and Prevention Program (NAEPP) Expert Panel. For acute asthma exacerbations, the NAEPP recommends 4 to 8 puffs using a VHC and face mask every 20 minutes for 3 doses, then 4 to 8 puffs every 1 to 4 hours as needed. The Global Initiative for Asthma (GINA) guidelines recommend 2 to 6 puffs every 20 minutes for the first hour, then 2 to 3 puffs every hour as needed for acute exacerbations. GINA recommends transfer to an acute care setting if there is no response to inhaled SABA within 1 to 2 hours or if more than 6 puffs are required during the first 2 hours; if more than 10 puffs are required in 3 to 4 hours, hospital admission is recommended. Three clinical trials of albuterol MDIs administered with a VHC and face mask failed to show a significant improvement in asthma symptom scores in infants and children younger than 4 years of age with bronchospasm associated with obstructive airway disease. Of note, safety profiles observed in patients younger than 4 years of age were comparable to those observed in older patients.
    Children 4 to 5 years: 2 puffs every 4 to 6 hours as needed for bronchospasm. In some patients, 1 puff every 4 hours may be sufficient. FDA-approved labeling recommends to not exceed 12 puffs/day. For acute asthma exacerbations, the National Asthma Education and Prevention Program (NAEPP) Expert Panel recommends 4 to 8 puffs every 20 minutes for 3 doses, then 4 to 8 puffs every 1 to 4 hours as needed. The Global Initiative for Asthma (GINA) guidelines recommend 2 to 6 puffs using a valved holding chamber (VHC) with mouthpiece and/or facemask every 20 minutes for the first hour, then 2 to 3 puffs every hour as needed for acute exacerbations. GINA recommends transfer to an acute care setting if there is no response to inhaled SABA within 1 to 2 hours or if more than 6 puffs are required during the first 2 hours; if more than 10 puffs are required in 3 to 4 hours, hospital admission is recommended.
    Children 6 to 12 years: 2 puffs every 4 to 6 hours as needed for bronchospasm. In some patients, 1 puff every 4 hours may be sufficient.FDA-approved labeling recommends to not exceed 12 puffs/day. For acute asthma exacerbations, the National Asthma Education and Prevention Program (NAEPP) Expert Panel recommends 4 to 8 puffs every 20 minutes for 3 doses, then 4 to 8 puffs every 1 to 4 hours as needed. The Global Initiative for Asthma (GINA) guidelines recommend up to 4 to 10 puffs administered with a spacer every 20 minutes for the first hour for mild to moderate exacerbations. After the first hour, the dose required may vary from 4 to 10 puffs every 3 to 4 hours up to 6 to 10 puffs every 1 to 2 hours, or more often.
    Adolescents: 2 puffs every 4 to 6 hours as needed for bronchospasm. In some patients, 1 puff every 4 hours may be sufficient.FDA-approved labeling recommends to not exceed 12 puffs/day. For the acute asthma exacerbations, the National Asthma Education and Prevention Program (NAEPP) Expert Panel recommends 4 to 8 puffs every 20 minutes for up to 4 hours, then 4 to 8 puffs every 1 to 4 hours as needed. The Global Initiative for Asthma (GINA) guidelines recommend up to 4 to 10 puffs administered with a spacer every 20 minutes for the first hour for mild to moderate exacerbations. After the first hour, the dose required may vary from 4 to 10 puffs every 3 to 4 hours up to 6 to 10 puffs every 1 to 2 hours, or more often.
    Oral inhalation dosage (dry-powder inhaler [DPI]; e.g., ProAir RespiClick, ProAir Digihaler):
    Children and Adolescents 4 years and older: 2 oral inhalations (90 mcg/inhalation) every 4 to 6 hours as needed. In some patients, 90 mcg (1 oral inhalation) every 4 hours may be sufficient. FDA-approved labeling recommends to not exceed 12 inhalations/day. Do not use the device with a spacer or volume holding chamber.
    Oral inhalation dosage (nebulized solution):
    Neonates*: 1.25 to 2.5 mg/dose was the most common nebulized dose reported in a survey of 68 academic medical center neonatal intensive care units (NICUs). While significantly less common, weight-based dosing of 0.05 to 0.1 mg/kg/dose was also reported by some centers as their usual dose. Published reports describe a wide range of effective doses; 0.2 to 5 mg/dose and 0.02 to 0.2 mg/kg/dose administered every 4 to 8 hours have been reported to improve pulmonary compliance and/or resistance in ventilator-dependent neonates. Frequency of administration has not been clearly defined in the neonatal population; albuterol administration is recommended every 1 to 6 hours as needed in other pediatric populations. Of note, significantly larger doses of albuterol are used in nebulization when compared to administration with metered-dose inhalers (MDIs) due to inefficiency of nebulized drug delivery.
    Infants* and Children younger than 2 years*: 0.63 to 2.5 mg/dose via oral inhalation every 4 to 6 hours as needed for symptoms of bronchospasm is recommended by the National Asthma Education and Prevention Program (NAEPP) Expert Panel. For acute asthma exacerbations, the NAEPP recommends 0.15 mg/kg/dose (Min: 2.5 mg/dose) vial oral inhalation every 20 minutes for 3 doses, then 0.15 to 0.3 mg/kg/dose (Max: 10 mg/dose) every 1 to 4 hours as needed or 0.5 mg/kg/hour by continuous nebulization. The Global Initiative for Asthma (GINA) guidelines recommend 2.5 mg via nebulization with face mask every 20 minutes for the first hour for acute exacerbations, with reassessment thereafter (further dosing not specified).
    Children 2 to 4 years: 0.63 to 2.5 mg/dose via oral inhalation every 4 to 6 hours as needed for symptoms of bronchospasm is recommended by the National Asthma Education and Prevention Program (NAEPP) Expert Panel. For acute asthma exacerbations, the NAEPP recommends 0.15 mg/kg/dose (Min: 2.5 mg/dose) via oral inhalation every 20 minutes for 3 doses, then 0.15 to 0.3 mg/kg/dose (Max: 10 mg/dose) every 1 to 4 hours as needed or 0.5 mg/kg/hour by continuous nebulization. The Global Initiative for Asthma (GINA) guidelines recommend 2.5 mg/dose via nebulization with mouthpiece (and facemask in those < 4 years) every 20 minutes for the first hour for acute exacerbations, with reassessment thereafter (further dosing not specified). According to FDA-approved labeling, initial dosing for albuterol 0.5% solution is 0.1 to 0.15 mg/kg/dose, with subsequent dosing titrated to achieve desired clinical response. Max: 2.5 mg/dose 3 to 4 times daily; do not exceed 4 doses/day. For patients weighing at least 15 kg, the 0.083% solution may be used at a dose of 2.5 mg/dose via oral inhalation 3 to 4 times daily as needed. Doses should be delivered over 5 to 15 minutes.
