Azelastine

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.

Information

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