Trade Names:Serevent Diskus- Inhalation powder 50 mcg (as salmeterol xinafoate salt)
Produces bronchodilation by relaxing bronchial smooth muscle through beta-2 receptor stimulation.
Salmeterol acts locally in the lung. Plasma levels do not predict therapeutic effect. Depending on dose, T max is 5 to 45 min, and mean C max is 167 pg/mL.
Protein binding is 96%; xinafoate moiety is greater than 99%.
Extensively metabolized by hydroxylation.
Eliminated in feces (60%) and urine (25%); t ½ is 6 days. Xinafoate moiety is 11 days.
Has not been studied in patients with renal function impairment.Hepatic Function Impairment
May lead to accumulation of salmeterol in plasma.
Maintenance treatment of asthma and prevention of bronchospasm with reversible obstructive airway disease; prevention of exercise-induced bronchospasm; maintenance treatment of bronchospasm associated with COPD (including emphysema and chronic bronchitis).
Inhalation 1 inhalation (50 mcg) twice daily, approximately 12 h apart.Exercise-Induced BronchospasmAdults and Children 4 yr of age and older
Inhalation 1 inhalation at least 30 min before exercise; additional doses should not be used for up to 12 h.COPDAdults
Inhalation 1 inhalation (50 mcg) twice daily, approximately 12 h apart.
Store at controlled room temperature (68° to 77°F) in a dry place. Protect from direct heat or sunlight. Discard 6 wk after removal from moisture-protective foil pouch or when the dose indicator reads “0.”
Pulmonary effects of salmeterol may be blocked and may produce severe bronchospasm in patients with COPD.Diuretics
ECG changes and hypokalemia associated with diuretics may worsen with coadministration.MAOIs, tricyclic antidepressants
May increase CV effects of salmeterol.
None well documented.
Hypertension (4%); palpitations, tachycardia; arrhythmias, including atrial fibrillation, extrasystoles, and supraventricular tachycardia (postmarketing).
Headache (17%); dizziness (4%); anxiety, migraine, nervousness, paresthesia, sleep disturbance, tremor (1% to 3%).
Rash (4%); urticaria (3%); contact dermatitis, eczema (1% to 3%); photodermatitis (1% to 2%).
Nasal sinus congestion, pallor (9%); throat irritation (7%); pharyngitis (6%); rhinitis (5%); ear signs/symptoms, nasal blockage/congestion, sinusitis (4%); conjunctivitis, keratitis, sinus headache (1% to 3%).
Nausea/vomiting (3%); dental pain, dyspepsia, GI infections, hyposalivation, oral candidiasis, oral mucosal abnormality (1% to 3%); GI signs/symptoms (1% to 2%).
Immediate hypersensitivity reactions (eg, angioedema, bronchospasm, rash); anaphylaxis (postmarketing).
Skeletal muscle pain (12%); muscle cramps/spasms (3%); arthralgia, articular rheumatism, bone/skeletal pain, inflammation, muscle pain, muscle stiffness, pain in joints, tightness, rigidity (1% to 3%).
Bronchitis, tracheitis (7%); cough, viral respiratory infection (5%); asthma (4%); lower respiratory signs/symptoms (1% to 3%); irritation or swelling (including stridor or choking), laryngeal spasm, oropharyngeal irritation, paradoxical bronchospasm, serious (some fatal) exacerbations of asthma (postmarketing).
Influenza (5%); body pain, edema, fever, hyperglycemia, pain, swelling (1% to 3%).
When added to usual asthma therapy, there may be an increase in asthma-related deaths. Only use salmeterol as additional therapy for patient not adequately controlled on other asthma-controller medications (eg, low- to medium-dose inhaled corticosteroids) or whose disease severity clearly warrants initiation of treatment with 2 maintenance therapies, including salmeterol.
Monitor for signs of worsening asthma.
Category C .
Not recommended for children younger than 4 yr of age.
Allergic reactions can occur after administration.
Do not use to treat acute symptoms.
Use with caution in patients with CV disease; toxic symptoms may occur.
Paradoxical bronchospasm and cardiac arrest have been associated with excessive inhalant use.
Decreases in potassium levels may occur.
Life-threatening paradoxical bronchospasm may occur.
Do not initiate salmeterol in this setting.
Arrhythmias and/or tachycardia, cardiac arrest, death, headache, hyperglycemia, hypokalemia, muscle cramps, palpitations, prolongation of the QTc interval, tremor.
Copyright © 2009 Wolters Kluwer Health.