CLASSES
Oral Beta-2 Agonists
Respiratory Short-Acting Beta-2 Agonists (SABA)
DESCRIPTION
Short-acting beta-2 agonist (SABA); primarily used as a nebulizer solution or oral inhaler
Used for the relief of acute bronchospasm and episodic wheezing in patients with asthma or exercise-induced bronchospasm; used as reliever-therapy for COPD in adults
Inhaled albuterol is preferred for all uses vs. oral albuterol due to side-effect profile
COMMON BRAND NAMES
Accuneb, ProAir digihaler, Proair HFA, ProAir RespiClick, Proventil, Proventil HFA, Proventil Repetabs, Respirol, Ventolin, Ventolin HFA, Ventolin Syrup, Volmax, VoSpire ER
HOW SUPPLIED
Accuneb/Albuterol/Albuterol Sulfate/Proventil Respiratory (Inhalation) Sol: 0.083%, 0.5%, 0.5mL, 0.63mg, 1.25mg, 2.5mg, 3mL
Albuterol/Albuterol Sulfate/Proventil Repetabs Oral Tab: 2mg, 4mg
Albuterol/Albuterol Sulfate/Ventolin/Ventolin Syrup Oral Syrup: 2mg, 5mL
Albuterol/Albuterol Sulfate/Volmax/VoSpire ER Oral Tab ER: 4mg, 8mg
Albuterol/Proair HFA/Proventil/Proventil HFA/Respirol/Ventolin/Ventolin HFA Respiratory (Inhalation) Aer Met: 1actuation, 90mcg
ProAir digihaler/ProAir RespiClick Respiratory (Inhalation) Inhalant: 1actuation, 90mcg
DOSAGE & INDICATIONS
For the treatment of asthma exacerbation.
Respiratory (Inhalation) dosage (inhalation aerosol; e.g., ProAir HFA, Proventil HFA, Ventolin HFA)
Adults
360 to 900 mcg (4 to 10 actuations of 90 mcg/actuation) inhaled by mouth every 20 minutes for the first hour for mild to moderate exacerbations, then 360 to 900 mcg (4 to 10 actuations) every 3 to 4 hours up to 540 to 900 mcg (6 to 10 actuations) every 1 to 2 hours, or more often.
Children and Adolescents 6 to 17 years
360 to 900 mcg (4 to 10 actuations of 90 mcg/actuation) inhaled by mouth every 20 minutes for the first hour for mild to moderate exacerbations, then 360 to 900 mcg (4 to 10 actuations) every 3 to 4 hours up to 540 to 900 mcg (6 to 10 actuations) every 1 to 2 hours, or more often.
Infants and Children 1 month to 5 years
180 to 540 mcg (2 to 6 actuations of 90 mcg/actuation) inhaled by mouth every 20 minutes for the first hour, then 180 to 270 mcg (2 to 3 actuations) every hour as needed. Delivery should occur with a spacer and a mask.
Respiratory (Inhalation) dosage (inhalation solution)
Adults
2.5 mg inhaled by nebulizer every 20 minutes for the first hour for mild to moderate exacerbations, then 2.5 mg every 3 to 4 hours and up to 2.5 mg every 1 to 2 hours, or more often. Usual dose: 2.5 mg inhaled by nebulizer 3 to 4 times daily.
Adolescents
2.5 mg inhaled by nebulizer every 20 minutes for the first hour for mild to moderate exacerbations, then 2.5 mg every 3 to 4 hours and up to 2.5 mg every 1 to 2 hours, or more often. Usual dose: 2.5 mg inhaled by nebulizer 3 to 4 times daily.
Children 6 to 12 years weighing 15 kg or more
2.5 mg inhaled by nebulizer every 20 minutes for the first hour for mild to moderate exacerbations, then 2.5 mg every 3 to 4 hours up to 2.5 mg every 1 to 2 hours, or more often. Usual dose: 0.63 to 2.5 mg inhaled by nebulizer 3 to 4 times daily.
Children 6 to 12 years weighing less than 15 kg
2.5 mg inhaled by nebulizer every 20 minutes for the first hour for mild to moderate exacerbations, then 2.5 mg every 3 to 4 hours up to 2.5 mg every 1 to 2 hours, or more often. Usual dose: 0.63 to 1.25 mg inhaled by nebulizer 3 to 4 times daily.
Children 2 to 5 years weighing 15 kg or more
2.5 mg inhaled by nebulizer every 20 minutes for the first hour for acute exacerbation, with subsequent reassessment. Usual dose: 0.63 to 2.5 mg inhaled by nebulizer 3 to 4 times daily.
Children 2 to 5 years weighing less than 15 kg
2.5 mg inhaled by nebulizer every 20 minutes for the first hour for acute exacerbation, with subsequent reassessment. Usual dose: 0.63 to 1.25 mg inhaled by nebulizer 3 to 4 times daily.
Infants† and Children† younger than 2 years
2.5 mg inhaled by nebulizer every 20 minutes for the first hour for acute exacerbation, with subsequent reassessment.
For the treatment of transient increase in bronchospasm (e.g., episodic wheezing) as asthma reliever therapy.
Respiratory (Inhalation) dosage (inhalation aerosol; e.g., ProAir HFA, Proventil HFA, Ventolin HFA)
Adults
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth every 4 to 6 hours as needed. In some patients, 90 mcg (1 actuation) every 4 hours may be sufficient. Max: 1,080 mcg/day (12 actuations/day).
Children and Adolescents 4 to 17 years
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth every 4 to 6 hours as needed. In some patients, 90 mcg (1 actuation) every 4 hours may be sufficient. Max: 1,080 mcg/day (12 actuations/day).
Respiratory (Inhalation) dosage (inhalation powder; e.g., ProAir RespiClick, ProAir Digihaler)
Adults
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth every 4 to 6 hours as needed. In some patients, 90 mcg (1 actuation) every 4 hours may be sufficient. Max: 1,080 mcg/day (12 actuations/day).
Children and Adolescents 4 to 17 years
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth every 4 to 6 hours as needed. In some patients, 90 mcg (1 actuation) every 4 hours may be sufficient. Max: 1,080 mcg/day (12 actuations/day).
Respiratory (Inhalation) dosage (inhalation solution)
Adults
2.5 mg inhaled by nebulizer 3 to 4 times daily as needed. Usual Max: 10 mg/day.
Adolescents
2.5 mg inhaled by nebulizer 3 to 4 times daily as needed. Usual Max: 10 mg/day.
Children 6 to 12 years weighing 15 kg or more
0.63 or 1.25 mg inhaled by nebulizer 3 or 4 times daily as needed. Those with more severe asthma (baseline FEV1 less than 60% predicted), weight more than 40 kg, or patients 11 to 12 years of age may achieve a better initial response with the 1.25 mg dose. Children weighing at least 15 kg may receive up to 2.5 mg inhaled by nebulizer 3 to 4 times daily if needed.
