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Pharmacology · Inhaled corticosteroids

Fluticasone !

A potent inhaled corticosteroid for asthma and, in combinations, COPD. Almost none of the swallowed drug reaches the blood.

Updated 2026-11-01

Also called: Fluticasone propionate, Fluticasone furoate

The figure shows fluticasone furoate bound to the human glucocorticoid receptor ligand-binding domain; fluticasone propionate is another ester of the same steroid and uses the same pocket.

Target in 3D: Glucocorticoid receptor. PDB structure 3CLD (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Fluticasone binds the glucocorticoid receptor with very high affinity. The receptor moves to the nucleus, blocks inflammatory transcription factors and switches on anti-inflammatory genes, lowering airway eosinophils, mast cells and cytokines. Oral bioavailability is negligible because the swallowed drug is poorly absorbed and destroyed on first pass, so systemic effects come mainly from the part absorbed through the lung.

  1. Fluticasone binds the glucocorticoid receptor with high affinity
  2. The receptor blocks inflammatory transcription factors in the nucleus
  3. Airway eosinophils and cytokines fall
  4. Asthma control improves and exacerbations decrease

Pharmacokinetics

Absorption
Swallowed drug has negligible oral bioavailability; the lung fraction is absorbed
Metabolism
In the liver by CYP3A4 to an almost inactive metabolite
Elimination
Mainly in the faeces
Half-life
About 8 hours after intravenous dosing

Indications

Adverse effects

Common

  • Oral thrush
  • Hoarseness (dysphonia) and throat irritation
  • Upper respiratory infection and sinusitis
  • Cough and headache

Contraindications

  • Primary treatment of status asthmaticus or acute attacks needing intensive measures
  • Hypersensitivity to any ingredient

Key interactions

Ritonavir and other strong CYP3A4 inhibitors (ketoconazole)
Large rise in fluticasone levels, with Cushing syndrome and adrenal suppression; the combination is not recommended

What is monitored

  • Asthma control and reliever use
  • Mouth for thrush
  • Growth in children; bone density and eyes with long use
  • Signs of hypercortisolism in patients on CYP3A4 inhibitors

Administration and safety

  • Oral inhalation by pressurised inhaler or dry powder inhaler; the pressurised inhaler is shaken and can be used with a spacer, especially in young children
  • After each use the mouth is rinsed with water and the water spat out
  • The medicine list is checked for ritonavir and azole antifungals before starting

Nursing care

  • Check inhaler technique and spacer use
  • Look at the mouth for thrush and ask about hoarseness
  • Ask about HIV medicines and antifungals; watch for moon face, weight gain or weakness
  • In COPD, watch for fever, cough or sputum changes (pneumonia)

Pregnancy and breastfeeding

Human data with inhaled fluticasone are limited; poorly controlled asthma raises the risk of preeclampsia and prematurity, so control is the aim.

Test yourself

Think of the answer, then tap the question to see it.

Why does swallowed fluticasone hardly reach the blood?

Its oral bioavailability is negligible: poor gut absorption plus extensive first-pass metabolism by CYP3A4.

A patient on ritonavir-boosted HIV therapy develops Cushing features while using a steroid inhaler. Which inhaler is the classic culprit?

Fluticasone: ritonavir blocks its CYP3A4 metabolism, raising systemic levels and suppressing the adrenals.

What is the main extra risk of inhaled fluticasone in COPD?

Pneumonia.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: DailyMed - FLUTICASONE PROPIONATE HFA- fluticasone propionate aerosol, metered (DailyMed (U.S. National Library of Medicine), 2023); Fluticasone inhalers: medicine to treat asthma and COPD - NHS (NHS, 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.