Long-acting beta-adrenoceptor agonist

Long-acting beta-adrenoceptor agonist (LABA) are a type of pharmacological agent that are designed to provide bronchodilation for an extended period of time. They are primarily used in the management of asthma and chronic obstructive pulmonary disease (COPD).

Mechanism of Action

LABAs work by stimulating the beta-2 adrenergic receptor on the smooth muscle cells that line the airways, leading to relaxation and bronchodilation. This action is achieved through the activation of adenylate cyclase, which increases the production of cyclic adenosine monophosphate (cAMP). The increased cAMP levels lead to the relaxation of bronchial smooth muscle, inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells, and a strengthened barrier function of the bronchial epithelium.

Clinical Use

LABAs are used in the long-term management of asthma and COPD. They are often used in combination with corticosteroids, which provide an anti-inflammatory action. This combination therapy is more effective in controlling symptoms and improving lung function than either drug used alone.

Examples

Examples of LABAs include salmeterol, formoterol, and indacaterol. These drugs have a duration of action of at least 12 hours, making them suitable for once or twice daily dosing.

Safety and Side Effects

While LABAs are generally well-tolerated, they can cause side effects such as tremor, palpitations, and a slight risk of cardiac arrhythmias. There has been some controversy over the safety of LABAs, particularly when used without a concomitant inhaled corticosteroid, due to a potential increased risk of asthma-related death.

See Also

• Short-acting beta-adrenoceptor agonist
• Inhaled corticosteroids
• Asthma management
• Chronic obstructive pulmonary disease