    Children 5 years: 1.25 to 5 mg/dose via oral inhalation every 4 to 8 hours as needed for bronchospasm is recommended by the National Asthma Education and Prevention Program (NAEPP) Expert panel. For acute asthma exacerbations, NAEPP recommends 0.15 mg/kg/dose (Min: 2.5 mg/dose) every 20 minutes for 3 doses, then 0.15 to 0.3 mg/kg/dose (Max: 10 mg/dose) every 1 to 4 hours as needed or 0.5 mg/kg/hour by continuous nebulization. The Global Initiative for Asthma (GINA) guidelines recommend 2.5 mg/dose via nebulization with mouthpiece every 20 minutes for the first hour for acute exacerbations, with reassessment thereafter (further dosing not specified). FDA-approved labeling for albuterol 0.083% solution recommends 2.5 mg via oral inhalation 3 to 4 times daily as needed; do not exceed 4 doses/day. For the 0.5% solution, the initial dose is 0.1 to 0.15 mg/kg/dose, with subsequent dosing titrated to achieve desired clinical response. Max: 2.5 mg/dose 3 to 4 times daily. Doses should be delivered over 5 to 15 minutes.
    Children 6 to 12 years: 1.25 to 5 mg/dose via oral inhalation every 4 to 8 hours as needed for bronchospasm is recommended by the National Asthma Education and Prevention Program (NAEPP) Expert panel. For acute asthma exacerbations, NAEPP recommends 0.15 mg/kg/dose (Min: 2.5 mg/dose) every 20 minutes for 3 doses, then 0.15 to 0.3 mg/kg/dose (Max: 10 mg/dose) every 1 to 4 hours as needed or 0.5 mg/kg/hour by continuous nebulization. The Global Initiative for Asthma (GINA) guidelines recommend continuous nebulization, followed by intermittent as-needed therapy for hospitalized patients >= 6 years (dose not specified); however, GINA emphasizes delivery via a metered dose inhaler with a spacer is most effective and efficient for mild to moderate exacerbations. FDA-approved labeling for albuterol 0.083% solution recommends 2.5 mg via oral inhalation 3 to 4 times daily as needed; do not exceed 4 doses/day. For the 0.5% solution, the initial dose is 0.1 to 0.15 mg/kg/dose, with subsequent dosing titrated to achieve desired clinical response. Max: 2.5 mg/dose 3 to 4 times daily. Doses should be delivered over 5 to 15 minutes.
    Adolescents: 1.25 to 5 mg/dose via oral inhalation every 4 to 8 hours as needed for bronchospasm is recommended by the National Asthma Education and Prevention Program (NAEPP) Expert panel. For acute asthma exacerbations, NAEPP recommends 2.5 to 5 mg/dose every 20 minutes for 3 doses, then 2.5 to 10 mg/dose every 1 to 4 hours as needed or 10 to 15 mg/hour by continuous nebulization. The Global Initiative for Asthma (GINA) guidelines recommend continuous nebulization, followed by intermittent as-needed therapy for hospitalized adolescents (dose not specified); however, GINA emphasizes delivery via a metered dose inhaler with a spacer is most effective and efficient for mild to moderate exacerbations. FDA-approved labeling recommend 2.5 mg/dose via oral inhalation 3 to 4 times daily as needed; do not exceed 4 doses/day. Doses should be delivered over 5 to 15 minutes.
    Oral inhalation dosage (albuterol nebulized solution, AccuNeb):
    Children younger than 2 years*: 0.63 to 2.5 mg/dose via oral inhalation every 4 to 6 hours as needed for symptoms of bronchospasm is recommended by the National Asthma Education and Prevention Program (NAEPP) Expert Panel. The manufacturer of AccuNeb recommends a higher concentration product (0.083% or 0.5% solution for inhalation) for treatment of acute asthma exacerbations.
    Children 2 to 4 years: 0.63 to 1.25 mg/dose via oral inhalation 3 to 4 times daily as needed. FDA-approved labeling recommends to not exceed 4 doses/day. Doses should be delivered over 5 to 15 minutes. A higher concentration product (0.083% or 0.5% solution for inhalation) may be more appropriate for treatment of acute asthma exacerbations. In general, the National Asthma Education and Prevention Program (NAEPP) Expert Panel recommends albuterol 0.63 to 2.5 mg/dose via oral inhalation every 4 to 6 hours as needed for symptoms of bronchospasm.
    Children 5 to 12 years: 0.63 to 1.25 mg/dose via oral inhalation 3 to 4 times daily as needed. FDA-approved labeling recommends to not exceed 4 doses/day. Doses should be delivered over 5 to 15 minutes. A higher concentration product (0.083% or 0.5% solution for inhalation) may be more appropriate for treatment of acute exacerbations. In general, the National Asthma Education and Prevention Program (NAEPP) Expert panel recommends albuterol 1.25 to 5 mg/dose via oral inhalation every 4 to 8 hours as needed for bronchospasm.
    Oral dosage (oral syrup):
    Neonates*: Limited data. In a randomized, placebo-controlled trial enteral albuterol 0.15 mg/kg/dose every 8 hours for 96 hours improved pulmonary resistance in ventilator dependent premature neonates at risk for developing chronic lung disease (n = 30). Improvement was achieved without major cardiovascular side effects, although patients did experience statistically significant heart and respiratory rate increases deemed clinically unimportant by investigators.
    Infants* and Children younger than 2 years*: Safety and efficacy have not been established. Dosing is not available for this age group; however, 0.1 to 0.2 mg/kg/dose PO every 8 hours has been used in neonates and young children.
    Children 2 to 5 years: Initially, 0.1 mg/kg/dose PO every 8 hours (Max: 6 mg/day). If an adequate response is not obtained, dose may be gradually increased to 0.2 mg/kg/dose PO every 8 hours (Max: 12 mg/day).
    Children and Adolescents 6 to 14 years: Initially, 2 mg PO 3 to 4 times per day. If an adequate response is not obtained, dose may be increased gradually with caution. Max: 24 mg/day.
    Adolescents 15 years and older: Initially, 2 to 4 mg PO 3 to 4 times per day. If adequate response not obtained, dose may be increased gradually with caution. Max: 32 mg/day.
    Oral dosage (immediate-release tablet):
    Children 6 to 12 years: Initially, 2 mg PO 3 to 4 times per day. If an adequate response is not obtained, dose may be increased gradually with caution. Max: 24 mg/day.
    Adolescents: Initially, 2 to 4 mg PO 3 to 4 times per day. If an adequate response is not obtained, dose may be increased gradually with caution. Max: 32 mg/day.
    Oral dosage (extended-release tablets):
    Children 6 to 12 years: Initially, 4 mg PO every 12 hours. If an adequate response is not obtained, dose may be increased gradually with caution. Max: 24 mg/day. Albuterol 2 mg immediate-release tablets PO every 6 hours = 4 mg extended-release PO every 12 hours. In general, inhaled long-acting beta-agonists are preferred because they are longer-acting and have fewer adverse effects than oral sustained-release agents.
    Adolescents : Initially, 4 to 8 mg PO every 12 hours. If an adequate response is not obtained, dose may be increased gradually with caution. Max: 32 mg/day. Albuterol 2 mg immediate-release tablets PO every 6 hours = 4 mg extended-release PO every 12 hours. In general, inhaled long-acting beta-agonists are preferred because they are longer-acting and have fewer adverse effects than oral sustained-release agents.

