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Xopenex for Asthma

Is Xopenex Better Than Albuterol For Asthma, And With Fewer Side Effects?

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Updated October 25, 2012

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Xopenex for Asthma

The available "rescue" inhalers available for the treatment of acute asthma symptoms. From left to right, ProAir HFA (albuterol), Proventil HFA (albuterol), Ventolin HFA (albuterol) and Xopenex HFA (levalbuterol).

© Daniel More, MD

What is Xopenex?

Xopenex (levalbuterol) is an inhaled medication for the treatment of acute asthma symptoms, including coughing, wheezing, shortness of breath and chest tightness. Xopenex works by relaxing the smooth muscles around the lungs, usually within a few minutes of taking the medication. Xopenex is available both as an inhaler as well as in a solution form delivered via nebulizer machine.

Xopenex is the active isomer of albuterol (called R-albuterol or levalbuterol). The chemical structures of medications exist as a mixture of mirror images of one another (referred to as a racemic mixture), and only one of these forms is the active medication. The inactive form (called S-albuterol or dextroalbuterol) serves no purpose except that it “gets in the way” of the active form and may still contribute to side effects. This was the purpose to why Xopenex was developed -– to improve the function of albuterol while decreasing the side effects.

Is Xopenex Better than Albuterol for Asthma?

It’s not completely clear. When Xopenex was first developed, animal studies suggested that S-albuterol caused inflammation in the lungs, which could possibly worsen asthma. It was also thought that as more racemic albuterol (mixture of the R and S-albuterol isomers) was taken, the S-albuterol isomer would accumulate within the lungs and result in contraction of the smooth muscles around the lungs, thereby worsening asthma symptoms. Xopenex was therefore expected to work better at treating asthma symptoms than racemic albuterol.

Early studies did show that Xopenex was better at treating asthma than albuterol, since less Xopenex was needed to achieve control of asthma symptoms than comparable amounts of albuterol. Since Xopenex is the active half of albuterol, one would expect that half the dose of Xopenex would be equivalent to twice the dose of albuterol; however, these studies suggested that only one-fourth of the dose of albuterol was needed to achieve the same result when using Xopenex. This was thought to be due to the lack of the S-albuterol isomer in Xopenex, which was working against the R-albuterol isomer.

Recent data on Xopenex, however, along with an overview of all of the available data, suggests that Xopenex is no better at treating asthma than would be expected. The dose of Xopenex required to achieve the same result of treating asthma does appear to be approximately one-half, which is what is expected since it contains the active isomer (R-albuterol). The S-albuterol isomer appears to be inert, meaning that it does not act for or against the treatment of asthma symptoms.

Does Xopenex Have Fewer Side Effects than Albuterol?

Albuterol is well-known to cause certain side effects, including muscle tremors, jitteriness, palpitations and increased heart rate. Early studies on Xopenex suggested that because far less medicine was needed to achieve the same benefit as albuterol, fewer side effects would occur. In addition, it was initially thought that the S-albuterol isomer was primarily responsible for many of the albuterol side effects, and therefore Xopenex, which does not contain the S-albuterol isomer, would cause few side effects.

Recent studies suggest, however, that the side effects of Xopenex are equivalent to albuterol, since it is actually the R-albuterol isomer that is responsible for the albuterol side effects. The S-albuterol isomer is inert, meaning is does not contribute to side effects. The package insert for Xopenex states that the rate of the above mentioned side effects are similar for equivalent doses of Xopenex and albuterol.

Learn how to use and clean a Xopenex inhaler.

Sources:

Xopenex package insert [PDF]. Sepracor corporation. Accessed January 13, 2011.

Ahrens R, Weinberger M. Levalbuterol and Racemic Albuterol: Are There Therapuetic Differences? J Allergy Clin Immunol. 2001;108:681-4.

Milgrom H, Skoner DP, Bensch G, et al. Low-Dose Levalbuterol in Children with Asthma: Safety and Efficacy in Comparison with Placebo and Racemic Albuterol. J Allergy Clin Immunol. 2001;108:938-45.

Lötvall J, Palmqvist M, Arvidsson P, et al. The Therapuetic Ratio of R-Albuterol is Comparable with that of RS-Albuterol in Asthmatic Patients. J Allergy Clin Immunol. 2001;108:681-4.

DISCLAIMER: The information contained in this site is for educational purposes only, and should not be used as a substitute for personal care by a licensed physician. Please see your physician for diagnosis and treatment of any concerning symptoms or medical condition.

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