Long acting beta-adrenoceptor agonist
Encyclopedia
Long-acting beta-adrenoceptor agonists (LABAs, more specifically β2-agonists) are usually prescribed for moderate to severe persistent asthma
patients or patients with chronic obstructive pulmonary disease
(COPD). They are designed to reduce the need for shorter-acting β2-agonists such as salbutamol
, as they have a duration of action of approximately 12 hours in comparison with the 4- to 6-hour duration of salbutamol, making them candidates for sparing high doses of corticosteroids or treating nocturnal asthma and providing symptomatic improvement in patients with COPD. With the exception of formoterol
, long-acting β2-agonists are not recommended for the treatment of acute asthma exacerbations because of their slower onset of action compared to salbutamol
. Their long duration of action is due to the addition of a long, lipophilic side-chain that binds to an exosite on adrenergic receptors. This allows the active portion of the molecule to continuously bind and unbind at β2 receptors
in the smooth muscle in the lungs.
Some currently available long-acting beta-adrenoceptor agonists are:
An ultra-long-acting beta-adrenoceptor agonist that has a duration of action of 24 hours, allowing for once-daily dosing is now approved for use in Europe:
Asthma
Asthma is the common chronic inflammatory disease of the airways characterized by variable and recurring symptoms, reversible airflow obstruction, and bronchospasm. Symptoms include wheezing, coughing, chest tightness, and shortness of breath...
patients or patients with chronic obstructive pulmonary disease
Chronic obstructive pulmonary disease
Chronic obstructive pulmonary disease , also known as chronic obstructive lung disease , chronic obstructive airway disease , chronic airflow limitation and chronic obstructive respiratory disease , is the co-occurrence of chronic bronchitis and emphysema, a pair of commonly co-existing diseases...
(COPD). They are designed to reduce the need for shorter-acting β2-agonists such as salbutamol
Salbutamol
Salbutamol or albuterol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. It is marketed as Ventolin among other brand names....
, as they have a duration of action of approximately 12 hours in comparison with the 4- to 6-hour duration of salbutamol, making them candidates for sparing high doses of corticosteroids or treating nocturnal asthma and providing symptomatic improvement in patients with COPD. With the exception of formoterol
Formoterol
Formoterol or eformoterol is a long-acting β2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease...
, long-acting β2-agonists are not recommended for the treatment of acute asthma exacerbations because of their slower onset of action compared to salbutamol
Salbutamol
Salbutamol or albuterol is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. It is marketed as Ventolin among other brand names....
. Their long duration of action is due to the addition of a long, lipophilic side-chain that binds to an exosite on adrenergic receptors. This allows the active portion of the molecule to continuously bind and unbind at β2 receptors
Beta-2 adrenergic receptor
The beta-2 adrenergic receptor , also known as ADRB2, is a beta-adrenergic receptor, and also denotes the human gene encoding it.-Gene:The gene is intronless...
in the smooth muscle in the lungs.
Some currently available long-acting beta-adrenoceptor agonists are:
- SalmeterolSalmeterolSalmeterol is a long-acting beta2-adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease. It is currently available as a dry powder inhaler that releases a powdered form of the drug...
- FormoterolFormoterolFormoterol or eformoterol is a long-acting β2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease...
- BambuterolBambuterolBambuterol is a long acting beta-adrenoceptor agonist used in the treatment of asthma; it also is a prodrug of terbutaline. Commercially, the AstraZeneca pharmaceutical company produces and markets bambuterol as Bambec and Oxeol ....
An ultra-long-acting beta-adrenoceptor agonist that has a duration of action of 24 hours, allowing for once-daily dosing is now approved for use in Europe:
- IndacaterolIndacaterolIndacaterol is an ultra-long-acting beta-adrenoceptor agonist developed by by Novartis.It was approved by the European Medicines Agency under the trade name Onbrez on November 30, 2009, and by the United States Food and Drug Administration , under the trade name Arcapta Neohaler, on July 1, 2011...