ThisiscontentfromElsevier'sDrugInformation
Albuterol
Learn more about Elsevier's Drug Information today! Get the drug data and decision support you need, including TRUE Daily Updates™ including every day including weekends and holidays.
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 of 90 mcg/actuation) every 3 to 4 hours up to 540 to 900 mcg (6 to 10 actuations of 90 mcg/actuation) every 1 to 2 hours, or more often.[69016]
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 of 90 mcg/actuation) every 3 to 4 hours up to 540 to 900 mcg (6 to 10 actuations of 90 mcg/actuation) every 1 to 2 hours, or more often.[69016]
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 of 90 mcg/actuation) every hour as needed. Delivery should occur with a spacer, with face mask for children younger than 3 years.[69016]
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 of 90 mcg/actuation) every hour as needed. Delivery should occur with a spacer, with face mask for children younger than 3 years.[69016]
2.5 to 5 mg inhaled by nebulizer every 20 minutes for the first hour, then 2.5 to 10 mg inhaled by nebulizer every 1 to 4 hours as needed.[33558]
2.5 to 5 mg inhaled by nebulizer every 20 minutes for the first hour, then 2.5 to 10 mg inhaled by nebulizer every 1 to 4 hours as needed.[33558]
2.5 mg inhaled by nebulizer every 20 minutes for the first hour, then 0.15 to 0.3 mg/kg/dose (Max: 10 mg/dose) inhaled by nebulizer every 1 to 4 hours as needed.[33558]
2.5 mg inhaled by nebulizer every 20 minutes for the first hour, then 0.15 to 0.3 mg/kg/dose (Max: 10 mg/dose) inhaled by nebulizer every 1 to 4 hours as needed.[33558]
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).[28532] [31823] [49951]
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).[28532] [31823] [49951]
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).[59350] [64470]
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).[59350] [64470]
2.5 mg inhaled by nebulizer 3 to 4 times daily as needed. Usual Max: 10 mg/day.[49953] [51872]
2.5 mg inhaled by nebulizer 3 to 4 times daily as needed. Usual Max: 10 mg/day.[49953] [51872]
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.[43674] [51872] [49953]
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.[43674] [51872] [49953]
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.[43674] [51872] [49953]
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.[43674] [51872] [49953]
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.[44003] 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.[66299] [64807]
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.[44003] 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.[66299] [64807]
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.[44003] 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.[66299] [64807]
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.[44003] 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.[66299] [64807]
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.[51897] [44003]
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.[44010] 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.[66299] [64807]
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.[44010] 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.[66299] [64807]
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.[44010] 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.[66299] [64807]
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.[44002] 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.[66299] [64807]
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.[44002] 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.[66299] [64807]
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.[44002] 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.[66299] [64807]
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth 15 to 30 minutes before exercise.[28532] [31823] [49951] 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.[56291] [64807]
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth 15 to 30 minutes before exercise.[28532] [31823] [49951] 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.[56291] [64807]
90 to 180 mcg (1 to 2 actuations of 90 mcg/actuation) inhaled by mouth 15 minutes (range: 5 to 20 minutes) before exercise.[56291]
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.[56291] [64807]
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.[56291] [64807]
