FLONASE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FLONASE (FLONASE).
Fluticasone propionate is a corticosteroid that binds to glucocorticoid receptors, inhibiting inflammatory mediators such as cytokines, leukotrienes, and prostaglandins, thereby reducing nasal inflammation.
| Metabolism | Primarily metabolized by CYP3A4 in the liver; extensive first-pass metabolism via hydrolysis to an inactive metabolite. |
| Excretion | Primarily hepatic metabolism (CYP3A4), with metabolites excreted in feces (approximately 87-90%) and urine (<5% unchanged). Less than 5% of a dose is excreted renally as unchanged drug. |
| Half-life | Terminal elimination half-life is approximately 3 hours (range 2-4 hours). This short half-life supports twice-daily dosing for systemic effects; however, intranasal administration achieves local therapeutic concentrations with minimal systemic exposure. |
| Protein binding | Approximately 99% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 4.2 L/kg (range 3.7-5.0 L/kg), indicating extensive tissue distribution. This high Vd suggests wide distribution into peripheral tissues. |
| Bioavailability | Intranasal: Systemic bioavailability is less than 2% due to extensive first-pass metabolism. Oral: Approximately 1-2% due to first-pass metabolism; not available as oral formulation. No IV formulation available. |
| Onset of Action | Intranasal: Symptom relief begins within 12 hours, with maximum benefit observed after several days of regular use. Not effective for immediate relief of acute symptoms. |
| Duration of Action | Duration of action is approximately 24 hours after achieving steady-state (typically after 3-4 days of twice-daily dosing). Clinical effect is sustained with regular use; intermittent dosing may not maintain efficacy. |
2 sprays (50 mcg/spray) per nostril once daily; may increase to 2 sprays per nostril twice daily if needed. Intranasal route.
| Dosage form | SPRAY, METERED |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Children 4-11 years: 1 spray (50 mcg) per nostril once daily; Children 12 years and older: same as adult. |
| Geriatric use | No specific dose adjustment; use with caution due to potential increased systemic exposure. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FLONASE (FLONASE).
| Breastfeeding | It is not known whether fluticasone propionate is excreted in human breast milk. After intranasal administration, systemic concentrations are low, and it is unlikely to be present in breast milk in clinically significant amounts. The M/P ratio is not available. However, caution should be exercised when administering to nursing mothers. The benefits of breastfeeding and the mother's need for the drug should be weighed against potential risks to the infant. |
| Teratogenic Risk | Fluticasone propionate, the active ingredient in FLONASE, is classified as FDA Pregnancy Category C. In animal studies, corticosteroids have been shown to be teratogenic at high systemic doses. However, the intranasal route results in minimal systemic absorption. For first trimester, the risk is considered low but not zero based on epidemiological data. Second and third trimester use is generally safe, but caution is advised as systemic corticosteroids may increase risk of maternal hypertension and gestational diabetes. Overall, fluticasone propionate is preferred over oral corticosteroids for asthma/allergic rhinitis during pregnancy. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to any component of the formulation","Untreated fungal, bacterial, or viral nasal infections"]
| Precautions | ["May cause nasal septal perforation or epistaxis","Risk of adrenal suppression with prolonged high-dose use","Caution in patients with recent nasal mucosal trauma or surgery","Avoid in patients with untreated local infections"] |
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| Fetal Monitoring | No specific maternal or fetal monitoring is required beyond routine prenatal care. However, if high doses are used or if the patient is using other corticosteroids, monitor for signs of adrenal suppression, maternal hypertension, or hyperglycemia. In asthmatic patients, monitor asthma control and fetal growth if systemic corticosteroids are also used. |
| Fertility Effects | There are no known adverse effects of intranasal fluticasone on human fertility. Animal studies did not show impairment of fertility at doses several times the maximum human daily intranasal dose. However, systemic corticosteroids may affect ovulation; this is unlikely with intranasal administration due to low systemic absorption. |