Fluticasone Propionate Inhaled

Fluticasone propionate is a potent, highly lipophilic inhaled corticosteroid. Its oral bioavailability is under 1%, but absorption from the lung can produce systemic effects at high doses.

Classification. Inhaled corticosteroid, glucocorticoid.

Mechanism. High-affinity glucocorticoid receptor agonist suppressing eosinophilic airway inflammation.

Pharmacokinetics. Lung deposition is slow-dissolving and prolonged. Cleared by CYP3A4 with high first-pass effect. Terminal half-life about 8 hours after inhalation.

First-line, persistent asthma, adults. Low 100 to 250 micrograms daily, medium over 250 to 500 micrograms daily, high over 500 micrograms daily. Usual 100 to 250 micrograms twice daily; up to 500 micrograms twice daily; up to 1000 micrograms twice daily only under specialist direction.

First-line, combined with salmeterol. Dry powder 50/100, 50/250 or 50/500 micrograms one inhalation twice daily, or inhaler 25/50, 25/125 or 25/250 micrograms two puffs twice daily. For COPD with frequent exacerbations, 50/500 micrograms one inhalation twice daily is used where licensed.

Children 4 to 16 years. 50 to 100 micrograms twice daily by inhaler with spacer; step up under specialist direction.

Alternative. Another ICS, especially beclometasone with ritonavir-boosted regimens.

Emergency. Not used.

Titration. Step down by about 25 to 50% every 3 months once control holds. No loading dose.

Contraindications. Hypersensitivity. Use with caution in active or quiescent pulmonary tuberculosis.

Serious adverse effects. Adrenal suppression, Cushing syndrome (especially with ritonavir or cobicistat), reduced growth velocity, cataract, glaucoma, osteoporosis, pneumonia in COPD, paradoxical bronchospasm.

Common adverse effects. Oropharyngeal candidiasis, hoarseness, bruising, cough.

Interactions. Ritonavir, cobicistat, ketoconazole, itraconazole and clarithromycin markedly raise systemic exposure. Avoid the combination unless the benefit outweighs the risk, and monitor for Cushingoid effects if used.

Common prescribing errors. High-dose use with ritonavir. Using the highest strength for mild disease. Forgetting the mouth rinse and spacer.

Special groups.

• Pregnancy: acceptable if needed. Breastfeeding: compatible at usual doses.

• Children: measure height at least annually.

• Older adults: monitor bone health and eyes.

• Kidney impairment: no adjustment. Liver impairment: exposure increases in severe disease.

• East Africa: where ritonavir-boosted antiretroviral regimens are used, choose beclometasone.

Formulations. Inhaler 50, 125 and 250 micrograms/actuation; dry powder 50, 100, 250 and 500 micrograms/dose; combinations with salmeterol.

Technique. Rinse the mouth and spit. Use a spacer with the inhaler. Dry powder devices need a fast, deep inhalation.

Baseline. Spirometry or peak flow, control score, height in children.

Monitoring. Symptoms, exacerbations, spirometry, technique, height, adrenal and bone effects at high doses. Consider an emergency steroid card at 1000 micrograms daily or more.

Stop and reduce rules. Step down when control holds. Therapeutic drug monitoring is not used.

Referral and escalation. Refer when control fails or oral corticosteroids are needed repeatedly.