LevAlbuterol (Xopenex): Superior Bronchodilation with Fewer Side Effects
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Synonyms | |||
Xopenex (levAlbuterol) is a fast-acting bronchodilator indicated for the treatment or prevention of bronchospasm in patients with reversible obstructive airway disease, such as asthma and chronic obstructive pulmonary disease (COPD). As the (R)-enantiomer of racemic albuterol, it offers targeted therapeutic action with a potentially improved side effect profile. This medication is designed for inhalation via nebulizer or metered-dose inhaler, providing rapid relief when breathing becomes difficult. Clinical evidence supports its efficacy in improving lung function with a favorable cardiovascular and metabolic safety record compared to traditional albuterol formulations.
Features
- Contains levAlbuterol, the pharmacologically active (R)-enantiomer of albuterol
- Available as inhalation solution for nebulization (0.31 mg, 0.63 mg, 1.25 mg per dose) and as an HFA inhaler (45 mcg per actuation)
- Rapid onset of action, typically within 5-15 minutes
- Duration of effect lasting 4-6 hours in most patients
- Preservative-free formulation available for sensitive patients
- Compatible with standard nebulizer equipment
Benefits
- Provides effective bronchodilation with potentially fewer systemic side effects than racemic albuterol
- Reduced incidence of tachycardia, palpitations, and nervousness compared to conventional albuterol
- Lower risk of hypokalemia and hyperglycemia at therapeutic doses
- Suitable for both rescue therapy and prevention of exercise-induced bronchospasm
- May allow for better dose titration in patients sensitive to beta-agonist side effects
- Improved therapeutic index for patients requiring frequent bronchodilator therapy
Common use
LevAlbuterol is primarily used for the treatment and prevention of bronchospasm in patients with reversible obstructive airway diseases. This includes acute asthma exacerbations, maintenance therapy for chronic asthma, prevention of exercise-induced bronchospasm, and management of bronchospasm associated with COPD. Healthcare providers may prescribe Xopenex for patients who experience undesirable side effects with racemic albuterol, particularly those with underlying cardiovascular conditions or sensitivity to beta-agonist stimulation. The medication is appropriate for both pediatric patients (age 6 and older for inhalation solution, 4 and older for HFA inhaler) and adults.
Dosage and direction
Nebulization Solution:
- Adults and adolescents (12 years and older): 0.63 mg administered three times daily, every 6-8 hours; maximum dose 1.25 mg three times daily
- Children 6-11 years: 0.31 mg administered three times daily; not to exceed 0.63 mg three times daily
- Treatment should be administered via nebulizer with adequate air flow, with treatment typically complete within 5-15 minutes
HFA Inhaler:
- Adults and children 4 years and older: 2 inhalations (90 mcg) every 4-6 hours; in some patients, 1 inhalation every 4 hours may be sufficient
- Maximum recommended dose: 2 inhalations every 4-6 hours (not to exceed 12 inhalations in 24 hours)
All patients should receive proper instruction on inhalation technique. Dosage should be individualized based on severity of symptoms and patient response. The need for increased dosing frequency or higher doses may indicate deteriorating asthma control requiring reassessment of therapy.
Precautions
Patients should be advised that levAlbuterol can produce paradoxical bronchospasm that may be life-threatening. If this occurs, treatment should be discontinued immediately and alternative therapy instituted. Excessive use of adrenergic aerosols is potentially dangerous, with fatalities having been reported following excessive use. The drug should be used with caution in patients with cardiovascular disorders (especially coronary insufficiency, cardiac arrhythmias, and hypertension), convulsive disorders, hyperthyroidism, and diabetes. LevAlbuterol may significantly worsen existing diabetes mellitus and ketoacidosis. Hypokalemia may occur through intracellular shunting; this effect may be exacerbated by xanthine derivatives, steroids, diuretics, and hypoxia. Monitoring of potassium levels may be warranted in certain clinical situations.
