.png?width=200&height=94&name=PDR_stacked_purple%20(002).png)
Xopenex
Classes
Respiratory Short-Acting Beta-2 Agonists (SABA)
Administration
Oral Inhalation (inhalation aerosol; metered-dose inhaler [MDI])
Instruct the patient and/or caregiver on proper inhalation technique. Make sure the canister is firmly seated in the plastic mouthpiece actuator before each use. Shake the inhaler well. Prime the inhaler prior to the initial use by releasing 4 sprays into the air, away from the eyes and face. If not used for more than 3 days, re-prime the inhaler.
For patients of any age unable to coordinate inhalation and actuation, a spacer or valved holding chamber (VHC) may be beneficial.
The choice of using a mouthpiece versus a face mask with a spacer/VHC device must be made based on the skills and understanding of each individual patient. However, in general, children younger than 4 years require administration with a tight-fitting face mask and spacer/VHC device to achieve optimal delivery. If a face mask is used, allow 5 to 6 inhalations per actuation. Administer 1 puff at a time.
If the patient is using other inhalers, instruct them to use levalbuterol first and wait 5 minutes, then use other inhalers as directed.
After administration, instruct patient to rinse mouth with water to minimize dry mouth.
The blue actuator (mouthpiece) supplied with levalbuterol (Xopenex HFA) should not be used with any other product canisters; conversely, actuators from other products should not be used with the levalbuterol (Xopenex HFA) canister.
The dose indicator on the canister indicates the number of remaining inhalations. The dose indication display will move every tenth actuation. Towards the end of the usable inhalations, the color behind the number in the dose indicator window will change to red. Discard when the dose indicator display window shows zero.
Clean the plastic mouthpiece of the inhaler at least once a week. After removing the medication canister wash the mouthpiece in warm running water. Shake excess water from the mouthpiece. Allow the actuator to air-dry completely. Blockage from medicine build up is more likely to occur if the actuator is not allowed to air-dry thoroughly. If build-up occurs, then washing the actuator will remove the blockage.
To avoid the spread of infection, do not use the inhaler for more than one person.
Inhalation Solution for Nebulization
For 3 mL inhalation solution vials: No dilution is necessary; the single-dose vials are ready-to-use.
For 0.5 mL inhalation solution concentrate vials: Squeeze entire contents of vial into nebulizer reservoir; then, dilute solution to a final volume of 3 mL with sterile 0.9% NaCl Injection, and gently swirl nebulizer reservoir to mix.
NOTE: For dosages less than 1.25 mg, the 3 mL inhalation solution vials must be used.
Deliver solution by nebulization over 5 to 15 minutes.
According to the manufacturer, the compatibility of levalbuterol inhalation solution with other drugs administered by nebulization has not been established; however, clinical guidelines state that levalbuterol nebulizer solution and budesonide suspension for nebulization are compatible in the same nebulizer.
Safety and efficacy have been established when administered via PARI LC Jet or PARI LC Plus nebulizers and via PARI Master Dura-Neb 2000 or Dura-Neb 3000 compressors.
The choice of using a mouthpiece versus a face mask must be made based on the skills and understanding of each individual patient.
Using the 'blow by' technique (i.e., holding the face mask or open tube near the patient's nose and mouth) is not recommended.
To avoid microbial contamination, aseptic technique should be used each time a multi-dose bottle is opened. Precautions should be taken to prevent contact of dropper tip with any surface, including nebulizer reservoir and ventilatory equipment. Each multi-dose bottle should be used for only 1 patient.
Discard the vial if the solution is not colorless.
Storage: Protect from light.
For 3 mL inhalation solution vials: Unit-dose vials should be stored in the protective foil pouch. If a vial is removed from the pouch and not used immediately, protect from light and use within 1 week. Once the protective foil pouch is opened use all contained vials within 2 weeks.
For 0.5 mL inhalation solution concentrate vials: Use the contents of the vial immediately after the foil pouch is opened; do not store for future use.
