Salmeterol

ATC CodeR03AC12
CAS number89365-50-4
PUB number5152
Drugbank IDDB00938
Empirical formulaC25H37NO4
Molar mass (g·mol−1)415,57
Physical statesolid
Melting point (°C)75,5–76,5
PKS value11.2

Basics

Salmeterol is a long-acting beta-2-adrenoreceptor agonist currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease COPD. It has a longer duration of action than the short-acting beta-2-adrenoreceptor agonist salbutamol. Salmeterol is only available as an antiasthmatic agent for inhalation and requires a prescription.

Pharmacology

Pharmacodynamics

Salmeterol is a long-acting beta-2-adrenoceptor agonist. Stimulation of the beta-2-adrenoceptor causes bronchial smooth muscle relaxation, bronchodilation, and improved airflow.

Pharmacokinetics

Salmeterol is 96% bound to albumin and alpha-1-acid glycoprotein in plasma. Salmeterol is metabolized predominantly by CYP3A4 to alpha-hydroxysalmeterol and to a lesser extent by an unknown mechanism to an O-dealkylated metabolite. Salmeterol is excreted 57.4% in feces and 23% in urine. Less than 5% of a dose is excreted in the urine as unchanged salmeterol. The half-life of salmeterol is 5.5 hours.

Toxicity

Side effects

Because of its vasodilator properties, the most common side effects of salmeterol are

  • Dizziness,
  • sinus infection
  • Migraine headache

Other side effects

  • Muscle tremors,
  • Hypokalemia

Certain side effects should be reported to a doctor or health care professional right away. Some of these more serious side effects include

  • very fast heartbeat,
  • high blood pressure
  • An exacerbation of breathing problems.

Toxicological Data

LD50 (rat, oral): > 1000 mg-kg-1

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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