Vilanterol
Vilanterol is a once-daily ultra-long-acting beta-2 agonist used only in fixed-combination inhalers — with the corticosteroid fluticasone furoate (Breo/Relvar) for asthma and COPD, and with the muscarinic antagonist umeclidinium for COPD. It is not sold as a standalone product and has no physique or fat-loss use.
01 Overview
Vilanterol is a selective beta-2 agonist with 24-hour duration, developed exclusively as a component of once-daily combination inhalers. Paired with fluticasone furoate it treats asthma and COPD; paired with umeclidinium (and optionally fluticasone furoate as a triple therapy) it treats COPD. It is never marketed alone, which sidesteps the LABA-monotherapy asthma safety concern by design.
Its pharmacology and side-effect profile are those of the ultra-LABA class: durable bronchodilation with systemic beta-2 effects (tremor, palpitations, hypokalaemia) at the margins. It has no role as a cutting or thermogenic drug; systemic exposure from inhaled combination products is low.
02 Mechanism
Ultra-long-acting selective beta-2 agonist. Sustained beta-2 receptor activation raises cyclic AMP and relaxes airway smooth muscle for ~24 hours, always delivered alongside a corticosteroid and/or muscarinic antagonist.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| Combination maintenance | 22–25 mcg/day | Inhaled | ~22-25 mcg once daily as part of a fixed-combination Ellipta inhaler; never used alone. |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| 24-hour bronchodilationDurable bronchodilation supporting once-daily combination therapy. | once-daily dosing | Clinical | |
| Improved control (with steroid/LAMA)In combination inhalers, improves lung function and reduces exacerbations in asthma and COPD. | fewer exacerbations | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Tremor and palpitationsFine tremor, palpitations and headache from systemic beta-2 stimulation. | Mild | Common | Clinical | |
| HypokalaemiaBeta-2-mediated intracellular potassium shift at high or combined dosing. | Moderate | With high doses | Clinical | |
| Pneumonia (in COPD combinations)Fluticasone-containing combinations carry a modest increased pneumonia risk in COPD, attributable to the corticosteroid component. | Moderate | With inhaled steroid combination | Clinical |