DYMISTA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for DYMISTA (DYMISTA).
Azelastine is a histamine H1-receptor antagonist; fluticasone propionate is a corticosteroid with anti-inflammatory activity. The combination reduces nasal symptoms by blocking histamine receptors and inhibiting inflammatory mediators.
| Metabolism | Azelastine: metabolized primarily by CYP3A4 and to a lesser extent by CYP2D6 and CYP1A2; fluticasone propionate: metabolized by CYP3A4. |
| Excretion | Azelastine: ~75% renal (primarily as parent and metabolites), ~25% fecal. Fluticasone propionate: <5% renal, >95% fecal as parent and metabolites. |
| Half-life | Azelastine: terminal half-life ~22 hours (plasma) with long-lasting antihistamine effect. Fluticasone propionate: terminal half-life ~7.8 hours (intravenous), but intranasal systemic exposure is very low. |
| Protein binding | Azelastine: ~88% bound to plasma proteins (primarily albumin). Fluticasone propionate: ~91% bound to plasma proteins (primarily albumin). |
| Volume of Distribution | Azelastine: Vd ~14.5 L/kg (extensive tissue distribution). Fluticasone propionate: Vd ~4.2 L/kg (moderate distribution due to high lipophilicity). |
| Bioavailability | Intranasal: Azelastine ~40% (due to absorption), fluticasone propionate <1% (due to extensive first-pass metabolism and low absorption). |
| Onset of Action | Intranasal: Azelastine provides relief of nasal symptoms within 15 minutes; fluticasone propionate typically requires several days of regular use for maximal effect, though some relief may occur within 12 hours. |
| Duration of Action | Azelastine: antihistamine effect lasts up to 12 hours, supporting twice-daily dosing. Fluticasone propionate: anti-inflammatory effect persists for 24 hours with once-daily dosing. |
One spray (137 mcg azelastine hydrochloride/50 mcg fluticasone propionate) per nostril twice daily, intranasal.
| Dosage form | SPRAY, METERED |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | Contraindicated in patients with severe hepatic impairment (Child-Pugh class C). Use with caution in moderate impairment (Child-Pugh class B). |
| Pediatric use | Approved for children ≥6 years: One spray per nostril twice daily. Weight-based dosing not established. |
| Geriatric use | No specific dose adjustment needed, but monitor for adverse effects due to potential increased systemic exposure. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for DYMISTA (DYMISTA).
| Breastfeeding | Unknown if azelastine or fluticasone are excreted in human milk. M/P ratio not determined. Caution advised; use only if clearly needed. |
| Teratogenic Risk | Pregnancy Category C. First trimester: No adequate human studies; animal studies show azelastine and fluticasone propionate have no major teratogenic effects at clinically relevant doses. Second and third trimesters: No known fetal risks, but use only if benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to any component of the formulation"]
| Precautions | ["Epistaxis","Nasal ulceration","Nasal candidiasis","Hypothalamic-pituitary-adrenal (HPA) axis suppression with higher doses","Immunosuppression and increased risk of infections"] |
Loading safety data…
| No routine monitoring required beyond standard prenatal care. Observe for intranasal side effects (epistaxis, nasal irritation). |
| Fertility Effects | No human data. Animal studies: Azelastine had no effect on fertility; fluticasone propionate at high subcutaneous doses caused reduced fertility in rats. |