For the maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD) including emphysema and chronic bronchitis.
Beta-2 Agonist; Antiasthmatic
Beta-2 adrenoceptor stimulation causes relaxation of bronchial smooth muscle, bronchodilation, and increased airflow. Salmeterol is hypothesized to bind to 2 sites on the beta-2 adrenoceptor.1 The saligenin moiety binds to the active site of the beta-2 adrenoceptor. The hydrophilic tail of salmeterol binds to leucine residues in the exo-site of the beta-2 adrenoceptor almost irreversibly, allowing salmeterol to persist in the active site, which is responsible for it's long duration of action. Another hypothesis is that the lipophilic drug diffuses into lipid bilayer of smooth muscle cells and provides a depot of drug to the cells over a longer period of time.
INHALATION Chronic asthma; Chronic obstructive pulmonary disease: Adult: As metereddose aerosol: 2 inhalations of 25 mcg bid up to 100 mcg bid. As dry powd inhalation: 50 mcg bid or 100 mcg bid if necessary. Child: As metered-dose aerosol: 4 yr: 50 mcg bid.
Monoamine Oxidase inhibitors and Tricyclic Antidepressants: These agents should be used with caution because Salmeterol may be potentiated by these agents.
Pregnancy. Arrhythmias, hyperthyroidism, hypertension, DM, myocardial insufficiency, susceptibility to QTinterval prolongation. May cause paradoxical bronchospasm. Not to be used for treatment of acute bronchospasm or patients w/ deteriorating asthma. Monitor serum K concentrations in severe asthma.
Fine skeletal muscle tremor esp hands, tachycardia. palpitations, muscle cramps, headache, paradoxical bronchospasm, angioedema, urticana, hypotension & collapse.
This drug should not be used during pregnancy unless the benefit outweighs the risk to the fetus. Caution is recommended for breastfeeding. Benefit should outweigh risk.
Store between 20-25°C. Protect from heat or sunlight. Keep out of reach of children.
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