Beta Adrenergic Receptor Agonists

Adrenergic ß2-agonists are a group of medications that are used to treat asthma, chronic obstructive pulmonary disorder (COPD) and other diseases and conditions of the lungs and respiratory system. These agents are also commonly referred to as ß2-adrenergic receptor agonists or ß2-adrenergic agonists.

Adrenergic ß2-agonist medications work by stimulating the ß2-adrenergic receptors. These receptors, when stimulated, cause relaxation of smooth muscles including those that line the bronchial tubes. ß2-adrenergic receptor agonists activate the response of these receptors, dilating the airway and facilitating respiration, making them especially useful in treating patients with asthma and COPD. These drugs also cause blood vessel dilation, which can aid in distribution of the steroid-based asthma medications.

ß2-adrenergic receptor agonists may also be used in some patients prior to exercise, to prevent coughing and shortness of breath that may occur during physical activity.

Adrenergic ß2-agonist products are available in several dosing forms, including metered-dose inhaler, pill, syrup, and nebulizer forms. Some ß2-agonist medications can be injected. Nebulizers are usually reserved for patient with severe and persistent symptoms, and achieve the same effects and fast action as injected medications.

ß2-adrenergic agonists are divided into two groups: short-acting ß2-adrenergic agonists, which are effective for four to six hours in most individuals; and long-acting ß2-adrenergic agonists (also referred to as LABA agents), which can remain active for 12 hours and longer.

Generally, short-acting ß2-adrenergic agonists are used to relieve symptoms in individuals with intermittent or mild symptoms of asthma or COPD, while long-acting ß2-adrenergic agonists are used to treat patients with chronic, persistent symptoms.

Long acting B2-agonists owe their duration to the addition of a molecule chain that allows the medication to continually bind and unbind at the gene receptor sites in the lungs.

Clinical studies are currently being conducted to evaluate an ultra-long-acting adrenergic ß2-agonist called indacaterol, which would be effective for 24 hours.

Short-acting ß2-adrenergic agonists include salbutamol or albuterol, which is marketed under the trade name Ventolin; pirbuterol, which is marketed under the trade name Maxair; metaproterenol, which is marketed under the trade name Alupent; levosalbuterol; terbutaline; procaterol; fenoterol; and bitolterol mesylate.

Long-acting ß2-adrenergic agonists include salmeterol, marketed as Serevent and is one of the active ingredients in Advair; formoterol, marketed as Foradil and is one of the active ingredients in Symbicort; clenbuterol; and bambuterol.

Side effects of ß2-adrenergic receptor agonists include insomnia, nervousness or anxiety, rapid or irregular heartbeat and tremor. The FDA has also reported that some long-acting ß2-adrenergic agonists are associated with an increased risk of worsening wheezing in some patients. Regularly inhaled ß2-adrenergic agonists have also been associated with an increased risk of respiratory death in some patients with COPD, according to a 2006 study conducted by researchers from Cornell University and Stanford University.

In 2008, the FDA banned the use of Serevent and Foradil in the treatment of asthma, after research indicated that these two drugs, when prescribed without accompanying steroids, increased the risk of more severe asthma attacks. Advair and Symbicort, two other long-acting adrenergic ß2-agonist medications, were not found to be associated with this particular increased risk. Like Foradil, Symbicort also contains formoterol, but in combination with the steroid Budesonide.

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