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Salmeterol

Generic Name: Salmeterol Xinafoate

Brand Names: Serevent

Salmeterol is a long-acting beta-agonist for maintenance treatment of asthma and COPD, not for acute symptoms.

RespiratoryLABABronchodilator

Side Effects

Common Side Effects:

  • Headache
  • Pharyngitis
  • Nasal congestion
  • Upper respiratory tract infection
  • Cough
  • Throat irritation

Serious Side Effects:

  • Asthma-related death (when used without ICS)
  • Paradoxical bronchospasm
  • Cardiovascular effects (tachycardia, arrhythmias)
  • Hypokalemia
  • Hyperglycemia

Additional Information

Salmeterol is a long-acting beta-2 adrenergic agonist (LABA) used for maintenance treatment of asthma and chronic obstructive pulmonary disease (COPD). It provides sustained bronchodilation and is always used in combination with an inhaled corticosteroid for asthma.

Mechanism of Action

Salmeterol works through beta-2 receptor stimulation:

  • Beta-2 receptor agonism: Binds to beta-2 receptors on bronchial smooth muscle
  • Increased cyclic AMP: Activates adenylyl cyclase, increasing intracellular cAMP
  • Bronchial smooth muscle relaxation: cAMP-dependent protein kinase mediates relaxation
  • Long duration of action: Lipophilic side chain allows prolonged receptor binding
  • Duration: ~12 hours of bronchodilation

Onset is slower than short-acting beta-agonists (15-20 minutes vs 5 minutes).

Available Formulations

  • Dry powder inhaler (Serevent Diskus): 50 mcg per inhalation
  • Combination products:
    • Salmeterol/fluticasone (Advair Diskus, Advair HFA)
    • Salmeterol/fluticasone (Wixela Inhub, AirDuo RespiClick)

Medical Uses

FDA-Approved Indications:

  • Asthma maintenance treatment in patients ≥4 years (in combination with inhaled corticosteroid only)
  • Prevention of exercise-induced bronchospasm (EIB) in patients ≥4 years
  • Maintenance treatment of COPD including chronic bronchitis and emphysema

Important: For asthma, salmeterol must be used with an inhaled corticosteroid (ICS).

Dosing Guidelines

Asthma Maintenance (with ICS):

  • Adults and children ≥4 years: 50 mcg (one inhalation) twice daily, approximately 12 hours apart

COPD Maintenance:

  • 50 mcg twice daily, approximately 12 hours apart

Exercise-Induced Bronchospasm:

  • 50 mcg at least 30 minutes before exercise
  • Do not use additional doses for 12 hours
  • Patients already on twice-daily dosing should not use additional doses for EIB prevention

Important Safety Information

Black Box Warning:

  • Asthma-related death: LABAs increase the risk of asthma-related death. This risk may be mitigated by using LABAs with ICS.
  • Use only in combination with an ICS for asthma
  • Do not use for acute bronchospasm

Contraindications:

  • Acute asthma or COPD exacerbation
  • Hypersensitivity to salmeterol or any component

Warnings and Precautions:

  • Not for acute symptoms (use short-acting beta-agonist)
  • Paradoxical bronchospasm may occur
  • Cardiovascular effects: May cause increased pulse, blood pressure, or arrhythmias
  • Hypokalemia possible
  • Hyperglycemia in diabetic patients

Drug Interactions

  • Strong CYP3A4 inhibitors (ketoconazole, ritonavir): May increase cardiovascular adverse effects; use with caution
  • Beta-blockers: May antagonize effects; use cardioselective beta-blockers with caution
  • Diuretics (non-potassium-sparing): May worsen hypokalemia
  • MAO inhibitors, tricyclic antidepressants: May potentiate cardiovascular effects

Special Populations

  • Hepatic Impairment: Use with caution (limited data)
  • Pregnancy: Use only if benefit outweighs risk
  • Lactation: Unknown if excreted in milk
  • Pediatric: Approved for ≥4 years with ICS for asthma; EIB in ≥4 years
  • Elderly: No specific adjustment

Medical Disclaimer: This information is for educational purposes only and should not be considered medical advice. Always consult with your healthcare provider before starting, stopping, or changing any medication. Your doctor can provide personalized recommendations based on your specific health condition and medical history.

Questions About This Medication?

Talk to your doctor or pharmacist about whether Salmeterol is right for you.

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