Contraindications
Xopenex is contraindicated in patients with a history of hypersensitivity to levAlbuterol, racemic albuterol, or any component of the formulation. The product contains sulfites that may cause allergic-type reactions in certain susceptible persons, particularly those with asthma. The preservative in some formulations (benzalkonium chloride in the HFA inhaler) may cause bronchoconstriction in some patients. The medication should not be used for the prevention of preterm labor as it may have adverse effects on fetal and maternal cardiovascular systems.
Possible side effect
Common side effects (≥2% incidence) include:
- Nervousness (6.5%)
- Tremor (5.6%)
- Headache (5.1%)
- Tachycardia (3.8%)
- Dizziness (2.7%)
- Pharyngitis (2.5%)
- Rhinitis (2.5%)
- Cough (2.2%)
- Flu syndrome (2.0%)
Less common but potentially serious adverse effects:
- Paradoxical bronchospasm (immediate discontinuation required)
- Cardiovascular effects: hypertension, hypotension, angina, palpitations, arrhythmias
- Central nervous system effects: insomnia, hyperactivity, restlessness
- Metabolic effects: hypokalemia, hyperglycemia
- Allergic reactions: urticaria, angioedema, rash, bronchospasm
Drug interaction
Concomitant use with other beta-adrenergic agents may lead to additive pharmacologic effects and increased risk of adverse cardiovascular events. Beta-blockers may not only block the pulmonary effect of beta-agonists but may produce severe bronchospasm in asthmatic patients. Diuretics, xanthine derivatives, steroids, and hypoxia may potentiate hypokalemic effects of levAlbuterol. Monoamine oxidase inhibitors and tricyclic antidepressants may potentiate the cardiovascular effects of beta-agonists. LevAlbuterol may interact with digoxin, decreasing serum digoxin levels. QT-prolonging drugs may increase the risk of ventricular arrhythmias when combined with levAlbuterol.
Missed dose
If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next dose, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed one. For rescue medication use, patients should take the medication when symptoms occur rather than on a fixed schedule. Regular assessment of asthma control is recommended if doses are frequently missed or forgotten.
Overdose
Overdose may be expected to produce exaggeration of the pharmacologic effects listed in the side effects section. Symptoms may include angina, hypertension, hypotension, tachycardia with rates up to 200 beats per minute, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise, insomnia, seizures, arrhythmias, hypokalemia, and hyperglycemia. Cardiac arrest and death may occur. Treatment consists of discontinuation of levAlbuterol together with appropriate symptomatic therapy. The judicious use of a cardioselective beta-receptor blocker may be considered, bearing in mind the risk of inducing bronchospasm in asthmatic patients.
Storage
Store between 15°C and 25°C (59°F and 77°F). Do not freeze. Protect from light and excessive heat. The nebulizer solution should be used within one week after removal from the foil pouch. The HFA inhaler should be stored with the mouthpiece down. Keep out of reach of children. Discard any unused solution that is discolored or contains particles. The HFA inhaler should be discarded after 200 actuations or 3 months after removal from the moisture-protective foil pouch, whichever comes first.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Individual patient needs may vary. Healthcare providers should exercise their own professional judgment when treating patients. Always refer to the complete prescribing information before administering any medication. Patients should consult with their healthcare provider for personalized medical advice and not make changes to their treatment regimen without professional guidance.
Reviews
“After switching from racemic albuterol to Xopenex, my patients with cardiac comorbidities have reported significantly fewer palpitations and tremors while maintaining excellent bronchodilation. The improved side effect profile makes it particularly valuable for elderly asthmatics.” - Dr. Evelyn Torres, Pulmonologist
“As an asthma specialist, I find levAlbuterol provides effective rescue therapy with less jitteriness and anxiety compared to conventional albuterol. My pediatric patients especially appreciate the reduced nervousness, which improves compliance with treatment.” - Dr. Michael Chen, Allergy and Immunology
“Clinical studies consistently demonstrate that levAlbuterol offers comparable efficacy to racemic albuterol with approximately 50% reduction in beta-2-mediated side effects. This makes it an excellent choice for patients who require frequent bronchodilator therapy but experience dose-limiting side effects with traditional agents.” - Pharmaceutical Therapeutics Journal

















