Vilanterol

• COPD Maintenance
• Asthma Maintenance
• Chronic Bronchitis

Vilanterol is a long-acting beta-2 adrenergic agonist (LABA) used in combination with other medications for maintenance treatment of COPD and asthma. It is only available in combination products due to safety concerns with LABA monotherapy in asthma.

Mechanism of Action

Vilanterol provides sustained bronchodilation:

• Beta-2 receptor agonism: Activates beta-2 adrenergic receptors on bronchial smooth muscle
• Increased cyclic AMP: Stimulates adenylyl cyclase, raising intracellular cAMP
• Bronchial relaxation: cAMP-dependent protein kinase mediates smooth muscle relaxation
• 24-hour duration: Lipophilic tail allows prolonged receptor engagement
• Fast onset: Bronchodilation begins within 15 minutes

Available Formulations

Vilanterol is only available in combination products:

• Breo Ellipta: Fluticasone furoate/vilanterol (100/25 mcg, 200/25 mcg)
• Anoro Ellipta: Umeclidinium/vilanterol (62.5/25 mcg)
• Trelegy Ellipta: Fluticasone furoate/umeclidinium/vilanterol (100/62.5/25 mcg, 200/62.5/25 mcg)

All are 30-dose dry powder inhalers.

Medical Uses

FDA-Approved Indications (in combination):

• COPD maintenance treatment (all combinations)
• Asthma maintenance treatment in patients ≥18 years (ICS/LABA combinations only)
• Asthma in adolescents ≥12 years (fluticasone/vilanterol at lower strength only for asthma control)

Not for:

• Primary treatment of acute bronchospasm
• Asthma without concurrent ICS

Dosing Guidelines

COPD (All combinations):

• One inhalation once daily

Asthma (ICS/vilanterol):

• One inhalation once daily
• Use lowest effective ICS dose

Administration:

• Same time each day
• Do not exceed one inhalation daily
• Rinse mouth after use (ICS-containing products)

Important Safety Information

Black Box Warning:

• LABAs increase the risk of asthma-related death
• Only use vilanterol for asthma in combination with ICS
• Not for asthma in patients adequately controlled on ICS alone

Contraindications:

• Severe hypersensitivity to milk proteins
• Known hypersensitivity to vilanterol or any component
• Asthma without concurrent ICS

Warnings and Precautions:

• Not for acute symptoms (not a rescue medication)
• Paradoxical bronchospasm
• Cardiovascular effects (increased pulse, blood pressure, arrhythmias)
• Hypokalemia
• Hyperglycemia

Drug Interactions

• Strong CYP3A4 inhibitors (ketoconazole, ritonavir): May increase vilanterol exposure; use with caution
• Beta-blockers: May antagonize effects; use cardioselective beta-blockers with caution
• Non-potassium-sparing diuretics: May worsen hypokalemia
• MAOIs, tricyclic antidepressants: May potentiate cardiovascular effects
• Other LABAs: Avoid concomitant use

Special Populations

• Hepatic Impairment: Use with caution; fluticasone/vilanterol may have increased exposure in severe impairment
• Renal Impairment: No adjustment expected
• Elderly: No adjustment needed
• Pregnancy: Limited data; use only if benefit outweighs risk
• Lactation: Unknown if excreted in milk
• Pediatric: Asthma approved ≥12 years (ICS/LABA); COPD products not for children