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth prior to other inhaled medications, every 8 to 24 hours depending on regimen.[43523] [56767] [66363] [68125] [68126] [68127]
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth prior to other inhaled medications, every 8 to 24 hours depending on regimen.[43523] [56767] [66363] [68125] [68126] [68127]
90 or 180 mcg (1 or 2 actuations of 90 mcg/actuation) inhaled by mouth every 1 hour for 2 to 3 doses, then 90 or 180 mcg (1 or 2 actuations of 90 mcg/actuation) inhaled by mouth every 2 to 4 hours as needed.[69470] The FDA-approved dosage is 180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth every 4 to 6 hours as needed. In some persons, 90 mcg (1 actuation of 90 mcg/actuation) every 4 hours may be sufficient. Max: 1,080 mcg/day (12 actuations/day).[28532] [31823] [49951] [59350] [64470] Guidelines recommend a short-acting inhaled beta-2 agonist (SABA), with or without a short-acting anticholinergic, as the initial bronchodilators for acute treatment of a COPD exacerbation. Use of a metered-dose inhaler is recommended rather than continuous nebulization to deliver the SABA. No significant differences in FEV1 have been demonstrated between metered-dose inhalers (with or without a spacer) or nebulizers to deliver the SABA; nebulizers may be more convenient for persons who are more acutely ill.[69470]
Optimal dosing is not established.[55976] 2.5 mg inhaled by nebulizer every 20 or 60 minutes for 2 hours.[56006] Alternatively, 2.5 mg inhaled by nebulizer every 4 hours as needed.[55975] The FDA-approved dosage is 2.5 mg inhaled by nebulizer every 6 to 8 hours as needed. Max: 10 mg/day.[43674] [49953] Guidelines recommend a short-acting inhaled beta-2 agonist (SABA), with or without a short-acting anticholinergic, as the initial bronchodilators for acute treatment of a COPD exacerbation. Use of a metered-dose inhaler is recommended rather than continuous nebulization to deliver the SABA. No significant differences in FEV1 have been demonstrated between metered-dose inhalers (with or without a spacer) or nebulizers to deliver the SABA; nebulizers may be more convenient for persons who are more acutely ill.[69470]
180 mcg (2 actuations of 90 mcg/actuation) inhaled by mouth every 4 to 6 hours as needed. In some persons, 90 mcg (1 actuation of 90 mcg/actuation) inhaled by mouth every 4 hours may be sufficient. Max: 1,080 mcg/day (12 actuations/day).[28532] [31823] [49951] [59350] [64470] Guidelines recommend a bronchodilator in persons with 0 or 1 moderate exacerbations per year (not leading to hospital admission) and modified Medical Research Council (mMRC) dyspnea questionnaire score of 0 to 1 and COPD Assessment Test (CAT) score of less than 10. Long-acting bronchodilators are preferred over short-acting bronchodilators except for persons with occasional dyspnea and for immediate relief of symptoms in persons already receiving long-acting bronchodilators for maintenance therapy. Inhaled bronchodilators are commonly given on a regular basis to prevent or reduce symptoms. Regular and as-needed use of a short-acting beta-2 agonist (SABA) improves FEV1 and symptoms.[69470]
2.5 mg inhaled by nebulizer every 6 to 8 hours as needed. Max: 10 mg/day.[43674] [49953] Guidelines recommend a bronchodilator in persons with 0 or 1 moderate exacerbations per year (not leading to hospital admission) and modified Medical Research Council (mMRC) dyspnea questionnaire score of 0 to 1 and COPD Assessment Test (CAT) score of less than 10. Long-acting bronchodilators are preferred over short-acting bronchodilators except for persons with occasional dyspnea and for immediate relief of symptoms in persons already receiving long-acting bronchodilators for maintenance therapy. Inhaled bronchodilators are commonly given on a regular basis to prevent or reduce symptoms. Regular and as-needed use of a short-acting beta-2 agonist (SABA) improves FEV1 and symptoms.[69470]
2 mg PO every 6 to 8 hours, initially. Increase the dose stepwise as tolerated if a favorable response is not achieved with the initial dose. Max: 32 mg/day.[44003] [44010] Inhaled bronchodilators are recommended over oral bronchodilators.[69470]
2 to 4 mg PO every 6 to 8 hours, initially. Increase the dose stepwise as tolerated if a favorable response is not achieved with the initial dose. Max: 32 mg/day.[44003] [44010] Inhaled bronchodilators are recommended over oral bronchodilators.[69470]
4 to 8 mg PO every 12 hours. Increase the dose stepwise as tolerated if a favorable response is not achieved with the initial dose. Max: 32 mg/day.[44002] Inhaled bronchodilators are recommended over oral bronchodilators.[69470]
