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. |
| Molecular Weight | 381.89 |
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 | Insufficient human data; animal studies show no teratogenic effects at low doses, but high doses may cause fetal loss. Use only if benefit outweighs risk, as azelastine/fluticasone are generally avoided in first trimester unless necessary. |
| 2nd trimester | No adequate human studies; animal studies not conclusive. Generally considered safe if benefits outweigh risks, but caution advised. |
| 3rd trimester | No reported adverse fetal effects; however, high systemic absorption may cause theoretical risk. Use with caution near term due to potential for fluticasone-related adrenal suppression in neonate. |
Clinical note
Comprehensive clinical and safety monograph for DYMISTA (DYMISTA).
| Placental transfer | Both components cross the placenta; fluticasone propionate demonstrates high placental transfer in animal studies with fetal concentrations up to 30% of maternal; azelastine also crosses with unknown degree in humans. |
| Breastfeeding |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to azelastine, fluticasone, or any excipientsStatus asthmaticusAcute bronchospasm
| Precautions | Epistaxis, Nasal ulceration, Nasal candidiasis, Hypothalamic-pituitary-adrenal (HPA) axis suppression with higher doses, Immunosuppression and increased risk of infections |
| Food/Dietary | No specific food interactions. Grapefruit products do not significantly affect fluticasone or azelastine metabolism. Alcohol may increase CNS depression risk; avoid or limit alcohol intake. |
| Clinical Pearls |
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| Both azelastine and fluticasone propionate are excreted into breast milk in small amounts. Azelastine may cause drowsiness in infants; fluticasone has low oral bioavailability. Consider risk-benefit and monitor infant for sedation or growth retardation. |
| Lactation Rating | L3: Limited data, potential risk |
| 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 | 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. |
| DYMISTA (azelastine/fluticasone) is a fixed-dose combination nasal spray for allergic rhinitis. Administer as 1 spray per nostril twice daily. Prime pump with 6 sprays before first use or after 7+ days of non-use. Avoid contact with eyes; if occurs, flush with water. Systemic anticholinergic effects are minimal at recommended doses. Monitor for nasal septal perforation with prolonged use. Not for acute asthma attacks. |
| Patient Advice | Use exactly as prescribed: 1 spray in each nostril twice daily (morning and evening). · Blow nose gently before use. Tilt head forward, insert nozzle into nostril, and spray while breathing in through the nose. · Do not spray into eyes; if contact occurs, rinse with water for at least 10 minutes. · Do not share the bottle with others to avoid infection. · Sneeze through the nose, not the mouth, after administration. · If you miss a dose, take it as soon as you remember unless it is almost time for the next dose. Do not double the dose. · Common side effects include bitter taste (dysgeusia), headache, and nasal irritation. The bitter taste can be minimized by using a flavored drink or food afterward. · Inform your doctor if you have glaucoma, cataracts, or a recent nasal injury/surgery. |