Children 6 to 12 years weighing less than 15 kg
0.63 or 1.25 mg inhaled by nebulizer 3 or 4 times daily as needed. Those with more severe asthma (baseline FEV1 less than 60% predicted) or patients 11 to 12 years of age may achieve a better initial response with the 1.25 mg dose.
Children 2 to 5 years weighing 15 kg or more
0.63 or 1.25 mg inhaled by nebulizer 3 or 4 times daily as needed. Those with more severe asthma (baseline FEV1 less than 60% predicted) may achieve a better initial response with the 1.25 mg dose. Children weighing at least 15 kg may receive up to 2.5 mg inhaled by nebulizer 3 to 4 times daily if needed.
Children 2 to 5 years weighing less than 15 kg
0.63 or 1.25 mg inhaled by nebulizer 3 or 4 times daily as needed. Those with more severe asthma (baseline FEV1 less than 60% predicted) may achieve a better initial response with the 1.25 mg dose.
Oral dosage (oral solution or syrup)
Adults
2 to 4 mg PO 3 to 4 times daily. Start with a 2 mg dose in the geriatric adult. If adequate response not obtained, dose may be increased gradually with caution, up to 8 mg PO 4 times daily. Max: 32 mg/day. Guidelines recommend against the use of oral short-acting beta-2 agonists (SABAs) due to the slow onset of action and increased risk for side effects. Use inhaled SABAs for acute bronchospasm; do not use oral agents.
Adolescents 15 to 17 years
2 to 4 mg PO 3 to 4 times daily. If adequate response not obtained, dose may be increased gradually with caution to 8 mg PO 4 times daily. Max: 32 mg/day. Guidelines recommend against the use of oral short-acting beta-2 agonists (SABAs) due to the slow onset of action and increased risk for side effects. Use inhaled SABAs for acute bronchospasm; do not use oral agents.
Children and Adolescents 6 to 14 years
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. Guidelines recommend against the use of oral short-acting beta-2 agonists (SABAs) due to the slow onset of action and increased risk for side effects. Use inhaled SABAs for acute bronchospasm; do not use oral agents.
Children 2 to 5 years
0.1 mg/kg/dose PO 3 times per day. If an adequate response is not obtained, may gradually increase, up to 0.2 mg/kg/dose PO 3 times per day. Max: 12 mg/day. Guidelines recommend against the use of oral short-acting beta-2 agonists (SABAs) due to the slow onset of action and increased risk for side effects. Use inhaled SABAs for acute bronchospasm; do not use oral agents.
Infants† and Children younger than 2 years†
Safety and efficacy have not been established. 0.1 to 0.2 mg/kg/dose PO every 8 hours has been used in neonates and young children.
Oral dosage (immediate-release tablets)
Adults
2 to 4 mg PO 3 to 4 times daily. Start with 2 mg per dose in the geriatric patient. If adequate response not obtained, dose may be increased gradually with caution to 8 mg PO 4 times daily. Max: 32 mg/day. Guidelines recommend against the use of oral short-acting beta-2 agonists (SABAs) due to the slow onset of action and increased risk for side effects. Use inhaled SABAs for acute bronchospasm; do not use oral agents.
Adolescents
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. Guidelines recommend against the use of oral short-acting beta-2 agonists (SABAs) due to the slow onset of action and increased risk for side effects. Use inhaled SABAs for acute bronchospasm; do not use oral agents.
Children 6 to 12 years
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. Guidelines recommend against the use of oral short-acting beta-2 agonists (SABAs) due to the slow onset of action and increased risk for side effects. Use inhaled SABAs for acute bronchospasm; do not use oral agents.
Oral dosage (extended-release tablets)
Adults
4 to 8 mg ER PO every 12 hours. Start with 4 mg per dose in the geriatric patient. If an adequate response is not obtained, dose may be increased gradually with caution. Max: 32 mg/day. DOSE CONVERSION: 2 mg immediate-release PO every 6 hours = 4 mg extended-release PO every 12 hours. Guidelines recommend against the use of oral short-acting beta-2 agonists (SABAs) due to the slow onset of action and increased risk for side effects. Use inhaled SABAs for acute bronchospasm; do not use oral agents.
Adolescents
4 to 8 mg ER PO every 12 hours. If an adequate response is not obtained, dose may be increased gradually with caution. Max: 32 mg/day. DOSE CONVERSION: 2 mg immediate-release PO every 6 hours = 4 mg extended-release PO every 12 hours. Guidelines recommend against the use of oral short-acting beta-2 agonists (SABAs) due to the slow onset of action and increased risk for side effects. Use inhaled SABAs for acute bronchospasm; do not use oral agents.
Children 6 to 12 years
4 mg ER PO every 12 hours. If an adequate response is not obtained, dose may be increased gradually with caution. Max: 24 mg/day. DOSE CONVERSION: 2 mg immediate-release PO every 6 hours = 4 mg extended-release PO every 12 hours. Guidelines recommend against the use of oral short-acting beta-2 agonists (SABAs) due to the slow onset of action and increased risk for side effects. Use inhaled SABAs for acute bronchospasm; do not use oral agents.
For the treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD) (e.g., chronic bronchitis or emphysema).
Respiratory (Inhalation) dosage (inhalation aerosol or powder; e.g., Proventil HFA, Ventolin HFA, ProAir HFA, ProAir Digihaler)
Adults
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth every 4 to 6 hours as needed for symptoms. In some patients, 90 mcg (1 actuation) every 4 hours may be sufficient. Max: 1,080 mcg/day (12 actuations/day). Optimal dosing for acute COPD exacerbation is not established; adjust dose according to clinical symptoms or the development of adverse effects; higher or more frequent dosing may be needed. According to the Global Initiative for Chronic Obstructive Lung Disease (GOLD) guidelines, inhaled albuterol may be used as first-line therapy in Group A and may also be used in Groups B, C, and D for additional symptom control. Short-acting beta-2 agonists (SABAs) are preferred therapy for acute COPD exacerbation, used with or without a short-acting anticholinergic. No significant differences in FEV1 have been demonstrated between metered-dose inhalers (with or without a spacer) and nebulizers for SABAs in clinical trials; nebulizers may be more convenient for patients who are more acutely ill.[63765]
Respiratory (Inhalation) dosage (inhalation solution)
Adults
2.5 mg inhaled by nebulizer every 6 to 8 hours as needed. Max: 10 mg/day. Optimal dosing for a COPD exacerbation is not established; adjust dose according to clinical symptoms or the development of adverse effects. A nebulized albuterol dose of 5 mg every 4 hours has been used, as well as a regimen of 2.5 mg given every 20 minutes for 2 hours. According to the Global Initiative for Chronic Obstructive Lung Disease (GOLD) guidelines for COPD, inhaled albuterol may be used as first-line therapy in Group A and may also be used in Groups B, C, and D for additional symptom control. Short-acting beta-2 agonists (SABAs) are preferred therapy for the treatment of acute COPD exacerbation, used with or without a short-acting anticholinergic. No significant differences in FEV1 have been demonstrated between metered-dose inhalers (with or without a spacer) and nebulizers for SABAs in clinical trials; nebulizers may be more convenient for patients that are more acutely ill.[63765]
Oral dosage (immediate-release tablets, oral solution or syrup)
Adults
2 to 4 mg PO every 6 to 8 hours. Geriatric patients should receive 2 mg PO every 6 to 8 hours initially. Maximum: 32 mg/day PO. Use not recommended by guidelines; inhaled bronchodilators are preferred.
