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Sunday, July 27, 2025

Fluticasone inhalers


Fluticasone inhalers are a class of prescription medications used in the management of asthma and chronic obstructive pulmonary disease (COPD). These inhalers contain either fluticasone propionate or fluticasone furoate, both of which are synthetic inhaled corticosteroids (ICS). Their primary function is to reduce airway inflammation, control respiratory symptoms, and prevent exacerbations of chronic respiratory conditions. Fluticasone is not a bronchodilator and must not be used for the relief of acute symptoms.

Pharmacological Classification

  • Drug class: Inhaled corticosteroid (ICS)

  • Therapeutic category: Anti-asthmatic, COPD maintenance

  • ATC codes: R03BA05 (Fluticasone propionate), R03BA08 (Fluticasone furoate)

  • Routes of administration: Inhalation via pressurized metered-dose inhalers (pMDI), dry powder inhalers (DPI), or breath-actuated devices

Mechanism of Action

Fluticasone, upon inhalation, exerts anti-inflammatory effects in the lungs by:

  • Inhibiting recruitment and activation of inflammatory cells (e.g., eosinophils, mast cells, T-lymphocytes)

  • Suppressing the synthesis and release of pro-inflammatory cytokines, histamines, and leukotrienes

  • Reducing capillary leakage and mucosal edema

  • Inhibiting airway hyperresponsiveness

This leads to improved airflow, decreased bronchial inflammation, and reduced airway remodeling over time.

Formulations and Brands

Fluticasone Propionate (FP) Inhalers

  • Brands: Flixotide®, Flovent®, Seretide® (when combined with salmeterol)

  • Available devices:

    • Metered-dose inhalers (MDIs)

    • Diskus (DPI)

    • Evohaler (pMDI)

Fluticasone Furoate (FF) Inhalers

  • Brands: Arnuity Ellipta®, Relvar Ellipta® (when combined with vilanterol)

  • Devices:

    • Ellipta DPI (dry powder inhaler)

Available Strengths

  • Propionate: 50 mcg, 100 mcg, 125 mcg, 250 mcg, 500 mcg per inhalation

  • Furoate: 100 mcg, 200 mcg per inhalation (Ellipta device)

Therapeutic Indications

Asthma (Maintenance Therapy)

  • Mild to severe persistent asthma in adults and children

  • Used regularly to prevent symptoms such as wheezing, coughing, and shortness of breath

  • Not for rapid symptom relief

Chronic Obstructive Pulmonary Disease (COPD)

  • Moderate to severe COPD (usually in combination with long-acting bronchodilators)

  • Reduces frequency of exacerbations

Other Uses (Specialist guidance)

  • Eosinophilic airway inflammation

  • Steroid-responsive non-infectious bronchitis

  • Asthma with allergic rhinitis (when combined with nasal corticosteroids)

Dosage and Administration

Asthma (Adults)

  • Mild: 100–250 mcg twice daily

  • Moderate: 250–500 mcg twice daily

  • Severe: 500–1000 mcg twice daily (max dose under supervision)

COPD (Adults)

  • Typically 250 mcg fluticasone propionate twice daily in combination with LABA (e.g., salmeterol)

  • Fluticasone furoate (100–200 mcg once daily) with vilanterol in COPD

Pediatrics

  • Children (4–11 years): 50–100 mcg twice daily (FP only)

  • Not all strengths are suitable for children; consult specific product labeling

Administration Notes

  • Inhale deeply using correct inhaler technique

  • Rinse mouth and gargle with water after use to reduce risk of oral candidiasis

  • Clean inhaler mouthpiece weekly

Contraindications

  • Hypersensitivity to fluticasone or formulation ingredients

  • Status asthmaticus or acute bronchospasm requiring rapid bronchodilation

  • Inhalation not suitable in patients unable to coordinate actuation and inhalation (use spacer or breath-actuated device)

Warnings and Precautions

Risk of Systemic Effects

Although systemic bioavailability is low, high-dose or prolonged use can result in:

  • Adrenal suppression

  • Cushing’s syndrome-like effects

  • Growth retardation in children

  • Bone mineral density reduction

  • Cataracts or glaucoma

Local Effects

  • Oral candidiasis (thrush)

  • Dysphonia (hoarseness)

  • Cough and throat irritation

Infections

  • May increase risk of pneumonia in COPD patients

  • Monitor for tuberculosis reactivation or fungal infection

Adverse Effects

Very Common

  • Oral thrush

  • Hoarseness

  • Headache (especially with FF inhalers)

Common

  • Cough, sore throat, nasal congestion

  • Dysphonia

  • Upper respiratory tract infections

  • Pneumonia (especially in COPD)

Rare

  • Allergic reactions, rash, urticaria

  • Adrenal insufficiency with long-term use

  • Eye disorders (glaucoma, cataract)

  • Behavioral changes in children (e.g., irritability, hyperactivity)

Drug Interactions

  • Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) increase systemic fluticasone levels, potentially causing adrenal suppression

  • Other corticosteroids (systemic or nasal) may have additive effects

  • Beta-agonists: Often co-prescribed for bronchodilation (e.g., salmeterol or vilanterol)

Comparison of Fluticasone Propionate vs Fluticasone Furoate

  • Fluticasone furoate has longer lung retention and requires once-daily dosing, improving adherence

  • Fluticasone propionate is well established with more available dosing flexibility

  • Furoate is considered slightly more potent on a microgram-per-microgram basis due to higher receptor affinity and prolonged tissue activity

  • Both are equally effective when dosed appropriately

Use in Special Populations

Pregnancy

  • Generally considered safe; use lowest effective dose

  • Extensive data supports its use in asthma management during pregnancy

Lactation

  • Low systemic absorption → low risk to nursing infant

  • Monitor infant for adrenal suppression if mother uses high doses

Pediatrics

  • Use lowest effective dose

  • Monitor for growth velocity in long-term treatment

Geriatrics

  • Increased risk of osteoporosis and pneumonia

  • Dose adjustment may not be required, but monitor closely

Patient Counseling Points

  • This is a controller, not a reliever inhaler—carry a short-acting beta agonist (e.g., salbutamol) for acute symptoms

  • Use inhaler daily at the same time, even if asymptomatic

  • Rinse mouth after each use to prevent fungal infection

  • Learn and practice correct inhaler technique

  • Do not stop abruptly; consult physician before dose adjustment

  • Track symptom control, peak flow, and adherence regularly

  • Store device in a dry place, away from direct heat

Storage

  • Store at room temperature, away from heat and moisture

  • Keep cap tightly closed

  • Do not puncture or incinerate pressurized containers

Alternatives

  • Other ICS: Budesonide, Beclometasone, Mometasone, Ciclesonide

  • Combination inhalers: ICS + LABA (e.g., Fluticasone/Salmeterol, Budesonide/Formoterol)

  • ICS + LABA + LAMA (for severe COPD): e.g., Trelegy Ellipta (Fluticasone furoate/Vilanterol/Umeclidinium)

Clinical Guidelines

  • GINA (Global Initiative for Asthma) recommends ICS as foundational therapy starting from step 2

  • GOLD guidelines endorse ICS/LABA in patients with COPD who have exacerbations and eosinophilic inflammation

  • In asthma, stepping up or down corticosteroid dose depends on symptom control, exacerbation history, and lung function




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