Levalbuterol and albuterol both work by binding to beta-2 receptors found within the lungs, relaxing pulmonary muscles and helping clear airways.
Both medications are widely prescribed to manage chronic conditions like asthma and COPD. Patients often rely on long-term inhaler treatments for managing their symptoms.
Albuterol vs. Levalbuterol: Key Differences in Asthma Medications

Albuterol: A Widely Used Asthma Medication
Albuterol has been a trusted medication for over four decades in treating acute asthma exacerbations. It is composed of equal parts of a racemic mixture of R- and S-enantiomers.
While it is the most commonly prescribed inhaled beta-2 agonist, it’s important to note that it can have paradoxical effects if the inactive S-enantiomer persists in the body. Despite this, albuterol remains a preferred choice for reversing acute bronchospasm.
Levalbuterol: A More Recent Single-Isomer Formulation
Levalbuterol, on the other hand, is composed solely of the active R-enantiomer. By stimulating beta receptors, it promotes relaxation of the bronchial muscles. It has been synthesized more recently and is available as a single-isomer formulation.
However, in terms of tolerability and clinical outcomes, levalbuterol has yet to demonstrate a consistent advantage over albuterol.
Considerations for Levalbuterol Use

Levalbuterol may hold potential benefits for certain patients, particularly those with moderate to severe asthma who have been overusing racemic albuterol. One study suggested that levalbuterol might be safer than albuterol for patients with tachyarrhythmia, a rapid heart rate.
However, it is essential to note that overall, there is no overwhelming superiority of levalbuterol over albuterol in terms of clinical efficacy or tolerability.
Determining the Ideal Medication
At present, it remains unclear which patients would benefit more from levalbuterol over albuterol. Further research is necessary to identify any specific patient populations that may gain greater advantages from one drug compared to the other.
It is important for healthcare professionals to carefully evaluate each patient’s needs and consider individual factors when selecting the most appropriate medication for their asthma treatment.
Other Considerations

Efficacy
Xopenex (levalbuterol) and albuterol are short-acting beta-2 agonists (SABAs) used to treat breathlessness caused by asthma or chronic obstructive pulmonary disease (COPD). Both medications work by binding to beta-2 receptors in the lungs, relaxing smooth muscle, and opening airways; typically taken as emergency rescue medication during an asthma attack or an exposure to an irritant.
One study demonstrated that levalbuterol outperformed albuterol for bronchodilation of asthma patients. Both medications demonstrated comparable improvements in pulmonary function after up to 6 hours of use.
Another research paper explored protection offered against methacholine challenge by (R)- and (R,S)-albuterol; both could prevent any decrease in FEV1, while the former achieved higher concentrations in vivo than its counterpart.
Levalbuterol also reduces its tendency to cause hyperkalemia, an potentially life-threatening electrolyte disturbance which impairs heart and other organ functions. This usually happens from taking too much albuterol, increasing levels of its mirror image molecules (enantiomers).
Studies suggest (S)-albuterol may increase mast cell activation and consequently allergic inflammation; however, this does not appear clinically relevant at therapeutic doses. Patients should avoid mixing levalbuterol with other medications that affect b2-receptors in the lung such as beta blockers used to manage heart rate and blood pressure.
Side effects
Levalbuterol and albuterol are two bronchodilators that target beta receptors, and have both been known to cause tremors, shaking, tachycardia (increased heart rate), and jitters in certain people. Albuterol may cause more marked heart rate increases among children than levalbuterol; however, most researchers do not consider these differences to be clinically significant.
Both medications can open airways during an asthma attack and relieve wheezing, shortness of breath, coughing and chest tightness caused by chronic obstructive pulmonary disease (COPD) and asthma.
Levalbuterol differs from albuterol by having a longer duration of action, making it more suitable as an emergency treatment for severe bronchospasms. Both drugs, however, share similar side effects and it remains unclear which is superior.
Albuterol and levalbuterol can both be purchased as generic and name-brand medications; levalbuterol tends to be cheaper when sold in solution form than albuterol. Both drugs can lead to serious side effects if taken in excess, so patients should adhere strictly to any dose prescribed by their physician and report any change in symptoms which might indicate destabilization.
Please remember this article is meant as general education only; do not use it as a replacement for professional advice, diagnosis or treatment from licensed healthcare professionals.
Dosage

Levalbuterol and albuterol are short-acting beta-2 agonists (SABAs) used to manage acute breathlessness associated with asthma or COPD. Both drugs bind to beta-2 receptors in the lungs to induce smooth muscle relaxation and open airways more freely so more oxygen reaches your lungs. They come packaged both as metered-dose inhalers as well as solutions designed for use in nebulizers.
Both medications may cause temporary increases in heart rate, also known as tachycardia. While there may be variations between them in terms of how quickly or steadily your heart beats, no statistical difference was noted between them in this respect.
Some experts also report that levalbuterol has fewer side effects than albuterol, though this claim has yet to be proven in controlled trials.
Levalbuterol may help lower potassium levels for patients suffering from hyperkalemia, while albuterol raises their levels. It should be noted that low serum potassium levels could potentially lead to hypokalemia in certain instances.
Both medications are highly effective and have similar side effect profiles, making the decision between levalbuterol and albuterol an economic one. Albuterol is more widely available, less costly, and eligible SingleCare coupons can even bring its price down to $30 at participating pharmacies.
A recent cost-utility and budget impact analysis performed on hospitalized COPD patients concluded that levalbuterol use was cost-saving compared with albuterol use; although authors cautioned this analysis may depend on variable assumptions and evidence sources.
Suitability for specific conditions
While both levalbuterol and albuterol can serve as rescue medications for asthmatics, their choice depends on each individual patient.
Both have been found effective at managing symptoms associated with COPD; however, their individual effectiveness and side effects differ considerably; especially among those suffering tachyarrhythmias; patients who respond better to levalbuterol’s R-isomer may find more relief than with its S-isomer; this difference could be related to COPD causing more common tachyarrhythmias than with albuterol’s S-isomer.
Levalbuterol is generally more expensive than albuterol; however, this should not be used as the deciding factor when selecting medication. Albuterol can be obtained in generic forms while levalbuterol is only sold under its brand name Xopenex; also, there are multiple ways of comparing costs across delivery methods for medication.
Recent research examined the costs and benefits associated with using nebulized levalbuterol for hospitalized patients with COPD, using cost-utility analysis (CUA) and budget impact analysis (BIA). According to its results, levalbuterol may be more cost-effective than albuterol; its use could potentially bring significant savings to healthcare systems worldwide.
Making the decision to enroll in a clinical study is an individual one and should be made with medical advice in mind, as risks vary based on age, medical history and genetic makeup of each participant.