Vilanterol
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| Surname | Vilanterol | |||||||||||||||||||||
| other names |
4 - {(1 R ) -2 - [(6- {2 - [(2,6-dichlorobenzyl) oxy] ethoxy} hexyl) amino] -1-hydroxyethyl} -2- (hydroxymethyl) phenol |
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| Molecular formula | C 24 H 33 C 12 NO 5 | |||||||||||||||||||||
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| ATC code |
R03 AK10 (fluticasone furoate); R03 AL03 (umeclidinium bromide) |
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| Molar mass | 486.43 g · mol -1 | |||||||||||||||||||||
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | ||||||||||||||||||||||
Vilanterol is a drug from the group of β 2 sympathomimetics that is used in the treatment of bronchial asthma and COPD . Vilanterol itself is not used as a single preparation , but as a powder inhaler either in combination with the corticosteroid fluticasone furoate or umeclidinium bromide , an anticholinergic .
Clinical information
Type and duration of application
Vilanterol is absorbed through inhalation. For a therapy, 22 µg of the active ingredient are absorbed in the fixed combination.
Drug interactions
It is known that beta-blockers can reduce the effects of vilanterol (weakening or abolishing), while adrenergic agents (acting on adrenoceptors ) increase them. The metabolism of vilanterol is slowed down by strong CYP3A4 inhibitors ( ketoconazole , clarithromycin , ritonavir ), so that the active ingredient is active longer and the risk of side effects is increased. It is also possible that a potassium deficiency caused by vilanterol is exacerbated by drugs that can also cause this deficiency (e.g. methylxanthine derivatives or steroids).
Use during pregnancy and breastfeeding
In animal studies, vilanterol has been shown to be toxic to reproduction. Therefore, use in humans is only appropriate if the benefit-risk assessment is positive.
It is not known whether vilanterol can pass into breast milk (analogous to other β 2 sympathomimetics).
Adverse effects (side effects)
Since vilanterol is always administered in a fixed combination, it is difficult to clearly assign side effects.
- In combination with fluticasone furoate (Relvar ® ), the following side effects are known:
- very common: headache, inflammation of the lining of the nose and throat ( nasopharyngitis ).
- Common: pneumonia , upper respiratory tract infections, bronchitis , flu , mouth and throat candidiasis , upper respiratory tract pain , sinus infection , throat infection , runny nose , cough, hoarseness , abdominal pain, fractures, fever and joint pain
- In combination with umeclidinium bromide (Anoro ® ), the following side effects are known:
- common: headache, cough, inflammation of the nasal and pharynx, upper respiratory tract pain, sinus infection, throat infection, urinary tract infection, dry mouth, and constipation .
- uncommon: skin rash, various cardiac arrhythmias ( atrial fibrillation , supraventricular tachycardias and extrasystoles, and idioventricular rhythms)
There is also a risk of paradoxical bronchospasm upon inhalation . It is also possible that vilanterol is causing a potassium deficiency.
Pharmacological properties
Mechanism of action (pharmacodynamics)
Vilanterol (as well as fluticasone furoate and umeclidinium bromide) act locally on the airways. In the cells of the respiratory tract, vilanterol activates adenylyl cyclase so that more cAMP becomes available. cAMP is a messenger substance that relaxes and relaxes the smooth muscles of the airways.
In addition, vilanterol inhibits an inflammatory reaction as part of an immediate allergic reaction, especially from the so-called mast cells.
Absorption and distribution in the body (pharmacokinetics)
Vilanterol is absorbed by inhalation, the bioavailability is 27%. In the body, the active ingredient is further metabolized by means of CYP3A4, so that it is then brought out of the cell as a substrate for the PGP pump . Eventually, vilanterol is excreted in the urine as metabolites. The half-life is about 11 hours.
Trade names
- As a powder inhaler in combination with fluticasone furoate: Relvar (D, CH)
- As a powder inhaler in combination with umeclidinium bromide: Anoro (D, CH)
literature
- Monika Neubeck: Vilanterol . In: Neue Arzneimittel, supplement to the Deutsche Apotheker-Zeitung . Volume 61, No. 10, October 2014, pp. 73–75.
Individual evidence
- ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
