Azelastine
- Atc Codes:R01AC03#R06AX19#S01GX07
- CAS Codes:79307-93-0#58581-89-8
- PHARMGKB ID:79307-93-0#58581-89-8
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
Brand Names
Europe
Austria: Allergodil, Allergodrop, Allergospray; Belgium: Allergodil, Otrivine Anti-Allergie; Bulgaria: Allergodil, Antalerg; Czech Republic: Allergodil; Denmark: Allergodil; Estonia: Allergodil; Finland: Lastin; France: Allergodil, Prorhinite; Germany: Allergodil, Loxin, Vividrin Akut Azelastin; Greece: Afluon; Hungary: Allergodil; Ireland: Azelastine, Optilast, Rhinolast; Italy: Allergodil, Lasticom; Latvia: Allergodil; Lithuania: Allergodil; Luxembourg: Allergodil; Netherlands: Allergodil, Oculastin, Otrivin Neusallergie Azelastine; Poland: Allergodil; Portugal: Allergodil, Azep, Oculastin; Romania: Allergodil; Slovakia: Allergodil, Antalerg; Slovenia: Allergodil; Spain: Afluón, Corifina; Sweden: Lastin, Oculastin; UK: Optilast, Rhinolast.
North America
USA: Astelin, Astepro, Azelastine, Optivar.
Latin America
Argentina: Alager, Brixia, Xanaes; Brazil: Azelastina, Rino-Lastin; Mexico: Amsler, Astelin, AZ Ofteno.
Asia
Japan: Adomessen, Armin, Asutoputin, Azelastine, Azen, Azepit, Azeptin, Bifertin, Cobatect, Raspjine, Shubittle, Verstatin, Yosinotin.
Drug combinations
Chemistry
Azelastine Hydrochloride: C~22~H~24~ClN~3~O HCl. Mw: 418.36. (1) 1(2H)-Phthalazinone, 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, monohydrochloride; (2) 4-(p-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone monohydrochloride. CAS-79307-93-0; CAS-58581-89-8 (azelastine)(1984).

Pharmacologic Category
EENT Preparations; Antiallergic Agents; Histamine H~1~ Antagonist. (ATC-Code: R01AC03; R06AX19; S01GX07).
Mechanism of action
Competes with histamine for H~1~-receptor sites on effector cells and inhibits the release of histamine and other mediators involved in the allergic response. Reduces hyper-reactivity of the airways. Increases the motility of bronchial epithelial cilia, improving mucociliary transport.
Therapeutic use
Seasonal allergic rhinitis. Vasomotor rhinitis. Itching of the eye associated with seasonal allergic conjunctivitis.
Pregnancy and lactiation implications
Use during pregnancy only if the potential benefit to the mother outweighs the possible risk to the fetus. Use with caution during lactation.
Unlabeled use
Contraindications
Hypersensitivity to azelastine or any component of the formulation.
Warnings and precautions
May cause drowsiness. Effects may be additive with CNS depressants and/or ethanol. Ophthalmic solution contains benzalkonium chloride.