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[1] is now approved for use in Europe:[2]
|
||||||||||||||||||||||||||||||||||||||||||||||||