fluticasone
inhaled corticosteroid· Brands: Flixotide, Flovent, Flutide, Arnuity ElliptaINH
Mechanism of action
Fluticasone is a synthetic corticosteroid with potent anti-inflammatory activity. It binds to the glucocorticoid receptor, modulating gene transcription to increase anti-inflammatory proteins and decrease pro-inflammatory cytokines. This reduces airway inflammation, eosinophil infiltration, and mucus secretion, and also causes vasoconstriction of bronchial vessels.
Pharmacokinetics
Fluticasone is administered by inhalation; most of the dose is swallowed, but oral bioavailability is minimal due to extensive first-pass metabolism. The fraction deposited in the lungs is absorbed systemically. It is highly lipophilic, leading to prolonged tissue retention. It is metabolised by hepatic CYP3A4 to inactive metabolites and excreted predominantly in faeces. The terminal half-life is about 8 hours for fluticasone propionate and 24 hours for fluticasone furoate.
Indications & dosing
Asthma (maintenance treatment)
Use the lowest effective dose once control is achieved. Rinse mouth after inhalation to reduce local side effects.
- adult · INH: 100–500 microgram BID · Use the lowest effective dose once control is achieved. Rinse mouth after inhalation to reduce local side effects.
Asthma (maintenance treatment)
Dose by age and severity. For children aged 1-4 years, typical dose is 50-100 micrograms twice daily.
- pediatric · INH: 50–200 microgram BID · Dose by age and severity. For children aged 1-4 years, typical dose is 50-100 micrograms twice daily.
Chronic obstructive pulmonary disease (COPD) as part of combination therapy with a long-acting beta-agonist (LABA)off-label
Fluticasone propionate alone is not licensed for COPD; use only in combination with a LABA (e.g., salmeterol).
- adult · INH: 250–500 microgram BID · Fluticasone propionate alone is not licensed for COPD; use only in combination with a LABA (e.g., salmeterol).
Contraindications & precautions
- Hypersensitivity to fluticasone or any excipient · Some formulations contain lactose, which may trigger allergic reactions in patients with severe milk protein allergy.
- Severe milk protein allergy (for preparations containing lactose) · Check the inhaler device's ingredients before prescribing.
- Advise patients to rinse mouth and gargle with water after inhalation, then spit out, to reduce the risk of oral candidiasis.
- Use the lowest effective dose to minimise systemic effects; review regularly.
- Caution during periods of stress (e.g. surgery, infection) in patients on long-term high-dose therapy due to risk of adrenal suppression.
- Avoid concomitant use of potent CYP3A4 inhibitors (e.g. ritonavir, cobicistat) unless benefit outweighs risk.
- Monitor growth in children and adolescents using inhaled corticosteroids at high doses for prolonged periods.
Adverse effects
- Oral candidiasis (thrush)
- Hoarseness or dysphonia
- Throat irritation
- Headache
- Adrenal suppression (with high doses or prolonged use)serious
- Growth retardation in children and adolescentsserious
- Pneumonia (in patients with COPD)serious
- Paradoxical bronchospasmserious
Renal & hepatic adjustment
- Hepatic impairment (mild): No dose adjustment required
- Hepatic impairment (moderate): No dose adjustment required
- Hepatic impairment (severe): Use with caution; consider dose reduction and monitor for systemic corticosteroid effects
Monitoring, pregnancy & toxicity
- Respiratory symptoms and peak expiratory flow (PEF) or spirometry · Regularly, as per asthma/COPD management plan
- Adrenal suppression (if high doses or long-term use) · Periodically, especially if concurrent systemic steroids or high-dose ICS
- Growth in children (using height velocity) · Every 6-12 months
- Oral and pharyngeal candidiasis · At each review
- Inhaler technique · At each review
- Pregnancy: Fluticasone is an inhaled corticosteroid with minimal systemic absorption. It is considered safe during pregnancy when used at the lowest effective dose to control asthma. Uncontrolled asthma poses a greater risk to mother and fetus than the use of this medication. Continue treatment for asthma control; discuss with specialist for individual management.
- Toxicity: Acute overdose: minimal systemic effects due to low bioavailability; transient adrenal suppression possible · Supportive care; monitor for signs of adrenal suppression; no specific antidote
- Toxicity: Chronic excessive use can cause systemic corticosteroid effects, including adrenal suppression, growth retardation in children, and features of Cushing's syndrome · Reduce dose gradually, monitor adrenal function, consider replacement therapy if adrenal crisis
- Toxicity: Oropharyngeal candidiasis (thrush) due to local immunosuppressive effect · Rinse mouth after inhalation; topical antifungal treatment; review inhaler technique
Clinical notes
Fluticasone is a first-line therapy for persistent asthma and is also used in COPD. It should be used regularly to achieve anti-inflammatory control, not as a reliever. Patients should rinse their mouth after inhalation to prevent oral candidiasis. Systemic absorption is low, but adrenal suppression and growth retardation can occur with high doses, especially in children. Doses should be titrated to the lowest effective dose, and therapy should be reviewed regularly.
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BNF; local formulary