Azelastine
Azelastine
Astelin, Astepro (intranasal); Optivar (ophthalmic); with fluticasone as Dymista
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Summary
Common uses
Allergic rhinitis (intranasal)0, Vasomotor rhinitis (intranasal)0, Allergic conjunctivitis (ophthalmic)0
Pharmacy
Starting dose
Intranasal 0.1% or 0.15%: 1-2 sprays/nostril BID; ophthalmic 0.05%: 1 drop in each eye BID
Preparations
0.1%, 0.15% intranasal spray; 0.05% ophthalmic solution; combination Dymista (azelastine 0.137 mg + fluticasone 50 mcg/spray)
US FDA Max
2 sprays/nostril BID
Pharmacology
Routes
Intranasal, topical ophthalmic
Onset
15 minutes
Duration
12 hours
Half-life
~22 hours; longer 54 hours (desmethylazelastine, active metabolite)[1]
Bioavailability
Intranasal ~40% systemic; ophthalmic minimal[1]
Pregnancy
Limited data; second-line to intranasal corticosteroids or PO loratadine/cetirizine.[citation needed]
Legal status
OTC (Astepro 0.15%) and Rx-only (other intranasal, ophthalmic, Dymista) in US
Purported mechanism
Azelastine is a phthalazinone H1 receptor antagonist with mast cell stabilizing activity; the dual mechanism provides faster nasal symptom relief than intranasal corticosteroids alone in allergic rhinitis.0 Topical application minimizes systemic antihistaminic burden; the characteristic bitter taste with nasal use (drainage to oropharynx) is the main tolerability issue[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Astepro (azelastine HCl) nasal spray, Bayer (now OTC), current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/021488s016lbl.pdf