FLOVENT DISKUS 100
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FLOVENT DISKUS 100 (FLOVENT DISKUS 100).
Fluticasone propionate is a synthetic trifluorinated corticosteroid with potent anti-inflammatory activity. It binds to the glucocorticoid receptor, leading to inhibition of inflammatory mediators such as cytokines, leukotrienes, and prostaglandins. It reduces airway hyperresponsiveness and suppresses eosinophil activity.
| Metabolism | Primarily hepatic via cytochrome P450 3A4 (CYP3A4). Metabolized to inactive metabolites. |
| Excretion | Fluticasone propionate is primarily eliminated via hepatic metabolism (CYP3A4) with less than 5% of a dose excreted unchanged in urine. Fecal excretion accounts for approximately 90% of the absorbed dose (as metabolites). Biliary elimination is minimal. |
| Half-life | The terminal elimination half-life of fluticasone propionate is approximately 7.8 hours (range 5-11 hours) following inhalation. This supports twice-daily dosing, though the therapeutic effect is driven by local lung retention rather than systemic half-life. |
| Protein binding | Fluticasone propionate is 91% bound to plasma proteins, primarily to albumin and alpha-1-acid glycoprotein. Binding is linear over the therapeutic concentration range. |
| Volume of Distribution | The volume of distribution at steady state is approximately 4.2 L/kg (range 3-6 L/kg), indicating extensive tissue distribution. This large Vd reflects high lipophilicity and binding to lung tissue, contributing to prolonged local retention. |
| Bioavailability | The absolute bioavailability of inhaled fluticasone propionate from FLOVENT DISKUS is approximately 13.9% of the nominal dose, with most of the drug swallowed and undergoing first-pass hepatic metabolism, resulting in negligible oral bioavailability (<1%). The lung-deposited fraction is about 13-17% of the metered dose. |
| Onset of Action | Clinical onset of action for FLOVENT DISKUS 100 (fluticasone propionate 100 mcg) occurs within 24 hours of initial inhalation, with significant improvement in peak expiratory flow seen by 2-7 days. Maximal benefit is achieved after 1-2 weeks of regular use. |
| Duration of Action | The clinical duration of action is approximately 12 hours, supporting twice-daily administration. However, for asthma control, regular dosing is required; acute bronchodilator effects are not expected due to its anti-inflammatory mechanism. |
| Molecular Weight | 500.57 |
| Action Class | Corticosteroid (inhaled) |
100 mcg inhaled orally twice daily
| Dosage form | POWDER |
| Renal impairment | No adjustment required |
| Liver impairment | No adjustment required |
| Pediatric use | Children 4-11 years: 50-100 mcg inhaled orally twice daily; Children 12+ years: adult dosing |
| Geriatric use | No specific adjustment; use lowest effective dose due to potential for increased systemic exposure |
| 1st trimester | Use only if clearly needed; limited human data, animal studies show no risk. |
| 2nd trimester | Use only if clearly needed; no known risk in human pregnancy. |
| 3rd trimester | Use only if clearly needed; potential risk of neonatal adrenal suppression if used in high doses. |
Clinical note
Comprehensive clinical and safety monograph for FLOVENT DISKUS 100 (FLOVENT DISKUS 100).
| Placental transfer | Crosses placenta; newborn serum concentrations approximately 38% of maternal after IV administration; limited data for inhaled route. |
| Breastfeeding | Fluticasone propionate is excreted in human breast milk at low levels; risk to infant is likely minimal with maternal inhaled doses. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Common Effects | Headache, Throat irritation, Hoarseness (dysphonia), Cough, Nausea and vomiting, Upper respiratory tract infection |
| Serious Effects | Adrenal insufficiency (with prolonged use or high doses), Increased risk of pneumonia in patients with COPD, Oropharyngeal candidiasis, Paradoxical bronchospasm, Growth suppression in children, Glaucoma and cataracts (with long-term use), Osteoporosis (with long-term use) |
Status asthmaticusPrimary treatment of acute asthma exacerbationHypersensitivity to fluticasone propionate or any excipient
| Precautions | Not indicated for relief of acute bronchospasm, Risk of adrenal insufficiency during and after withdrawal from systemic corticosteroids, Increased susceptibility to infections; avoid exposure to chickenpox or measles, Potential for systemic corticosteroid effects such as hypercorticism and HPA axis suppression at high doses, Paradoxical bronchospasm may occur; discontinue if immediate wheezing occurs, Monitor for eosinophilic conditions (e.g., Churg-Strauss syndrome) during reduction of oral corticosteroids, May cause reduction in growth velocity in children, monitor growth regularly |
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| Teratogenic Risk | Insufficient human data; animal studies show no teratogenic effects at inhaled doses. Risk cannot be excluded; use only if benefit outweighs risk. No known fetal risks in any trimester. |
| Fetal Monitoring | Monitor maternal asthma control and fetal growth; no specific fetal monitoring required beyond routine prenatal care. |
| Fertility Effects | No known adverse effects on fertility in animal studies; human data lacking. |
| Food/Dietary | No significant food interactions. Grapefruit juice does not affect fluticasone. |
| Clinical Pearls | Fluticasone propionate via Diskus is a dry powder inhaler (DPI) for maintenance therapy of asthma, not for acute attacks. Rinse mouth after each use to prevent oral candidiasis and dysphonia. Dose counter indicates remaining doses; discard after reaching zero or 6 weeks after opening pouch. Titrate to lowest effective dose for long-term control. |
| Patient Advice | Use every day as prescribed, even if you feel well. · Do not use for sudden breathing problems; have a rescue inhaler (e.g., albuterol) available. · Rinse mouth with water (do not swallow) after each use to prevent thrush. |