fluticasone furoate
Brand: Arnuity Ellipta (ICS alone), Breo Ellipta (with vilanterol), Trelegy Ellipta (with vilanterol + umeclidinium)
Prototype: fluticasone propionate
Drug Class: inhaled corticosteroid (ICS)
Drug Family: corticosteroid
Subclass: synthetic glucocorticoid — once-daily ICS
Organ Systems: respiratory
Mechanism of Action
Synthetic glucocorticoid with high glucocorticoid receptor affinity (approximately 29-fold greater than fluticasone propionate for GR); binds intracellular GR, translocates to the nucleus, transactivates anti-inflammatory genes and transrepresses pro-inflammatory transcription factors (NF-kB, AP-1), reducing airway eosinophilic inflammation and cytokine production.
glucocorticoid receptor (GR)airway inflammatory cells
Indications
- asthma maintenance therapy
- COPD with frequent exacerbations (in combination products)
Contraindications
- primary treatment of acute bronchospasm
- hypersensitivity to fluticasone furoate or milk proteins
Adverse Effects
Common
- oropharyngeal candidiasis
- nasopharyngitis
- upper respiratory infection
- headache
- dysphonia
Serious
- adrenal suppression (high doses, prolonged use)
- systemic corticosteroid effects (osteoporosis, cataracts, growth suppression in children)
- increased pneumonia risk in COPD patients
Pharmacokinetics (ADME)
| Absorption | inhaled; Cmax within 0.5-1 hour; absolute systemic bioavailability approximately 15% |
| Distribution | Vd approximately 661 L; 99.7% protein bound |
| Metabolism | extensive hepatic CYP3A4 first-pass metabolism; rapidly inactivated to inactive carboxylic acid metabolite |
| Excretion | fecal (~101%) — enterohepatic cycling; renal minimal |
| Half-life | approximately 24 hours |
| Onset | anti-inflammatory effect within days; maximal benefit over weeks |
| Peak | 0.5-1 hour (systemic) |
| Duration | 24 hours (once-daily dosing) |
| Protein Binding | 99.7% |
| Vd | approximately 661 L |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| strong CYP3A4 inhibitors (ketoconazole, ritonavir) | increase systemic fluticasone furoate exposure; risk of adrenal suppression and systemic corticosteroid effects | major |
| other inhaled corticosteroids | additive systemic corticosteroid exposure if combined; avoid unless intentional | moderate |
Nursing Considerations
- Instruct patients to rinse mouth with water and spit immediately after each inhalation to prevent oropharyngeal candidiasis; inspect mouth at each visit for white plaques.
- Fluticasone furoate is once-daily, unlike fluticasone propionate which is twice-daily; verify the formulation on the prescription and confirm the patient understands the correct dosing frequency.
- Monitor for systemic corticosteroid effects with prolonged high-dose use: assess for cushingoid features, bone density (particularly in postmenopausal women), and screen for cataracts and glaucoma annually.
- Do not use for acute asthma exacerbations; instruct patients that slow onset makes ICS unsuitable for rescue use; a SABA must be prescribed alongside for acute symptom relief.
Clinical Pearls
- Fluticasone furoate's superior glucocorticoid receptor binding affinity compared with fluticasone propionate supports once-daily dosing rather than twice-daily, but no head-to-head trial has shown clinical superiority over fluticasone propionate at equivalent doses.
- In COPD patients, ICS therapy including fluticasone furoate is associated with increased pneumonia risk; the ACC/AHA and GOLD guidelines recommend reserving ICS use for COPD patients with frequent exacerbations and blood eosinophil counts above 100-300 cells/mcL.
Safety Profile
Pregnancy use-with-caution
Lactation insufficient-data
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
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