BREO ELLIPTA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for BREO ELLIPTA (BREO ELLIPTA).
Combination of fluticasone furoate, a corticosteroid that binds to glucocorticoid receptors to inhibit inflammatory gene transcription, and vilanterol, a long-acting beta2-adrenergic agonist that activates adenylate cyclase leading to bronchodilation.
| Metabolism | Fluticasone furoate: primarily metabolized by CYP3A4; Vilanterol: primarily metabolized by CYP3A4. |
| Excretion | Fluticasone furoate is eliminated primarily via fecal excretion (approximately 101% of an oral dose) due to biliary clearance, with minimal renal excretion (<1%). Vilanterol is eliminated via metabolism and subsequent renal (approximately 70% of an IV dose) and fecal (approximately 30% of an IV dose) excretion. |
| Half-life | Fluticasone furoate: 24 hours (supports once-daily dosing). Vilanterol: 11 hours (supports once-daily dosing). |
| Protein binding | Fluticasone furoate: >99.8% (primarily albumin). Vilanterol: approximately 94% (albumin and alpha-1-acid glycoprotein). |
| Volume of Distribution | Fluticasone furoate: approximately 4.5 L/kg (extensive tissue distribution). Vilanterol: approximately 165 L (large Vd, extensive distribution). |
| Bioavailability | Inhaled: Fluticasone furoate absolute bioavailability approximately 15% (lung deposition). Vilanterol absolute bioavailability approximately 27% (lung deposition). Oral bioavailability is negligible for both (<2% for fluticasone furoate, <5% for vilanterol). |
| Onset of Action | Inhaled: Bronchodilation observed within 15 minutes; maximal improvement in lung function within 1 hour. |
| Duration of Action | Inhaled: 24 hours (maintained bronchodilation and anti-inflammatory effect). |
| Molecular Weight | Fluticasone furoate: 538.6 Da; Vilanterol: 487.6 Da |
One inhalation (100 mcg fluticasone furoate / 25 mcg vilanterol) once daily via oral inhalation.
| Dosage form | POWDER |
| Renal impairment | No dosage adjustment required for renal impairment. However, use with caution in severe renal impairment due to potential for increased systemic exposure. |
| Liver impairment | Child-Pugh Class A and B: No dosage adjustment recommended. Child-Pugh Class C: Contraindicated. |
| Pediatric use | Indicated for children aged 5 years and older with asthma. For ages 5-11: one inhalation of 100 mcg/25 mcg once daily. For ages 12 and older: same as adult dosing. |
| Geriatric use | No dose adjustment required for elderly patients. Use with caution due to increased risk of comorbidities and adverse effects. |
| 1st trimester | Insufficient human data; avoid unless benefit outweighs risk. In animal studies, corticosteroids caused malformations. |
| 2nd trimester | Use only if clearly needed; minimal data suggests no major teratogenic risk, but avoid unnecessary exposure. |
| 3rd trimester | Risk of neonatal adrenal suppression if used near term; monitor newborn. Use lowest effective dose. |
Clinical note
Comprehensive clinical and safety monograph for BREO ELLIPTA (BREO ELLIPTA).
| Placental transfer | Placental transfer occurs for inhaled corticosteroids (e.g., fluticasone furoate) and LABA (vilanterol) to a limited extent; clinical significance unknown. |
| Breastfeeding | Inhaled corticosteroids and LABA are excreted in breast milk in low amounts; consider risk-benefit. Monitor infant for adverse effects. |
■ FDA Black Box Warning
Long-acting beta2-adrenergic agonists (LABAs) increase the risk of asthma-related death. Use only as additional therapy for patients not adequately controlled on a long-term asthma control medication or whose disease severity warrants initiation of both an inhaled corticosteroid and a LABA.
| Serious Effects |
Hypersensitivity to fluticasone furoate, vilanterol, or any excipientStatus asthmaticus or acute bronchospasmNon-allergic bronchospasm without established asthma/COPD diagnosisAs monotherapy for asthma without inhaled corticosteroid
| Precautions | Increased risk of asthma-related death when used as monotherapy for asthma without inhaled corticosteroid, Candida infections of the mouth and pharynx, Pneumonia in patients with COPD, Adrenal insufficiency, Hypercorticism and adrenal suppression, Paradoxical bronchospasm, Hypersensitivity reactions including anaphylaxis, Cardiovascular effects like increased blood pressure and heart rate, Eosinophilic conditions, Reduced bone mineral density, Glaucoma and cataracts |
| Food/Dietary | No specific food interactions reported. However, grapefruit juice may increase systemic exposure to fluticasone furoate via CYP3A4 inhibition; although clinical significance is low, avoid excessive grapefruit consumption. No dietary restrictions necessary. |
Loading safety data…
| Lactation Rating |
| L3: Limited data - probably compatible but caution advised. |
| Teratogenic Risk | Insufficient human data; based on animal studies, corticosteroids (fluticasone furoate) and LABA (vilanterol) show no major teratogenicity but may cause fetal growth restriction at high systemic exposures. Avoid in first trimester unless benefit outweighs risk; use lowest effective dose in later trimesters. |
| Fetal Monitoring | Monitor maternal asthma control (peak expiratory flow, symptoms), fetal growth (ultrasound for growth restriction if high-dose or prolonged use), and signs of maternal adrenal suppression. Assess neonatal respiratory status if used near term. |
| Fertility Effects | No known effects on fertility based on limited human data; animal studies show no impairment at clinically relevant doses. |
| Clinical Pearls | Breo Ellipta (fluticasone furoate/vilanterol) is an ICS/LABA combination indicated for maintenance treatment of COPD and asthma. It is not for acute bronchospasm. The ELLIPTA inhaler is a once-daily, dry powder inhaler; each actuation delivers a fixed dose. Rinse mouth with water after use without swallowing to reduce oral candidiasis. Monitor for pneumonia in COPD patients. In asthma, it is not indicated for patients under 18 years; for COPD, use only in patients with a history of exacerbations. Do not discontinue abruptly. |
| Patient Advice | Use exactly as prescribed; it is not a rescue inhaler for sudden breathing problems. · Rinse mouth with water after each dose without swallowing to prevent oral thrush. · Do not stop taking this medication without consulting your doctor; stopping can worsen breathing. · Tell your doctor if you have any signs of infection, pneumonia, or worsening breathing. · Store the inhaler at room temperature away from moisture and heat; keep it closed when not in use. |