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.[51912] 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.[51895] [51908] [51909] [51910] [51911] 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.[51901]
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.[51908] [51913] [51914] [51915] In a survey of 68 academic medical center neonatal intensive care units (NICUs), 95% reported 1 to 2 actuations as the average dose used.[51912] 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.[51901]
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.[51897]
NOTE: Place patients on a cardiac monitor. Avoid in patients with preexisting cardiac arrhythmias.[64934] 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).[30594] Albuterol decreases serum potassium by approximately 1 to 1.5 mEq/L within an hour of administration.[64934] Concentrations begin to fall within 30 minutes of administration and may remain depressed up to 300 minutes when albuterol is nebulized.[30591]
10 to 20 mg inhaled by nebulizer as a single dose.[30591]
10 mg/dose inhaled by nebulizer every 20 minutes for 1 to 2 doses.[64934]
5 mg/dose inhaled by nebulizer every 20 minutes for 1 to 2 doses.[64934] In a small study (n = 11), doses were repeated every 2 hours as needed.[30593]
2.5 mg/dose inhaled by nebulizer every 20 minutes for 1 to 2 doses.[64934] In a small study (n = 11), doses were repeated every 2 hours as needed.[30593]
2.5 mg/dose inhaled by nebulizer every 20 minutes for 1 to 2 doses.[64934] 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]
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.[30594]
2.5 to 5 mg inhaled by nebulizer; repeat every 15 minutes as necessary.[60464]
2.5 mg inhaled by nebulizer; repeat every 15 minutes as necessary.[60464]
32 mg/day PO for syrup and tablets; FDA-approved labeling for inhaler recommends not exceeding 12 actuations/day (1,080 mcg/day); FDA-approved labeling for nebulizer solution for oral inhalation recommends not exceeding 4 doses/day (10 mg/day). Higher maximum dosages for inhalation products have been recommended in guidelines for asthma exacerbation.
32 mg/day PO for syrup and tablets; FDA-approved labeling for inhaler recommends not exceeding 12 actuations/day (1,080 mcg/day); FDA-approved labeling for nebulizer solution for oral inhalation recommends not exceeding 4 doses/day (10 mg/day). Higher maximum dosages for inhalation products have been recommended in guidelines for asthma exacerbation.
15 to 17 years: 32 mg/day PO for syrup and tablets; FDA-approved labeling for inhaler recommends not exceeding 12 actuations/day (1,080 mcg/day); FDA-approved labeling for nebulizer solution for oral inhalation recommends not exceeding 4 doses/day (10 mg/day). Higher maximum dosages for inhalation products have been recommended in guidelines for asthma exacerbation.
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 actuations/day (1,080 mcg/day); FDA-approved labeling for nebulizer solution for oral inhalation recommends not exceeding 4 doses/day (10 mg/day). Higher maximum dosages for inhalation products have been recommended in guidelines for asthma exacerbation.
6 to 12 years: 24 mg/day PO for syrup and tablets; FDA-approved labeling for inhaler recommends not exceeding 12 actuations/day (1,080 mcg/day); FDA-approved labeling for nebulizer solution for oral inhalation recommends not exceeding 4 doses/day (10 mg/day). Higher maximum dosages for inhalation products have been recommended in guidelines for asthma exacerbation.
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 actuations/day (1,080 mcg/day); FDA-approved labeling for nebulizer solution for oral inhalation recommends not exceeding 4 doses/day (10 mg/day). Higher maximum dosages for inhalation products have been recommended in guidelines for asthma exacerbation.
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 (10 mg/day). Higher maximum dosages for inhalation products have been recommended in guidelines for asthma exacerbation.
1 year: Safety and efficacy have not been established; nebulizer inhalation maximum dependent on patient response and formulation used.
Safety and efficacy have not been established; nebulizer inhalation maximum dependent on patient response and formulation used.
Safety and efficacy have not been established; nebulizer inhalation maximum dependent on patient response and formulation used.
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
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.
