Inhaled Beta-2 Agonists

Inhaled beta-2 agonists are bronchodilators. They dilate (open) the bronchial tubes (airways) in the lungs. By stimulating specific areas called beta-2 receptors in the airways, bronchodilators allow the airway muscles to relax. This causes the airways to expand and allows more air to pass through the lungs. Inhaled beta-2 agonists are available in both short-acting and long-acting forms.

One of the short-acting beta-2 agonists is usually prescribed for patients with asthma. Short-acting beta agonists include albuterol, levalbuterol, metaproterenol, and pirbuterol. In Europe and Canada, albuterol is known as salbutamol. These drugs are called rescue medications because they can stop difficult breathing, shortness of breath, and other symptoms once an asthma attack begins. Generally, the effects of short-acting beta-2 agonists last for only a few hours.

Long-acting beta-2 agonists are often called controllers because patients with moderate-to-severe asthma use them regularly to control asthma. Both formoterol and salmeterol are long-acting beta-2 agonists. They can prevent asthma attacks because their effects persist for several hours. However, long-acting beta-2 agonists cannot stop an asthma attack that has already started. They are usually added to therapy when the patient still has asthma symptoms despite using another asthma medication, such as an inhaled corticosteroid. Long-acting beta-2 agonists must be used on a continual basis to be effective.

Drugs in this Class
Albuterol Sulfate Inhaler (Proair HFA Inhalation Aerosol, Proventil HFA Inhalation Aerosol, Ventolin HFA Inhalation Aerosol)
Formoterol Powder Capsules for Inhalation  (Foradil Aerolizer Powder for Inhalation, Formoterol Fumarate Powder Capsules for Inhalation )
Albuterol Nebulizer Solution (Accuneb Solution for Inhalation)
Metaproterenol Inhalation Suspension (Alupent Inhalation)
Levalbuterol Nebulizer (Xopenex Nebulizer, Xopenex Pediatric Nebulizer)
Salmeterol Aerosol Inhalation (Serevent)
Albuterol Inhaler (Proventil Inhaler)
Metaproterenol Nebulizer Solution ()
Levalbuterol (Levalbuterol Inhaler, Xopenex HFA Inhaler)
Pirbuterol Inhaler (Maxair Autohaler, Pirbuterol Acetate Inhaler)
Salmeterol Powder Inhalation (Servent Diskus)

Summarizing the Evidence

Short-Acting Inhaled Beta-2 Agonists:

  • Many clinical studies have been conducted to study short-acting inhaled bronchodilators in patients with asthma. However, no large-scale studies have compared all the medications in this category. In general, each short-acting beta-2 agonist produces about the same response when administered in equivalent doses.
  • The oldest short-acting beta-2 agonist is albuterol. Albuterol is the one studied most in clinical trials. It is also the one most commonly prescribed.
  • Newer drugs, such as pirbuterol and levalbuterol, are comparable in effectiveness and safety to albuterol, but their cost may be much higher.
  • Compared to metaproterenol, albuterol and levalbuterol stimulate the heart less and may work longer to open the airways. Thus, metaproterenol is not often used for the treatment of asthma.
  • Many newly diagnosed asthma patients begin therapy with albuterol. Generally, however, the selection of a short-acting beta-2 agonist typically depends on the doctor's preference, the patient's experience with previous treatment, and other medications the patient may be taking (to avoid potential drug interactions).
  • Short-acting beta-2 agonist inhalers that contain chlorofluorocarbon (CFC) will be removed from the market by December 31, 2008. CFC is a chemical that pollutes the environment. Some manufacturers are now using hydrofluoroalkane (HFA) in place of CFC.

Long-Acting Inhaled Beta-2 Agonists:

  • Several studies have compared the effects of formoterol and salmeterol for patients with asthma. In one study, the effectiveness of each drug was measured using peak expiratory flow rate (PEFR) during the last week in an 8-week study. PEFR is a breathing test commonly used to determine asthma severity and to assess lung function. After the first 4 weeks of treatment, patients in the formoterol group experienced greater improvements in lung function and fewer daytime asthma symptoms. However, there were no significant differences between the treatments by the end of the study
  • Results from another study also suggest that formoterol may have a faster onset of action as demonstrated by a higher initial increase in PEFR. However, the duration of action (the amount of time that the medication's effects last) for both formoterol and salmeterol is about the same.
  • The safety of both formoterol and salmeterol also appear to be similar, but more studies are needed for confirmation.

Dosing and Administration

Short-Acting Inhaled Beta-2 Agonists:
Most short-acting beta-2 agonists come as aerosols which are inhaled by mouth. Most of them are available both as solutions to be used with a nebulizer machine and as metered-dose inhalers (MDIs), which can be carried easily in a pocket or purse. For the prevention and treatment of acute bronchospasm (asthma attacks), a typical dose for albuterol, levalbuterol, or pirbuterol inhalers is one inhalation or two inhalations every 4 hours to 6 hours. Usually, one nebulizer treatment of levalbuterol is recommended three times a day. One inhalation or two inhalations of metaproterenol may be taken every 3 hours to 4 hours (up to 12 doses in a 24-hour period). Often short-acting beta agonists are used only when needed to control the symptoms of asthma.

Long-Acting Inhaled Beta-2 Agonists:
Both formoterol and salmeterol are dry powders with special inhalers. Formoterol is available as sheets of six capsules, which are removed from the sheet and placed into the inhaler device individually. Salmeterol comes in a sealed inhaler containing 60 doses and indicating the remaining number of doses on the inhaler device. For the maintenance treatment of asthma, formoterol can be inhaled once daily while salmeterol typically is used twice daily. Both are inhaled through the mouth.

Generic Availability

Short Acting Inhaled Beta-2 Agonists:

  • Currently, only albuterol inhalers, albuterol solution for inhalation, and metaproterenol solution for inhalation are available generically. Generic medications may be a less expensive but comparably effective treatment option.
  • However, an international agreement known as the Montreal Protocol requires countries to decrease the amount of ozone-lowering chemicals released into the air. Reducing that type of pollution means that inhalers containing a specific kind of propellant (chlorofluorocarbon or CFC) will be removed from the worldwide market by the end of 2008. Since generic albuterol inhalers use the banned propellant, generic albuterol inhalers may be in short supply well before the deadline, when they will not be available at all.

Long Acting Inhaled Beta-2 Agonists:

  • Neither formoterol nor salmeterol is available as a generic.

Drug Interactions

Some interactions between medications can be more severe than others. The best way for you to avoid harmful interactions is to tell your doctor and/or pharmacist what medications you are currently taking, including any over-the-counter products, vitamins, and herbals. For specific information on how the drugs interact and the severity of the interaction, please use our Drug Interactions Checker.

Side Effects

To view specific side effect information, please use our Side Effect Checker.

Additional Information

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Last Updated: August 2008

Note: The above information is intended to supplement, not substitute for, the expertise and judgment of your physician, pharmacist, or other healthcare professional. It should not be construed to indicate that the use of the product is safe, appropriate, or effective for you. Consult your healthcare professional before taking any medication.

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