Azelastine

Azelastine is a potent, second-generation, selective, histamine antagonist used as a first line therapy of mild intermittent, moderate/severe intermittent and mild persistent rhinitis.

Azelastine

Azelastine; Azelastinum; Azelastina; Optivar; 4-(4-chlorobenzyl)-2-(1-methylazepan-4-yl) phthalazin-1(2H)-one

Arzep, Azelast, Azeflo, DPS, Azelast Combinase-AQ, Azep, Flutiair-AZ, Duonase, Furamist-AZ, Nezalast, Nazomac-AF, Oculast, Sarnase

4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-1,2-dihydrophthalazin-1-one

• Absorption: Systemic bioavailability
• Distribution: 88-97% protein binding
• Metabolism: Hepatic
• Excretion: Via faeces.

Azelastine competes with histamine for the H1-receptor sites on effectors cells and show antagonist activity by inhibiting the release of other mediators and histamine involved in the allergic response.

• Instill 1-2 drops of 0.05% solution into the affected eye/s bid for conjunctivitis
• 140 mcg by nasal spray into each nostril bid for rhinitis.

Treatment of seasonal allergic rhinitis and non-allergic rhinitis, relief of ocular itching associated with allergic conjunctivitis.

Sneezing, irritation, stinging and itching of the nasal mucosa, nosebleeds, nausea, headache; somnolence, taste disturbances and dry mouth.

Hypersensitivity

• Store at 20-25°C-nasal drops.
• Store at 2-25°C-opthalmic solution

Molecular weight

381.898

Molecular formula

C22H24ClN3O

CAS number

58581-89-8

Precautions

• After every use, the Tip of the bottle should be dipped in boiling water, dried and capped appropriately.
• Pregnancy
• Lactation.