Oral dosage (extended-release tablets)
Adults
4 to 8 mg PO every 12 hours (Maximum: 32 mg/day PO). Use not recommended by guidelines; inhaled bronchodilators are preferred.
For bronchospasm prophylaxis, including exercise-induced bronchospasm prophylaxis and bronchospasm prophylaxis in persons with cystic fibrosis†.
For exercise-induced bronchospasm prophylaxis.
Respiratory (Inhalation) dosage (inhalation aerosol; e.g., ProAir HFA, Proventil HFA, Ventolin HFA)
Adults
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth 15 to 30 minutes before exercise. A controller agent (e.g., daily inhaled corticosteroid) is recommended to be used along with as-needed and pre-exercise short-acting beta-agonists like albuterol.
Children and Adolescents 4 to 17 years
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth 15 to 30 minutes before exercise. A controller agent (e.g., daily inhaled corticosteroid) is recommended to be used along with as-needed and pre-exercise short-acting beta-agonists like albuterol.
Children† 1 to 3 years
90 to 180 mcg (1 to 2 actuations of 90 mcg/actuation) inhaled by mouth 15 minutes (range: 5 to 20 minutes) before exercise.
Respiratory (Inhalation) dosage (inhalation powder; ProAir RespiClick, ProAir Digihaler)
Adults
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth 15 to 30 minutes before exercise.[59350] [64470] A controller agent (e.g., daily inhaled corticosteroid) is recommended to be used along with as-needed and pre-exercise short-acting beta-agonists like albuterol.
Children and Adolescents 4 to 17 years
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth 15 to 30 minutes before exercise.[59350] [64470] A controller agent (e.g., daily inhaled corticosteroid) is recommended to be used along with as-needed and pre-exercise short-acting beta-agonists like albuterol.
For bronchospasm prophylaxis prior to the administration of other inhaled medications in persons with cystic fibrosis†.
Respiratory (Inhalation) dosage (inhalation aerosol; e.g., ProAir HFA, Proventil HFA, Ventolin HFA)
Adults
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth prior to other inhaled medications, every 8 to 24 hours depending on regimen.
Children and Adolescents 6 to 17 years
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth prior to other inhaled medications, every 8 to 24 hours depending on regimen.
For adjunctive treatment of neonatal respiratory illness, such as those with suspected airway reactivity†, bronchopulmonary dysplasia†, or chronic lung disease (CLD)†.
Respiratory (Inhalation) dosage (inhalation solution)
Neonates†
1.25 to 2.5 mg inhaled by nebulizer was the most common 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 NICUs 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. The optimal frequency of administration has not been clearly defined in the neonatal population. Of note, significantly larger doses of albuterol are used in nebulization when compared to administration with metered-dose inhalers (MDIs) due to the inefficiency of nebulized drug delivery.
Respiratory (Inhalation) dosage (inhalation aerosol)
Neonates†
90 to 180 mcg (1 to 2 actuations of 90 mcg/actuation) via the inspiratory limb of the mechanical ventilator circuit appeared 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 actuations as the average dose used. Frequency of administration has not been clearly defined in the neonatal population. Of note, MDIs with inline spacers have demonstrated superior drug delivery when compared to jet nebulizers in simulated neonatal lung models.
Oral dosage (oral solution or syrup)
Neonates†
Limited data. 0.15 mg/kg/dose enterally every 8 hours for 96 hours improved pulmonary resistance in ventilator-dependent premature neonates at risk for developing chronic lung disease (n = 30). Major cardiovascular side effects did not occur; heart and respiratory rate increases were deemed clinically unimportant by investigators.
For the adjunctive emergency acute treatment of hyperkalemia†.
NOTE: Place patients on a cardiac monitor. Avoid in patients with preexisting cardiac arrhythmias. Adjuvant or alternative therapy is warranted for patients experiencing ECG changes or significantly elevated serum potassium concentrations (e.g., more than 7.5 mmol/L). Albuterol decreases serum potassium by approximately 1 to 1.5 mEq/L within an hour of administration. Concentrations begin to fall within 30 minutes of administration and may remain depressed up to 300 minutes when albuterol is nebulized.
Respiratory (Inhalation) dosage (inhalation solution)
Adults
10 to 20 mg inhaled by nebulizer as a single dose.
Children and Adolescents weighing more than 50 kg
10 mg/dose inhaled by nebulizer every 20 minutes for 1 to 2 doses.
Children and Adolescents weighing 25 to 50 kg
5 mg/dose inhaled by nebulizer every 20 minutes for 1 to 2 doses. In a small study (n = 11), doses were repeated every 2 hours as needed.[30593]
Children weighing less than 25 kg
2.5 mg/dose inhaled by nebulizer every 20 minutes for 1 to 2 doses. In a small study (n = 11), doses were repeated every 2 hours as needed.[30593]
Infants
2.5 mg/dose inhaled by nebulizer every 20 minutes for 1 to 2 doses. In a small study (n = 11), doses were repeated every 2 hours as needed.[30593] Smaller doses for younger/premature infants may be necessary (e.g., 400 mcg every 2 hours).[30594]
Neonates
400 mcg inhaled by nebulizer administered every 2 hours was effective in a study of mechanically ventilated neonates weighing less than 2,000 g (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.
†Indicates off-label use
MAXIMUM DOSAGE
Adults
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.
Geriatric
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.
Adolescents
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.
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.
Children
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.
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.
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.
1 year: 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.
Neonates
Safety and efficacy have not been established; nebulizer inhalation maximum dependent on patient response and formulation used.
DOSING CONSIDERATIONS
Hepatic Impairment
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Renal Impairment
Specific guidelines for dosage adjustments in renal impairment are not available. Caution may be warranted during the administration of high doses in patients with renal impairment, as renal clearance is reduced.
ADMINISTRATION
Oral Administration
Administer with meals to minimize gastric irritation.
Oral Solid Formulations
Immediate release tablets:
Administer orally on a regular dosage schedule as directed by prescriber.
Extended-release tablets:
Swallow whole, do not chew or crush the extended-release tablets.
Oral Liquid Formulations
Administer using a calibrated oral measuring device to ensure accurate dosing.
Inhalation Administration
Aerosol inhalation (e.g., ProAir HFA, Ventolin HFA)
Instruct patient on proper inhalation technique; see the specific product's "Instructions for Use" from the manufacturer.
Make sure the canister is firmly seated in the plastic mouthpiece adapter before each use.
