What are examples of long-acting bronchodilators?

Examples of Long-Acting Bronchodilators

Long-acting bronchodilators include two main classes: long-acting beta-2 agonists (LABAs) such as formoterol, salmeterol, indacaterol, olodaterol, and vilanterol; and long-acting muscarinic antagonists (LAMAs) such as tiotropium, glycopyrronium, aclidinium, and umeclidinium.

Long-Acting Beta-2 Agonists (LABAs)

Twice-Daily LABAs

• Formoterol: A LABA with duration of action exceeding 12 hours and rapid onset of action within minutes 1, 2. Formoterol has more than 200-fold greater activity at beta-2 receptors than beta-1 receptors 2.
• Salmeterol: Requires twice-daily administration but has a slower onset of action compared to formoterol 1, 3. Unlike formoterol, salmeterol should not be used for acute symptom relief 1.

Once-Daily LABAs (Ultra-Long-Acting)

• Indacaterol: A once-daily LABA with 24-hour duration of action 4, 3.
• Olodaterol: A once-daily LABA that exerts effects through beta-2 adrenoceptor activation, with 241-fold greater activity at beta-2 receptors compared to beta-1 receptors 5, 4, 3.
• Vilanterol: A once-daily LABA under development and approval for COPD and asthma 4, 3.
• Other emerging agents: Milveterol, carmoterol, and abediterol are in development 3.

Long-Acting Muscarinic Antagonists (LAMAs)

Once-Daily LAMAs

• Tiotropium bromide: A long-acting anticholinergic with similar affinity to muscarinic receptor subtypes M1-M5, providing bronchodilation through M3-receptor inhibition at airway smooth muscle 6, 5, 3.
• Glycopyrronium bromide (NVA-237): A once-daily LAMA 4, 3.
• Umeclidinium bromide (GSK573719): A once-daily LAMA 4, 3.

Twice-Daily LAMA

• Aclidinium bromide: Administered every 12 hours 3.

Important Clinical Considerations

For Asthma Management

• LABAs must NEVER be used as monotherapy in asthma and should always be combined with inhaled corticosteroids due to safety concerns 6, 1, 2.
• LABAs are reserved for moderate-to-severe chronic asthma when short-acting bronchodilators and inhaled corticosteroids (400-800 mcg daily) provide insufficient control 6.
• Formoterol is preferred for SMART (Single Maintenance And Reliever Therapy) regimens due to its rapid onset, while salmeterol should not be used for this purpose 1.

For COPD Management

• Both LABAs and LAMAs are effective as monotherapy in COPD, with LAMAs showing greater efficacy in preventing exacerbations compared to LABAs 7.
• Tiotropium provides superior outcomes including improved health status, reduced dyspnea, enhanced exercise capacity, and reduced COPD exacerbation rates 8.
• Long-acting bronchodilators are preferred over short-acting agents for maintenance therapy in COPD 7.

Combination Therapies

• LAMA/LABA fixed-dose combinations are increasingly used and include indacaterol/glycopyrronium, umeclidinium/vilanterol, and olodaterol/tiotropium 3.
• These combinations provide superior symptom control and exacerbation prevention compared to monotherapies 7.
• Combined use of LABAs with LAMAs provides complementary pharmacological actions through distinct mechanisms 9.

For Bronchiectasis

• Both long-acting beta-2 agonists (such as formoterol) and long-acting anticholinergics may be beneficial for patients with breathlessness symptoms 6.
• Evidence is limited, but a trial of long-acting bronchodilator therapy is recommended for patients with significant breathlessness 6.