Fluticasone nasal

Fluticasone nasal

Generic Name

Fluticasone nasal

Mechanism

  • Glucocorticoid receptor agonism → formation of a receptor‑ligand complex that translocates to the nucleus.
  • Modulates gene transcription:
  • Up‑regulates anti‑inflammatory proteins (e.g., lipocortin‑1).
  • Down‑regulates pro‑inflammatory cytokines (IL‑4, IL‑5, IL‑13), chemokines (MCP‑1), and eosinophil‐activating factors.
  • Inhibits mast‑cell degranulation and reduces the recruitment of eosinophils & neutrophils to the nasal mucosa.
  • Suppresses the late‑phase allergic response, leading to decreased nasal congestion, rhinorrhea, and pruritus.

Pharmacokinetics

ParameterTypical value (nasal spray)
Oral bioavailability<0.1 % (due to extensive first‑pass metabolism)
Systemic absorption<0.7 µg/day (minimal, ~1 % of dose)
Half‑life13–15 h systemic; nasal residence time ~24 h
MetabolismHepatic CYP3A4 → inactive metabolites (e.g., 3‑OH‑fluticasone)
ExcretionFecal (biliary) ≥ 90 % and urinary 10–20 %

*Key point*: The intranasal route yields high local concentrations with negligible systemic exposure, minimizing endocrine and immunosuppressive side effects.

Indications

  • Allergic rhinitis (seasonal or perennial) – improves symptom control in adults and adolescents ≥ 12 y.
  • Chronic rhinosinusitis with nasal polyps – reduces polyp size and improves airflow.
  • Non‑allergic rhinitis (e.g., vasomotor) – evidence for symptom containment in selected patients.
  • Adjunct to intranasal antihistamine for refractory chronic rhinitis.

Contraindications

  • Contraindications
  • Known hypersensitivity to fluticasone or any component.
  • Uncontrolled systemic fungal infections of the respiratory tract.
  • Warnings & Precautions
  • Use with caution in patients on systemic CYP3A4 inhibitors (ketoconazole, ritonavir) to reduce metabolism and risk of systemic absorption.
  • Rare occurrence of nasal septal perforation in long‑term use; monitor for nasal crusting or septal pain.
  • Not advised in patients with pediatric < 4 y due to lack of safety data.
  • Avoid concurrent use with other topical steroids in same area to prevent cumulative iatrogenic effects.

Dosing

  • Adults & Adolescents (≥ 12 y)
  • *Typical*: 1–2 sprays (40 µg per spray) into each nostril once daily.
  • *Maximum*: 4 sprays per nostril per day or 80 µg/day.
  • Children (4–11 y)
  • *Typical*: 1 spray (40 µg) per nostril twice daily.
  • Administration technique
  • Tilt head forward, gently blow nose to clear mucosa.
  • Shake bottle, place tip against one nostril, inhale gently while spraying.
  • Switch nostrils after each spray; do not aspirate or speak during administration.
  • On alternate days, consider double‑dose (4 sprays) for breakthrough symptoms.

Adverse Effects

CategoryCommon (≤ 5 %)Serious (≤ 1 %)
LocalNasal irritation, burning, crusting, epistaxisSeptal perforation, nasal septal necrosis
SystemicOral candidiasis, mild HPA axis suppressionSuppressed adrenal function (report), cough, upper‑respiratory infection

*Mitigation*: Lidocaine spray or saline rinse before use to reduce irritation; antifungal rinses (nystatin) for persistent candidiasis.

Monitoring

  • Clinical response: Symptom diary, nasal endoscopy (for polyps) at baseline and 4–6 weeks.
  • Adrenal axis: Consider baseline morning cortisol if > 6 months therapy expected, especially in patients on systemic steroids.
  • Nasal mucosa: Inspect for septal perforation or ulceration at follow‑up visits.
  • Serum potassium: For patients on concurrent ACE inhibitors/ARBs (rare mineralocorticoid effect).

Clinical Pearls

1. Bioavailability ≈ 1 % – enables high local potency with virtually no systemic effects, a major advantage over oral steroids.

2. “Bio‑dice” rule – Scale dose by patient’s age & polyp burden: children receive  10 mg/day.”

8. Checking patient’s technique – 5–10 % of patients misuse spray; provide visual‑audio instruction, especially in pediatrics.

9. Avoid over‑inflation – Over‑dose > 80 µg/day increases risk of septal perforation; educate patients on “one-too‑few” principle.

10. Advancing to biologics – In uncontrolled CRSwNP after ≥ 12 wk of fluticasone + oral systemic steroids, consider A2AR (dupilumab) or anti‑IL‑5 therapy.

--
References *(for quick consultation)*

1. FDA Label – Fluticasone Propionate Nasal Spray.

2. American Academy of Otolaryngology‑Head & Neck Surgery Guidelines, 2023.

3. Smart RCTs – Combined Antihistamine‑Corticosteroid Therapy.

4. Emanouchi et al., *Journal of Allergy & Clinical Immunology*, 2022 – Candidiasis mitigation.

5. Rosen et al., *Clinical Endocrinology*, 2021 – Adrenal suppression risk assessment.

Medical & AI Content Disclaimers
Medical Disclaimer: Medical definitions are provided for educational purposes and should not replace professional medical advice, diagnosis, or treatment.

AI Content Disclaimer: Some definitions may be AI-generated and may contain inaccuracies. Always verify with authoritative medical references.

Scroll to Top