† Off-label indicationAlbuterol is a moderately selective short-acting beta-2-receptor agonist (SABA). Albuterol is a racemic mixture of R- and S-isomers, and is widely used as a bronchodilator. The R-enantiomer is the therapeutically active moiety. It is indicated for the management of asthma and acute bronchospasm in adult and pediatric patients, and for the treatment of bronchospasm due to chronic obstructive pulmonary disease (COPD) in adults.[28532][43993][49951][49953][43674][59350] It is also used off-label as an adjuvant treatment for hyperkalemia in certain clinical situations. Albuterol is similar in structure to terbutaline, and when compared to non-selective beta-agonists, produces equivalent bronchodilation with less cardiac stimulation.[51896] Outside the U.S., albuterol is referred to as salbutamol. Orally inhaled SABAs are recommended for the management of asthma exacerbations. SABAs should not be used alone to manage asthma, but continue to be an option for reliever therapy in adult and pediatric patients with intermittent asthma and those with mild or moderate persistent asthma who are taking controller therapy such as inhaled corticosteroid (ICS) or ICS-long-acting beta-agonist (LABA) regimens. SABAs remain a key reliever therapy for infants and very young children (less than 4 years of age).[64807][66299] However, guidelines now promote the use of "SMART" (single maintenance and reliever therapy) inhaler dosing strategies as preferred asthma management for selected adult and pediatric patients; such regimens usually combine an ICS with formoterol.[64807][66299] SABAs also prevent exercise-induced bronchospasm (EIB), however, tolerance can develop with regular use and the incidence of EIB can usually be reduced with maintenance ICS therapy.[56291][64807] Although historically a trial of albuterol was an option for infants and young children presenting with bronchiolitis, this practice is no longer recommended due to a lack of clinical benefit.[58442] According to guidelines, albuterol may be used for first-line therapy in patients with mild COPD (group A) and in combination with other treatments in those with more severe disease (groups B and E); inhaled SABAs are preferred for rescue therapy and for the management of acute COPD exacerbations, with or without an inhaled short-acting anticholinergic.[69470] Due to the increased risks associated with systemic therapy, the use of oral albuterol is not recommended in the management of asthma or COPD.[64807][69470]
For storage information, see the specific product information within the How Supplied section.
Immediate release tablets:
Extended-release tablets:
Administer using a calibrated oral measuring device to ensure accurate dosing.[44003]
Aerosol inhalation (e.g., ProAir HFA, Ventolin HFA)
Valved holding chamber (VHC) with aerosol inhalation:
Powder for Inhalation (e.g., ProAir RespiClick, ProAir Digihaler)
Inhalation solution for nebulization
Like other sympathomimetics, albuterol can cause various adverse cardiovascular effects. Although incidences of the adverse effects are often unavailable, systemic albuterol formulations are generally expected to have a higher incidence of adverse effects compared to inhaled formulations. Hypertension (1% to less than 5% incidence from data of various inhaled formulations), angina, palpitations (less than 1% to less than 10%, various formulations), sinus tachycardia (1% to 10%), chest pain (unspecified) (less than 3%), or arrhythmia exacerbation or precipitation have been reported, especially in patients with preexisting cardiovascular disease. Peripheral vasodilation (e.g., hypotension) can also occur from beta-2 stimulation of the vasculature. Albuterol can produce clinically significant cardiovascular effects in some patients, as measured by pulse rate, blood pressure, and/or symptoms. Although such effects are uncommon after administration of albuterol at recommended doses, if they occur, the drug may need to be discontinued. In addition, beta-agonists have been reported to produce ECG changes, ST-T wave changes (e.g., flattening of the T wave, ST segment depression) and QT prolongation. Arrhythmias such as atrial fibrillation, supraventricular tachycardia (SVT), and extrasystole have been reported with albuterol use. Cardiac effects may be related to sympathomimetic effects and/or beta-agonist-induced hypokalemia. Albuterol can cause hyperglycemia and hypokalemia. Both of these effects occur from stimulation of beta-2 receptors, resulting in gluconeogenesis and intracellular movement of potassium. These effects occur most commonly with inhalation (via nebulization) of relatively large doses of albuterol (e.g., 5 to 10 mg).[28532] [40947] [43993] [44010]
