umeclidinium
Brand: Incruse Ellipta, Anoro Ellipta (with vilanterol)
Prototype: tiotropium
Drug Class: muscarinic receptor antagonist (LAMA)
Drug Family: bronchodilator
Subclass: long-acting anticholinergic — once-daily LAMA
Organ Systems: respiratory
Mechanism of Action
Competitive antagonist at muscarinic receptors in airway smooth muscle; kinetically selective for M3 receptors (slow dissociation) with faster dissociation from M2 receptors, minimizing pre-junctional M2-mediated acetylcholine feedback inhibition; blockade of M3 receptors prevents bronchoconstriction and reduces mucus secretion.
M1, M2, M3 muscarinic receptors (airway smooth muscle)
Indications
- COPD maintenance bronchodilator therapy
Contraindications
- hypersensitivity to umeclidinium or milk proteins
- severe milk protein allergy (lactose excipient)
Adverse Effects
Common
- nasopharyngitis
- upper respiratory tract infection
- cough
- dry mouth
- urinary retention
Serious
- acute urinary retention
- narrow-angle glaucoma exacerbation
- paradoxical bronchospasm
Pharmacokinetics (ADME)
| Absorption | inhaled; peak plasma within 5-15 minutes; absolute systemic bioavailability approximately 13% |
| Distribution | Vd approximately 86 L; 89% protein bound |
| Metabolism | hepatic CYP2D6 (minor); primarily oxidative metabolism |
| Excretion | fecal (primary) and renal (minor) |
| Half-life | approximately 19 hours |
| Onset | within 15 minutes |
| Peak | 3 hours |
| Duration | 24 hours |
| Protein Binding | 89% |
| Vd | approximately 86 L |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| other anticholinergic agents | additive anticholinergic effects — urinary retention, constipation, dry mouth, blurred vision | moderate |
| CYP2D6 inhibitors | minor effect on umeclidinium metabolism; generally not clinically significant | minor |
Nursing Considerations
- Administer via Ellipta inhaler once daily at the same time each day; instruct patients to slide the cover fully open, exhale away from device, inhale deeply, then hold breath 3-4 seconds.
- Screen for benign prostatic hyperplasia and urinary retention history; umeclidinium's anticholinergic effect can precipitate acute urinary retention in susceptible patients.
- Counsel patients with narrow-angle glaucoma that umeclidinium should be used cautiously; if inadvertent eye exposure occurs from inhaler, flush eyes immediately and seek ophthalmic evaluation for eye pain or visual changes.
- Remind patients that umeclidinium is a maintenance medication and cannot be used for acute bronchospasm relief; prescribe a SABA for rescue use.
Clinical Pearls
- Umeclidinium's 24-hour duration enables once-daily dosing with the Ellipta inhaler — the single inhalation technique and click confirmation of dose delivery support adherence in elderly COPD patients who may have coordination difficulties.
- In combination with vilanterol (Anoro Ellipta), umeclidinium provides dual bronchodilation with complementary mechanisms; clinical trials demonstrate greater bronchodilation than either agent alone without additive adverse effects.
Safety Profile
Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Not required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.