Overview
Fluticasone is a synthetic corticosteroid with potent anti-inflammatory and immunosuppressive properties, primarily used in respiratory conditions. It has high glucocorticoid receptor affinity and undergoes extensive first-pass metabolism when administered orally, making it suitable for topical use in asthma and allergic rhinitis with minimal systemic absorption.
Mechanism of Action
Fluticasone binds to glucocorticoid receptors, inhibiting the production of inflammatory mediators (cytokines, leukotrienes, prostaglandins) and reducing infiltration of inflammatory cells (eosinophils, mast cells). It also enhances the expression of anti-inflammatory proteins while suppressing genes encoding pro-inflammatory proteins.
Indications
- Asthma (maintenance treatment)
- Allergic rhinitis
- Chronic obstructive pulmonary disease (COPD) maintenance
- Atopic dermatitis (topical formulation)
- Nasal polyps
Dosage
Asthma (inhalation): Adults: 100-1000 mcg twice daily; Children (4+ years): 50-200 mcg twice daily. Allergic rhinitis (nasal spray): Adults: 2 sprays (100 mcg) per nostril once daily; Children (4+ years): 1 spray (50 mcg) per nostril once daily. Dosage should be individualized based on severity and response.
Contraindications
- Hypersensitivity to fluticasone or any component
- Primary treatment of status asthmaticus or acute bronchospasm
- Untreated fungal, bacterial, or viral respiratory infections
- Active or quiescent tuberculosis
Side Effects
- Headache
- Nasal irritation or epistaxis (nasal spray)
- Oral candidiasis (inhaled)
- Hoarseness or throat irritation
- Cough
- Nausea
- Adrenal suppression (with high doses)
- Growth retardation in children
- Increased intraocular pressure
Interactions
- Strong CYP3A4 inhibitors (ketoconazole, ritonavir) increase fluticasone exposure
- Other corticosteroids may increase systemic effects
- May reduce efficacy of vaccines (avoid live vaccines)