FLUNISOLIDE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FLUNISOLIDE (FLUNISOLIDE).
Corticosteroid with anti-inflammatory action; inhibits release of inflammatory mediators (e.g., histamine, leukotrienes), reduces eosinophil migration, and stabilizes mast cells. Suppresses cytokine production and adhesion molecule expression.
| Metabolism | Primarily hepatic via CYP3A4; also metabolized by other CYP450 enzymes. Undergoes first-pass metabolism. |
| Excretion | Renal (50%) as metabolites, fecal (40%) as metabolites via bile, <5% unchanged in urine. |
| Half-life | Terminal elimination half-life is 1.8 hours (range 1.3–2.5 h) after intravenous administration; clinically, endogenous suppression persists up to 24 h post-inhalation. |
| Protein binding | Approximately 40% bound to plasma proteins (albumin); metabolites may have lower binding. |
| Volume of Distribution | Approximately 1.8 L/kg (range 1.3–2.5 L/kg), indicating extensive tissue distribution. |
| Bioavailability | Intranasal: <50% (due to mucociliary clearance and minimal absorption; systemic bioavailability ~21%). Oral inhalation: Not indicated; swallowed portion has ~20% oral bioavailability due to first-pass metabolism. |
| Onset of Action | Intranasal: 2–3 hours (relief of nasal symptoms). Oral inhalation: not applicable (primarily intranasal use). |
| Duration of Action | Intranasal: 12–24 hours (once-daily dosing for maintenance; may require twice-daily dosing initially). |
| Molecular Weight | 434.5 |
50 mcg per nostril twice daily (total daily dose 200 mcg), via nasal spray.
| Dosage form | SPRAY, METERED |
| Renal impairment | No adjustment required; flunisolide is primarily hepatically cleared. |
| Liver impairment | No specific guidelines; use caution in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Children 6-14 years: 50 mcg per nostril twice daily (total daily dose 200 mcg). Children <6 years: not recommended. |
| Geriatric use | No specific dose adjustment; use lowest effective dose due to potential increased sensitivity. |
| 1st trimester | Limited human data; generally avoided unless benefit outweighs risk. Animal studies show some adverse effects at high doses. |
| 2nd trimester | Limited human data; use only if clearly needed. No well-controlled studies. |
| 3rd trimester | Limited human data; use only if clearly needed. Potential for adrenal suppression in neonate if used near term. |
Clinical note
Comprehensive clinical and safety monograph for FLUNISOLIDE (FLUNISOLIDE).
| Placental transfer | Unknown; likely minimal due to low systemic absorption after intranasal administration. |
| Breastfeeding | Minimal excretion into breast milk expected due to low systemic bioavailability; however, use with caution, especially with high doses or prolonged treatment. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to flunisolide or any component of the formulationUntreated nasal mucosal infectionsRecent nasal surgery or nasal trauma (until healing)
| Precautions | May cause growth retardation in children, Risk of adrenal suppression with prolonged use, Increased risk of nasal septal perforation and Candida infections, May mask signs of infection, Avoid use in patients with active tuberculosis or untreated fungal/bacterial/viral infections |
| Food/Dietary | No significant food interactions; grapefruit juice does not affect flunisolide due to low systemic absorption. |
| Clinical Pearls |
Loading safety data…
| L3: Limited Data - Probably Compatible |
| Teratogenic Risk | Flunisolide is an inhaled corticosteroid. Data on use in pregnant women are limited but suggest low risk. Systemic absorption is minimal, and no increased risk of major congenital malformations has been reported. However, animal studies at high doses have shown fetal harm. First trimester: No specific pattern; background risk. Second/third trimester: Potential for fetal growth restriction with prolonged high-dose systemic exposure, but minimal with inhaled route. Avoid excessive doses. |
| Fetal Monitoring | No specific monitoring required, but assess asthma control regularly. Monitor fetal growth if high-dose or prolonged use. In cases of poor asthma control, consider pulmonary function tests. |
| Fertility Effects | No known effect on fertility in humans. In animal studies, no impairment was observed. |
| Flunisolide is a synthetic corticosteroid used intranasally for allergic rhinitis; onset of action is 3-7 days; maximum benefit may require 2-3 weeks; use with caution in patients with nasal septal ulcers, recent nasal surgery, or trauma; avoid concurrent use with other intranasal corticosteroids; may cause adrenal suppression at high doses or prolonged use; monitor for growth suppression in children. |
| Patient Advice | Do not use for acute asthma attacks; it is for maintenance therapy only. · Use regularly as prescribed; do not increase dose or frequency without consulting your doctor. · Rinse the applicator after each use to prevent clogging. · Avoid spraying into the eyes; if contact occurs, rinse with water. · Report signs of nasal infection (e.g., pain, crusting, bleeding) or vision changes. · Shake the bottle gently before each use. · Clear nasal passages before administration. · Avoid alcohol and tobacco which may reduce efficacy. |