XHANCE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XHANCE (XHANCE).
XHANCE (fluticasone propionate) is an anti-inflammatory corticosteroid that inhibits multiple inflammatory cell types and mediators (e.g., histamine, leukotrienes, cytokines) involved in nasal and sinus inflammation. It reduces nasal polyp size and nasal congestion.
| Metabolism | Fluticasone propionate is metabolized primarily by cytochrome P450 3A4 (CYP3A4) to an inactive carboxylic acid metabolite. |
| Excretion | Primarily hepatic metabolism; renal excretion of metabolites accounts for <10% of the dose as unchanged drug; fecal excretion is minimal. |
| Half-life | Terminal half-life is approximately 2-3 hours; short half-life supports twice-daily dosing for sustained local effect. |
| Protein binding | Approximately 99% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is approximately 0.7 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Intranasal: systemic bioavailability is approximately 5-10% due to extensive first-pass metabolism; local nasal bioavailability is high. |
| Onset of Action | Intranasal: clinical effect (reduction in nasal congestion) observed within 12 hours of first dose. |
| Duration of Action | Intranasal: duration of clinical effect is approximately 12 hours; consistent with twice-daily dosing regimen. |
| Molecular Weight | 500.57 |
1 spray (93 mcg fluticasone propionate) per nostril twice daily (total daily dose 372 mcg). Intranasal route.
| Dosage form | SPRAY, METERED |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No specific guidelines; caution in severe hepatic impairment due to potential increased systemic exposure. |
| Pediatric use | Not approved for pediatric patients aged <18 years; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment; use with caution due to potential increased sensitivity. |
| 1st trimester | Insufficient human data; based on animal studies, there is no evidence of teratogenicity. Use only if potential benefit justifies risk. |
| 2nd trimester | Insufficient human data; use only if clearly needed. |
| 3rd trimester | Insufficient human data; use only if clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for XHANCE (XHANCE).
| Placental transfer | Unknown in humans; fluticasone propionate crosses placenta in animal studies. |
| Breastfeeding | No human data available. Fluticasone propionate is excreted in rat milk at low concentrations. Consider risk-benefit. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to fluticasone propionate or any excipientUntreated nasal mucosal infectionsRecent nasal surgery or trauma
| Precautions | Risk of HPA axis suppression with prolonged or high-dose use, Increased susceptibility to infections (e.g., chickenpox, measles) due to immunosuppression, Potential for growth suppression in children (though not indicated for pediatric use), Local nasal effects: epistaxis, nasal septal perforation, Candida albicans infection, Impaired wound healing after nasal surgery, Glaucoma and cataracts with prolonged use |
| Food/Dietary | No known food interactions. Avoid grapefruit products if taking with systemic corticosteroids; not specifically contraindicated with XHANCE. |
Loading safety data…
| L3 |
| Teratogenic Risk | XHANCE (fluticasone propionate) is an intranasal corticosteroid. In animal reproduction studies, fluticasone propionate caused teratogenic effects (cleft palate, skeletal abnormalities) at subcutaneous doses 1-5 times the maximum recommended human daily intranasal dose (MRHDID) in mice and 5 times in rats, but no teratogenic effects were observed in rabbits at 2.5 times MRHDID. However, there are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, XHANCE should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Systemic absorption after intranasal administration is minimal, reducing fetal exposure. First trimester risk is unknown; second and third trimester risks are low based on minimal systemic bioavailability. |
| Fetal Monitoring | No specific maternal or fetal monitoring is routinely required for intranasal fluticasone propionate during pregnancy. However, standard prenatal care should include monitoring of fetal growth and development, especially if the patient uses other corticosteroids concurrently. In animal studies, high systemic doses were associated with fetal growth restriction; thus, in cases of prolonged or high-dose use, consider periodic fetal ultrasound to assess growth. |
| Fertility Effects | There is no known effect of intranasal fluticasone propionate on human fertility. In animal studies, fluticasone propionate had no adverse effects on fertility in rats at subcutaneous doses up to 50 mcg/kg/day (approximately 1.5 times MRHDID based on body surface area). No human data are available. |
| Clinical Pearls | XHANCE (fluticasone propionate and oxymetazoline) is an intranasal spray indicated for chronic rhinosinusitis with nasal polyps. The unique exhalation delivery system delivers drug to the sinonasal cavities. Prime device before first use or after 14 days of non-use. Use only in patients ≥18 years. Monitor for nasal bleeding and adrenal insufficiency with prolonged use. |
| Patient Advice | Shake the bottle gently before each use. · Exhale into the mouthpiece to activate drug delivery, not inhale. · Prime device by actuating into the air until fine mist appears. · Use at regular intervals; do not exceed 2 sprays per nostril twice daily. · Do not share the device with others. · Clean the device weekly according to instructions. · Avoid use with other intranasal steroids or decongestants without consulting physician. · Report persistent nasal bleeding or white patches in the nose. |