Azelastine Hydrochloride
Azelastine Hydrochloride Prescribing Information
Azelastine hydrochloride ophthalmic solution is indicated for the treatment of itching of the eye associated with allergic conjunctivitis.
The recommended dose is one drop instilled into each affected eye twice a day.
Azelastine hydrochloride ophthalmic solution is contraindicated in persons with known or suspected hypersensitivity to any of its components.
In controlled multiple-dose studies where patients were treated for up to 56 days, the most frequently reported adverse reactions were transient eye burning/stinging (approximately 30%), headaches (approximately 15%) and bitter taste (approximately 10%). The occurrence of these events was generally mild.
The following events were reported in 1 to 10% of patients: asthma, conjunctivitis, dyspnea, eye pain, fatigue, influenza-like symptoms, pharyngitis, pruritus, rhinitis and temporary blurring. Some of these events were similar to the underlying disease being studied.
Azelastine hydrochloride ophthalmic solution, 0.05% is a sterile ophthalmic solution containing azelastine hydrochloride, a relatively selective H1-receptor antagonist for topical administration to the eyes. Azelastine hydrochloride is a white crystalline powder with a molecular weight of 418.37. Azelastine hydrochloride is sparingly soluble in water, methanol and propylene glycol, and slightly soluble in ethanol, octanol and glycerine. Azelastine hydrochloride is a racemic mixture with a melting point of 225°C. The chemical name for azelastine hydrochloride is (±)-1-(2H)-phthalazinone,4-[(4-chlorophenyl) methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, monohydrochloride and is represented by the following chemical structure:
Empirical chemical structure: C22H24CIN3O•HCl
Each mL of azelastine hydrochloride ophthalmic solution, 0.05% contains:
Azelastine hydrochloride is a relatively selective histamine H1 antagonist and an inhibitor of the release of histamine and other mediators from cells (e.g., mast cells) involved in the allergic response. Based on in-vitro studies using human cell lines, inhibition of other mediators involved in allergic reactions (e.g., leukotrienes and PAF) has been demonstrated with azelastine hydrochloride. Decreased chemotaxis and activation of eosinophils has also been demonstrated.