Shake the inhaler well. Prime the inhaler before the first use by spraying four times into the air, away from the eyes and face. When the inhaler has not been used for a prolonged period or it has been dropped, prime by spraying two to four (2 to 4) times into the air away from the face, according to the specific inhaler type.[31823] [33925]
For patients of any age unable to coordinate inhalation and actuation, a spacer or valved holding chamber (VHC) should be used.
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 3 to 5 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. The patient will breathe out through the mouth and push as much air from the lungs as the patient can. Put the mouthpiece in the mouth and have patient close their 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.
Following administration, instruct patient to rinse the mouth with water to minimize dry mouth.
To avoid the spread of infection, do not use the inhaler for more than one person.
Clean the plastic mouthpiece of the inhaler at least once a week; some manufacturers advocate daily cleaning. 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 before next use (e.g., over-night).[31823] [33925]
Discard medication and inhaler after expired or once the labeled number of inhalations have been used, whichever comes first; some products may have an inhalation counter. Ventolin HFA expires 12 months after medication removal from the foil pouch.[49951] Other products should be discarded when the labeled number of actuations has been used or by the expiration date printed on original packaging; whichever comes first.[31823] [28532]
Valved holding chamber (VHC) with aerosol inhalation:
Delivery of a pressurized metered-dose inhaler (MDI) with a spacer with or without a mouthpiece may be preferred in adults and children with asthma exacerbation. Nebulizers can transmit respiratory viral particles.
For infants and children up to 3 years of age, a pressurized MDI plus spacer with face mask is recommended; a nebulizer with a face mask is an alternative.
For children 4 to 5 years old, a pressurized MDI plus spacer is recommended; a pressurized MDI plus spacer with face mask or a nebulizer with a face mask is an alternative.
In children 2 years and older with acute asthma, the use of an MDI plus valved holding chamber (VHC) is as effective as nebulized therapy when appropriate administration technique is used. The method of delivery does not result in a significant difference in hospital admission rates in children seen in the emergency department or equivalent community setting. Additionally, the length of stay in the emergency department is shorter when a VHC was used.[56384]
Powder for Inhalation (e.g., ProAir RespiClick, ProAir Digihaler)
Instruct patient on proper inhalation technique; see the specific product's "Instructions for Use" from the manufacturer.
Before using for the first time, check the dose counter window to ensure that the inhaler is full and the number "200" is in the window. The dose counter will count down each time the mouthpiece cap is opened and closed. The dose counter only displays even numbers (example: 200, 198, 196, etc.) in the window.
Hold the inhaler upright while opening the cap fully. When the cap is opened, a dose of albuterol will be activated for delivery of the medicine. Make sure a "click" sound is heard; if not, the inhaler may not be activated to give a dose of medicine.
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 they can. Be careful that the patient does not breathe out into the inhaler mouthpiece. Put the mouthpiece in the mouth and have the patient close their 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. The patient should hold their breath for about 10 seconds or as long as they comfortably can.
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.
The inhaler contains a powder and must be kept clean and dry at all times. Do not wash or put any part of the inhaler in water. If the mouthpiece needs cleaning, gently wipe it with a dry cloth or tissue.
When there are "20" doses left, the dose counter will change to red; refill the prescription or contact the doctor for another prescription.
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.
Throw away the inhaler 13 months after removing it from the foil pouch for the first time, when the dose counter displays "0", or after the expiration date on the package, whichever comes first.[59350] [64470]
Inhalation solution for nebulization
For 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 0.9% Sodium Chloride Solution 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.
Some nebulizer solutions state a grace period of 1 week is allowed after removal from the foil pouch.[43674] Other products state that the vials should be stored in the foil pouch until time of use.[49953] Refer to the specific product for this information.
STORAGE
Generic:
- Protect from light
- Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F
- Store in original package until time of use
Accuneb:
- After opening the foil pouch, product should be used within 2 weeks
- Avoid excessive heat (above 104 degrees F)
- Discard product if it contains particulate matter, is cloudy, or discolored
- Protect from light
- Store between 36 to 77 degrees F
- Store unused product in foil pouch
ProAir digihaler:
- Avoid excessive humidity
- Store away from excessive heat and cold
- Store between 59 to 77 degrees F
Proair HFA:
- Avoid extreme temperatures
- Exposure to temperatures above 120 degrees F may cause bursting
- For best results, product should be at room temperature before use
- Keep away from heat and flame
- Store at controlled room temperature (between 68 and 77 degrees F)
- Store inhaler with mouthpiece down
ProAir RespiClick:
- Avoid excessive humidity
- Store away from excessive heat and cold
- Store between 59 to 77 degrees F
Proventil:
- Avoid extreme temperatures
- Exposure to temperatures above 120 degrees F may cause bursting
- For best results, product should be at room temperature before use
- Keep away from heat and flame
- Store at controlled room temperature (between 68 and 77 degrees F)
- Store inhaler with mouthpiece down
Proventil HFA:
- Avoid extreme temperatures
- Exposure to temperatures above 120 degrees F may cause bursting
- For best results, product should be at room temperature before use
- Keep away from heat and flame
- Store at controlled room temperature (between 68 and 77 degrees F)
- Store inhaler with mouthpiece down
Proventil Repetabs:
- Keep away from heat and flame
- Protect from light
- Protect from moisture
- Store at controlled room temperature (between 68 and 77 degrees F)
- Store in a cool, well ventilated, dry place
Respirol :
- Avoid extreme temperatures
- Exposure to temperatures above 120 degrees F may cause bursting
- For best results, product should be at room temperature before use
- Keep away from heat and flame
- Store at controlled room temperature (between 68 and 77 degrees F)
- Store inhaler with mouthpiece down
Ventolin:
- Avoid extreme temperatures
- Exposure to temperatures above 120 degrees F may cause bursting
- For best results, product should be at room temperature before use
- Keep away from heat and flame
- Store at controlled room temperature (between 68 and 77 degrees F)
- Store inhaler with mouthpiece down
Ventolin HFA:
- Avoid extreme temperatures
- Exposure to temperatures above 120 degrees F may cause bursting
- For best results, product should be at room temperature before use
- Keep away from heat and flame
- Store at controlled room temperature (between 68 and 77 degrees F)
- Store inhaler with mouthpiece down
Ventolin Syrup:
- Store at controlled room temperature (between 68 and 77 degrees F)
Volmax:
- Store at controlled room temperature (between 68 and 77 degrees F)
VoSpire ER:
- Store at controlled room temperature (between 68 and 77 degrees F)
CONTRAINDICATIONS / PRECAUTIONS
Deterioration of asthma, paradoxical bronchospasm
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. Additionally, increased albuterol use 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 during therapy with albuterol, 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. 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.
