Usage
Fluticasone furoate + vilanterol is prescribed for the maintenance treatment of asthma in patients aged 5 years and older, and for the treatment and prevention of exacerbations of chronic obstructive pulmonary disease (COPD) in adults. It is not for the relief of acute bronchospasm or acute asthma attacks.
Its pharmacological classifications are:
- Corticosteroid (Fluticasone furoate)
- Long-acting beta2-adrenergic agonist (LABA) (Vilanterol)
Mechanism of Action: Fluticasone furoate reduces airway inflammation by binding to glucocorticoid receptors. Vilanterol relaxes airway smooth muscle by binding to beta2-adrenergic receptors, leading to bronchodilation.
Alternate Names
Fluticasone furoate/vilanterol trifenatate.
Brand Name: Breo Ellipta, Relvar Ellipta.
How It Works
Pharmacodynamics: Fluticasone furoate exerts its anti-inflammatory effects by binding to glucocorticoid receptors in the cytoplasm of airway cells. This interaction leads to the modulation of gene transcription, inhibiting the production of inflammatory mediators and reducing airway inflammation. Vilanterol binds to beta2-adrenergic receptors on airway smooth muscle, activating adenylate cyclase and increasing intracellular cyclic AMP levels. This process results in smooth muscle relaxation and bronchodilation.
Pharmacokinetics:
- Absorption: Both drugs are absorbed through the lungs after inhalation.
- Metabolism: Fluticasone furoate is primarily metabolized by CYP3A4. Vilanterol is also metabolized by CYP3A4, with minor contributions from CYP2D6.
- Elimination: Primarily through feces.
Mode of Action: Fluticasone furoate modulates gene expression to suppress inflammation. Vilanterol activates beta2-adrenergic receptors to relax bronchial smooth muscle.
Receptor Binding: Fluticasone furoate binds to glucocorticoid receptors. Vilanterol binds to beta2-adrenergic receptors.
Elimination Pathways: Primarily hepatic metabolism and fecal excretion.
Dosage
Standard Dosage
Adults:
- Asthma: Breo Ellipta 100/25 mcg or 200/25 mcg, one inhalation once daily.
- COPD: Breo Ellipta 100/25 mcg, one inhalation once daily.
Children:
- Asthma (5-11 years): Breo Ellipta 50/25 mcg, one inhalation once daily.
- Asthma (12-17 years): Breo Ellipta 100/25 mcg, one inhalation once daily.
- COPD: Not recommended.
Special Cases:
- Elderly Patients: No dose adjustment is typically required.
- Patients with Renal Impairment: No dose adjustment is required.
- Patients with Hepatic Dysfunction: Caution is advised. For moderate to severe hepatic impairment, the lower strength of Relvar Ellipta (92/22 mcg) is recommended.
- Patients with Comorbid Conditions: Close monitoring may be necessary.
Clinical Use Cases
Fluticasone furoate/vilanterol is not indicated for:
- Intubation
- Surgical Procedures
- Mechanical Ventilation
- Intensive Care Unit (ICU) Use
- Emergency Situations
Dosage Adjustments
Dose adjustments may be necessary in patients with hepatic impairment or those taking strong CYP3A4 inhibitors.
Side Effects
Common Side Effects
Headache, upper respiratory tract infection, runny nose, sore throat, oral candidiasis (thrush), back pain, cough, joint pain, influenza, fever.
Rare but Serious Side Effects
Worsening of breathing problems, allergic reactions (rash, hives, swelling), cardiovascular effects (chest pain, palpitations, increased blood pressure), pneumonia, low adrenal gland function, high blood sugar.
Long-Term Effects
Reduced growth in children, glaucoma, cataracts, osteoporosis, immunosuppression.
Adverse Drug Reactions (ADR)
Severe allergic reactions, paradoxical bronchospasm, cardiac arrhythmias.
Contraindications
Hypersensitivity to fluticasone furoate, vilanterol, or any of the excipients. Primary treatment of status asthmaticus or other acute episodes of COPD or asthma where intensive measures are required.
Drug Interactions
- Strong CYP3A4 Inhibitors: Can increase systemic exposure to fluticasone furoate.
- Long-acting beta2-agonists: Concurrent use is contraindicated.
- Beta-blockers: Can antagonize the bronchodilatory effects of vilanterol.
- MAOIs and TCAs: Can potentiate cardiovascular effects.
- Diuretics: Can potentiate hypokalemia.
Pregnancy and Breastfeeding
- Pregnancy: Use only if the potential benefit outweighs the potential risk to the fetus. Not assigned to a US FDA pregnancy category.
- Breastfeeding: Caution is recommended. Limited data available.
Drug Profile Summary
- Mechanism of Action: Fluticasone furoate: anti-inflammatory (corticosteroid); Vilanterol: bronchodilator (LABA).
- Side Effects: Headache, upper respiratory tract infection, oral candidiasis, etc. Serious: worsening breathing, allergic reactions, cardiovascular effects.
- Contraindications: Hypersensitivity, acute asthma or COPD exacerbations.
- Drug Interactions: Strong CYP3A4 inhibitors, other LABAs, beta-blockers.
- Pregnancy & Breastfeeding: Limited data, use with caution if benefits outweigh risks.
- Dosage: Asthma (Adults): 100/25 mcg or 200/25 mcg once daily; COPD (Adults): 100/25 mcg once daily. Pediatric dosing available.
- Monitoring Parameters: Lung function, blood pressure, potassium levels, blood glucose, growth in children, eye examinations.
Popular Combinations
Fluticasone furoate/vilanterol is itself a combination product. It is not typically combined with other long-acting inhaled bronchodilators.
Precautions
- Monitor for adverse effects, especially in patients with comorbidities.
- Regular monitoring of lung function, growth in children (if applicable), and eye exams may be necessary.
- Avoid use in acute exacerbations.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Fluticasone Furoate + Vilanterol?
A: See dosage section above.
Q2: Can Fluticasone Furoate + Vilanterol be used as a rescue inhaler?
A: No. It is for maintenance treatment only and should not be used to relieve acute symptoms.
Q3: What are the common side effects?
A: Common side effects include headache, upper respiratory tract infection, runny nose, sore throat, and oral candidiasis.
Q4: What are the serious side effects?
A: Serious side effects can include worsening of breathing problems, allergic reactions, cardiovascular effects, and pneumonia.
Q5: Can this medication be used during pregnancy?
A: It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Q6: What are the drug interactions I should be aware of?
A: Significant interactions can occur with strong CYP3A4 inhibitors, other long-acting beta2-agonists, and beta-blockers.
Q7: What should I advise patients with hepatic impairment?
A: Patients with moderate to severe hepatic impairment should use the lower strength formulation and be monitored closely.
Q8: How should patients administer this medication?
A: The medication is administered by oral inhalation using the Ellipta inhaler once daily. Patients should be instructed on proper inhaler technique.
Q9: Should patients rinse their mouth after using the inhaler?
A: Yes, rinsing the mouth with water after each inhalation can help prevent oral candidiasis (thrush).
Q10: Can patients with COPD use the same dose as patients with asthma?
A: The recommended dose for COPD is Breo Ellipta 100/25 mcg once daily. Asthma patients may require the 200/25 mcg dose.
