Salmeterol is a long-acting beta-2 adrenergic receptor agonist used to treat asthma and COPD. It has a longer duration of action than the short-acting beta-2 adrenergic receptor agonist, salbutamol.
- Mechanism
- Curator reviewed · 6 references
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. 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.
- Primary indication
- Salmeterol is indicated in the treatment of asthma with an inhaled corticosteroid, prevention of exercise induced bronchospasm, and the maintenance of airflow obstruction and prevention of exacerbations of chronic obstructive pulmonary disease.Curator reviewed · 5 structured indications
- Formula / weight
- C25H37NO4 · 415.5656 g/mol (avg)
- First approval
- Canada, 2001 · United States, 1997 · European Union, 2021
- Also known as
- Salmaterol
- Code names
- GR-33343-X · SN408D
- Brand names
Resolves to
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Which drugs share a target with Salmeterol, and which of those have an active Phase 3 trial?
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