azelastine/fluticasone intranasal (Dymista)
Dosing and uses of Dymista (azelastine/fluticasone intranasal)
Adult dosage forms and strengths
azelastine/fluticasone
nasal spray
- (137mcg/50mcg)/spray
Seasonal Allergic Rhinitis
1 spray per nostril BId
Administration
Administer by intranasal route only
Shake bottle gently prior to each use
Prime the bottle before initial use by releasing 6 sprays or more until a fine mist sprays
Reprime the bottle if unused for >14 days by spraying once or more until fine mist appears
Pediatric dosage forms and strengths
azelastine/fluticasone
nasal spray
- (137mcg/50mcg)/spray
Seasonal Allergic Rhinitis
<6 years: Safety and efficacy not established
≥6 years: 1 spray per nostril BId
Administration
Administer by intranasal route only
Shake bottle gently prior to each use
Prime the bottle before initial use by releasing 6 sprays or more until a fine mist sprays
Reprime the bottle if unused for >14 days by spraying once or more until fine mist appears
Geriatric dosage forms and strengths
Seasonal allergic rhinitis: Clinical trials did not include sufficient numbers of patients older than 65 years to determine whether they respond differently from younger patients
Initiate at low end of dosing range and exercise caution
Dymista (azelastine/fluticasone intranasal) adverse (side) effects
1-10%
Dysgeusia (4%)
Headache (2%)
Epistaxis (2%)
Frequency not defined
Somnolence
Nasal effects (eg, nasal ulceration, nasal septal perforation)
Impaired wound healing
Candida albicans infection
Glaucoma
Cataracts
Immunosuppression
Hypothalamic-pituitary-adrenal (HPA) axis suppression
Warnings
Contraindications
None
Cautions
For intranasal use only
Avoid spraying directly into eyes; if drug is sprayed into eyes, flush with water for a minimum of 10 minutes
May cause somnolence; avoid operating heavy machinery or engaging in tasks that require mental alertness and coordination
Do not use with history of recent nasal ulcers, nasal surgery, or any nasal trauma
May cause glaucoma or cataracts
As corticosteroids may cause immunosuppression, patients should notify healthcare providers if they experience any symptoms of tuberculosis, viral, bacterial, fungal or parasitic infections or ocular herpes simplex
Due to the potential reduction in growth velocity in children, patients must be monitored routinely
Pregnancy and lactation
Pregnancy category: C
Lactation: Unknown whether distributed in breast milk, exercise caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Dymista (azelastine/fluticasone intranasal)
Mechanism of action
Azelastine: Phthalazinones derivative; elicits histamine H1-receptor antagonist activity; major metabolite (desmethylazelastine) also exhibits histamine H1-receptor antagonist activity
Fluticasone: Corticosteroid possessing anti-inflammatory activity; exact mechanism of action unknown, but shown to exhibit anti-inflammatory effect on multiple cells (eg, neutrophils, eosinophils, macrophages, mast cells, lymphocytes) and mediators (eg, histamine, leukotrienes, cytokines and eicosanoids)
Absorption
Bioavailability: azelastine (40%); fluticasone (44-61% higher than fluticasone alone)
Peak Plasma Time: azelastine (0.5 hr); fluticasone (1 hr)
Peak Plasma Concentration: azelastine (194.5 pg/mL); fluticasone 10.3 pg/mL
AUC: azelastine (4217 pg/mL•hr); fluticasone (97.7 pg/mL•hr)
Distribution
Protein Bound: azelastine hydrochloride (88%), desmethylazelastine (97%)
Vd: azelastine (14.5 L/kg)
Metabolism
Metabolism: azelastine (CYP450 enzyme system [specific enzyme unknown]), fluticasone (CYP3A4)
Elimination
Half-life: azelastine (25 hours), fluticasone (7.8 hours)
Excretion: azelastine (feces 75%); fluticasone (urine <5%, feces >95%)
