Description
Azelastine has potent, long-lasting histamine
H1-receptor blocking activity and several other
interesting anti-inflammatory properties related
to its antiallergic efficacy .
Uses
anesthetic, anticonvulsant
Definition
ChEBI: A phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position.
brand name
Astelin
(Medpointe); Optivar (Medpointe).
Clinical Use
Azelastine, although not a close structural analogue to the benzimidazoles, has some
structural similarities to them. It is used as a nasal spray for allergic rhinitis and as eye drops
for allergic conjunctivitis.Like olopatadine, azelastine also stabilizes mast cells, preventing
degranulation and subsequent release of histamine, leukotrienes, and PGD2. It is available in
Europe for systemic use in the treatment of asthma and seasonal allergies. Besides
antihistaminic effects, it also may block release of histamine and other inflammatory
mediators from mast cells. When administered orally, the N-dealkylated metabolite appears to
contribute significantly to its pharmacological effects.
Safety Profile
Poison by ingestion,subcutaneous, intravenous, and intraperitoneal routes.Experimental reproductive effects. When heated todecomposition it emits toxic fumes of NOx and Cl
- .
