fluticasone propionate
Brand: Flovent, Flonase
Prototype Drug
Drug Class: inhaled corticosteroid
Drug Family: corticosteroid
Subclass: glucocorticoid receptor agonist
Organ Systems: respiratoryimmunology
Mechanism of Action
Inhaled synthetic glucocorticoid with high local potency and low systemic bioavailability; binds GR reducing transcription of inflammatory cytokines; suppresses eosinophilic airway inflammation.
glucocorticoid receptor (GR)
Indications
- asthma maintenance (ICS — first-line)
- allergic rhinitis (nasal spray)
- COPD with frequent exacerbations (combined with LABA)
Contraindications
- active pulmonary infection (TB, fungal)
- hypersensitivity
Adverse Effects
Common
- oropharyngeal candidiasis
- dysphonia
- HPA axis suppression (high doses)
- growth suppression in children (high doses)
Serious
- adrenal crisis (abrupt withdrawal after prolonged use)
- paradoxical bronchospasm
- cataracts and glaucoma (long-term high doses)
Pharmacokinetics (ADME)
| Absorption | inhaled: <1% systemic (extensive first-pass in GI/liver); intranasal: low systemic |
| Distribution | high local tissue binding |
| Metabolism | extensive hepatic CYP3A4 to inactive 17β-carboxylic acid |
| Excretion | fecal ~87%, renal |
| Half-life | ~3-10 hours (inhaled) |
| Onset | minutes (local); hours (anti-inflammatory onset days) |
| Peak | 1-3 hours |
| Duration | 24 hours |
| Protein Binding | 91% |
| Vd | low systemic |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| strong CYP3A4 inhibitors (ritonavir, itraconazole) | systemic fluticasone levels increase — adrenal suppression, Cushing risk | major |
Nursing Considerations
- Rinse mouth and gargle after EVERY use (prevents oral candidiasis and dysphonia)
- Anti-inflammatory effect: days to weeks — not for acute bronchospasm
- Use lowest effective dose in children to minimize growth suppression
- GINA: ICS is cornerstone of asthma management in all but mildest disease
- HPA axis suppression with systemic absorption — do not abruptly discontinue after prolonged high-dose use
Clinical Pearls
- First-line controller for asthma: suppresses eosinophilic inflammation, reduces exacerbations and mortality
- Oral candidiasis: Candida colonizes with inhaled steroid — spacer and mouth rinse are preventive
Safety Profile
Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Not required
TDM Not required
Guideline Update pending
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.