    For exercise-induced bronchospasm prophylaxis:
    Oral inhalation dosage (metered-dose inhaler [MDI]; e.g., ProAir HFA, Ventolin HFA):
    Children younger than 4 years*: 1 to 2 puffs administered 5 to 20 minutes before exercise. Protection may last 2 to 4 hours. For those who use a short-acting beta-agonist on a daily basis, a controller agent (e.g., inhaled corticosteroid, leukotriene receptor antagonist) should be considered if albuterol tolerance develops.
    Children 4 years: 1 to 2 puffs administered 5 to 30 minutes before exercise. Protection may last 2 to 4 hours. For those who use a short-acting beta-agonist on a daily basis, a controller agent (e.g., inhaled corticosteroid, leukotriene receptor antagonist) should be considered if albuterol tolerance develops.
    Children and Adolescents 5 years and older: 2 puffs administered 5 to 30 minutes before exercise. Protection may last 2 to 4 hours. For those who use a short-acting beta-agonist on a daily basis, a controller agent (e.g., inhaled corticosteroid, leukotriene receptor antagonist) should be considered if albuterol tolerance develops.
    Oral inhalation dosage (dry-powder inhaler [DPI]; e.g., ProAir RespiClick, ProAir Digihaler):
    Children and Adolescents 4 years and older: 2 oral inhalations (90 mcg/inhalation) administered 15 to 30 minutes before exercise. The action of albuterol inhalation powder should last for 4 to 6 hours. Do not use the device with a spacer or volume holding chamber. For those who use a short-acting beta-agonist daily, a controller agent (e.g., an inhaled corticosteroid, leukotriene receptor antagonist) should be considered if albuterol tolerance develops.

