Long-acting beta-2 agonist (LABA) bronchodilator indicated for asthma treatment and bronchospasm prevention only as concomitant therapy with an inhaled corticosteroid (ICS), and for maintenance of COPD.
Also known as: Serevent, salmeterol xinafoato, salmeterol xinafoate
DailyMed approved label (SEREVENT DISKUS, salmeterol; setID 1349a04c-2024-42b9-b81d-a7d995716ade).
DailyMed approved label (SEREVENT DISKUS, salmeterol; setID 1349a04c-2024-42b9-b81d-a7d995716ade).
Sotalol may reduce the bronchodilator effect of salmeterol and increase the risk of bronchospasm.
Salmeterol is a LABA (long-acting beta2-agonist) and sotalol a non-selective beta-blocker with QT prolongation (class III). Sotalol blocks bronchial beta2 receptors, opposing the bronchodilation of salmeterol, and beta-agonists "may produce significant hypokalaemia in some patients, possibly through intracellular shunting, with the potential to produce adverse cardiovascular effects" (salmeterol label). Hypokalaemia, in turn, "can exaggerate the degree of QT prolongation, and increase the potential for Torsade de Pointes" (sotalol label). In patients with asthma/COPD and cardiovascular disease, the combination adds bronchoconstriction, hypokalaemia and arrhythmogenic risk. Avoid non-selective beta-blockers in patients using a LABA; if unavoidable, monitor respiratory symptoms, potassium/magnesium and ECG.
Salmeterol + sotalol: beta2 antagonism (sotalol opposes the LABA) + salmeterol hypokalaemia potentiating sotalol QT. Avoid or monitor ECG and electrolytes.
β2-receptor antagonism between the LABA and the non-selective beta-blocker.
Monitor for bronchospasm and bronchodilator efficacy.
Bronchospasm, lack of response to salmeterol.
Avoid the combination in asthma; monitor respiratory function.
DailyMed (FDA) — approved Salmeterol label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=12d9728e-6b5c-4aee-bfb0-745e542ed2e4 ; 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)
Salmeterol is given by inhalation; food does not affect its pharmacokinetics.
May be administered regardless of meals.
DailyMed/FDA (NIH/NLM) — approved Salmeterol label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=12d9728e-6b5c-4aee-bfb0-745e542ed2e4
Caffeine can potentiate the sympathomimetic effects of salmeterol (tachycardia, tremor).
Moderate caffeine intake during treatment.
DailyMed/FDA (NIH/NLM) — approved Salmeterol label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=12d9728e-6b5c-4aee-bfb0-745e542ed2e4
β2-agonists may raise blood pressure and heart rate.
Control blood pressure before and during treatment.
EMC-UK (MHRA) — approved Salmeterol SmPC: https://www.medicines.org.uk/emc/product/848/smpc
LABAs may cause tachycardia and arrhythmias in patients with cardiovascular disease.
Use with caution; monitor heart rhythm and ischaemic symptoms.
EMC-UK (MHRA) — approved Salmeterol SmPC: https://www.medicines.org.uk/emc/product/848/smpc
Data on salmeterol in pregnancy are limited; use only if the benefit outweighs the risk.
Avoid in the 1st trimester unless strictly necessary.
Excretion into breast milk is unknown; use with caution.
No specific additional contraception.
EMC-UK (MHRA) — approved Salmeterol SmPC: https://www.medicines.org.uk/emc/product/848/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: stimulation of intracellular adenyl cyclase increases cyclic AMP, relaxing bronchial smooth muscle and inhibiting release of immediate-hypersensitivity mediators from cells, especially mast cells. Bronchodilation lasts ≥ 12 hours.
Selective agonism of beta-2-adrenergic receptors (≥ 50x more selective than albuterol in vitro), with prolonged bronchodilator effect; beta-2 receptors in the heart (10–50% of total) explain possible cardiac effects.
After inhalation, most of the dose is swallowed; plasma levels are very low (mean peak of 167 pg/mL at 20 min, no accumulation with repeated doses); the inhaled fraction acts locally.
Extensively hydroxylated (aliphatic) by CYP3A4; metabolites are excreted predominantly in feces.
Elimination half-life ~5.5 h (the swallowed portion has a half-life of ~11 days due to slow absorption, but systemic exposure is minimal).
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
