Azelastine

Brand/Trade Names: Astelin (nasal spray), Optivar (eye drops)

Description: Azelastine is a relatively selective histamine H1 antagonist and an inhibitor of the release of histamine and other mediators from cells (e.g. mast cells) involved in the allergic response. Based on in vitro studies using human cell lines, inhibition of other mediators involved in allergic reactions (e.g. leukotrienes and PAF) has been demonstrated with azelastine. Decreased chemotaxis and activation of eosinophils has also been demonstrated.
Antihistamines such as azelastine appear to compete with histamine for histamine H1- receptor sites on effector cells (mast cells). The antihistamines antagonize those pharmacological effects of histamine which are mediated through activation of H1- receptor sites and thereby reduce the intensity of allergic reactions and tissue injury response involving histamine release.
Available as a nasal spray (Astelin) for hay fever and as eye drops (Optivar) for allergic conjunctivitis.

Uses: As eye drops is indicated for the treatment of itching of the eye associated with allergic conjunctivitis.
Nasal Spray is indicated for the treatment of the symptoms of seasonal allergic rhinitis such as rhinorrhea, sneezing, and nasal pruritus in adults and children 5 years and older, and for the treatment of the symptoms of vasomotor rhinitis, such as rhinorrhea, nasal congestion and postnasal drip in adults and children 12 years and older.

Azelastine Structural Formula


Additional Information Data And Resources:
Astelin Prescribing Information
Optivar Prescribing Information