    For the adjunctive acute treatment of hyperkalemia*:
    Oral inhalation dosage (nebulized solution):
    Neonates: 400 mcg via oral inhalation administered every 2 hours was effective in a study of mechanically ventilated neonates weighing less than 2,000 grams (n = 19). Doses were repeated every 2 hours until serum potassium concentrations fell to less than 5 mmol/L, the patient experienced adverse effects, or the maximum of 12 doses was reached. Adjuvant or alternative therapy is warranted for patients experiencing electrocardiographic (ECG) changes or significantly elevated serum potassium concentrations (e.g., more than 7.5 mmol/L).
    Infants: Although not specifically studied in this population, nebulized albuterol 2.5 mg in children weighing less than 25 kg every 2 hours was effective in pediatric end-stage renal failure patients. Smaller doses for younger infants may be necessary. A dose of 400 mcg every 2 hours was effective in lowering serum potassium concentrations to less than 5 mmol/L in mechanically ventilated newborns weighing less than 2,000 grams. Adjuvant or alternative therapy is warranted for patients experiencing electrocardiographic changes or significantly elevated serum potassium concentrations.
    Children weighing less than 25 kg: 2.5 mg/dose via oral inhalation was effective in a small study of pediatric patients (5 to 18 years of age) with end-stage renal failure (n = 11). Doses were repeated every 2 hours as needed. Adjuvant or alternative therapy is warranted for patients experiencing electrocardiographic (ECG) changes or significantly elevated serum potassium concentrations.
    Children and Adolescents weighing 25 kg or more: 5 mg/dose via oral inhalation was effective in a small study of pediatric patients (5 to 18 years of age) with end-stage renal failure (n = 11). Doses were repeated every 2 hours as needed. Adjuvant or alternative therapy is warranted for patients experiencing electrocardiographic (ECG) changes or significantly elevated serum potassium concentrations.

