Generic Name

Fluticasone

Mechanism

• Fluticasone (high‑potency inhaled glucocorticoid)
• Binds glucocorticoid receptors → transcriptional activation/repression of inflammatory genes.
• Reduces cytokine production (IL‑4, IL‑5, IL‑13), eosinophil recruitment, and vascular permeability.
• Dampens airway hyperresponsiveness and mucus hypersecretion.
• Salmeterol (selective β₂‑adrenergic agonist)
• Activates Gs protein → ↑cAMP → smooth‑muscle relaxation.
• Provides bronchodilation with a duration of ≈12 h.
• The combined effect yields synergistic control of inflammation and bronchoconstriction, improving lung function and reducing exacerbations.

Pharmacokinetics

Indications

• Asthma:
• Maintenance therapy for patients ≥12 yrs or children 4–11 yrs (dose‑adjusted).
• Replacement for oral prednisone in flare‑up management.
• Chronic Obstructive Pulmonary Disease (COPD):
• Maintenance bronchodilation and exacerbation reduction in moderate–severe COPD (≥12 yrs).
• Allergic Rhinitis (in certain formulations, e.g., Seretide Rine).

Contraindications

• Allergy to fluticasone, salmeterol, or any excipients.
• Uncontrolled infections (e.g., tuberculosis).
• Active upper respiratory tract infection – risk of worsening.
• Pregnancy: Classified as category C; use only if benefits outweigh risks, with minimal systemic absorption.
• Pediatric: Use with caution; monitor growth and adrenal axis.

Warnings
• Systemic glucocorticoid side effects (HPA suppression, Cushingoid appearance).
• Immunosuppression → opportunistic infections (e.g., fungal).
• Potential for tachyphylaxis if used as rescue inhaler.
• Hyperglycemia in susceptible patients (especially with concurrent oral steroids).

Dosing

* Children 4–11 yrs: 1 puff BID (100/50 mcg).
• Use after rinsing mouth and tongue unless inhaled with a spacer.
• Do not use as a rescue inhaler; rescue requires short‑acting β₂ agonist (SABA).
• Adjust dose up to a maximum of 2 puffs (500/50 mcg) BID for severe asthma/COPD.

Adverse Effects

Common (≥1 % incidence)
• Oral candidiasis (thrush).
• Hoarseness, cough, sore throat.
• Headache, dizziness.
• Nasopharyngitis.

Serious (rare)
• Systemic adrenal suppression (Cushingoid features, HPA axis inhibition).
• Ocular effects (glaucoma, cataract, increased intra‑ocular pressure).
• Severe hypersensitivity (anaphylaxis).
• Fungal infections (aspergillosis, candidiasis).
• Exacerbation of heart failure (rare).

Monitoring

• Pulmonary Function (spirometry): FEV₁, peak flow at least every 3 months.
• Growth (children): Height and weight ≤ every 6 months.
• Adrenal Axis: Morning cortisol if systemic exposure suspected (>10 %).
• Infection signs: Frequent sore throat, cough, and oral thrush.
• Blood pressure & glucose: For patients with comorbid conditions.

Clinical Pearls

• Spacers or nebulizers significantly improve drug delivery to the lungs and reduce local side effects.
• Mouthwash after inhalation (alcohol‑free) lowers thrush risk; repeat 3–4 × daily in children.
• Dose titration: Start low, increase slowly; avoid abrupt discontinuation to prevent adrenal crisis.
• Combination vs. monotherapy: For patients with uncontrolled asthma on single‑class therapy, add the LABA component only if the patient meets criteria for combination therapy (e.g., persistent symptoms).
• Avoid using the LABA alone for acute bronchospasm; always pair with an inhaled steroid for safety.
• Pregnancy: Use the lowest effective dose; alternatives include short‑acting β₂ agonists or leukotriene modifiers if corticosteroid exposure is a concern.
• Elderly patients: Monitor for cardiovascular events; consider lower starting doses.
• Drug interactions: Strong CYP3A4 inhibitors (ketoconazole, clarithromycin) can increase systemic fluticasone levels; monitor and adjust if needed.

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• References:

1. Global Initiative for Asthma (GINA) 2025 guideline update.

2. U.S. FDA prescribing information for Advair Diskus and Seretide Turbuhaler.

3. Pharmacology Textbook, 12th ed., L. J. Katz, 2021.