Paradoxical bronchospasm can occur after treatment with albuterol and can be life threatening. If this occurs albuterol should be discontinued immediately. Rare cases of anaphylactoid reactions have been reported with beta-agonist therapy. Immediate hypersensitivity reactions may occur after administration of racemic albuterol, as demonstrated by rare cases of anaphylaxis, angioedema, bronchospasm, oropharyngeal swelling, rash (unspecified), and urticaria. Stevens-Johnson syndrome and erythema multiforme have been reported rarely in children who received albuterol.[44003] In clinical trials of albuterol inhalation, bronchospasm (8% to 15.4%), asthma exacerbation, allergic reactions (0.9% to 6%), and urticaria (0.9% to 1.7%) were reported.[28532] [43674] [43993] Use of albuterol inhalation solution produces adverse effects similar to those observed with the inhalation aerosol.[40947]
Central nervous system (CNS) adverse reactions are common with the use of both oral and inhaled albuterol. Tremor is one of the most common adverse effects and has been reported in less than 1% to 20% of patients who received inhaled albuterol in clinical trials. In controlled trials of albuterol oral extended-release tablets, tremor was reported in 24.2% of patients overall; however, the incidence of tremor increased with increasing age with up to 37.9% of adults aged 41 to 50 years experiencing tremor. Other adverse effects associated with albuterol use include headache (3% to 7% with inhaled formulations, 18.8% with extended-release tablet), migraine (1% to 2%), nervousness (1% to 15%), dizziness (3% to 7% and less than 5% with inhaled formulations, 1.5% with extended-release tablets), and insomnia (1% to 3.1%).[43674] [43993] [44002] [44010] Anxiety (less than 3%) and nightmares (1%) have also been reported with some formulations of albuterol inhalation aerosol.[28532] [40947] Emotional lability was reported in 1% of children 2 to 6 years of age receiving albuterol oral solution and agitation, aggressive behavior, and lightheadedness were reported in 1% or less of children 4 to 11 years of age receiving albuterol inhalation aerosol.[40947] [44003] Gastrointestinal (GI) adverse effects associated with both oral and inhaled albuterol include nausea (less than 15%) and vomiting (4.2% to 7%). Throat irritation (6% to 10%), dyspepsia (less than 5%), abdominal pain (3%), diarrhea (less than 3%), tooth discoloration (1%), eructation (less than 3%), and flatulence (less than 3%) have all been reported with inhaled albuterol therapy.[28532] [40947] [31823] Appetite stimulation (3%), abdominal pain (less than 1%), and decreased appetite (1%) have been reported in clinical trials of patients receiving albuterol oral solution. Dry mouth (xerostomia) (less than 3%), throat hoarseness, and unusual taste have also been reported with albuterol therapy.[44003] Other adverse effects occurring with albuterol therapy include epistaxis (1% to 3%) and cough (5% or less).[33925] [40947]
Musculoskeletal pain (3% to 5%), hyperkinesis (4% or less), weakness (2% or less), malaise (1.5%), ataxia (less than 3%), vertigo (less than 3%), rigors (less than 3%), edema (less than 3%), increased sweating (hyperhidrosis) (less than 3%), drowsiness (less than 3%), dysphonia (less than 3%, inhaled formulations) and excitability (2%) have been reported with albuterol use during clinical trials.[28532] [33925] [44002] [44003] [49953] Some adverse effects appear to occur more frequently in young children (2 to 6 years of age) than in older children or adults especially excitability, which occurred in roughly 20% of young children receiving albuterol oral solution in clinical trials.[44003] Muscle cramps (2.7% or less) have been reported with inhaled and oral dosage forms. In controlled trials of albuterol extended-release tablets, the incidence of muscle cramps increased with age (12 to 20 years, 1.2%; 21 to 30 years, 2.6%; 31 to 50 years, 6.9%). Less frequent adverse reactions occurring in less than 1% of patients include flushing, restlessness, irritability, and urinary retention.[44010] Hyperactivity has been reported with postmarketing experience.[49951] A case of hypokalemic periodic muscle paralysis, possibly precipitated by inhaled albuterol, was reported in a patient with a medical history of hypokalemic periodic paralysis (HPP).[56005]
Metabolic acidosis has been reported in post-marketing experience with albuterol inhalation solution and aerosol. A causal relationship has not been established.[43674] [49951] The potential for this effect following the use of oral albuterol dosage forms is unknown.
