ARNUITY ELLIPTA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ARNUITY ELLIPTA (ARNUITY ELLIPTA).
Fluticasone furoate is a synthetic trifluorinated corticosteroid with potent anti-inflammatory activity. It binds to the glucocorticoid receptor, leading to inhibition of inflammatory mediators such as cytokines, prostaglandins, and leukotrienes. This reduces airway inflammation and hyperresponsiveness.
| Metabolism | Fluticasone furoate is extensively metabolized in the liver via CYP3A4 to a less active metabolite. Systemic exposure is low due to high first-pass metabolism and oral bioavailability of less than 2%. |
| Excretion | Fluticasone furoate is eliminated primarily via hepatic metabolism and subsequent biliary excretion. Following oral administration, approximately 90% of the dose is excreted in feces as metabolites, with less than 1% excreted unchanged in urine. Renal excretion of unchanged drug is negligible. |
| Half-life | The terminal elimination half-life of fluticasone furoate is approximately 24 hours. This long half-life supports once-daily dosing and contributes to sustained anti-inflammatory effects in the lungs. |
| Protein binding | Fluticasone furoate is highly protein bound (>99%) primarily to albumin. Minimal binding to alpha-1-acid glycoprotein occurs. |
| Volume of Distribution | The volume of distribution of fluticasone furoate is approximately 4.2 L/kg, indicating extensive tissue distribution. This large Vd reflects high lipophilicity and tissue binding. |
| Bioavailability | The absolute bioavailability of inhaled fluticasone furoate is approximately 15.2%. Oral bioavailability is extremely low (<2%) due to extensive first-pass metabolism. The swallowed portion contributes minimally to systemic exposure. |
| Onset of Action | Inhaled fluticasone furoate demonstrates onset of action within 2-4 hours after administration, with peak bronchodilator effects observed by 12 hours for the LABA component (vilanterol) when present. For fluticasone furoate alone, onset of anti-inflammatory effect is typically seen within 24 hours. |
| Duration of Action | The duration of action for fluticasone furoate is approximately 24 hours, allowing once-daily dosing. Clinical efficacy in asthma and COPD is maintained over 24 hours with consistent dosing. |
1 inhalation (100 mcg fluticasone furoate) once daily via oral inhalation, with or without a spacer.
| Dosage form | POWDER |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | For Child-Pugh class C: use with caution; maximum dose 100 mcg once daily. For Child-Pugh A or B: no adjustment needed. |
| Pediatric use | Not approved for children under 12 years of age. For adolescents 12 years and older: same as adult dose (100 mcg once daily). |
| Geriatric use | No specific dose adjustment required; use with caution due to potential decreased renal function and increased risk of adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ARNUITY ELLIPTA (ARNUITY ELLIPTA).
| Breastfeeding | Limited data; fluticasone furoate likely excreted in breast milk in low amounts (M/P ratio unknown). Consider benefit to breastfeeding vs. potential risk to infant, especially at high doses. |
| Teratogenic Risk | No human data; animal studies show no teratogenicity at clinically relevant doses. Avoid use in first trimester unless benefit outweighs risk. In second/third trimester, use with caution due to potential for fetal growth restriction from systemic corticosteroid exposure. |
| Fetal Monitoring |
■ FDA Black Box Warning
Long-term use of inhaled corticosteroids may result in a reduction of growth velocity in children. The lowest effective dose should be used to minimize systemic effects.
| Serious Effects |
["Primary treatment of status asthmaticus or other acute episodes of asthma where intensive measures are required","Known hypersensitivity to fluticasone furoate or any ingredient in the formulation"]
| Precautions | ["Candida albicans infection of the mouth and pharynx","Increased risk of pneumonia in patients with COPD","Systemic corticosteroid effects with prolonged use (e.g., HPA axis suppression, growth reduction in children)","Paradoxical bronchospasm","Hypersensitivity reactions including anaphylaxis, rash, urticaria, and angioedema","Monitor for ocular effects (e.g., glaucoma, cataracts)"] |
| Food/Dietary | No significant food interactions known. Avoid grapefruit juice? No specific interactions reported; routine dietary restrictions are not required. |
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| Monitor maternal lung function, fetal growth (ultrasound) and amniotic fluid index if used long-term; assess for maternal adrenal suppression. |
| Fertility Effects | No reported effects on fertility in animal studies; human data lacking. |
| Clinical Pearls | ARNUITY ELLIPTA (fluticasone furoate) is an inhaled corticosteroid (ICS) indicated for once-daily maintenance treatment of asthma in patients aged ≥5 years. It is not indicated for acute bronchospasm or status asthmaticus. Rinse mouth with water after each use to reduce risk of oropharyngeal candidiasis. Monitor for signs of adrenal insufficiency during stress or conversion from systemic corticosteroids. Not for use in COPD. |
| Patient Advice | Use exactly as prescribed; do not use for sudden breathing problems. · Rinse mouth with water after each inhalation; do not swallow. · Do not stop therapy abruptly; consult healthcare provider before discontinuing. · Store at room temperature away from moisture and heat; keep the device closed. · Clean the mouthpiece weekly with a dry cloth; do not wash with water. · Seek medical attention if symptoms worsen or if rescue inhaler use increases. |