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.
Drug Class
Long-Acting Beta-2 Adrenergic Agonist (LABA)
Pregnancy
Category C; no adequate well-controlled studies in pregnant women. Animal studies showed teratogenic effects at very high doses. Use during pregnancy only if the potential benefit justifies the potential risk. Poorly controlled asthma poses its own pregnancy risks.
Available Forms
50 mcg/blister inhalation powder (Serevent Diskus)
What It's Used For
Dosage Quick Reference
These are general dosage guidelines. Your doctor will determine the appropriate dose for your specific situation.
| Condition | Starting Dose | Maintenance Dose |
|---|---|---|
| Asthma (adults and children ≥ 4 years) | 1 inhalation (50 mcg) twice daily, every 12 hours | 50 mcg twice daily; must always be used with an inhaled corticosteroid (ICS) |
| COPD (maintenance) | 1 inhalation (50 mcg) twice daily, every 12 hours | 50 mcg twice daily |
| Exercise-Induced Bronchospasm (prevention) | 1 inhalation (50 mcg) at least 30 minutes before exercise | 50 mcg before exercise; do not use if already on twice-daily salmeterol |
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
Drug Interactions
- Beta-blockers (propranolol, metoprolol, atenolol): Non-selective beta-blockers can antagonize the bronchodilator effect of salmeterol and may provoke severe bronchospasm in asthma patients. If a beta-blocker is needed, cardioselective agents are preferred with caution.
- Strong CYP3A4 inhibitors (ketoconazole, ritonavir, clarithromycin): Co-administration with ketoconazole significantly increased salmeterol systemic exposure in studies, increasing the risk of cardiovascular side effects (QT prolongation, palpitations). Avoid combination.
- MAO inhibitors and tricyclic antidepressants: These can potentiate the cardiovascular effects of salmeterol (hypertension, tachycardia, arrhythmias). Use extreme caution if combined.
- Other long-acting beta-agonists (formoterol, vilanterol, olodaterol): Do not use two LABAs together. This does not increase efficacy but increases the risk of cardiovascular adverse effects.
- QT-prolonging medications (sotalol, amiodarone, certain fluoroquinolones): Salmeterol can prolong the QTc interval; combining it with other QT-prolonging agents increases the risk of serious arrhythmias.
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
Frequently Asked Questions
Questions to Ask Your Doctor
Consider discussing these topics at your next appointment:
- ✓Am I also on an inhaled corticosteroid, as required when using salmeterol for asthma?
- ✓Could I switch to a combination inhaler for better adherence?
- ✓How often should I be using my rescue inhaler, and does the frequency suggest my asthma is not well controlled?
- ✓Should my lung function be retested to see if salmeterol is providing adequate control?
Related Health Conditions
This medication is commonly used to treat or manage the following conditions:
Asthma
Asthma, a chronic lung disease, causes airway inflammation and narrowing, resulting in wheezing, coughing, and shortness of breath, triggered by allergens, irritants, infections, or stress.
Chronic Obstructive Pulmonary Disease (COPD)
COPD, a progressive lung disease causing irreversible airflow limitation, encompassing emphysema and chronic bronchitis, is primarily driven by irritant exposure like smoking, leading to shortness of breath and chronic cough.
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.
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Questions About This Medication?
Talk to your doctor or pharmacist about whether Salmeterol is right for you.
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