Umeclidinium

• Chronic Obstructive Pulmonary Disease (COPD)
• Chronic Bronchitis
• Emphysema

Umeclidinium is a long-acting muscarinic antagonist (LAMA) used as maintenance bronchodilator therapy for chronic obstructive pulmonary disease (COPD). It provides sustained bronchodilation through anticholinergic effects, reducing airway smooth muscle tone and decreasing mucus secretion for 24 hours with once-daily dosing.

Mechanism of Action

Umeclidinium works through muscarinic receptor blockade in the airways:

• Long-acting anticholinergic: Competitively inhibits muscarinic M3 receptors in airway smooth muscle
• Bronchodilation: Blocks acetylcholine-induced bronchoconstriction
• Reduces mucus secretion: Decreases parasympathetic stimulation of mucus glands
• 24-hour duration: Slow dissociation from M3 receptors provides sustained effect
• Kinetic selectivity: Faster dissociation from M2 receptors (reduces cardiac effects) than from M3 receptors

Available Formulations

Umeclidinium is available as:

• Incruse Ellipta: 62.5 mcg umeclidinium per inhalation (30-dose dry powder inhaler)
• Anoro Ellipta: Umeclidinium 62.5 mcg/vilanterol 25 mcg (LAMA/LABA combination)
• Trelegy Ellipta: Umeclidinium 62.5 mcg/vilanterol 25 mcg/fluticasone furoate 100 mcg (LAMA/LABA/ICS triple therapy)

Medical Uses

FDA-Approved Indication:

• Long-term, once-daily maintenance bronchodilator treatment of airflow obstruction in patients with COPD, including chronic bronchitis and/or emphysema

Umeclidinium is not indicated for acute bronchospasm relief or asthma treatment.

Dosing Guidelines

Adults (COPD):

• Incruse Ellipta: One inhalation (62.5 mcg) once daily
• Maximum: 62.5 mcg in 24 hours

Administration:

• Inhale at the same time each day
• Do not use with other anticholinergic-containing medications
• Do not exceed one inhalation daily
• Do not wash the inhaler; keep dry

Important Safety Information

Contraindications:

• Severe hypersensitivity to milk proteins
• Known severe hypersensitivity to umeclidinium or any component

Warnings and Precautions:

• Not for acute use: Do not use for acute bronchospasm or deteriorating COPD
• Paradoxical bronchospasm: Discontinue immediately if occurs
• Cardiovascular effects: Use with caution in cardiovascular disease, arrhythmias, or QT prolongation
• Narrow-angle glaucoma: May worsen; instruct patients to contact provider if eye symptoms develop
• Urinary retention: Use with caution in prostatic hyperplasia or bladder-neck obstruction
• Worsening COPD: Rescue inhaler use increasing may indicate worsening disease

Drug Interactions

• Other anticholinergics: Avoid concurrent use with other anticholinergic medications (ipratropium, tiotropium) due to additive effects
• QT-prolonging drugs: Use with caution with other drugs that prolong QT interval
• Beta-blockers: May diminish bronchodilator effects; use cardioselective beta-blockers cautiously if needed
• Strong CYP3A4 inhibitors: Minor interaction; no dose adjustment required
• P-glycoprotein inhibitors: May increase exposure; clinical significance uncertain

Special Populations

• Renal Impairment: No dose adjustment required (minimal renal elimination)
• Hepatic Impairment: No dose adjustment required in mild-moderate impairment; not studied in severe impairment
• Elderly: No dose adjustment needed; monitor for anticholinergic effects
• Pregnancy: Limited human data; use only if benefit outweighs risk
• Lactation: Unknown if excreted in breast milk; consider benefit-risk
• Pediatric: Safety and efficacy not established; COPD does not normally occur in children
• Cardiovascular Disease: Use with caution in patients with cardiovascular disorders