Drug reference

Salmeterol

LABA · Asthma management

LABAAsthma managementATC R03AC10

CDSCO approvedSchedule HATC R03AC10

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 12 →

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Mechanism

Salmeterol is a long-acting beta-2 adrenergic agonist (LABA) with a unique molecular structure: its long lipophilic side chain anchors the molecule within the cell membrane lipid bilayer adjacent to the beta-2 receptor, allowing the active saligenin head to repeatedly engage and disengage the receptor binding site. This 'exosite' binding model explains its slow onset (15-20 minutes vs 3-5 minutes for salbutamol) but sustained duration of bronchodilation (12+ hours), enabling twice-daily dosing for maintenance asthma and COPD therapy.

Indications

Asthma (as initial add-on therapy to low-dose inhaled corticosteroids when asthma is uncontrolled)nocturnal asthma (in patients symptomatic despite anti-inflammatory agents)COPDAsthma (always in combination with an ICS)Bronchial asthmaMaintenance therapy for asthmaNocturnal asthma

Dosing

Adult: range of doses that are generally regarded as being suitable for adults. Complementary and alternative medicine Prescribing unlicensed medicines An increasing amount of information on complementary and alternative medicine is becoming available.…

Pharmacokinetics

Onset

relatively slow onset of action

Duration

prolonged duration of action (>12 h)

Metabolism

metabolized by CYP3A4 to α-hydroxy-salmeterol

Contraindications

monotherapy for acute attacks of bronchospasm
acute asthma symptoms
used more than twice daily

Side effects

Common

increased heart rateincreased plasma glucose concentrationtremorsdecreased plasma K+ concentrationnasopharyngitispneumoniaMuscle tremorTachycardiaPalpitations

Serious

increased risk of fatal or near-fatal asthmatic attacks (when added to usual therapy without inhaled corticosteroid)
Hypokalemia
Ventilation-perfusion (V/Q) mismatch (fall in arterial oxygen tension)
Metabolic effects (increase in free fatty acid, insulin, glucose, pyruvate, and lactate)
Life-threatening and fatal asthma exacerbations (if used alone in asthma)
Increased risk of life-threatening asthma attacks with regular use (unless used in combination with an inhaled steroid)
Excess mortality among asthmatics treated continuously with long acting β2 agonist inhalations