Olodaterol
Beta-2 adrenergic agonists
Beta-2 adrenergic agonists
A once-daily inhaled long-acting beta-2 agonist for COPD maintenance, alone or with tiotropium; not for sudden attacks.
Quick facts
- Group
- Beta-2 adrenergic agonists
- Target
- Beta-2 adrenergic receptor
- Used for
- Maintenance bronchodilator treatment
- Key effects
- Runny nose · Joint pain · Nervousness
- Monitor
- Symptoms · Heart rate and rhythm in heart disease
- ATC
- R03AC19
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows olodaterol bound to the human beta-2 adrenergic receptor (cryo-EM of an engineered receptor).
Olodaterol is a very long-acting beta-2 agonist. It activates beta-2 receptors on airway smooth muscle, which raises cyclic AMP through Gs and adenylyl cyclase and relaxes the muscle. Its effect lasts long enough for once-daily use. It is also combined with tiotropium, a muscarinic antagonist, for additive bronchodilation in COPD.
- Olodaterol activates beta-2 receptors on airway muscle
- Gs and adenylyl cyclase raise cyclic AMP
- Airway smooth muscle relaxes
- Bronchodilation lasts about a day
Indications
- Maintenance bronchodilator treatment of COPD (alone or with tiotropium) Chronic obstructive pulmonary disease (COPD) →
Adverse effects
Common
- Runny nose, cough and fever
- Joint pain
- Nervousness, tremor and muscle cramps
- Trouble sleeping and constipation
Contraindications
- Asthma without an inhaled corticosteroid (LABA monotherapy)
- Not for sudden attacks or rapidly worsening COPD
- Not combined with another long-acting beta-2 agonist
Key interactions
- Other long-acting beta-2 agonists (salmeterol, formoterol)
- Duplicate therapy and more adverse effects; only one is kept
- Tiotropium
- Additive bronchodilation; available as a fixed combination
What is monitored
- Symptoms, rescue inhaler use and spirometry
- Heart rate and rhythm in heart disease
- Potassium and glucose when risk is high
Administration and safety
- Inhaled with its own soft-mist inhaler; the cartridge fits only that device
- The inhaler is primed before first use and after a period without use
- Not sprayed into the eyes; the mouthpiece is cleaned regularly
Pregnancy and breastfeeding
Data in pregnancy are limited; use is weighed with the treating doctor.
Nursing care
- Teach the inhaler technique and priming, and check it at visits
- Make sure a short-acting reliever is available for sudden symptoms
- Teach to report wheeze right after an inhalation
- Ask about heart disease, seizures, diabetes and thyroid disease
Pharmacokinetics
- Absorption
- Inhaled as a soft mist from a dedicated inhaler
- Onset and duration
- Long-acting: used once daily for maintenance, not for relief
Test yourself
Think of the answer, then tap the question to see it.
Why is olodaterol not used for a sudden COPD attack?
It is a long-acting maintenance bronchodilator; attacks are treated with a short-acting reliever such as salbutamol.
With which muscarinic antagonist is olodaterol combined?
Tiotropium.
Why is olodaterol not used alone in asthma?
Long-acting beta-2 agonists without an inhaled corticosteroid are unsafe in asthma.
Connections
← Back to the class: Beta-2 adrenergic agonists
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Olodaterol Oral Inhalation: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); RCSB PDB - 8JJL: cryo-EM structure of the beta2-AR-mBRIL/1b3 Fab/Glue complex with a full agonist (RCSB Protein Data Bank, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.