Adverse Reactions
bronchospasm / Rapid / Incidence not known
arrhythmia exacerbation / Early / Incidence not known
atrial fibrillation / Early / Incidence not known
lymphadenopathy / Delayed / 0-3.0
sinus tachycardia / Rapid / 2.7-2.8
migraine / Early / 2.7-2.7
wheezing / Rapid / 0-2.0
chest pain (unspecified) / Early / 0-2.0
hypertension / Early / 0-2.0
hypotension / Rapid / 0-2.0
conjunctivitis / Delayed / 0-2.0
hyperesthesia / Delayed / 0-2.0
constipation / Delayed / 0-2.0
hematuria / Delayed / 0-2.0
candidiasis / Delayed / 0-2.0
dysphonia / Delayed / Incidence not known
supraventricular tachycardia (SVT) / Early / Incidence not known
hyperglycemia / Delayed / Incidence not known
hypokalemia / Delayed / Incidence not known
peripheral vasodilation / Rapid / Incidence not known
QT prolongation / Rapid / Incidence not known
metabolic acidosis / Delayed / Incidence not known
headache / Early / 7.6-11.9
vomiting / Early / 11.0-11.0
pharyngitis / Delayed / 3.0-10.4
fever / Early / 3.0-9.1
tremor / Early / 6.8-6.8
diarrhea / Early / 1.5-6.0
cough / Delayed / 1.4-4.0
asthenia / Delayed / 3.0-3.0
dizziness / Early / 1.4-3.0
sinusitis / Delayed / 1.4-2.7
dyspepsia / Early / 1.4-2.7
muscle cramps / Delayed / 0-2.7
epistaxis / Delayed / 0-2.0
syncope / Early / 0-2.0
ocular pruritus / Rapid / 0-2.0
acne vulgaris / Delayed / 0-2.0
insomnia / Early / 0-2.0
anxiety / Delayed / 0-2.0
paresthesias / Delayed / 0-2.0
nausea / Early / 0-2.0
xerostomia / Early / 0-2.0
myalgia / Early / 1.5-2.0
dysmenorrhea / Delayed / 0-2.0
chills / Rapid / 0-2.0
abdominal pain / Early / 1.5-1.5
infection / Delayed / Incidence not known
vertigo / Early / Incidence not known
gastroesophageal reflux / Delayed / Incidence not known
Common Brand Names
Xopenex, Xopenex HFA, Xopenex Pediatric
Dea Class
Rx
Description
Moderately selective short-acting beta-2 receptor agonist (SABA); r-enantiomer of racemic albuterol; available as oral inhaler and nebulizer treatment
Used clinically in adult and pediatric patients for acute bronchospasm due to asthma as a reliever therapy and for asthma exacerbations; also used in adults with COPD
Clinical activity similar to racemic albuterol
Dosage And Indications
1.25 to 2.5 mg inhaled by nebulizer every 20 minutes for the first hour, then 1.25 to 5 mg inhaled by nebulizer every 1 to 4 hours as needed.
1.25 to 2.5 mg inhaled by nebulizer every 20 minutes for the first hour, then 1.25 to 5 mg inhaled by nebulizer every 1 to 4 hours as needed.
1.25 mg inhaled by nebulizer every 20 minutes for the first hour, then 0.075 to 0.15 mg/kg/dose (Max: 5 mg/dose) inhaled by nebulizer every 1 to 4 hours as needed.
1.25 mg inhaled by nebulizer every 20 minutes for the first hour, then 0.075 to 0.15 mg/kg/dose (Max: 5 mg/dose) inhaled by nebulizer every 1 to 4 hours as needed.
180 to 360 mcg (4 to 8 actuations of 45 mcg/actuation) every 20 minutes for up to 4 hours, then every 1 to 4 hours as needed.
180 to 360 mcg (4 to 8 actuations of 45 mcg/actuation) every 20 minutes for the first hour, then every 1 to 4 hours as needed.
180 to 360 mcg (4 to 8 actuations of 45 mcg/actuation) every 20 minutes for the first hour, then every 1 to 4 hours as needed. Delivery should occur with a spacer, with a mask for children younger than 4 years.
90 mcg (2 actuations of 45 mcg/actuation) inhaled by mouth every 4 to 6 hours as needed; 45 mcg (1 actuation) every 4 hours may be sufficient. Max: 540 mcg/day (12 actuations/day).
90 mcg (2 actuations of 45 mcg/actuation) inhaled by mouth every 4 to 6 hours as needed; 45 mcg (1 actuation) every 4 hours may be sufficient. Max: 540 mcg/day (12 actuations/day).
0.63 or 1.25 mg inhaled by nebulizer 3 times daily, every 6 to 8 hours, as needed. Max: 3.75 mg/day.
0.63 or 1.25 mg inhaled by nebulizer 3 times daily, every 6 to 8 hours, as needed. Max: 3.75 mg/day.
0.31 or 0.63 mg inhaled by nebulizer 3 times daily as needed. Max: 1.89 mg/day.
