Vilanterol Trifenatate + Fluticasone Furoate

• Asthma: Maintenance treatment of asthma in adults and adolescents (≥12 years) not adequately controlled with inhaled corticosteroids (ICS) alone or ICS plus other bronchodilators.
• Chronic Obstructive Pulmonary Disease (COPD): Maintenance treatment of airflow obstruction in patients with moderate to very severe COPD to reduce exacerbations.
• Off-label: Use in asthma-COPD overlap syndrome (ACO) when dual therapy is insufficient, under clinical judgment.

• Dosage Form: Dry powder inhaler (Ellipta).
• Recommended Dose: One inhalation once daily containing:
• Vilanterol Trifenatate 25 mcg
• Fluticasone Furoate 100 mcg or 200 mcg (dose tailored by disease severity).
• Route: Oral inhalation only.
• Special Populations:
• Pediatrics (<12 years): Not established.
• Elderly: No dose adjustment required.
• Renal impairment: No adjustment necessary.
• Hepatic impairment: Use with caution in severe impairment.
• Administration Tips: Use regularly at the same time daily. Rinse mouth after inhalation to reduce candidiasis risk. Not for acute symptom relief.

Vilanterol is a long-acting selective β2-adrenergic receptor agonist (LABA) that relaxes airway smooth muscle by stimulating β2 receptors, increasing cyclic AMP, and promoting bronchodilation. Fluticasone furoate is a potent inhaled corticosteroid (ICS) that binds glucocorticoid receptors, reducing airway inflammation via suppression of inflammatory gene expression and mediator release. The combination produces complementary effects: vilanterol provides sustained bronchodilation, while fluticasone furoate controls airway inflammation, improving airflow and symptom control in asthma and COPD.

• Absorption: Rapid pulmonary absorption; peak plasma concentrations within 5–30 minutes.
• Bioavailability: Approximately 27% for vilanterol and 15% for fluticasone furoate after inhalation.
• Distribution: Extensive volume of distribution (~165 L for vilanterol, ~661 L for fluticasone furoate).
• Metabolism: Both extensively metabolized by CYP3A4 into inactive metabolites.
• Half-life: Approximately 21 hours for vilanterol and 24 hours for fluticasone furoate.
• Excretion: Mainly via feces (>90%); renal elimination minimal (<2%).

• Pregnancy: Limited human data. Use only if benefits justify potential risks. Animal studies show adverse effects at high doses. No FDA pregnancy category assigned.
• Lactation: Unknown if excreted in human milk. Caution advised due to potential infant exposure.
• Recommendation: Use only when clearly needed; monitor mother and infant if used during breastfeeding.

• Primary Class: Combination inhaled corticosteroid and long-acting beta2-agonist (ICS/LABA).
• Subclasses: Fluticasone furoate (ICS), Vilanterol (LABA).
• Use: Maintenance treatment of obstructive airway diseases.

• Known hypersensitivity to vilanterol, fluticasone furoate, or any formulation excipients.
• Primary treatment of acute bronchospasm or status asthmaticus.
• Concurrent use with other LABA-containing products.

• Not indicated for relief of acute bronchospasm.
• Increased risk of asthma-related deaths with LABA monotherapy; always combine with ICS.
• Elevated risk of pneumonia in COPD patients receiving ICS.
• Monitor for paradoxical bronchospasm; discontinue immediately if it occurs.
• Caution in patients with cardiovascular disease, hypertension, diabetes, osteoporosis, or immunosuppression.
• Prolonged high-dose corticosteroid use may cause systemic effects such as adrenal suppression.
• Patients should rinse their mouth after inhalation to reduce oral candidiasis.

• Common: Headache, nasopharyngitis, cough, oropharyngeal candidiasis, dysphonia, upper respiratory infections.
• Serious but rare: Pneumonia, paradoxical bronchospasm, hypersensitivity reactions (including rash, angioedema), adrenal suppression.

• CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) may increase systemic exposure, elevating corticosteroid and LABA-related adverse effects.
• Beta-blockers may antagonize LABA effects and precipitate bronchospasm.
• Diuretics may potentiate hypokalemia.
• MAO inhibitors or tricyclic antidepressants may amplify cardiovascular effects of vilanterol.
• Avoid concomitant use with other LABA-containing drugs.

• GINA 2024: Endorses ICS/LABA such as vilanterol/fluticasone for asthma maintenance in moderate to severe disease.
• GOLD 2024: Supports ICS/LABA combinations for COPD patients with frequent exacerbations and eosinophilic inflammation.
• No recent major FDA or EMA changes to indications or safety profiles.

• Store at 20°C to 30°C (68°F to 86°F).
• Protect from moisture and light by keeping the inhaler in its original packaging until use.
• Do not freeze or refrigerate.
• Do not wash or immerse inhaler in water.
• Discard 6 weeks after opening or when dose counter reaches zero.
• Keep out of reach of children.