Drug intelligence / Profile preview

azelastine

Development stage
Approved
Lead developer
Meda
Modality
Small Molecules
Administration
Intranasal, Ophthalmic
01

Overview

Azelastine is a second-generation antihistamine and phthalazine derivative primarily used as a nasal spray to treat allergic rhinitis (hay fever) and vasomotor (nonallergic) rhinitis, as well as in ophthalmic solution form for allergic conjunctivitis. It works mainly by antagonizing the histamine H1 receptor, thereby blocking the effects of histamine—a key mediator in allergy symptoms such as sneezing, runny or stuffy nose, itching, and watery eyes. In addition to its antihistaminic action, azelastine exhibits mast cell-stabilizing properties that inhibit the release of inflammatory mediators including interleukin-6, tryptase, TNF-alpha from mast cells and leukotrienes from eosinophils. The onset of action is rapid (within 15 minutes intranasally; within 3 minutes ophthalmically), with effects lasting up to 12 hours. Azelastine was first patented in 1971 and approved for medical use in 1986[5][7].

Brand names
AstelinAsteproAstepro AllergyOptivar
Other names
azelastine hydrochloride
02

Targets

HRH1 (Histamine H1 Receptor)

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