Formoterol is a long-acting bronchodilator (beta-2 agonist) used for the maintenance treatment of chronic obstructive pulmonary disease (COPD), by inhalation, twice daily. It is not intended for immediate relief of an acute attack of breathlessness.
Also known as: Oxis, Atimos, eformoterol
Sotalol antagonises the effect of formoterol and may cause bronchospasm in predisposed patients.
Formoterol is a long-acting beta2-agonist (LABA) and sotalol a non-selective beta-blocker with class III antiarrhythmic activity (QT prolongation). Sotalol blocks beta2 receptors, opposing the bronchodilator effect of formoterol (risk of asthma/COPD exacerbation), and beta2-agonists "may produce significant hypokalaemia in some patients, possibly through intracellular potassium shunting, with the potential to produce adverse cardiovascular effects" (formoterol label) — and hypokalaemia "can exaggerate the degree of QT prolongation, and increase the potential for Torsade de Pointes" (sotalol label). The combination is particularly risky in patients with underlying heart disease or long QT. Whenever possible, avoid non-selective beta-blockers in patients using a LABA; if unavoidable, monitor respiratory function, potassium/magnesium and ECG.
Formoterol + sotalol: sotalol blocks beta2 receptors (antagonises the LABA) and formoterol-induced hypokalaemia may potentiate sotalol QT. Avoid or monitor ECG and potassium.
β2-receptor antagonism between formoterol (LABA) and sotalol (non-selective beta-blocker).
Monitor respiratory function and bronchodilator response.
Bronchospasm, worsening of airway obstruction.
Do not use non-selective beta-blockers in patients with obstructive airways disease.
DailyMed (FDA) — approved Formoterol label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=35538d89-a984-4335-acdf-85a893f51eee ; approved Sotalol label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=9a36d95c-6e93-4e57-befe-b5274f359244 — additional reference: Prontuário Terapêutico do INFARMED (11th ed., 2012)
Formoterol is given by inhalation; food does not affect its pharmacokinetics.
May be administered regardless of meals.
DailyMed/FDA (NIH/NLM) — approved Formoterol label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=35538d89-a984-4335-acdf-85a893f51eee
Caffeine and other stimulants can potentiate the sympathomimetic effects of formoterol (tachycardia, tremor).
Moderate caffeine intake during treatment.
DailyMed/FDA (NIH/NLM) — approved Formoterol label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=35538d89-a984-4335-acdf-85a893f51eee
Formoterol may cause tachycardia and arrhythmias in cardiac patients.
Use with caution and monitor cardiovascular signs.
EMC-UK (MHRA) — approved Formoterol SmPC: https://www.medicines.org.uk/emc/product/6316/smpc
Data on formoterol in pregnancy are limited; use only if the benefit outweighs the risk.
Avoid unless asthma requires it, at the lowest effective dose.
Excretion into breast milk is unknown; use with caution.
No specific additional contraception.
EMC-UK (MHRA) — approved Formoterol SmPC: https://www.medicines.org.uk/emc/product/6316/smpc
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Long-acting beta-2 agonist (LABA) with rapid onset (minutes), indicated for maintenance of bronchoconstriction in COPD (twice daily); not indicated for asthma as monotherapy (risk of asthma-related events).
Selective agonist of beta-2 adrenergic receptors on bronchial smooth muscle: activates adenylyl cyclase, raises cAMP and activates protein kinase A, causing smooth muscle relaxation (bronchodilation) and mast cell stabilisation; prolonged effect (>12 h) due to persistent receptor binding.
Low systemic exposure via inhalation: after 244 mcg nebulised (≈12x the clinical dose), Cmax of 72 pg/mL within ~12 min; at therapeutic doses (10-20 mcg) plasma concentrations are undetectable or sporadic; slight accumulation with repeated dosing (index 1.19-1.38).
Extensive hepatic metabolism (glucuronidation and O-demethylation; CYP2D6/CYP2C/2A6 involved in demethylation); renal excretion of metabolites and unchanged drug (urinary excretion of unchanged drug is used as an indirect measure of systemic exposure).
Elimination half-life ~10 h (calculated from urinary and plasma excretion); bronchodilation lasts ≥12 h, allowing twice-daily administration.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
