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By Libby Pellegrini, MMS, PA-C
July 23, 2025
If you have a reactive airway disease such as asthma or COPD, you understand the importance of having a rescue medication on hand. Short-acting bronchodilator medications, such as albuterol and levalbuterol (Xopenex), can play a crucial role in relaxing the muscles surrounding the airways, making it easier to breathe during a respiratory flare. However, you may be curious about the difference between levalbuterol and albuterol. When it comes to a levalbuterol vs albuterol comparison, there are a few key considerations. Read on to learn more about Xopenex vs albuterol and why you would give levalbuterol instead of albuterol when considering rescue medications.
So, levalbuterol vs albuterol—what is the difference between these medications in the first place? You can be pardoned for thinking of these medications interchangeably, as they belong to the same medication class of short-acting bronchodilators, and they have the same mechanism of action. Both medications bind to beta-2 adrenergic receptors on bronchial smooth muscle cells, allowing for the relaxation of these muscles and a reduction in bronchial tube constriction. The original form of albuterol is a 50-50 mix of two molecules that are mirror images of one another (a phenomenon known as “enantiomers”). One of these molecules, known as R-albuterol, is more specific for the respiratory beta2-adrenergic receptors than its mirror image, the S-albuterol molecule. The R-albuterol is known as the “active form” of the molecule, while its mirror image is inactive. Theoretically, then, a medication that is composed of only R-albuterol molecules would be more specific for treating asthma and might have fewer side effects when comparing levalbuterol tartrate vs albuterol.
Levalbuterol is a bronchodilating medication that is composed only of the R-albuterol molecule of albuterol. Levalbuterol is also known by the brand name Xopenex. Levalbuterol was chemically derived decades after the original albuterol medication was introduced to the market, with the intention that it might be more specific in treating respiratory diseases. This is because when comparing albuterol vs Xopenex, albuterol contains a mixture of albuterol molecules, only half of which are specific to receptors on airway cells. The other molecules are considered to be “inactive” or inert, and they don’t provide any bronchodilating effects.
Albuterol is a short-acting beta agonist (SABA) medication that belongs to a class of bronchodilators. Albuterol is a rescue medication that helps open up the airways during an asthma or COPD exacerbation by binding to beta-2 adrenergic receptors on bronchial smooth muscle cells, thereby relaxing and dilating the constricted airways. Pharmacologically, albuterol is made up of two molecules that are mirror images of each other, S-albuterol and R-albuterol. Only the R-albuterol molecule is the active form that binds in the respiratory tract, whereas S-albuterol is the inert, or inactive form.
When considering levalbuterol vs albuterol for asthma symptoms, it’s essential to understand how both of these medications work. Asthma is a reactive and reversible airway condition in which the passageways of the respiratory tract, known as bronchial tubes, begin to constrict because they have been exposed to some sort of trigger. Levalbuterol and albuterol are bronchodilating medications that help relax the smooth muscles surrounding the bronchial tubes, keeping the airways open and relieving asthma symptoms such as wheezing, shortness of breath, and chest pain.
When contemplating albuterol vs xopenex, or levalbuterol tartrate vs albuterol sulfate, it’s important to understand the two medications fully.
Levalbuterol | Albuterol | |
Molecular composition | Made of 100% R-albuterol isomer molecules | Made of a 50:50 mixture of R-albuterol and S-albuterol isomer molecules |
Length of time in use | Introduced in 1999 | Introduced in 1968 |
Cost of medication | Higher cost | Lower cost |
Medication mechanism of action | Bronchodilates by binding to beta-2 adrenergic receptors | Bronchodilates by binding to beta-2 adrenergic receptors |
Patient population | Approved for use in children aged 4 or greater | Approved for use in children aged 2 or greater |
The medication levalbuterol is not identical to albuterol, although both medications are helpful for asthma and work similarly. Levalbuterol is made up of only one type of albuterol molecule (the R-albuterol form), whereas albuterol contains both the R-albuterol and S-albuterol forms. It is more expensive to isolate the active form of R-albuterol, so levalbuterol tends to be a bit pricier compared to albuterol.
