vilanterol/fluticasone furoate inhaled (Breo Ellipta)
Classes: Respiratory Inhalant Combos; Beta2 Agonists; Corticosteroids, Inhalants
Dosing and uses of Breo Ellipta (vilanterol fluticasone inhaled)
Adult dosage forms and strengths
vilanterol/fluticasone furoate inhaled
powder for inhalation
- 25mcg/100mcg per actuation
- 25mg/200mcg per actuation
- Ellipta inhaler contains 2 double-foil blister strips, 1 containing fluticasone furoate and the other strip contains vilanterol; after the inhaler is activated, the powder within both blisters is exposed and ready for dispersion
Chronic Obstructive Pulmonary Disease
Indicated for long-term, once-daily, maintenance treatment of airflow obstruction with COPD, including chronic bronchitis and/or emphysema; also approved to reduce COPD exacerbations
25 mcg/100 mcg (1 actuation) inhaled PO qDay
Asthma
Indicated for once-daily treatment of asthma for patients not adequately controlled on a long-term asthma control medication (eg, inhaled corticosteroid), or whose disease severity clearly warrants initiation of treatment with both an inhaled corticosteroid and a long-acting beta agonist (LABA)
Use prescribe strength (25 mcg/100 mcg or 25 mcg/200 mcg per actuation) once daily via oral inhalation
Dosage modifications
Hepatic or renal impairment: No dosage adjustment required
Geriatric patients: No dosage adjustment required
Dosing Considerations
Limitations of use: NOT indicated for the relief of acute bronchospasm
Asthma indication
- LABAs (eg, vilanterol) increase the risk of asthma-related death
- Available data from controlled clinical trials suggest that LABAs increase the risk of asthma-related hospitalization in pediatric and adolescent patients
- Therefore, when treating patients with asthma, physicians should only prescribe vilanterol/fluticasone furoate inhaled for patients not adequately controlled on a long-term asthma control medication (eg, inhaled corticosteroid), or whose disease severity clearly warrants initiation of treatment with both an inhaled corticosteroid and a LABA
- Once asthma control is achieved and maintained, assess the patient at regular intervals and step down therapy (eg, discontinue vilanterol/fluticasone furoate inhaled) if possible without loss of asthma control and maintain the patient on a long-term asthma control medication (eg, inhaled corticosteroid)
- Do not use for patients whose asthma is adequately controlled on low- or medium-dose inhaled corticosteroids
Pediatric dosage forms and strengths
Safety and efficacy not established
Breo Ellipta (vilanterol fluticasone inhaled) adverse (side) effects
1-10%
Nasopharyngitis (9%)
Upper respiratory infection (7%)
Headache (7%)
Oropharyngeal candidiasis (5%)
Postmarketing reports
Anxiety
Tremors
Palpitations, tachycardia
Anaphylaxis, angioedema, rash, urticaria
Muscle spasms
Tremor
Nervousness
Warnings
Black box warnings
Long-acting beta2-adrenergic agonists (LABAs), such as vilanterol, increase the risk for asthma-related death
A placebo-controlled trial with another LABA (salmeterol) showed an increase in asthma-related deaths; this finding is considered a class effect of all LABA, including vilanteroL
Therefore, when treating patients with asthma, physicians should only prescribe vilanterol/fluticasone furoate inhaled for patients not adequately controlled on a long-term asthma control medication (eg, inhaled corticosteroid), or whose disease severity clearly warrants initiation of treatment with both an inhaled corticosteroid and a LABA
Once asthma control is achieved and maintained, assess the patient at regular intervals and step down therapy (eg, discontinue vilanterol/fluticasone furoate inhaled) if possible without loss of asthma control and maintain the patient on a long-term asthma control medication (eg, inhaled corticosteroid)
Do not use for patients whose asthma is adequately controlled on low- or medium-dose inhaled corticosteroids
Contraindications
Primary treatment of status asthmaticus or other acute episodes of COPD or asthma where intensive measures are required
Hypersensitivity to drug, any components/excipients, or milk proteins
Cautions
LABAs (eg, vilanterol) increase the risk of asthma-related death (see Black box warnings)
Increasing use of inhaled, short-acting beta2-agonists (ie, rescue inhalers) is a marker of deteriorating disease and acute episodes; reevaluate the patient immediately