    Maximum Dosage Limits:
    -Neonates
    Safety and efficacy have not been established; nebulizer inhalation maximum dependent on patient response and formulation used.
    -Infants
    Safety and efficacy have not been established; nebulizer inhalation maximum dependent on patient response and formulation used.
    -Children
    1 year: Safety and efficacy have not been established; nebulizer inhalation maximum dependent on patient response and formulation used.
    2 to 3 years: 0.6 mg/kg/day PO (Max: 12 mg/day PO) for albuterol syrup; FDA-approved labeling for nebulizer solution for oral inhalation recommends not exceeding 4 doses/day or 10 mg/day (0.083% or 0.5% nebulizer solution), 2.5 mg/day (0.63 mg/3 mL nebulizer solution), and 5 mg/day (1.25 mg/3 mL nebulizer solution). Higher maximum dosages for inhalation products have been recommended in NAEPP guidelines for acute exacerbations of asthma.
    4 to 5 years: 0.6 mg/kg/day PO (Max: 12 mg/day PO) for albuterol syrup; FDA-approved labeling for inhaler recommends not exceeding 12 puffs/day; FDA-approved labeling for nebulizer solution for oral inhalation recommends not exceeding 4 doses/day or 10 mg/day (0.083% or 0.5% nebulizer solution), 2.5 mg/day (0.63 mg/3 mL nebulizer solution), and 5 mg/day (1.25 mg/3 mL nebulizer solution). Higher maximum dosages for inhalation products have been recommended in NAEPP guidelines for acute exacerbations of asthma.
    6 to 12 years: 24 mg/day PO for syrup and tablets; FDA-approved labeling for inhaler recommends not exceeding 12 puffs/day; FDA-approved labeling for nebulizer solution for oral inhalation recommends not exceeding 4 doses/day or 10 mg/day (0.083% or 0.5% nebulizer solution), 2.5 mg/day (0.63 mg/3 mL nebulizer solution), and 5 mg/day (1.25 mg/3 mL nebulizer solution). Higher maximum dosages for inhalation products have been recommended in NAEPP guidelines for acute exacerbations of asthma.
    -Adolescents
    13 to 14 years: 24 mg/day PO for syrup; 32 mg/day PO for tablets; FDA-approved labeling for inhaler recommends not exceeding 12 puffs/day; FDA-approved labeling for nebulizer solution for oral inhalation recommends not exceeding 4 doses/day or 10 mg/day (0.083% or 0.5% nebulizer solution), 2.5 mg/day (0.63 mg/3 mL nebulizer solution), and 5 mg/day (1.25 mg/3 mL nebulizer solution). Higher maximum dosages for inhalation products have been recommended in NAEPP guidelines for acute exacerbations of asthma.
    15 to 17 years: 32 mg/day PO for syrup and tablets; FDA-approved labeling for inhaler recommends not exceeding 12 puffs/day; FDA-approved labeling for nebulizer solution for oral inhalation recommends not exceeding 4 doses/day or 10 mg/day (0.083% or 0.5% nebulizer solution), 2.5 mg/day (0.63 mg/3 mL nebulizer solution), and 5 mg/day (1.25 mg/3 mL nebulizer solution). Higher maximum dosages for inhalation products have been recommended in NAEPP guidelines for acute exacerbations of asthma.