When levalbuterol first came to market, it was hypothesized that it might be more effective than albuterol because it was made of purely the active form of albuterol. However, this has not borne out in practice. Many studies have shown that albuterol and levalbuterol are essentially equivalent when it comes to treating asthma and COPD symptoms. Although they have different molecular compositions, they both help reduce asthma symptoms in the same way.
Albuterol and levalbuterol tend to have similar side effects. Both medications can cause nausea, tremors, and anxiety. Some studies have shown that levalbuterol has a less pronounced effect on heart rate, especially in children. However, this is not a universal finding.
Albuterol and levalbuterol are the same medication with the same side effect profiles. Because levalbuterol contains only the active R-albuterol molecule, some have suspected that it may have fewer unwanted side effects compared to the 50:50 mix of generic albuterol. However, studies show that the impact on heart rate and other side effects is not different between levalbuterol and albuterol.
Levalbuterol can be highly effective in treating asthma when used as directed. Many asthma experts recommend pairing a SABA medication like levalbuterol with an inhaled corticosteroid, which has the most significant effect on asthma symptoms.
Albuterol is highly effective in treating asthma and has been used for many decades. Albuterol can be used at home, in a clinic, and even in an emergency setting to help quickly relieve symptoms of asthma. Many asthma experts recommend pairing a SABA medication like albuterol with an inhaled corticosteroid has the most significant effect on asthma symptoms.
Why would you give levalbuterol instead of albuterol for asthma treatment? When comparing levalbuterol tartrate to albuterol, the research indicates that the medications are essentially the same, with similar efficacy and side effect profiles. Some studies have shown that for individuals with cardiac conditions, such as a fast heart rate, levalbuterol may be a preferable option. However, this is not a universal recommendation.
No, researchers have studied levalbuterol vs albuterol, and they have found no clinically significant difference in these medications when it comes to asthma or COPD management. Levalbuterol contains a molecular form of albuterol that is active only in the respiratory system. However, a systemic review did not find that levalbuterol was stronger than albuterol.
Universally, it is not recommended to use levalbuterol over albuterol in any specific scenario. However, some clinicians may recommend using levalbuterol for patients who have underlying problems with a fast heart rate, because it may cause fewer potential cardiac side effects. This may be the most pronounced in the pediatric population.
The difference between levalbuterol tartrate vs albuterol sulfate lies in their molecular composition. Levalbuterol is made of one form of the albuterol molecule, known as the R-albuterol isomer. This is the active form of the molecule. Albuterol is made of a 50-50 mixture of the R-albuterol isomer and the S-albuterol isomer.
There is no clear-cut answer about which medication is better when comparing albuterol vs xopenex. The difference between albuterol and levalbuterol lies in their chemical composition. However, there are no clinically discernible differences in how these medications work to treat asthma symptoms.
No, it is not recommended to combine these medications. If you are prescribed levalbuterol, it is essential to take only levalbuterol, and the same is true for albuterol. There is no need to combine these medications, alternate them, or make any other adjustments, because they are essentially the same medication.
When it comes to pediatric asthma, there is no obvious preferred agent. Ultimately, the decision to use levalbuterol vs albuterol will come down to availability and the price of the medication. Both medications are available in generic form; however, levalbuterol tends to be more expensive than albuterol. Only albuterol is indicated for treating exercise-induced asthma, and it is approved for use in children ages two and older. In contrast, levalbuterol is approved for use in children ages four and older.
https://pmc.ncbi.nlm.nih.gov/articles/PMC5990133/
https://www.sciencedirect.com/science/article/abs/pii/S109455391200171X
https://www.aafp.org/pubs/afp/issues/2008/0501/p1214.html
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