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Sunday, July 27, 2025

Fluticasone nasal spray and drops


Fluticasone nasal spray and drops are intranasal corticosteroid formulations containing fluticasone propionate or fluticasone furoate, designed for local anti-inflammatory treatment of nasal and sinus conditions. These preparations are considered first-line therapy for allergic and non-allergic rhinitis, nasal polyps, and chronic rhinosinusitis. Their mechanism of action, localized effects, and minimal systemic absorption make them highly effective for long-term management of upper airway inflammation.

Pharmacological Classification

  • Class: Topical corticosteroid (intranasal)

  • ATC Code: R01AD08 (Fluticasone propionate), R01AD12 (Fluticasone furoate)

  • Formulations:

    • Nasal spray (fluticasone propionate 50 mcg/dose)

    • Nasal spray (fluticasone furoate 27.5 mcg/dose)

    • Nasal drops (rare; used for polyps or ENT-guided procedures)

  • Common brand names:

    • Fluticasone propionate: Flixonase®, Flonase®, Nasofan®, Pirinase®

    • Fluticasone furoate: Avamys®, Veramyst®

Mechanism of Action

Fluticasone is a synthetic glucocorticoid with potent anti-inflammatory action. When administered intranasally, it:

  • Inhibits cytokine and mediator release from mast cells, eosinophils, basophils, neutrophils

  • Suppresses vascular permeability, edema, and leukocyte migration

  • Reduces histamine release and hyperresponsiveness

  • Decreases nasal mucosal swelling, congestion, sneezing, itching, and rhinorrhea

The onset of action begins within 12 hours, but peak effect may take 3–7 days of continuous use.

Therapeutic Indications

Approved Uses

  • Seasonal allergic rhinitis (hay fever)

  • Perennial allergic rhinitis

  • Non-allergic (vasomotor) rhinitis

  • Nasal polyposis

  • Chronic rhinosinusitis (with or without nasal polyps)

  • Prevention of nasal symptoms of allergy

Off-Label or Specialist Uses

  • Eustachian tube dysfunction

  • Post-nasal drip

  • Rhinosinusitis-related facial pressure

  • Adjunct to systemic steroids or biologics in chronic rhinosinusitis with polyps (CRSwNP)

Dosage and Administration

Adults and Adolescents (≥12 years)

  • Fluticasone propionate nasal spray:

    • 2 sprays per nostril once daily (total 200 mcg/day)

    • Maintenance: 1 spray per nostril once daily

  • Fluticasone furoate (Avamys):

    • 2 sprays per nostril once daily (110 mcg/day)

    • Maintenance: 1 spray per nostril once daily

Children (4–11 years)

  • Fluticasone propionate:

    • 1 spray per nostril once daily (100 mcg/day)

  • Fluticasone furoate:

    • 1 spray per nostril once daily (55 mcg/day)

Nasal Drops (Specialist Use Only)

  • Usually used for nasal polyps, often administered head down and forward to reach the upper nasal cavity

  • Dosage: 400 mcg/day, typically 10 drops (400 mcg) once daily

  • Duration: Typically limited to 4–6 weeks under ENT supervision

Pharmacokinetics

  • Bioavailability: <1% due to extensive first-pass metabolism and low systemic absorption

  • Metabolism: Hepatic (CYP3A4-mediated)

  • Excretion: Primarily in feces via bile

  • Systemic activity is negligible when used appropriately

Contraindications

  • Hypersensitivity to fluticasone or any excipients

  • Recent nasal surgery or trauma (until healing has occurred)

  • Untreated localized infections in the nasal mucosa (e.g., herpes simplex, tuberculosis)

Precautions and Warnings

Local effects

  • Epistaxis (especially with long-term use or incorrect technique)

  • Nasal septal perforation (rare; due to chronic trauma or poor technique)

  • Nasal or throat irritation

  • Candida albicans infection in the nasal passages or pharynx

Systemic risks

  • Suppression of hypothalamic-pituitary-adrenal (HPA) axis (rare with proper intranasal use)

  • Growth suppression in children has been reported with prolonged high-dose use

  • Glaucoma and cataracts (with prolonged or excessive use)

Technique-dependent efficacy

  • Inadequate spray technique reduces effectiveness and increases side effect risk

  • Avoid direct spray onto nasal septum

Side Effects

Common

  • Nasal irritation

  • Dryness of nasal mucosa

  • Mild epistaxis (nosebleeds)

  • Unpleasant taste or smell

  • Headache

Less Common

  • Nasal septal perforation

  • Pharyngitis

  • Oral or nasal Candida infections

Rare/Systemic

  • Hypersensitivity reactions (urticaria, angioedema)

  • Systemic corticosteroid effects (Cushingoid features, adrenal suppression)

  • Growth retardation (pediatric)

Drug Interactions

  • CYP3A4 inhibitors (e.g., ritonavir, ketoconazole, itraconazole) may increase systemic fluticasone levels, especially if used concurrently with inhaled or topical fluticasone

  • Avoid combining multiple corticosteroid formulations unless necessary and supervised

  • Minimal interactions when used locally at recommended doses

Use in Special Populations

Pregnancy

  • Considered low risk due to minimal systemic absorption

  • Use the lowest effective dose under medical guidance

Lactation

  • Compatible with breastfeeding; systemic absorption is minimal

Pediatrics

  • Approved in children ≥4 years (some products for ≥2 years)

  • Long-term use may affect growth: monitor height periodically

Elderly

  • No special precautions; generally well-tolerated

Patient Instructions and Counseling

  • Shake the bottle well before each use

  • Clear the nose before spraying

  • Direct spray away from the nasal septum

  • Prime the spray before first use or after long storage

  • Use daily, even if symptoms are absent (for seasonal prevention)

  • Relief begins in 12–24 hours, full benefit after 3–5 days

  • Avoid blowing nose immediately after spraying

  • Do not exceed prescribed dose

Comparison: Fluticasone Propionate vs Fluticasone Furoate

  • Furoate has greater glucocorticoid receptor affinity and longer half-life → once-daily dosing

  • Propionate is often more widely available and less expensive

  • Both are similarly effective in allergic rhinitis

  • Furoate (Avamys) has a more ergonomic applicator and is odorless and alcohol-free

Clinical Notes

  • First-line for allergic rhinitis, especially in moderate-to-severe disease

  • More effective than oral antihistamines for nasal congestion

  • Can be used with oral antihistamines or leukotriene receptor antagonists

  • Nasal decongestants (e.g., oxymetazoline) may be used briefly before starting fluticasone to relieve blockage and improve steroid delivery

Storage and Shelf-life

  • Store at room temperature

  • Do not freeze

  • Discard after 2 months of opening (product-specific)

  • Keep nozzle clean to avoid clogging and contamination



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