Vilanterol

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.

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.

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).

The following side effects may occur:

• allergic reactions
• acute respiratory problems
• Pneumonia

Very common:

• Headache
• Common cold

Frequent:

• Fungal infection in the mouth and throat area
• Inflammation of the bronchial tubes (bronchitis)
• Flu
• Pain in the mouth and throat
• Inflammation of the sinuses
• Rhinitis
• Cough
• Impairment of the voice
• Weakening of bones with bone fractures as a complication
• abdominal pain
• Back pain
• Fever
• Joint pain
• Muscle cramps

Occasionally:

• irregular heartbeat
• blurred vision
• increased blood sugar (hyperglycemia)

Rarely:

• accelerated heartbeat (tachycardia)
• palpitations
• tremor
• Anxiety

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

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

• Beta-blockers, such as metoprolol, in high blood pressure or heart disease.
• ketoconazole, in fungal infections
• ritonavir or cobicistat, for HIV infection
• long-acting beta-2-adrenergic agonists, such as salmeterol

Vilanterol must NOT be taken in the following cases:

• In case of allergy to vilanterol, fluticasone or umeclidinium.

Vilanterol should NOT be used under 12 years of age.

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.