Olodaterol

Monotherapy (without concurrent use of an inhaled corticosteroid) in the treatment of asthma.

Patient with CV disease (e.g. hypertension, cardiac arrhythmia, ischaemic heart disease, severe cardiac decompensation, coronary insufficiency, hypertrophic obstructive cardiomyopathy, history of MI, known or suspected QT interval prolongation); aneurysm, diabetes mellitus, hyperthyroidism, hypokalaemia, seizure disorder. Patients who are unusually unresponsive to sympathomimetic amines. Not indicated for the treatment of asthma, acute bronchospastic episodes, or acutely deteriorating COPD. Pregnancy and lactation.

Significant: Immediate hypersensitivity reactions (e.g. angioedema), CV effects (e.g. increased pulse rate or blood pressure, CV disease symptoms, ECG changes); increased plasma glucose, exacerbation of pre-existing diabetes mellitus, ketoacidosis; transient decreased serum potassium; thyroid activity stimulation; CNS stimulation or excitation.
Gastrointestinal disorders: Diarrhoea.
Musculoskeletal and connective tissue disorders: Arthralgia, back pain.
Nervous system disorders: Dizziness.
Renal and urinary disorders: UTI.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, bronchitis, URTI, cough.
Skin and subcutaneous tissue disorders: Rash.
Potentially Fatal: Paradoxical bronchospasm.

Inhalation/Respiratory: Z (Not recommended during pregnancy or only use during labour when benefits outweigh risks due to the effects of β-agonists on uterine contraction (manufacturer specific).)

Monitor FEV₁, forced vital capacity (FVC) and other pulmonary function tests; blood pressure, heart rate, serum glucose and potassium levels; CNS stimulation. Assess for signs of paradoxical bronchospasm or chest pain.

Symptoms: Dizziness, headache, hypertension, hypotension, tachycardia, palpitation, arrhythmia, angina pectoris, myocardial ischaemia, anxiety, nervousness, insomnia, dry mouth, nausea, fatigue, malaise, tremor, muscle spasm, hypokalaemia, hyperglycaemia, and metabolic acidosis.

Management: Symptomatic and supportive treatment. May consider use of cardioselective β-blockers with extreme caution.

Additive sympathetic effects with other adrenergic drugs. Increased risk of adverse CV effects with halogenated hydrocarbon anaesthetics. Hypokalaemic effects may be potentiated with xanthine derivatives, steroids, and loop or thiazide diuretics. β-blockers may antagonise the therapeutic effects of olodaterol and cause severe bronchospasm. May increase CV effects or risk of ventricular arrhythmias with MAOIs, TCAs and other agents known to prolong the QT interval. Increased plasma concentration with ketoconazole.
Potentially Fatal: May result in clinically significant CV effects with other long-acting β₂-adrenergic agonists (e.g. salmeterol, indacaterol, formoterol).

Description:
Mechanism of Action: Olodaterol is a long-acting β₂-adrenergic agonist. It binds to and activates the β₂ airway receptors, resulting in the stimulation of intracellular adenyl cyclase and a subsequent elevation in cyclic-3',5' adenosine monophosphate (cAMP) synthesis. The increase in cAMP levels induces bronchodilation by relaxing the airway smooth muscle cells.
Onset: 5 minutes.
Duration: 24 hours.
Pharmacokinetics:
Absorption: Rapidly absorbed systemically from the lungs. Absolute bioavailability: Approx 30%. Time to peak plasma concentration: 10-20 minutes.
Distribution: Volume of distribution: 1,110 L. Plasma protein binding: Approx 60%.
Metabolism: Metabolised via direct glucuronidation by UGT2B7, UGT1A1, UGT1A7, and UGT1A9 and via O-demethylation primarily by CYP2C9 and CYP2C8; further metabolised via conjugation.
Excretion: Via urine (5-7% as unchanged drug); faeces. Elimination half-life: 7.5 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 11504295, Olodaterol. https://pubchem.ncbi.nlm.nih.gov/compound/Olodaterol. Accessed Sept. 26, 2025.

Store between 20-25°C. Do not freeze.

Antiasthmatic & COPD Preparations

R03AC19 - olodaterol ; Belongs to the class of adrenergic inhalants, selective beta-2-adrenoreceptor agonists. Used in the treatment of obstructive airway diseases.

Brayfield A, Cadart C (eds). Olodaterol Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/09/2025.

Joint Formulary Committee. Olodaterol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/09/2025.

Olodaterol Hydrochloride. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 02/09/2025.

Olodaterol. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 02/09/2025.

Striverdi Respimat 2.5 microgram Inhalation Solution (Boehringer Ingelheim International GmbH). MHRA. https://products.mhra.gov.uk. Accessed 02/09/2025.

Striverdi Respimat 2.5 microgram per Actuation Inhalation Solution (Boehringer Ingelheim [Hong Kong] Ltd). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 02/09/2025.

Striverdi Respimat Inhalation Spray, Metered (Boehringer Ingelheim Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/09/2025.