FLOVENT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FLOVENT (FLOVENT).
Fluticasone propionate is a synthetic corticosteroid with anti-inflammatory activity. It binds to the glucocorticoid receptor, leading to inhibition of pro-inflammatory transcription factors (e.g., NF-κB) and increased synthesis of lipocortin-1, which reduces phospholipase A2 activity and subsequent release of arachidonic acid metabolites (prostaglandins, leukotrienes). In the lungs, it decreases airway inflammation by reducing eosinophil infiltration, mast cell degranulation, and cytokine release.
| Metabolism | Hepatic metabolism primarily via cytochrome P450 enzyme CYP3A4 to an inactive metabolite (17β-carboxylic acid derivative). First-pass metabolism is extensive, resulting in low systemic bioavailability after intranasal and inhaled administration. |
| Excretion | Primarily hepatic metabolism (CYP3A4) with fecal excretion of metabolites; renal excretion accounts for <5% of the dose as unchanged drug and metabolites combined. |
| Half-life | Approximately 14.4 hours (range 7.8–24.6 hours) for the inhaled route; supports twice-daily dosing; prolonged in hepatic impairment. |
| Protein binding | Approximately 91% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | At steady state, Vd is approximately 3.7 L/kg (range 2.0–5.6 L/kg), indicating extensive tissue distribution. |
| Bioavailability | Inhaled: Approximately 20% reaches systemic circulation (orally inhaled fluticasone propionate absolute bioavailability ~13.5% from the Diskus device); oral bioavailability is <1% due to extensive first-pass metabolism. |
| Onset of Action | Inhaled: 12–24 hours for initial bronchodilator effect; maximal improvement may require 1–2 weeks of regular use. |
| Duration of Action | Approximately 12 hours after inhalation; allows twice-daily dosing for maintenance therapy; not indicated for acute bronchospasm. |
| Molecular Weight | 500.57 |
| Action Class | Corticosteroid |
Inhalation aerosol: 88-880 mcg twice daily; typical starting dose: 88 mcg twice daily. Max: 880 mcg twice daily. Oral inhalation powder: 100-1000 mcg twice daily; typical starting: 100 mcg twice daily. Max: 1000 mcg twice daily.
| Dosage form | POWDER |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Children 4-11 years: Inhalation aerosol 88 mcg twice daily; max 88 mcg twice daily. Children 12 years and older: same as adult dosing. |
| Geriatric use | No specific dose adjustment; use lowest effective dose due to potential for increased systemic effects. |
| 1st trimester | No adequate studies in pregnant women; use only if potential benefit justifies risk. Inhaled corticosteroids are preferred for asthma control. Animal studies show some risk but human data limited. |
| 2nd trimester | Similar to first trimester; inhaled corticosteroids are generally considered safe and preferred over oral corticosteroids. Monitor for maternal glucose intolerance. |
| 3rd trimester | No known fetal harm from inhaled corticosteroids; however, avoid high doses. Use lowest effective dose. |
Clinical note
Comprehensive clinical and safety monograph for FLOVENT (FLOVENT).
| Placental transfer | Placental transfer occurs; animal studies show transfer. In humans, limited data suggest minimal systemic absorption after inhaled doses, but transfer cannot be excluded. |
| Breastfeeding | Fluticasone propionate is excreted in breast milk, but concentrations are likely low after inhaled doses. Use with caution; consider the benefits of breastfeeding and the mother's need for asthma control. Monitor infant for potential adverse effects. |
■ FDA Black Box Warning
None
| Common Effects | Headache, Throat irritation, Hoarseness, Cough, Oral thrush, Nausea |
| Serious Effects | Adrenal suppression, Growth retardation in children, Osteoporosis, Cataracts, Glaucoma, Increased risk of pneumonia in patients with COPD, Oropharyngeal candidiasis, Paradoxical bronchospasm |
Primary treatment of status asthmaticusHypersensitivity to fluticasone propionate or any excipients
| Precautions | Risk of adrenal suppression, especially with higher doses or prolonged use; patients may require dose adjustment during stress. Increased risk of pneumonia in patients with COPD. Oropharyngeal candidiasis and hoarseness (local effects). Monitor for growth velocity in children. Avoid abrupt discontinuation in asthma; use with caution in patients with active or quiescent tuberculosis, ocular herpes simplex, or untreated fungal/bacterial infections. Systemic corticosteroid therapy should be tapered when transitioning to inhaled fluticasone. |
Loading safety data…
| Lactation Rating | L3 - Probably Compatible |
| Teratogenic Risk | Fluticasone propionate (FLOVENT) is classified as Pregnancy Category C. Inhaled corticosteroids are generally considered low risk during pregnancy. No adequate and well-controlled studies in pregnant women. Animal studies showed fetal toxicity at high systemic exposures, but inhaled use minimizes systemic absorption. First trimester: no increased risk of major congenital malformations reported in human studies. Second and third trimesters: monitor for potential fetal adrenal suppression with prolonged high-dose use, though rare. Overall, benefits typically outweigh risks for asthma control. |
| Fetal Monitoring | Maternal: Monitor asthma symptoms, peak expiratory flow, and lung function regularly. Assess for oral candidiasis and hoarseness. Fetal: Standard prenatal monitoring including ultrasound for growth and well-being. No specific fetal monitoring required beyond routine care, but assess for possible fetal adrenal suppression with prolonged high-dose use (rare). |
| Fertility Effects | No known adverse effects on fertility in humans based on available data. Animal studies showed no impairment of fertility at inhaled doses. Asthma control itself may improve fertility outcomes by reducing hypoxia and systemic inflammation. |
| Food/Dietary |
| No clinically significant food interactions with Flovent. Avoid grapefruit and grapefruit juice only if directed by a prescriber due to potential mild CYP3A4 inhibition (though clinically insignificant with inhaled route). |
| Clinical Pearls | Fluticasone propionate (FLOVENT) is an inhaled corticosteroid (ICS) used for maintenance therapy of asthma, not for acute exacerbations. For optimal deposition, patients should shake the inhaler well before each use, exhale fully, then inhale slowly and deeply (for HFA) or rapidly and deeply (for Diskus). Rinse mouth with water (do not swallow) after each dose to reduce oropharyngeal candidiasis and dysphonia. Dosing should be titrated to the lowest effective dose to minimize systemic effects. Use with caution in patients with active or quiescent tuberculosis, untreated fungal/bacterial infections, or ocular herpes simplex. |
| Patient Advice | Use Flovent exactly as prescribed: it is a controller medication, not a rescue inhaler for sudden breathing problems. · Rinse your mouth with water after each use (do not swallow) to prevent thrush (white patches in mouth) and hoarseness. · Do not stop using Flovent suddenly; it may worsen asthma. Always have a rescue inhaler (e.g., albuterol) available. · If you experience worsening of asthma symptoms (e.g., increased wheezing, shortness of breath) or need more rescue inhaler than usual, contact your healthcare provider immediately. · Store Flovent at room temperature away from moisture and heat. Do not puncture or incinerate the canister (HFA). |