    Patients with Hepatic Impairment Dosing
    Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

    Patients with Renal Impairment Dosing
    Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

    *non-FDA-approved indication

    Monograph content under development

    Mechanism of Action: Albuterol is a moderately selective beta2-adrenergic agonist that stimulates receptors of the smooth muscle in the lungs, uterus, and vasculature supplying skeletal muscle. Albuterol is racemic beta-agonist, comprised of an equal mixture of R- and S-isomers.

    Relief of Bronchoconstriction
    The R-isomer, known as levalbuterol, is primarily responsible for bronchodilation. Although not confirmed during clinical trials in humans, the S-isomer of albuterol has been shown to increase airway reactivity in animal models. The net result of beta2-receptor agonism in the lungs is relaxation of bronchial and tracheal smooth muscles, which in turn relieves bronchospasm, reduces airway resistance, facilitates mucous drainage, and increases vital capacity. Stimulation of beta2-receptors on peripheral vascular smooth muscle can cause vasodilation and a modest decrease in diastolic blood pressure. Intracellularly, the actions of albuterol are mediated by cyclic-3',5'-adenosine monophosphate (cAMP), the production of which is augmented by beta2-stimulation. Albuterol is believed to work by activating adenyl cyclase, the enzyme responsible for generating cAMP, an intracellular mediator. Increased cAMP leads to activation of protein kinase A, which inhibits phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in bronchial smooth muscle relaxation. Increased cAMP also inhibits the release of histamine, leukotriene, and prostaglandin D2, and tumor necrosis factor alpha from mast cells. Inhibition of mediator release is believed to inhibit bronchoconstriction secondary to exercise and cold dry air.

    Treatment of Hyperkalemia
    Albuterol is an effective adjunctive treatment for hyperkalemia; beta2-adrenergic stimulation results in intracellular accumulation of serum potassium due to stimulation of the sodium-potassium adenosine triphosphatase (Na/K ATPase) pump, leading to moderate degrees of hypokalemia.