Albuterol hypersensitivity, levalbuterol hypersensitivity, milk protein hypersensitivity
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 since the formulation contains lactose, which contains milk proteins.[59350] [64470] 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.[31823] [43674] [44010] [49951] [59350] [64470]
Hyperthyroidism, pheochromocytoma, seizure disorder, thyrotoxicosis
Albuterol, like other sympathomimetic amines, should be used cautiously in patients with a history of seizure disorder, hyperthyroidism (thyrotoxicosis), pheochromocytoma, or unusual responsiveness to other sympathomimetic amines.
Cardiac arrhythmias, coronary artery disease, hypertension, hypokalemia, QT prolongation
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. Albuterol, like other beta2-agonists and sympathomimetic amines, should be used with caution in patients with cardiovascular disorders, especially coronary insufficiency (coronary artery disease), cardiac arrhythmias, and hypertension. Albuterol can produce a clinically significant cardiovascular effect in some patients as measured by increases in pulse rate, systolic or diastolic blood pressure, and cardiac arrhythmias, such as supraventricular tachycardia and extrasystoles. If such effects occur, albuterol may need to be discontinued. In addition, beta-agonists have been reported to produce electrocardiographic (ECG) changes, such as flattening of the T wave, QT prolongation, and ST segment depression, although the clinical significance of these findings is unknown. Fatalities have been reported in association with excessive use of inhaled sympathomimetic drugs. Beta-adrenergic agonist therapies like albuterol may produce significant hypokalemia in some patients, possibly through intracellular shunting, which has the potential to produce adverse cardiovascular effects. The decrease is usually transient, not requiring supplementation.
Diabetes mellitus, diabetic ketoacidosis
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.[31823] [43674] [44010] [49951] [59350] [64470]
Labor, obstetric delivery, pregnancy
There are no randomized clinical studies of use of albuterol during pregnancy. Available data from published epidemiological studies and postmarketing case reports of pregnancy outcomes following inhaled albuterol use do not consistently demonstrate a risk of major birth defects or miscarriage. Poorly controlled or moderately controlled asthma represents risks in pregnant women; there is an increased risk of preeclampsia in the mother and prematurity, low birth weight, and small for gestational age in the neonate. Pregnant women should be closely monitored and medication adjusted as necessary to maintain optimal control.[31823] [43674] [44010] [49951] [59350] [64470] The National Asthma Education and Prevention Program (NAEPP) Asthma and Pregnancy Working Group include short-acting inhaled beta-2 agonists (SABAs) as first-line therapy for mild intermittent asthma during pregnancy, if treatment is required. Inhalation therapy is preferred to oral albuterol treatment. Albuterol is preferred over other SABAs due to extensive safety-related information during pregnancy. However, there is no evidence of fetal injury with the use of other inhaled SABAs, and maintaining a previously established treatment regimen may be more beneficial to the patient. Due to the potential for beta-agonist interference with uterine contractility, the use of albuterol for acute relief of bronchospasm during labor and obstetric delivery should be restricted to those patients in whom the benefits clearly outweigh the risks. Additionally, albuterol is not approved for the management of pre-term labor; serious adverse events, including pulmonary edema, have been reported after treatment of premature labor with beta-2 agonists. A pregnancy registry is available to monitor pregnancy outcomes in women exposed to asthma medications, including levalbuterol. To enroll in MotherToBaby Pregnancy Studies' Asthma and Pregnancy Study, patients should call 1-877-311-8972 or visit www.mothertobaby.org/ongoing-study/asthma.[31823] [43674] [44010] [49951] [59350] [64470]
Breast-feeding
According to the National Asthma Education and Prevention Program (NAEPP) for managing asthma during pregnancy, there is currently no contraindication for the use of short-acting inhaled beta-2 agonists, including albuterol, during breast-feeding. Inhaled albuterol therapy is preferred over oral treatment.[31822] Systematic data regarding the presence of albuterol in human milk, the effects on the breastfed child, or the effects on milk production are lacking. Plasma concentrations of albuterol after inhalation of therapeutic doses are very low in humans and substantially lower than systemically-administered albuterol. If present in breast milk, albuterol has low oral bioavailability in the infant.[31823] [43674] [44010] [49951] [59350] [64470]
Geriatric
Reported clinical experience with inhaled albuterol has not identified any differences in safety, efficacy, or clinical responsiveness with geriatric vs. younger adult patients. Geriatric patients may be more sensitive to the side effects of inhaled and systemic beta-agonists, especially tremor and tachycardia. Geriatric patients may be at increased risk for developing a prolonged QT interval when using albuterol. Although not clearly established, airway responsiveness to albuterol may also change with age. The federal Omnibus Budget Reconciliation Act (OBRA) regulates medication use in residents of long-term care facilities (LTCFs). Monitor for adverse effects, as inhaled beta-agonists, such as albuterol, can cause restlessness, increased heart rate, and anxiety.[28432] [28457] [31823] [43674] [49951] [56592] [59350] [64470]
MAOI therapy
Albuterol should be administered with extreme caution to patients being treated with monoamine oxidase inhibitor therapy (MAOI therapy) or within 2 weeks of discontinuation of such agents, because the action of albuterol on the vascular system may be potentiated.
