Azelastine Azelastine

Azelastine Azelastine

Uses of azelastine

It is an antihistamine that, in addition to blocking the activity of histamine H2 receptor, inhibits the release of inflammatory mediators from mast cells. It is used in the symptomatic treatment of allergic conditions such as rhinitis and conjunctivitis, as well as in the treatment of non-allergic rhinitis (vasomotor).

Mechanism of action of aclastin

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Histamine H1 receptor antagonist
Decreased release of histamine and other inflammatory mediators of allergic reactions
– Reduction of airway irritability
Improving the function of the mucosiliary system (by increasing the movement of bronchial epithelial cilia)

Pharmacokinetics of azlastine

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Bioavailability: 40%
Onset of effect: 30-15 minutes
Peak effect: 3 hours
Effect length: 12 hours
Plasma peak: 4-2 hours
Protein binding: 88%
Metabolism: Hepatic (by the enzyme CYP450 to the active metabolite of methyl azlastin)
half life:
Alastine 25-22 hours
The active metabolite of azelastine is 57-52 hours
Excretion: feces (75%, less than 10% as unchanged drug)