Do not initiate during rapidly deteriorating or potentially life-threatening episodes of COPD, or as rescue therapy acute bronchospasm, which should be treated with an inhaled, short-acting beta2-agonist LABAs increase asthma-related death (see Black box warnings)
Do not use in combination with another medication containing a LABA because of risk for overdose
Caution with underlying cardiovascular disease because of beta-adrenergic stimulation
Risk of paradoxical bronchospasm, which may be life-threatening; discontinue and treat immediately with inhaled SABA
Decreases bone mineral density following long-term administration of corticosteroids; bone fractures reported with inhaled corticosteroid use; assess upon initiation and periodically thereafter
Corticosteroids increase risk of pneumonia; monitor for S/S of pneumonia and lung infections
Corticosteroids increase risk of cataracts, glaucoma, and increased IOP Excessive use (or at regular dose in susceptible individuals) may result in hypercorticism and suppress HPA function; monitor closely, especially postoperatively or during periods of stress
Corticosteroids increase risk for potential worsening of existing tuberculosis; fungal, bacterial, viral, or parasitic infections; or ocular herpes simplex
Risk for more serious or fatal course of chickenpox or measles in susceptible patients (eg, unvaccinated or immunologically unexposed individuals); care must be taken to avoid exposure to corticosteroids
Particular care is needed to transfer patients from systemic to inhaled corticosteroids; potentially fatal adrenal insufficiency may occur before/after; taper withdrawal gradually by reducing daily prednisone dose by 2.5 mg on weekly basis
Risk of hypokalemia and hyperglycemia
Caution with convulsive disorders, thyrotoxicosis, diabetes mellitus, and ketoacidosis
Close monitoring for glaucoma and cataracts is warranted
Angioedema, rash, or urticaria may occur after administration
Pregnancy and lactation
Pregnancy category: C
Lactation: Unknown whether distributed in human breast milk
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Breo Ellipta (vilanterol fluticasone inhaled)
Mechanism of action
Vilanterol: Long-acting selective beta2-adrenergic agonist (LABA); stimulates intracellular adenyl cyclase resulting in increased cAMP levels causing bronchial smooth muscle relaxation; also inhibits release of mediators of immediate hypersensitivity from cells, especially from mast cells
Fluticasone furoate (FF): Long-acting inhaled trifluorinated corticosteroid with potent anti-inflammatory activity; inhibits multiple cell types (eg, mast cells, eosinophils, basophils, lymphocytes, macrophages, neutrophils) and mediator production or secretion (eg, histamine, eicosanoids, leukotrienes, cytokines) involved in the asthmatic response
Fluticasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor that is approximately 29.9 times that of dexamethasone and 1.7 times that of fluticasone propionate
Absorption
Bioavailability: 27.3% (vilanterol); 15.2% (FF)
Peak plasma time: 10 minutes (vilanterol); 0.5-1 hr (FF)
AUC: 46% lower in patients with COPD compared with healthy individuals
Distribution
Following IV administration of each component
Protein bound: 93.9% (vilanterol); 99.6% (FF)
Vd: 165 L (vilanterol); 661 L (FF)
Metabolism
Vilanterol is mainly metabolized, principally via CYP3A4, to a range of metabolites with significantly reduced beta1- and beta2-agonist activity
Fluticasone furoate is cleared from systemic circulation principally by hepatic metabolism via CYP3A4 to metabolites with significantly reduced corticosteroid activity
Elimination
Half-life: 21.3 hr (vilanterol); 24 hr (FF)
Excretion
- Pharmacokinetic studies following oral and IV administration
- Vilanterol and metabolites: 30% feces; 70% urine
- Fluticasone furoate and metabolites: 90-100% feces; 1-2% urine
Administration
Instructions
After inhalation, rinse mouth with water and expectorate to help reduce risk of oropharyngeal candidiasis
Take at same time each day
Do not exceed 1 administration/24 hr
More frequent administration or a greater number of inhalations (>1 inhalation daily) of the prescribed strength is not recommended as some patients are more likely to experience adverse effects with higher doses
Patients should not use an additional long-acting beta agonist (LABA) for any reason