ADVERSE REACTIONS
Severe
bronchospasm / Rapid / 8.0-15.4
arrhythmia exacerbation / Early / Incidence not known
atrial fibrillation / Early / Incidence not known
Stevens-Johnson syndrome / Delayed / Incidence not known
erythema multiforme / Delayed / Incidence not known
angioedema / Rapid / Incidence not known
anaphylactoid reactions / Rapid / Incidence not known
Moderate
excitability / Early / 1.0-20.0
palpitations / Early / 0-10.0
sinus tachycardia / Rapid / 1.0-10.0
hypertension / Early / 0-5.0
chest pain (unspecified) / Early / 0-3.0
edema / Delayed / 0-3.0
ataxia / Delayed / 0-3.0
dysphonia / Delayed / 0-3.0
glossitis / Early / 0-3.0
dyspnea / Early / 0-3.0
lymphadenopathy / Delayed / 0.9-2.6
migraine / Early / 1.0-2.0
wheezing / Rapid / 1.0-1.5
urinary retention / Early / 0-1.0
conjunctivitis / Delayed / 1.0-1.0
QT prolongation / Rapid / Incidence not known
ST-T wave changes / Rapid / Incidence not known
hyperglycemia / Delayed / Incidence not known
hypotension / Rapid / Incidence not known
hypokalemia / Delayed / Incidence not known
angina / Early / Incidence not known
peripheral vasodilation / Rapid / Incidence not known
supraventricular tachycardia (SVT) / Early / Incidence not known
metabolic acidosis / Delayed / Incidence not known
Mild
tremor / Early / 0-37.9
infection / Delayed / 0-21.0
headache / Early / 3.0-18.8
rhinitis / Early / 4.0-16.0
nausea / Early / 0-15.0
pharyngitis / Delayed / 7.0-14.0
throat irritation / Early / 6.0-10.0
vomiting / Early / 4.2-7.0
dizziness / Early / 0-7.0
muscle cramps / Delayed / 0-6.9
fever / Early / 6.0-6.0
cough / Delayed / 0-5.0
dyspepsia / Early / 0-5.0
musculoskeletal pain / Early / 3.0-5.0
hyperkinesis / Delayed / 0-4.0
insomnia / Early / 1.0-3.1
xerostomia / Early / 0-3.0
flatulence / Early / 0-3.0
epistaxis / Delayed / 1.0-3.0
abdominal pain / Early / 0-3.0
anxiety / Delayed / 0-3.0
diarrhea / Early / 0-3.0
drowsiness / Early / 0-3.0
hyperhidrosis / Delayed / 0-3.0
laryngitis / Delayed / 0-3.0
otalgia / Early / 0-3.0
tinnitus / Delayed / 0-3.0
weakness / Early / 0-2.0
urticaria / Rapid / 0.9-1.7
malaise / Early / 1.5-1.5
nightmares / Early / 1.0-1.0
emotional lability / Early / 1.0-1.0
agitation / Early / 1.0-1.0
irritability / Delayed / 0-1.0
restlessness / Early / 0-1.0
flushing / Rapid / 0-1.0
nasal congestion / Early / 1.0-1.0
rash / Early / Incidence not known
tooth discoloration / Delayed / Incidence not known
hoarseness / Early / Incidence not known
eructation / Early / Incidence not known
vertigo / Early / Incidence not known
hyperactivity / Early / Incidence not known
DRUG INTERACTIONS
Abarelix: (Major) Since abarelix can cause QT prolongation, abarelix should be used cautiously, if at all, with other drugs that are associated with QT prolongation. Prescribers need to weigh the potential benefits and risks of abarelix use in patients with prolonged QT syndrome or in patients taking other drugs that may prolong the QT interval. Agents associated with a lower, but possible risk for QT prolongation and torsade de pointes (TdP) based on varying levels of documentation include the beta-agonists. Beta-agonists may cause cardiovascular effects, particularly when used in high doses and/or when associated with hypokalemia.
Acebutolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Acetaminophen; Aspirin, ASA; Caffeine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Acetaminophen; Caffeine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Acetaminophen; Caffeine; Dihydrocodeine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Acetaminophen; Caffeine; Pyrilamine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Acetaminophen; Chlorpheniramine; Phenylephrine : (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Acetaminophen; Dextromethorphan; Guaifenesin; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Acetaminophen; Dextromethorphan; Guaifenesin; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Acetaminophen; Dextromethorphan; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Acetaminophen; Dextromethorphan; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Acetaminophen; Dichloralphenazone; Isometheptene: (Major) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Acetaminophen; Guaifenesin; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Acetaminophen; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Acetazolamide: (Moderate) Albuterol may cause additive hypokalemia when coadministered with carbonic anhydrase inhibitors. These combinations can lead to symptomatic hypokalemia and associated ECG changes in some susceptible individuals. Monitoring of potassium levels would be advisable.
Acrivastine; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Amphetamine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and amphetamine; dextroamphetamine use. Concomitant use may potentiate sympathetic effects.
Amphetamine; Dextroamphetamine Salts: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and amphetamine; dextroamphetamine use. Concomitant use may potentiate sympathetic effects.
Amphetamine; Dextroamphetamine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and amphetamine; dextroamphetamine use. Concomitant use may potentiate sympathetic effects.
Articaine; Epinephrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and epinephrine use. Concomitant use may potentiate sympathetic effects.
Aspirin, ASA; Butalbital; Caffeine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Aspirin, ASA; Butalbital; Caffeine; Codeine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Aspirin, ASA; Caffeine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Aspirin, ASA; Caffeine; Orphenadrine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Atenolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Atenolol; Chlorthalidone: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Bendroflumethiazide; Nadolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Benzphetamine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Beta-adrenergic blockers: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Betaxolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Bisoprolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Bisoprolol; Hydrochlorothiazide, HCTZ: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Brimonidine; Timolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Brompheniramine; Dextromethorphan; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Brompheniramine; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Brompheniramine; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Brompheniramine; Pseudoephedrine; Dextromethorphan: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Bumetanide: (Moderate) Use beta-agonists and loop diuretics with caution due to risk for ECG changes and/or hypokalemia. The ECG changes and/or hypokalemia that may result from administration of loop diuretics can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded.
Bupivacaine; Epinephrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and epinephrine use. Concomitant use may potentiate sympathetic effects.
Butalbital; Acetaminophen; Caffeine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Butalbital; Acetaminophen; Caffeine; Codeine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Caffeine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Caffeine; Sodium Benzoate: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Carbinoxamine; Dextromethorphan; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Carbinoxamine; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Carbinoxamine; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Carbonic anhydrase inhibitors: (Moderate) Albuterol may cause additive hypokalemia when coadministered with carbonic anhydrase inhibitors. These combinations can lead to symptomatic hypokalemia and associated ECG changes in some susceptible individuals. Monitoring of potassium levels would be advisable.
Carteolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Carvedilol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Cetirizine; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Chlophedianol; Dexchlorpheniramine; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Chlorpheniramine; Dextromethorphan; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Chlorpheniramine; Dextromethorphan; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Chlorpheniramine; Dihydrocodeine; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Chlorpheniramine; Ibuprofen; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Chlorpheniramine; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Chlorpheniramine; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Cisapride: (Contraindicated) QT prolongation and ventricular arrhythmias, including torsade de pointes (TdP) and death, have been reported with cisapride. Because of the potential for TdP, use of other drugs that might increase the QT interval is contraindicated with cisapride. Beta-agonists may be associated with adverse cardiovascular effects including QT interval prolongation, usually at higher doses and/or when associated with hypokalemia.
Cocaine: (Moderate) Additive effects and increased toxicity might be observed when using cocaine with beta-agonists, which are sympathomimetic agents. The combined use of these agents may have the potential for additive adrenergic stimulation and side effects, such as nervousness, insomnia, palpitations, or adverse cardiovascular effects.
Codeine; Guaifenesin; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Codeine; Phenylephrine; Promethazine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Desloratadine; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Dexbrompheniramine; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Dexchlorpheniramine; Dextromethorphan; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Dextroamphetamine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and amphetamine; dextroamphetamine use. Concomitant use may potentiate sympathetic effects.
Dextromethorphan; Diphenhydramine; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Dextromethorphan; Guaifenesin; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Dextromethorphan; Guaifenesin; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Dichlorphenamide: (Moderate) Use dichlorphenamide and albuterol together with caution. Metabolic acidosis has been reported with dichlorphenamide and albuterol aerosol and inhalation solution. Concurrent use may increase the severity of metabolic acidosis. Measure sodium bicarbonate concentrations at baseline and periodically during dichlorphenamide treatment. If metabolic acidosis occurs or persists, consider reducing the dose or discontinuing dichlorphenamide therapy.
