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Am Fam Physician. 2007;75(2):247-248

Author disclosure: Nothing to disclose.

Levalbuterol tartrate (Xopenex hFa) is a beta2-agonist, hydrofluoroalkane inhalation aerosol labeled for the treatment or prevention of bronchospasm in patients with reversible obstructive airway disease. Levalbuterol is the active R-isomer of albuterol (Proventil), which contains both the R- and S-isomers.

NameStarting dosageDose formApproximate monthly cost*
Levalbuterol tartrate (Xopenex HFA)Two inhalations every four to six hours in persons four years or older; in some patients, one inhalation every four hours issufficient.15-g metered-dose inhaler providing 45 mcg per actuation$50 for one inhaler (200 metered actuations)


Levalbuterol tartrate shares the same safety concerns as albuterol and other drugs in this class. Class labeling on safety includes warnings about paradoxical bronchospasm, cardiovascular effects (because of the concern about a heightened risk of cardiovascular complications from long-acting beta2 agonist use), and use in patients with worsening or deteriorating asthma. However, these effects have not been demonstrated with albuterol and levalbuterol tartrate specifically. Levalbuterol tartrate is a U.S. Food and drug administration pregnancy category C drug.


Levalbuterol tartrate is well tolerated and seems to have a side-effect profile similar to that of albuterol; studies have not demonstrated any reduction in side effects with levalbuterol tartrate at equivalent doses. Dizziness (2.7 percent), pharyngitis (7.9 percent), and rhinitis (7.4 percent) occur infrequently but more often than with albuterol or placebo.1


Results from clinical trials in adults show levalbuterol tartrate to be as effective as albuterol in improving lung function as measured by percent change in forced expiratory volume in one second (FEV1).1,2 The duration of action is approximately four hours in most persons and is similar to that of albuterol. Improved lung function is sustained over at least two months of continuous dosing. Based on one small study, the effect in children seems to be similar.1 pre-dose FEV1 values during chronic dosing (compared with baseline) have been significantly lower in patients receiving racemic albuterol compared with levalbuterol tartrate, suggesting a role of the S-isomer in the declining lung function observed during albuterol therapy.3

No research has compared levalbuterol tartrate inhalers and albuterol inhalers with regard to reduction in acute exacerbations, normalization of physical activity, symptom-free days, improvements in quality of life, control of airway hyperresponsiveness, normalization of chronic airway inflammation, or avoidance of adverse effects. However, there are studies that show comparable effectiveness in the nebulized forms of levalbuterol and albuterol.4


One levalbuterol tartrate inhaler (200 metered actuations) will cost patients approximately $50 for a typical one-month supply. This is higher than the cost of a generic albuterol inhaler, which ranges from $5 to $30. Levalbuterol tartrate currently is considered a nonformulary medication by most managed care insurers.


The usual dose of levalbuterol tartrate is two inhalations (90 mcg) every four to six hours in persons four years or older.2 In some patients, one inhalation every four hours may be sufficient. As with all inhalers, it is important to remind patients to prime the inhaler before initial use and after three days of inactivity. The mouthpiece also should be washed weekly to maintain proper medication dosing.

Bottom Line

Levalbuterol tartrate appears to be no more effective and offers no improvement in the side-effect profile compared with albuterol. The higher cost may make it appropriate for only a limited group of patients.

STEPS new drug reviews cover Safety, Tolerability, Effectiveness, Price, and Simplicity. Each independent review is provided by authors who have no financial association with the drug manufacturer.

This series is coordinated by Allen F. Shaughnessy, PharmD, assistant medical editor.

A collection of STEPS published in AFP is available at

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