Dosing and uses of Arnuity Ellipta (fluticasone furoate inhaled)
Adult dosage forms and strengths
powder for inhalation
- 100mcg/actuation
- 200mcg/actuation
Asthma
Indicated for maintenance treatment of asthma as prophylactic therapy
1 inhalation PO qDay; not to exceed 1 inhalation every 24 hr
Starting dose is based on asthma severity; the usual recommended starting dose is 100 mcg/day
May increase to 200 mcg/day after 2 weeks if patient does not respond to 100 mcg/day
Dosage modifications
Renal impairment (all severities): No dosage adjustment required
Mild hepatic impairment: No dosage adjustment required
Moderate-to-severe impairment: Caution advised; monitor patients for corticosteroid-related adverse effects
Dosing Considerations
Not indicated for relief of acute bronchospasm
Administration
For oral inhalation only
Rinse mouth with water and expectorate after each dose to prevent oral/esophageal candidiasis
Pediatric dosage forms and strengths
powder for inhalation
- 100mcg/actuation
- 200mcg/actuation
Asthma
Indicated for maintenance treatment of asthma as prophylactic therapy
<12 years: Safety and efficacy not established
≥12 years: 1 inhalation PO qDay; not to exceed 1 inhalation every 24 hr
Starting dose is based on asthma severity; the usual recommended starting dose is 100 mcg/day
May increase to 200 mcg/day after 2 weeks if patient does not respond to 100 mcg/day
Dosage modifications
Renal impairment (all severities): No dosage adjustment required
Mild hepatic impairment: No dosage adjustment required
Moderate-to-severe hepatic impairment: Caution advised; monitor patients for corticosteroid-related adverse effects
Dosing Considerations
Not indicated for relief of acute bronchospasm
Administration
For oral inhalation only
Rinse mouth with water and expectorate after each dose to prevent oral/esophageal candidiasis
Arnuity Ellipta (fluticasone furoate inhaled) adverse (side) effects
>10%
Nasopharyngitis (8-13%)
Headache (6-13%)
1-10%
Bronchitis (4-7%)
Sinusitis (4-7%)
Influenza (4-7%)
Pharyngitis (3-6%)
URT infection (2-6%)
Oropharyngeal pain (3-4%)
Toothache (3%)
Back pain (3%)
Viral gastroenteritis (3%)
Abdominal pain (3%)
Cough (3%)
Oropharyngeal candidiasis (3%)
Dysphonia (2-3%)
Oral candidiasis (<1-3%)
Procedural pain (<1-3%)
Rhinitis (<1-3%)
Throat irritation (<1-3%)
Warnings
Contraindications
Status asthmaticus or other acute episodes of asthma
Hypersensitivity, including severe allergy to milk protein
Cautions
Localized infections of the mouth and pharynx with Candida albicans reported with inhaled corticosteroids
Not indicated for use as rescue therapy for acute bronchospasm (see Contraindications)
Potential worsening of existing tuberculosis; fungal, bacterial, viral, or parasitic infections; or ocular herpes simplex; more serious or even fatal course of chickenpox or measles in susceptible patients; use caution because of potential for worsening of these infections; if exposed to chickenpox, prophylaxis with varicella-zoster immune globulin or pooled IV immunoglobulin may be indicated; if a patient is exposed to measles, prophylaxis with pooled IM immunoglobulin (IG) may be indicated
Caution when withdrawing from systemic corticosteroids and transferring to inhaled corticosteroids; taper systemic corticosteroids gradually and monitor for symptoms of HPA axis suppression and adrenal insufficiency
Systemic absorption from inhaled corticosteroids is low, but hypercorticism and adrenal suppression may occur with very high dosages or at regular dosage in susceptible individuals; if changes occur, discontinue therapy slowly
CYP3A4 substrate; strong CYP3A4 inhibitors may increase fluticasone systemic exposure
Paradoxical bronchospasm with immediate increase in wheezing after dosing reported; treat immediately with inhaled short-acting bronchodilator and discontinue fluticasone inhaled
Hypersensitivity reactions (eg, urticaria, flushing, allergic dermatitis, bronchospasm) reported; anaphylaxis in patients with severe milk protein allergy observed with other inhaled powder products that contain lactose
Long-term use decreases bone mineral density
May cause reduction in growth velocity when administered to children and adolescents
Glaucoma, increased intraocular pressure, and cataracts have been reported in patients following the long-term administration of inhaled corticosteroids
Epistaxis, nasal ulceration, Candida albicans infection, nasal septal perforation, impaired wound healing; monitor patients periodically for signs of adverse effects on nasal mucosa; avoid use in patients with recent nasal ulcers, nasal surgery, or nasal trauma
Pregnancy and lactation
Pregnancy category: C
Lactation: Unknown if 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 Arnuity Ellipta (fluticasone furoate inhaled)
Mechanism of action
Synthetic trifluorinated corticosteroid that elicits anti-inflammatory activity
Exact mechanism of action is unknown, but corticosteroids have shown to exhibit anti-inflammatory effect on neutrophils, eosinophils, macrophages, mast cells, lymphocytes, and mediators (histamine, leukotrienes, cytokines, eicosanoids)
Exhibits 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, inhaled: 13.9% (inhaled portion of the dose delivered to the lung)
Bioavailability, oral: 1.3% (low from swallowed portion due to extensive first-pass metabolism)
Peak plasma time: 0.5-1 hr
AUC: 26% lower in patients with asthma compared with healthy volunteers
Distribution
Protein bound: 99.6%
Vd: 661 L
Metabolism
Cleared from systemic circulation principally by hepatic metabolism via CYP3A4
Metabolites have significantly reduced activity
Elimination
Half-life: 24 hr (with repeat dosing)
Excretion: >99% feces; ~1% urine
