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Fluticasone

Fluticasone

Flonase Flovent Cutivate Veramyst Arnuity Ellipta Xhance

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Updated: December 06, 2025

Overview

Fluticasone is a synthetic trifluorinated glucocorticoid with potent anti-inflammatory and immunosuppressive properties. It is widely used in various formulations (nasal spray, inhaler, topical cream) to manage inflammatory conditions. The drug exhibits high receptor affinity and minimal systemic absorption when used appropriately, making it a preferred choice for long-term management of chronic inflammatory conditions. As a corticosteroid, fluticasone modulates the immune response and reduces inflammation by inhibiting multiple inflammatory cells and mediators. Its localized effects make it particularly useful for respiratory and dermatological conditions, with different formulations optimized for specific therapeutic targets.

Drug Class

Corticosteroid / Glucocorticoid receptor agonist Therapeutic categories: • Anti-inflammatory agent • Immunosuppressant • Respiratory agent • Dermatological agent

Mechanism of Action

Fluticasone binds to intracellular glucocorticoid receptors, forming a complex that translocates to the nucleus: • Inhibits phospholipase A2 production (reducing arachidonic acid metabolites) • Suppresses pro-inflammatory cytokines (IL-1, IL-2, IL-6, TNF-α) • Decreases eosinophil survival and migration • Reduces capillary permeability and mucus secretion • Upregulates anti-inflammatory proteins (lipocortin-1) This multi-target action results in reduced inflammation, swelling, and hypersensitivity reactions.

Pharmacokinetics

Absorption: • Low systemic bioavailability (inhaled: 30%, nasal: <2%, topical: <1%) • Pulmonary absorption depends on particle size and inhalation technique Distribution: • Extensive tissue distribution • 91% plasma protein bound • Volume of distribution: ~4 L/kg Metabolism: • Hepatic metabolism via CYP3A4 • Forms inactive metabolites (17β-carboxylic acid derivative) Excretion: • Primarily fecal elimination (via bile) • <5% renal excretion Half-life: • ~8 hours (route-dependent) • Longer terminal half-life with repeated dosing due to tissue retention

Pharmacodynamics

• Dose-dependent suppression of HPA axis at high systemic concentrations • Onset of action: 1-3 days (nasal), 24 hours (inhaled), 3-5 days (topical) • Maximum effect: 1-2 weeks (respiratory forms) • Reduces airway hyperresponsiveness in asthma • Decreases nasal allergen challenge response by 80-90%

Indications

• Allergic rhinitis: Management of seasonal/perennial allergic rhinitis symptoms (sneezing, rhinorrhea, nasal itching) • Asthma: Maintenance treatment for persistent asthma (all severity levels) • Atopic dermatitis/eczema: Topical treatment of inflammatory dermatoses • Chronic obstructive pulmonary disease (COPD): Maintenance treatment in combination with long-acting bronchodilators • Nasal polyps: Reduction of polyp size and associated symptoms

Contraindications

Absolute: • Hypersensitivity to fluticasone or components • Untreated localized infections (herpes simplex, fungal/bacterial) • Status asthmaticus (not for acute relief) Relative: • Active or latent tuberculosis • Ocular herpes simplex • Systemic fungal infections • Recent nasal surgery/trauma (for nasal forms)

Dosage & Administration

Allergic rhinitis (nasal spray): • Adults: 100-200 mcg/day (1-2 sprays/nostril) • Children ≥4 years: 100 mcg/day (1 spray/nostril) Asthma (inhaled): • Adults: 88-880 mcg twice daily (dose varies by device) • Children 4-11 years: 44-88 mcg twice daily Atopic dermatitis (topical): • Apply thin layer to affected area 1-2 times daily COPD (inhaled combination): • Fluticasone furoate/vilanterol 100/25 mcg once daily

Special Populations

Pediatric: • Safety established ≥4 years for nasal, ≥1 year for topical • Monitor growth velocity in chronic use Geriatric: • No dosage adjustment needed • Increased fracture risk with long-term use Renal impairment: • No significant changes required Hepatic impairment: • Use with caution (CYP3A4 metabolism) • Consider dose reduction in severe impairment

Adverse Effects

Common (>10%): • Nasal irritation/epistaxis (nasal forms) • Oral candidiasis (inhaled forms) • Headache • Skin atrophy (topical forms) Serious (<1%): • Adrenal suppression • Glaucoma/cataracts • Hypersensitivity reactions • Osteoporosis with long-term use • Growth suppression in children

Drug Interactions

• CYP3A4 inhibitors (ketoconazole, ritonavir): Increase fluticasone exposure • Live vaccines: Reduced immune response • Other corticosteroids: Additive HPA axis suppression • Beta-agonists: Synergistic bronchodilation (in combination products)

Warnings & Precautions

• May cause immunosuppression (risk of infections) • Potential for HPA axis suppression with high doses • Monitor for ocular effects (glaucoma, cataracts) • Increased mortality risk in COPD patients • Paradoxical bronchospasm possible • Withdrawal symptoms if discontinued abruptly

Pregnancy & Lactation

Pregnancy: • Category C (risk cannot be ruled out) • Use only if potential benefit justifies risk • Monitor infants for adrenal suppression Lactation: • Low systemic absorption minimizes exposure • Consider topical/nasal forms first • Monitor infant for adverse effects

Monitoring Parameters

• Growth velocity in pediatric patients • Adrenal function tests with chronic use • Bone mineral density (long-term therapy) • Intraocular pressure • Asthma control (FEV1, ACT scores) • Signs of local infection

Patient Counseling

• Demonstrate proper administration technique • Rinse mouth after inhaled use • Never exceed prescribed dose • Report vision changes or persistent sore throat • Don't stop abruptly without medical advice • Use spacer with MDI for better delivery • Clean nasal applicator regularly

Storage & Stability

• Store at 20-25°C (68-77°F) • Protect from light and moisture • Do not freeze • Discard nasal spray after 120 doses • Inhalers: Prime before first use • Topical forms: Tightly closed containers

Clinical Pearls

• Most potent inhaled corticosteroid available • Consider stepping down therapy once controlled • Use lowest effective dose to minimize side effects • Watch for candidiasis in elderly/diabetic patients • Nasal forms may take 3-4 days for full effect • Combine with saline nasal irrigation for better efficacy

References

• Lexicomp Online, Fluticasone monograph. Wolters Kluwer Clinical Drug Information, Inc. • Global Initiative for Asthma (GINA) 2023 Guidelines • FDA Prescribing Information: Flonase, Flovent • Barnes PJ. Inhaled corticosteroids. Pharmaceuticals 2010;3(3):514-540