Diethylpropion: (Major) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Digoxin: (Moderate) Mean decreases of 16% and 22% in serum digoxin levels were demonstrated after single-dose intravenous and oral administration of racemic albuterol, respectively, to normal volunteers who had received digoxin for 10 days. The clinical significance of these findings for patients with obstructive airway disease who are receiving albuterol or levalbuterol and digoxin on a chronic basis is unclear. The manufacturer of digoxin recommends measuring serum digoxin concentrations prior to initiation of albuterol or levalbuterol. Continue monitoring during concomitant treatment and increase the digoxin dose by 20 to 40% as necessary.
Diphenhydramine; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Dobutamine: (Major) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Dopamine: (Major) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Dorzolamide; Timolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Doxapram: (Major) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Ephedrine: (Major) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Ephedrine; Guaifenesin: (Major) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Epinephrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and epinephrine use. Concomitant use may potentiate sympathetic effects.
Ergotamine; Caffeine: (Moderate) Caffeine may enhance the cardiac inotropic effects of beta-agonists.
Esmolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Ethacrynic Acid: (Moderate) Use beta-agonists and loop diuretics with caution due to risk for ECG changes and/or hypokalemia. The ECG changes and/or hypokalemia that may result from administration of loop diuretics can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded.
Fexofenadine; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Furosemide: (Moderate) Use beta-agonists and loop diuretics with caution due to risk for ECG changes and/or hypokalemia. The ECG changes and/or hypokalemia that may result from administration of loop diuretics can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded.
Green Tea: (Moderate) Some green tea products contain caffeine, which is a CNS-stimulant. Additive effects are expected if used in combination with other CNS stimulants including the beta-agonists.
Guaifenesin; Hydrocodone; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Guaifenesin; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Guaifenesin; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Hydrocodone; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Ibuprofen; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Isocarboxazid: (Moderate) Use beta-agonists with caution in patients receiving concomitant monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping treatment with MAOIs because the action of beta-agonists on the cardiovascular system may be potentiated.
Isoproterenol: (Major) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Labetalol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Levobetaxolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Levobunolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Levothyroxine: (Moderate) Monitor blood pressure and heart rate during concomitant beta-agonist and thyroid hormone use. Concurrent use may increase the effects of sympathomimetics or thyroid hormone. Thyroid hormones may increase the risk of coronary insufficiency when sympathomimetic agents are administered to patients with coronary artery disease.
Levothyroxine; Liothyronine (Porcine): (Moderate) Monitor blood pressure and heart rate during concomitant beta-agonist and thyroid hormone use. Concurrent use may increase the effects of sympathomimetics or thyroid hormone. Thyroid hormones may increase the risk of coronary insufficiency when sympathomimetic agents are administered to patients with coronary artery disease.
Levothyroxine; Liothyronine (Synthetic): (Moderate) Monitor blood pressure and heart rate during concomitant beta-agonist and thyroid hormone use. Concurrent use may increase the effects of sympathomimetics or thyroid hormone. Thyroid hormones may increase the risk of coronary insufficiency when sympathomimetic agents are administered to patients with coronary artery disease.
Lidocaine; Epinephrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and epinephrine use. Concomitant use may potentiate sympathetic effects.
Linezolid: (Moderate) Linezolid may enhance the hypertensive effect of beta-agonists. Closely monitor for increased blood pressure during coadministration. Linezolid is an antibiotic that is also a weak, reversible nonselective inhibitor of monoamine oxidase (MAO). Therefore, linezolid has the potential for interaction with adrenergic agents, such as the beta-agonists.
Liothyronine: (Moderate) Monitor blood pressure and heart rate during concomitant beta-agonist and thyroid hormone use. Concurrent use may increase the effects of sympathomimetics or thyroid hormone. Thyroid hormones may increase the risk of coronary insufficiency when sympathomimetic agents are administered to patients with coronary artery disease.
Lisdexamfetamine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and lisdexamfetamine use. Concomitant use may potentiate sympathetic effects.
Loop diuretics: (Moderate) Use beta-agonists and loop diuretics with caution due to risk for ECG changes and/or hypokalemia. The ECG changes and/or hypokalemia that may result from administration of loop diuretics can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded.
Loratadine; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Methacholine: (Major) Discontinue use of short-acting beta-agonists 6 hours before a methacholine challenge test. Beta-agonists inhibit the airway response to methacholine.
Methamphetamine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Methazolamide: (Moderate) Albuterol may cause additive hypokalemia when coadministered with carbonic anhydrase inhibitors. These combinations can lead to symptomatic hypokalemia and associated ECG changes in some susceptible individuals. Monitoring of potassium levels would be advisable.
Metoprolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Metoprolol; Hydrochlorothiazide, HCTZ: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Midodrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Mobocertinib: (Minor) QT/QTc prolongation can occur with concomitant use of mobocertinib and short-acting beta-agonists although the risk of developing torsade de pointes (TdP) is low. Additional steps to minimize the risk of QT/QTc interval prolongation and TdP, such as avoidance, electrolyte monitoring and repletion, and ECG monitoring, may be considered in patients with additional risk factors for TdP. The risk for QT/QTc prolongation may be greater with long-acting beta-agonists than short-acting beta-agonists.
Monoamine oxidase inhibitors: (Moderate) Use beta-agonists with caution in patients receiving concomitant monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping treatment with MAOIs because the action of beta-agonists on the cardiovascular system may be potentiated.
Nadolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Naproxen; Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Nebivolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Nebivolol; Valsartan: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Norepinephrine: (Major) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Penbutolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Phendimetrazine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Phenelzine: (Moderate) Use beta-agonists with caution in patients receiving concomitant monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping treatment with MAOIs because the action of beta-agonists on the cardiovascular system may be potentiated.
Phentermine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and phentermine use. Concomitant use may potentiate sympathetic effects.
Phentermine; Topiramate: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and phentermine use. Concomitant use may potentiate sympathetic effects.
Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Pindolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Prilocaine; Epinephrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and epinephrine use. Concomitant use may potentiate sympathetic effects.
Procarbazine: (Major) Procarbazine has MAOI activity and the cardiovascular effects of beta-2 agonists may be potentiated by concomitant use of MAOIs. Although no data are available, procarbazine may interact similarly. Close observation for such effects is prudent, particularly if beta-agonists are administered within two weeks of stopping the MAOI.
Promethazine; Phenylephrine: (Moderate) Caution and close observation should be used when albuterol is used concurrently with other adrenergic sympathomimetics, administered by any route, to avoid potential for increased cardiovascular effects.
Propranolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Propranolol; Hydrochlorothiazide, HCTZ: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Pseudoephedrine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Pseudoephedrine; Triprolidine: (Moderate) Monitor blood pressure and heart rate during concomitant albuterol and pseudoephedrine use. Concomitant use may potentiate sympathetic effects.
Racepinephrine: (Major) Racepinephrine is a sympathomimetic drug with agonist actions at both the alpha and beta receptors. Patients using prescription beta-agonists for the treatment of asthma should generally avoid the concurrent use of racepinephrine inhalation since additive cardiovascular and nervous system adverse effects are possible, some which may be undesirable.