90 mcg (2 actuations of 45 mcg/actuation) via oral inhalation every 4 to 6 hours as needed; in some patients, 45 mcg (1 actuation) every 4 hours may be sufficient. More frequent administration or a larger number of inhalations is not routinely recommended. The optimal dosage of levalbuterol for the treatment of an acute COPD exacerbation is not established; adjust dose according to clinical symptoms or the development of adverse effects. According to the Global Initiative for Chronic Obstructive Lung Disease (GOLD) guidelines for COPD, levalbuterol 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 with SABAs in clinical trials; nebulizers may be more convenient for patients that are more acutely ill.[63765]
Initially, 0.63 mg via nebulizer 3 times per day, given every 6 to 8 hours. Patients who do not respond adequately may benefit from a dosage of 1.25 mg via nebulizer 3 times per day.[51793] Optimal dosing for a COPD exacerbation is not established; adjust dose according to clinical symptoms or the development of adverse effects.[55976] According to the Global Initiative for Chronic Obstructive Lung Disease (GOLD) guidelines for COPD, levalbuterol 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 with SABAs in clinical trials; nebulizers may be more convenient for patients that are more acutely ill.[63765]
90 mcg (2 actuations of 45 mcg/actuation) via oral inhalation, administered 15 minutes (range, 5 to 20 minutes) before exercise. A controller agent (e.g., daily inhaled corticosteroid) is recommended to be used along with as-needed and pre-exercise SABAs like levalbuterol.
90 mcg (2 actuations of 45 mcg/actuation) via oral inhalation, administered 15 minutes (range, 5 to 20 minutes) before exercise. A controller agent (e.g., daily inhaled corticosteroid) is recommended to be used along with as-needed and pre-exercise SABAs like levalbuterol.
Single doses of levalbuterol 2.5 mg have been administered in one trial of healthy adults and are reportedly as effective as albuterol 10 mg nebulized. K+ concentrations usually fall within 30 minutes of treatment. Levalbuterol reportedly results in fewer reported side effects than albuterol; however, it is more costly. Beta-agonists can be effective treatments for hyperkalemia via beta-adrenergic induction of potassium (K+) uptake. However, they are a temporary adjunctive measure.
0.31 mg via nebulizer every 8 hours was used in a retrospective analysis comparing levalbuterol (n = 31, mean corrected gestational age 31.4 weeks, mean birth weight 1.1 kg) to albuterol (1.25 mg every 8 hours, n = 16, mean corrected gestational age 29.9 weeks, mean birth weight 817 g). Investigators found no difference between albuterol and levalbuterol groups in relation to heart rate, oxygen supplementation, oxygen saturations, respiratory rate, hypokalemia, or hyperglycemia. A significant decrease in mean arterial blood pressure was observed in patients given albuterol versus levalbuterol; however, dosing differed between the 2 groups with patients administered albuterol receiving a dose that is twice the equivalent dose of levalbuterol.
†Indicates off-label use
Dosing Considerations
No dosage adjustments are needed.
No specific dosage adjustments are recommended; caution may be warranted during the administration of high doses in patients with renal impairment, as renal clearance is reduced.
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; 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; 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.
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.
Butalbital; Aspirin; 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.
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; 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.
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.
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.
How Supplied
Levalbuterol/Levalbuterol Hydrochloride/Xopenex/Xopenex Pediatric Respiratory (Inhalation) Sol: 0.31mg, 0.5mL, 0.63mg, 1.25mg, 3mL
Levalbuterol/Levalbuterol Tartrate/Xopenex Respiratory (Inhalation) Aer Met: 1actuation, 45mcg
Maximum Dosage
2 puffs (MDI) every 4 hours as needed for treatment/prevention of bronchospasm; higher doses may be required acutely during severe exacerbations. For nebulized solution, 1.25 mg/dose given 3 times/day for treatment/prevention of bronchospasm.
2 puffs (MDI) every 4 hours as needed for treatment/prevention of bronchospasm; higher doses may be required acutely during severe exacerbations. For nebulized solution, 1.25 mg/dose given 3 times/day for treatment/prevention of bronchospasm.
2 puffs (MDI) every 4 hours as needed for treatment/prevention of bronchospasm; higher doses may be required acutely during severe asthma exacerbations. For nebulized solution, 1.25 mg/dose given 3 times/day for treatment/prevention of bronchospasm; doses up to 5 mg/dose have been used off-label for acute exacerbations.
12 years: 2 puffs (MDI) every 4 hours as needed for treatment/prevention of bronchospasm; higher doses may be required acutely during severe asthma exacerbations. For nebulized solution, 1.25 mg/dose given 3 times/day for treatment/prevention of bronchospasm; doses up to 5 mg/dose have been used off-label for acute exacerbations.
