Vilanterol

Vilanterol

Basics

Vilanterol is an active ingredient used to treat chronic obstructive pulmonary disease (COPD ) and bronchial asthma. It belongs to the group of beta-2 sympathomimetics and is given in combination with fluticasone furoate, an anti-inflammatory glucocorticoid. Vilanterol is usually present as vilanterol trifenate. It is a white powder. Structurally, it is related to epinephrine and salbutamol. It is a saligenin derivative of vilanterol. Vilanterol is effective for a very long time and thus has the advantage that it only needs to be used once a day.

Effect

Vilanterol acts by binding to the beta-2 adrenoceptors. It acts very specifically and also for a very long time. Binding of vilanterol to the beta-2 adrenoceptors stimulates intracellular adenylyl cyclase, which in turn converts adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). This increases cAMP concentration and results in relaxation of bronchial smooth muscle, leading to improvement of symptoms. In addition, the release of mast cell mediators, which are responsible for hypersensitivity reactions, is inhibited. The effect sets in very quickly, after only 5-15 minutes, and lasts for about 24 hours.

The bioavailability of vilanterol, i.e. the percentage of the active substance available in the blood, is approx. 27%.

Half-life, the time it takes the body to excrete half of the active ingredient, is 11-20 hours, depending on the dosage of the active ingredient. The maximum plasma concentration (Cmax), which is the maximum concentration of the drug in the blood plasma (liquid cell-free portion of the blood), is reached after 5-15 minutes.

Vilanterol is degraded in the liver by CYP3A4 enzymes and excreted in urine and feces.

Dosage

Always take vilanterol exactly as described in the package leaflet or exactly as your doctor has told you.

The usual recommended dose of vilanterol is 22 micrograms daily.

The usual dose of fluticasone varies from 92 to 184 micrograms daily.

The usual dosage of umeclidinium is 55 micrograms daily.

It is taken one inhalation per day at a time. So if you need a higher dosage, do NOT inhale twice. You will be given a different, higher dose preparation.

Vilanterol is only available as a combination preparation with fluticasone (as a 2-dose combination) and umeclidinium (as a 3-dose combination).

Side Effects

The following side effects may occur:

  • allergic reactions
  • acute respiratory problems
  • Pneumonia

Very common:

Frequent:

Occasionally:

Rarely:

Overdose of more than 20 times the dose may result in the formation of mesovarial tumors.

Interactions

Drug interactions may occur if the following drugs are taken at the same time:

Contraindications

Vilanterol must NOT be taken in the following cases:

Age Restriction

Vilanterol should NOT be used under 12 years of age.

Pregnancy & Lactation

In pregnancy, vilanterol should be used only in consultation with your doctor. In studies in rats and rabbits, no risk of malformation was observed in relation to organ formation. However, malformations related to bone were observed. Among other things, there was a lack of ossification (ossification) of the bones.

During breastfeeding, vilanterol should be used only in consultation with your doctor. No transfer of vilanterol into breast milk was observed in animal studies.

Chemical & physical properties

Formula C24H33Cl2NO5
Molar Mass (g·mol−1) 486,428
Physical State solid
Density (g·cm−3) 1,3
Boiling Point (°C) 646,7
PKS Value 10,12
CAS Number 503068-34-6
PUB Number 10184665
Drugbank ID DB09082

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.
Thomas Hofko

Thomas Hofko
Author

Thomas Hofko is in the final third of his bachelor's degree in pharmacy and is an author and lecturer on pharmaceutical topics. He is particularly interested in the fields of clinical pharmacy and phytopharmacy.

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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The contents shown do not replace the original package insert of the medicinal product, especially with regard to dosage and effect of the individual products. We cannot assume any liability for the correctness of the data, as the data was partly converted automatically. A doctor should always be consulted for diagnoses and other health questions. Further information on this topic can be found here.