Rasagiline: (Moderate) The concomitant use of rasagiline and sympathomimetic agents was not allowed in clinical studies; therefore, caution is advised during concurrent use of rasagiline and respiratory adrenergic agents (e.g., the beta-agonists). Although sympathomimetic agents are contraindicated for use with traditional non-selective monoamine oxidase inhibitors (MAOIs), hypertensive reactions generally are not expected to occur during concurrent use with rasagiline because of the selective monoamine oxidase-B (MAO-B) inhibition of rasagiline at manufacturer recommended doses. However, the cardiovascular effects of beta-2 agonists may be potentiated by concomitant use of MAOIs. At least one case of hypertension occurred in a patient with previous episodes of high blood pressure who was receiving albuterol and selegiline, a selective MAOI related to rasagiline, concurrently. Close observation for such effects is prudent, particularly if beta-2 agonists are administered during or within 2 weeks of use of an MAOI.
Theophylline, Aminophylline: (Moderate) Beta-agonists are commonly used in conjunction with aminophylline or theophylline therapy. Concomitant use can cause additive CNS stimulation; some patients may experience tremor or nervousness with combined use. More serious effects are rare, but may result in additive cardiovascular effects such as increased blood pressure and heart rate. Methylxanthine derivatives, ((e.g., theophylline and aminophylline) may rarely aggravate the hypokalemic effect seen with beta-agonists. Consider checking potassium levels if clinically indicated. (Moderate) Beta-agonists are commonly used in conjunction with aminophylline or theophylline therapy. Concomitant use can cause additive CNS stimulation; some patients may experience tremor or nervousness with combined use. More serious effects are rare, but may result in additive cardiovascular effects such as increased blood pressure and heart rate. Methylxanthine derivatives, (e.g., theophylline, aminophylline) may rarely aggravate the hypokalemic effect seen with beta-agonists. Consider checking potassium levels if clinically indicated.
Thiazide diuretics: (Minor) Hypokalemia associated with thiazide diuretics can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded. Although the clinical significance of these effects is unknown, use caution when coadministering beta-agonists with thiazide diuretics and monitor serum potassium as clinically indicated.
Thyroid hormones: (Moderate) Monitor blood pressure and heart rate during concomitant beta-agonist and thyroid hormone use. Concurrent use may increase the effects of sympathomimetics or thyroid hormone. Thyroid hormones may increase the risk of coronary insufficiency when sympathomimetic agents are administered to patients with coronary artery disease.
Timolol: (Moderate) Beta-blockers will block the pulmonary effects of inhaled beta-agonists, and in some cases may exacerbate bronchospasm in patients with reactive airways. Beta-agonists can sometimes increase heart rate or have other cardiovascular effects, particularly when used in high doses or if hypokalemia is present. Use of a beta-1-selective (cardioselective) beta blocker is recommended whenever possible when this combination of drugs must be used together. Monitor the patient's lung and cardiovascular status closely. Beta-agonists and beta-blockers are pharmacologic opposites and will counteract each other to some extent when given concomitantly, especially when non-cardioselective beta blockers are used.
Torsemide: (Moderate) Use beta-agonists and loop diuretics with caution due to risk for ECG changes and/or hypokalemia. The ECG changes and/or hypokalemia that may result from administration of loop diuretics can be acutely worsened by beta-agonists, especially when the recommended dose of the beta-agonist is exceeded.
Tranylcypromine: (Moderate) Use beta-agonists with caution in patients receiving concomitant monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping treatment with MAOIs because the action of beta-agonists on the cardiovascular system may be potentiated.
PREGNANCY AND LACTATION
Pregnancy
According to the National Asthma Education and Prevention Program (NAEPP) for managing asthma during pregnancy, there is currently no contraindication for the use of short-acting inhaled beta-2 agonists, including albuterol, during breast-feeding. Inhaled albuterol therapy is preferred over oral treatment.[31822] Systematic data regarding the presence of albuterol in human milk, the effects on the breastfed child, or the effects on milk production are lacking. Plasma concentrations of albuterol after inhalation of therapeutic doses are very low in humans and substantially lower than systemically-administered albuterol. If present in breast milk, albuterol has low oral bioavailability in the infant.[31823] [43674] [44010] [49951] [59350] [64470]
MECHANISM OF ACTION
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. The R-isomer, known as levalbuterol, is primarily responsible for bronchodilation. Although not confirmed during clinical trials, the S-isomer of albuterol has bronchoconstrictive properties in animal models.Intracellularly, the actions of albuterol are mediated by cyclic AMP, the production of which is augmented by beta2-stimulation. Albuterol is believed to work by activating adenylate cyclase, the enzyme responsible for generating cyclic AMP, an intracellular mediator. Increased cyclic AMP leads to activation of protein kinase A, which inhibits phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in relaxation. 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.Albuterol can also inhibit the degranulation and subsequent release of inflammatory autocoids from mast cells. Stimulation of beta2-receptors on peripheral vascular smooth muscle can cause vasodilation and a modest decrease in diastolic blood pressure. Albuterol is an effective adjunctive treatment for hyperkalemia; beta2-adrenergic stimulation results in intracellular accumulation of serum potassium due to stimulation of the Na/K ATPase pump, leading to moderate degrees of hypokalemia.
PHARMACOKINETICS
Albuterol can be administered as oral tablets or oral solution but is more commonly administered by oral inhalation. Albuterol crosses the blood-brain barrier and may cross the placenta. The liver metabolizes albuterol extensively to inactive compounds. Excretion of albuterol occurs through the urine and feces. The elimination half-life of albuterol ranges from 2.7 to 6 hours, with orally administered albuterol having a shorter half-life than the inhaled product.
Oral Route
When administered orally, albuterol is well absorbed through the GI tract. Onset of action begins within 30 minutes, peak levels are reached in 2 to 3 hours, and duration of action is 4 to 6 hours for the conventional-release tablets and 8 to 12 hours for the sustained-release product. After oral administration, 75% of a dose is excreted in urine within 72 hours as metabolites; 4% may be found in feces.
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.[44002][44003][44010]
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.[44002]
Inhalation Route
Following oral inhalation, albuterol is absorbed over several hours from the respiratory tract. It is postulated from studies with other inhaled bronchodilators that most of an albuterol inhaled dose (approximately 90%) is swallowed and absorbed through the GI tract. The systemic exposure in children 6 to 11 years of age is similar to that of adults after 180 mcg single dose oral inhalation. Onset of bronchodilation occurs within 5 to 15 minutes after oral inhalation, peaks in 0.5 to 2 hours, and lasts 2 to 6 hours. Administration via nebulization does not appear to significantly alter the pharmacokinetics of albuterol. After oral inhalation, 80% to 100% of a dose is excreted via the kidneys within 72 hours; up to 10% may be eliminated in feces.[31823][49951][59350]