Products
Salmeterol is commercially available as metered-dose inhalers and discs (Serevent, Seretide + fluticasone). It has been approved in many countries since 1995.
Structure and properties
Salmeterol (C25H37NO4, Mr = 415.6) is present in the drugs as a racemate and as salmeterol xinafoate, a white powder that is sparingly soluble in water. It is structurally related to epinephrine and other beta2-sympathomimetics such as its precursor salbutamol and is a saligenin derivative. Its long duration of action is due to its long side chain.
Effect
Salmeterol (ATC R03AC12) has sympathomimetic, bronchodilator (bronchospasmolytic), and anti-inflammatory properties. It is one of the long-acting inhaled beta2-sympathomimetics (LABA). Its bronchodilator effect lasts up to 12 hours. The follow-up product vilanterol is even effective for 24 hours. The effects are due to selective binding to β2-adrenoceptors. Because the effect is delayed within 10 to 20 minutes, the drug is not suitable for treating an acute asthma attack.
Indications
- Bronchial asthma, exertional asthma.
- Chronic bronchitis
- Chronic obstructive pulmonary disease (COPD)
Dosage
According to the drug label. The drug is usually inhaled twice daily with a metered-dose inhaler or a discus.
Abuse
Salmeterol may be abused as a doping agent.
Contraindication
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Drug-drug interactions are possible with nonselective beta blockers such as propranolol, MAO inhibitors, tricyclic antidepressants, levodopa, levothyroxine, oxytocin, xanthines, and antiarrhythmic agents. Salmeterol is a substrate of CYP3A4 and interactions with CYP inhibitors such as ketoconazole are possible.
Adverse effects
The most common possible adverse effects include palpitations, muscle cramps, tremor, headache, and agitation.