6 to 11 years: 2 puffs (MDI) every 4 hours as needed for treatment/prevention of bronchospasm; higher doses may be required acutely during severe asthma exacerbations. For nebulized solution, 0.63 mg/dose given 3 times/day for treatment/prevention of bronchospasm; doses up to 0.15 mg/kg/dose (Max: 5 mg/dose) have been used off-label for acute exacerbations.
4 to 5 years: 2 puffs (MDI) every 4 hours as needed for treatment/prevention of bronchospasm; higher doses may be required acutely during severe asthma exacerbations. Safety and efficacy of the nebulized oral solution has not been established; however, doses up to 0.15 mg/kg/dose (Max: 5 mg/dose) have been used off-label for acute exacerbations.
1 to 3 years: Safety and efficacy have not been established.
Safety and efficacy have not been established.
Safety and efficacy have not been established; however, 0.31 mg via nebulizer every 8 hours has been used off-label for bronchodilation.
Mechanism Of Action
Mechanism of Action: Levalbuterol is the R-isomer of albuterol. It is a moderately selective beta2-adrenergic agonist that stimulates receptors of the smooth muscle in the lungs, uterus, and vasculature supplying skeletal muscle. Results from an in vitro study of binding to human beta-adrenergic receptors demonstrated that levalbuterol has approximately 2-fold greater binding affinity than racemic albuterol and approximately 100-fold greater binding affinity than (S)-albuterol. The R-isomer of albuterol, levalbuterol, is primarily responsible for bronchodilation, while the S-isomer lacks significant bronchodilator effects. Although not confirmed during clinical trials in humans, the S-isomer of albuterol has bronchoconstrictive properties in animal models. Data showing an increase in airway reactivity from the administration of S-albuterol are lacking in humans.Intracellularly, the actions of levalbuterol are mediated by cyclic AMP, the production of which is augmented by beta2-stimulation. Levalbuterol 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.Levalbuterol 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. Beta2-adrenergic stimulation also results in intracellular accumulation of serum potassium, possibly due to stimulation of the Na/K ATPase pump, leading to moderate degrees of hypokalemia.
Pharmacokinetics
Levalbuterol is administered via nebulized or aerosolized oral inhalation. Racemic albuterol crosses the blood-brain barrier and may cross the placenta. R-albuterol appears to be preferentially metabolized in the gastrointestinal tract, presumably by SULT1A3 (sulfotransferase). The primary route of elimination of R-albuterol is through renal excretion (80% to 100%), with 25% to 46% being excreted as unchanged drug in the urine. Less than 20% of the drug is excreted in the feces. The half-life is 3.3 to 4 hours in patients 12 years and older.
Affected cytochrome P450 (CYO450) isoenzymes or drug transporters: None
Following oral inhalation, levalbuterol is absorbed over several hours from the respiratory tract. Most of an inhaled dose is actually swallowed and absorbed through the GI tract. Plasma levels of levalbuterol after oral inhalation of therapeutic doses are very low. Peak serum concentrations of R-albuterol occur in 0.2 hours.
Oral inhalation solution: The mean onset time (15% increase in FEV-1) for nebulized doses of 0.63 mg and 1.25 mg levalbuterol was approximately 17 and 10 minutes, respectively. The mean time to peak effect is approximately 1.5 hours. The mean duration (more than a 15% increase in FEV-1) following administration of 0.63 and 1.25 mg doses of levalbuterol is 5 and 6 hours, respectively. In some patients, the duration of effect was as long as 8 hours.
Oral inhalation aerosol: The mean onset time (15% increase in FEV-1) for aerosolized doses of 90 mcg of levalbuterol (2 inhalations) ranges from 4.5 to 10.2 minutes. The mean time to peak effect is 76 to 78 minutes. The mean duration (more than a 15% increase in FEV-1) following administration of 90 mcg of levalbuterol is 3 hours, with a duration of effect as long as 6 hours in some patients.
Pregnancy And Lactation
There are no available data on the presence of levalbuterol in human milk, the effects on the breast-fed infant, or the effects on milk production. According to the National Asthma Education and Prevention Program (NAEPP) working group for managing asthma during pregnancy, there is no contraindication for use of short-acting inhaled beta-2 agonists (SABAs) during breast-feeding. Plasma concentrations of levalbuterol after inhalation of therapeutic doses are very low in humans, but it is not known whether levalbuterol is excreted in human milk. Gastrointestinal absorption is likely low in the breastfed infant.