Arformoterol
Arformoterol is the (R,R)-enantiomer of formoterol, a long-acting beta-2 agonist delivered by nebulised solution for the maintenance treatment of COPD. It offers the same 12-hour bronchodilation as racemic formoterol in a single-isomer nebulised form. It has no meaningful physique or fat-loss use; its role is COPD maintenance in patients who benefit from nebulisation.
01 Overview
Arformoterol is the pharmacologically active (R,R)-enantiomer isolated from racemic formoterol. It is a long-acting selective beta-2 agonist supplied as a nebuliser solution and dosed twice daily for the long-term maintenance of bronchoconstriction in COPD. Isolating the active enantiomer was intended to deliver bronchodilation at a lower total drug mass.
As a LABA it carries the class warning against monotherapy in asthma (it is licensed for COPD, not asthma). Its systemic sympathomimetic effects — tremor, palpitations, hypokalaemia — parallel those of other beta-2 agonists. It is not used as a cutting or thermogenic agent; the nebulised route and low systemic exposure give little metabolic effect.
02 Mechanism
Single (R,R)-enantiomer long-acting beta-2 agonist. Selectively activates beta-2 receptors to raise cyclic AMP and relax airway smooth muscle, giving ~12-hour bronchodilation from a nebulised dose.
03 Dosing
| Tier | Dose | Route | Notes |
|---|---|---|---|
| COPD maintenance | 15 mcg | Inhaled | 15 mcg nebulised twice daily; not for acute relief or asthma. |
04 Effects
| Effect | Magnitude | Evidence | |
|---|---|---|---|
| Sustained bronchodilationLong-acting relief of airflow obstruction in COPD from a nebulised dose. | ~12 hour duration | Clinical | |
| Improved lung functionImproves FEV1 and symptom control as COPD maintenance therapy. | FEV1 improvement | Clinical |
05 Side effects
| Effect | Severity | Frequency | Evidence | Countermeasures |
|---|---|---|---|---|
| Tremor and palpitationsFine tremor, palpitations and nervousness from systemic beta-2 stimulation. | Mild | Common | Clinical | |
| Increased severe events (asthma monotherapy)Class effect: LABA monotherapy in asthma is associated with increased severe asthma events; arformoterol is licensed only for COPD. | Severe | Rare, off-label asthma use | Clinical | |
| HypokalaemiaBeta-2-mediated intracellular potassium shift. | Moderate | With high doses | Clinical |