Azelastine hydrochloride

Description

Azelastine hydrochloride is an orally effective antihistamine useful in the treatment of asthma and nasal allergy. It appears to inhibit release of histamine, in addition to antagonizing its action.

Chemical properties

White or almost white, crystalline powder.

Originator

Asta-Werke(Degussa) (W. Germany)

The Uses of Azelastine hydrochloride

Orally active H1-hystamine receptor antagonist. Antihistaminic

Definition

ChEBI: The hydrochloride salt of azelastine.

brand name

Astelin (Medpointe); Optivar (Medpointe);AZEPTIN.

General Description

Azelastine hydrochloride (HCl) is an antihistamine administered in aqueous solution as a nasal spray. It exhibits histamine H1 receptor antagonist activity and is used as a racemic mixture. No difference in pharmacologic activity between its enantiomers has been observed.

Azelastine HCl is used to treat seasonal allergic rhinitis (e.g., hay fever) and perennial rhinitis (including runny nose, sneezing, and nasal itching). It is also used in eyedrops to treat allergic conjunctivitis. It is considered to be a very safe drug with no serious side effects.

Biochem/physiol Actions

H1 histamine receptor antagonist; NF-kB activator.

Safety Profile

Poison by ingestion andintravenous routes. An experimental teratogen. Otherexperimental reproductive effects. When heated todecomposition it emits toxic fumes of NOx and HCl.

Mechanism of action

Azelastine has a triple mode of action:

Anti-histamine effect,

Mast-cell stabilizing effect and

Anti-inflammatory effect.

Side Effects

Common side effects include headache, sleepiness, change in taste, and sore throat. It is unclear if use is safe during pregnancy or breastfeeding. It is a second-generation antihistamine and works by blocking the release of a number of inflammatory mediators including histamine.