Salmeterol

Salmeterol

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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.

Effect

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

Chemical & physical properties

ATC Code R03AC12
Formula C25H37NO4
Molar Mass (g·mol−1) 415,57
Physical State solid
Melting Point (°C) 75,5–76,5
PKS Value 11.2
CAS Number 89365-50-4
PUB Number 5152
Drugbank ID DB00938

Sources

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

Editorial principles

All information used for the content comes from verified sources (recognised institutions, experts, studies by renowned universities). We attach great importance to the qualification of the authors and the scientific background of the information. Thus, we ensure that our research is based on scientific findings.
Markus Falkenstätter, BSc

Markus Falkenstätter, BSc
Author

Markus Falkenstätter is a writer on pharmaceutical topics in Medikamio's medical editorial team. He is in the last semester of his pharmacy studies at the University of Vienna and loves scientific work in the field of natural sciences.

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer
Lector

Stefanie Lehenauer has been a freelance writer for Medikamio since 2020 and studied pharmacy at the University of Vienna. She works as a pharmacist in Vienna and her passion is herbal medicines and their effects.

The content of this page is an automated and high-quality translation from DeepL. You can find the original content in German here.

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