    Pharmacokinetics: Albuterol can be administered as oral tablets or syrup, but is more commonly administered by oral inhalation. Intravenous studies in animals have shown that albuterol crosses the blood-brain barrier, reaching brain concentrations that amount to 5% of the plasma concentrations. After systemic administration to healthy adult volunteers, the volume of distribution was found to be is relatively large (156 +/- 381 L), indicating extensive extravascular uptake. Protein binding is negligible (10%). Albuterol is preferentially metabolized in the gastrointestinal tract via sulfotransferase to inactive compounds; however, a significant amount (25% to 45%) is excreted as unchanged drug. The primary route of elimination is through renal excretion; a small amount (< 20%) can be detected in the feces. In adults, the elimination half-life of albuterol is approximately 4 to 6 hours, with the extended release oral product having a longer half-life of approximately 9 hours.

    Affected cytochrome P450 isoenzymes: none


    -Route-Specific Pharmacokinetics
    Oral Route
    Immediate-release formulations
    Immediate-release albuterol is rapidly absorbed after oral administration, obtaining Cmax (14 to 18 ng/mL) within 2 to 3 hours. Onset of pulmonary improvement can usually be seen within 30 minutes. Clinically significant improvement (defined as maintaining at least a 15% increase in FEV1 and a 20% increase in mid-expiratory flow rate over baseline) was recorded for up to 6 hours in a controlled clinical trial of 55 children. Elimination half-life is 5 hours.

    Extended-release formulations
    The bioavailability of extended-release (ER) tablets is 100% relative to the immediate-release (IR) tablets at steady state. Albuterol ER has a lower mean Cmax (14 ng/mL) and longer Tmax (6 hours) when compared to IR formulations. Fluctuations in plasma concentrations are similar for albuterol extended-release tablets administered at 12-hour intervals and immediate-release tablets administered at 6-hour intervals. AUC for both formulations is similar (130 ng x hr/mL). Elimination half-life of the ER formulation is approximately 9 hours. Food decreases the rate of absorption without altering the extent of bioavailability. Single dose studies have indicated administration with food causes a more gradual increase in the fraction of the dose absorbed compared to fasting conditions.

    Inhalation Route
    During studies, the majority of the nebulized albuterol dose administered has been recovered from the nebulizer apparatus and/or expired air; less than 20% of albuterol administered is systemically absorbed. At recommended doses, the bioavailability of inhaled albuterol is low. Onset of pulmonary improvement occurs within 2 to 20 minutes. After a 3 mg nebulized dose, peak concentrations of 2.1 ng/mL (range: 1.4 to 3.2 ng/mL) are reached in approximately 30 minutes and peak pulmonary improvement is seen at 1 to 2 hours. Duration of action is 2 to 6 hours. Half-life is approximately 4.6 to 6 hours. Administration via nebulization does not appear to significantly alter the pharmacokinetics of albuterol. The systemic exposure in children 6 to 11 years of age is similar to that of adults after 180 mcg single dose oral inhalation. A small study in 11 healthy children (aged 4 to 11 years) who received a single dose of albuterol inhalation aerosol 180 mcg via metered-dose inhaler, demonstrated a least square mean (SE) Cmax and AUC of 1100 (+/-1.18) pg/mL and 5120 (+/-1.15) pg x hr/mL, respectively. The least square mean (SE) terminal plasma half-life was 166 (+/-7.8) minutes. In a cumulative dose study, the AUC of the dry powder inhalation was similar to the aerosol formulation (metered dose inhaler); however, the Cmax was about one-third higher in the dry powder inhalation group.


    -Special Populations
    Renal Impairment
    The pharmacokinetics of albuterol were studied in a small number of subjects with creatinine clearances between 7 to 53 mL/minute in comparison to healthy volunteers. The half-life was unchanged; however, albuterol clearance was decreased by 67% in those with renal impairment. Caution should be used when administering high doses of inhaled albuterol to patients with renal impairment.

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