FLUTICASONE PROPIONATE
Clinical safety rating: safe
Animal studies have demonstrated safety
Glucocorticoid receptor agonist; binds to cytosolic glucocorticoid receptors, leading to inhibition of inflammatory mediators (e.g., cytokines, prostaglandins, leukotrienes) and suppression of immune cell activity.
| Metabolism | Hepatic via CYP3A4; undergoes extensive first-pass metabolism; main metabolite is 17β-carboxylic acid derivative (inactive). |
| Excretion | Primarily hepatic metabolism via CYP3A4 to inactive metabolites; <5% excreted unchanged in urine; biliary/fecal elimination accounts for >90% of metabolites. |
| Half-life | Terminal elimination half-life is approximately 7.8 hours after intravenous administration; extends to 10-14 hours following intranasal or inhaled routes due to slow absorption from the lung/nasal mucosa. |
| Protein binding | 99% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Approximately 4.2 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Intranasal: <2% due to mucociliary clearance and hepatic first-pass metabolism; Inhaled: approximately 15-20% reaching systemic circulation; Oral: negligible (<1%). |
| Onset of Action | Intranasal: 2-4 hours; Inhaled: 24 hours for peak effect, with some improvement noted within 12 hours. |
| Duration of Action | Intranasal: 24 hours with once-daily dosing; Inhaled: 12-24 hours, typically dosed once or twice daily. |
| Molecular Weight | 500.57 |
| Action Class | Inhaled Corticosteroid |
Inhalation: 88-440 mcg twice daily for asthma (DPI: 100-500 mcg twice daily; HFA: 44-220 mcg twice daily). Intranasal: 2 sprays (50 mcg/spray) per nostril once daily (total 200 mcg/day). Topical: Apply thin layer to affected area 1-2 times daily.
| Dosage form | OINTMENT |
| Renal impairment | No dose adjustment required. Renal impairment does not significantly alter pharmacokinetics due to minimal renal excretion. |
| Liver impairment | Use with caution in severe hepatic impairment (Child-Pugh Class C). No specific dose guidelines; monitor for systemic effects. |
| Pediatric use | Inhalation (asthma): 4-11 years: 88 mcg twice daily (DPI 100-200 mcg twice daily; HFA 88 mcg twice daily). Intranasal: 2-11 years: 1 spray (50 mcg) per nostril once daily (total 100 mcg/day). Topical: Use lowest potency formulation; apply sparingly. |
| Geriatric use | No specific dose adjustments, but initiate at lower end of dosing range and monitor for increased risk of adverse effects (e.g., adrenal suppression, osteoporosis). |
| 1st trimester | Limited human data; use only if clearly needed and potential benefit justifies potential risk to fetus. |
| 2nd trimester | No known teratogenicity; use only if clearly needed. |
| 3rd trimester | Use only if clearly needed; may cause fetal adrenal suppression if high doses used near term. |
Clinical note
Strong CYP3A4 inhibitors like ketoconazole may increase systemic exposure Rinse mouth after inhalation to prevent oral candidiasis.
| Placental transfer | Fluticasone propionate crosses the placenta; extent is limited due to high protein binding and rapid metabolism. |
| Breastfeeding | Fluticasone propionate is excreted into breast milk in low amounts; risk to infant is minimal with usual doses. Use with caution, especially with high doses or prolonged use. |
■ FDA Black Box Warning
None.
| Common Effects | COPD |
| Serious Effects | Adrenal insufficiency (with high doses or prolonged use), Increased risk of pneumonia in patients with COPD, Oropharyngeal candidiasis, Dysphonia, Paradoxical bronchospasm, Growth suppression in children, Osteoporosis with long-term use, Cataracts and glaucoma, Hypersensitivity reactions (e.g., angioedema, rash) |
Hypersensitivity to fluticasone propionate or any component of the formulationStatus asthmaticus (for immediate relief)
| Precautions | Risk of adrenal insufficiency with systemic absorption, Increased susceptibility to infections (e.g., chickenpox, measles), Potential for growth retardation in children, Oropharyngeal candidiasis with inhaled use, Monitor for glaucoma and cataracts with long-term use, Avoid in patients with active tuberculosis or untreated fungal/bacterial/viral infections |
| Food/Dietary |
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| Lactation Rating |
| L2 (Safer) |
| Teratogenic Risk | Fluticasone propionate is an inhaled corticosteroid. Data from large prospective cohort studies and meta-analyses do not indicate a significantly increased risk of major congenital malformations. In the first trimester, risk is low and no specific pattern of defects identified. Second and third trimester exposure may slightly increase risk of preterm birth and low birth weight, but underlying maternal asthma itself is a confounder. Animal studies show fetal harm only at high systemic doses. |
| Fetal Monitoring | Monitor maternal asthma control (peak expiratory flow, symptoms, rescue inhaler use). Assess fetal growth (serial ultrasound) if asthma is poorly controlled or if high doses are used for prolonged periods. No specific fetal monitoring required for fluticasone itself. |
| Fertility Effects | Fluticasone propionate at therapeutic inhaled doses is not associated with impaired fertility in humans. Animal studies at high systemic doses showed reduced fertility, but these doses far exceed clinical inhalation exposure. No clinical evidence of fertility effects in women or men. |
| No significant food interactions. Grapefruit juice may increase systemic exposure via CYP3A4 inhibition, but clinical relevance is low with inhaled/nasal use. Avoid excessive alcohol as it may worsen gastric irritation if using oral formulations (not common). |
| Clinical Pearls | For optimal efficacy in asthma, ensure proper inhaler technique and use a spacer with MDI. Rinse mouth after inhalation to reduce oropharyngeal candidiasis and dysphonia. In allergic rhinitis, counsel patients on consistent use for 1-2 weeks before maximal effect. Monitor for adrenal suppression during prolonged use or when switching from oral steroids. Abrupt discontinuation after long-term use may precipitate adrenal crisis. |
| Patient Advice | Rinse your mouth with water after each use to prevent thrush and hoarseness. · Use a spacer device if prescribed; it helps the medication reach your lungs better. · Do not stop taking this medication suddenly; consult your doctor before discontinuing. · It may take 1-2 weeks to see full benefits for nasal allergies; use regularly. · Carry a steroid warning card if you are on high doses or have been on long-term treatment. · Report any signs of infection (fever, sore throat) or vision changes (blurred vision, eye pain). |