Infectious and respiratory adverse effects have been reported with inhaled albuterol therapy. In clinical trials of Accuneb (albuterol solution for nebulizer inhalation), otitis media (0.9% to 4.3% vs 0% placebo), gastroenteritis (0.9% to 3.4% vs 0.9% placebo), cold symptoms (3.4% vs 1.7% placebo), flu syndrome (2.6% vs 1.7% placebo), lymphadenopathy (0.9% to 2.6% vs 1.7% placebo), skin/appendage infection (1.7% vs 0% placebo), and bronchitis (0.9% to 1.7% vs 0.9% placebo) were all reported.[43674] Other infectious and respiratory adverse events reported with inhaled albuterol therapy include respiratory tract infection (7% to 21%), pharyngitis (7% to 14%), rhinitis (4% to 16%), fever (6%, reported with albuterol HFA MDI formulation), dyspnea (less than 3%), laryngitis (less than 3%, reported with inhalational formulations), ear disorder (less than 3%), ear pain or otalgia (less than 3%), glossitis (less than 3%), tinnitus (less than 3%), urinary tract infection (less than 3%), increased sputum (1.5%), wheezing (1% to 1.5%), nasopharyngitis (2%), oropharyngeal pain (2%), and nasal congestion (1%).[28532] [31823] [43993] [59350] Conjunctivitis has also been reported in 1% of patients receiving albuterol oral solution.[44003] Eye irritation may occur if formulations for inhalation are inadvertently sprayed in the eyes; patients should prime inhalers into the air and away from the eyes or face.
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. Paradoxical bronchospasm, when it occurs, frequently occurs with the first use of a new canister or vial of inhaled formulations of albuterol. 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.[31823] [43674] [44010] [49951] [59350] [64470] 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.[31823] [43674] [49951] [59350] [64470]
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.[31823] [43674] [44010] [49951] [59350] [64470]
Albuterol, like other sympathomimetic amines, should be used cautiously in patients with a history of seizure disorder, hyperthyroidism (thyrotoxicosis), or unusual responsiveness to other sympathomimetic amines.[28532] [49951]
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.[31823] [43674] [44010] [49951] [59350] [64470]
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]
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.[31822] 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]
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]
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.[31823] [59350]
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.[44010][40947][28532][49951]
Revision Date: 05/24/2024, 01:33:00 AMAlbuterol 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.[44002][44003][44010][28532][49951]
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]
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; 10% to 20% may be eliminated in feces.[31823] [49951] [59350]
The pharmacokinetics of albuterol were studied in a small number of subjects with creatinine clearances between 7 to 53 mL/minute in comparison to healthy volunteers. The half-life was unchanged; however albuterol clearance was decreased by 67% in those with renal impairment. The manufacturer (specifically of ProAir HFA) recommends caution during administration of high doses of inhaled albuterol to patients with renal impairment.[31823]
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
During studies, the majority of the nebulized albuterol dose administered has been recovered from the nebulizer apparatus and/or expired air; less than 20% of albuterol administered is systemically absorbed.[43674] At recommended doses, the bioavailability of inhaled albuterol is low. Onset of pulmonary improvement occurs within 2 to 20 minutes. After a 3 mg nebulized dose, peak concentrations of 2.1 ng/mL (range: 1.4 to 3.2 ng/mL) are reached in approximately 30 minutes and peak pulmonary improvement is seen at 1 to 2 hours.[49953] Duration of action is 2 to 6 hours. Half-life is approximately 4.6 to 6 hours.[31823] [43674] [49951] [59350] Administration via nebulization does not appear to significantly alter the pharmacokinetics of albuterol. The systemic exposure in children 6 to 11 years of age is similar to that of adults after 180 mcg single dose oral inhalation.[59350] A small study in 11 healthy children (aged 4 to 11 years) who received a single dose of albuterol inhalation aerosol 180 mcg via metered-dose inhaler, demonstrated a least square mean (SE) Cmax and AUC of 1100 (+/-1.18) pg/mL and 5120 (+/-1.15) pg x hr/mL, respectively. The least square mean (SE) terminal plasma half-life was 166 (+/-7.8) minutes.[31823] In a cumulative dose study, the AUC of the dry powder inhalation was similar to the aerosol formulation (metered dose inhaler); however, the Cmax was about one-third higher in the dry powder inhalation group.[59350]
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.[31822] 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]
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]
Cookies are used by this site. To decline or learn more, visit our cookie notice.
Copyright © 2024 Elsevier, its licensors, and contributors. All rights are reserved, including those for text and data mining, AI training, and similar technologies.