Fluticasone furoate/umeclidinium bromide/vilanterol (Trelegy)
Fluticasone furoate/umeclidinium bromide/vilanterol
It is a combination of Fluticasone furoate, a corticosteroid, Umeclidinium bromidea a muscarinic antagonist, and Vilanterol an ultra-long-acting β2 agonist
Trade names Trelegy Ellipta, Elebrato Ellipta, Temybric Ellipta
Pregnancy category AU: B3
Routes of administration Inhalation
It is a fixed-dose combination inhaled medication that is used for the maintenance treatment of chronic obstructive pulmonary disease (COPD).
The medications work in different ways: fluticasone furoate is an inhaled corticosteroid (ICS), umeclidinium is a long-acting muscarinic antagonist (LAMA), and vilanterol is a long-acting beta-agonist (LABA).
Approved by the US Food and Drug Administration with an indication for the maintenance treatment of a chronic obstructive pulmonary disease (COPD) in adults who (1) have already tried fluticasone furoate/vilanterol but are still experiencing symptoms of airway obstruction or who want to reduce the risk for COPD exacerbations and are already receiving umeclidinium and fluticasone furoate/vilanterol and would like to consolidate their inhaler therapy into a single product.
In the European Union, FF/UMEC/VI is indicated for the maintenance treatment in adults with moderate to severe COPD who are not adequately treated by an inhaled corticosteroid (ICS) plus long-acting beta-agonist (LABA) combination or a LABA plus long-acting muscarinic antagonist (LAMA) combination.
It is not used when people are experiencing acute symptoms consistent with worsening airway obstruction (i.e. COPD exacerbation or an asthma exacerbation).
Fluticasone furoate/umeclidinium bromide/vilanterol is only available as an inhaler.
FF/UMEC/VI exists as a dry-powder inhaler, which means that the force of the user’s breath causes the medicated powder to leave the device and enter the lungs: this is unlike, a metered-dose inhaler which includes a propellant).
It is contraindicated in people who are allergic to any of the individual medication components or who are severely allergic to milk proteins.
This is because each dose of FF/UMEC/VI is formulated with lactose monohydrate a portion of which contains detectable milk proteins.
The adverse effects of fluticasone furoate/umeclidinium bromide/vilanterol include those that are characteristic of its individual components.
There is a risk for anticholinergic side effects with difficulty urinating due to umeclidinium.
Effects on the cardiovascular system, such as increased pulse, elevated blood pressure, and abnormal heart rhythms, can occur due to vilanterol.
Fluticasone furoate, as an inhaled corticosteroid (ICS), can cause side effects that are characteristic of corticosteroids, such as decreased bone mineral density, adrenal suppression and a weakened immune system.
There is an elevated risk of pneumonia with FF/UMEC/VI; in clinical trials, there was a 1.53-fold higher risk of pneumonia in people that received FF/UMEC/VI,
Fluticasone furoate/umeclidinium bromide/vilanterol may have drug–drug interactions that are both pharmacokinetic related to metabolism and pharmacodynamic related to the effect of medications.
FF/UMEC/VI is susceptible to drug–drug interactions that would normally arise from any of the individual components of the medication.
All three components are substrates of the efflux transporter p-glycoprotein a protein that causes drugs to be transported out of cells.
Fluticasone furoate is metabolized by cytochrome P450 3A4 (CYP3A4).
Medications that are inhibitors of CYP3A4 may decrease fluticasone’s metabolism in the body, causing levels to accumulate.
The bioavailability of fluticasone in the FF/UMEC/VI product is low (15.2%), decreasing the risk of acute toxicity in overdose/accumulation situations.
Exposure to high doses of fluticasone over time, it may increase their risk of experiencing Cushing’s syndrome
In drug interaction studies of FF/UMEC/VI in the presence of the CYP3A4 inhibitor ketoconazole, adrenal insufficiency was noted at 24 hours.
Umeclidinium is primarily metabolized by CYP2D6, in addition to a few secondary metabolism pathways.
Vilanterol is also a CYP3A4 substrate.
CYP3A4 inhibitors may increase the levels of vilanterol in the body.
Fluticasone furoate is a corticosteroid, and can suppress the function of the immune system increasing the risk of infection, especially oral fungal infections when people do not rinse out their mouths with water after using fluticasone.
Umeclidinium is a medication with anticholinergic properties: side effects dry mouth, constipation.
Vilanterol is a beta2-adrenergic receptor agonist.
Pharmacology Fluticasone furoate/umeclidinium bromide/vilanterol is a combination product made up of three medications:
fluticasone, an inhaled corticosteroid (ICS) umeclidinium, a long-acting muscarinic antagonist (LAMA) (i.e. an anticholinergic medication) vilanterol, a long-acting beta-agonist (LABA) (specifically, a beta2-adrenergic receptor agonist)