Fluticasone

Corticosteroid, Glucocorticoid, Inhaled corticosteroid (ICS)

Fluticasone

Flonase (intranasal, OTC); Flovent (inhaled, asthma); Cutivate (topical)

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Summary

Classes

Corticosteroid, Glucocorticoid, Inhaled corticosteroid (ICS)

Common uses

Asthma controller▲0▼, Allergic rhinitis▲0▼, COPD▲0▼, Inflammatory dermatoses (topical)▲0▼

Pharmacy

Starting dose

Inhaled (Flovent HFA) 88 mcg BID; intranasal (Flonase) 2 sprays/nostril daily; topical (Cutivate) 0.05% cream BID

Preparations

Inhaled MDI 44/110/220 mcg per actuation; DPI (Diskus) 50/100/250 mcg; nasal spray 50 mcg/actuation; cream/ointment 0.005%, 0.05%

US FDA Max

ICS 880 mcg/d (asthma); intranasal 200 mcg/d

Pharmacology

Routes

Inhaled, intranasal, topical

Onset

Inhaled: bronchial effect 1-2 weeks; nasal: symptom relief 12-24 hours; topical: hours

Duration

12-24 hours per dose

Half-life

~7.8 hours (fluticasone propionate, inhaled systemic exposure)

Bioavailability

<1% oral (extensive first-pass via CYP3A4); ~30% inhaled lung deposition

Pregnancy

Inhaled and intranasal generally considered safe; widely used in asthma in pregnancy.^{[citation needed]}

Legal status

OTC (intranasal Flonase) and Rx-only (inhaled, topical) in US

Purported mechanism

Fluticasone is a potent topical glucocorticoid receptor agonist designed for high local receptor affinity and extensive hepatic first-pass to minimize systemic glucocorticoid exposure.▲0▼ Suppresses inflammatory gene transcription (NF-κB, AP-1), induces lipocortin, downregulates mast cells and eosinophils. CYP3A4 substrate; strong CYP3A4 inhibitors (ritonavir, ketoconazole) can raise systemic levels enough to produce iatrogenic Cushing's.