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Antiallergic compound and an antihistamine. The compositions are used to prevent allergic responses while also treating existing allergic conditions present in the eye. The invention is also directed to methods of preventing and treating allergic responses with the compositions.


Antiallergics are compounds which prevent, inhibit or alleviate allergic reactions. It is believed that these compounds characteristically function as cell stabilizers and/or mast cell inhibitors preventing the usual degranulation of the mast cells in response to the presence of allergens. The eye, particularly the conjunctiva, has a relatively large number of mast cells. When allergens are present, they can bind to the immunoglobulin on the surface of these mast cells and trigger the breakdown, or what is known as the degranulation, of the cell. On degranulation, mast cell components, including histamines, are released into the environment outside the mast cell. Through a variety of mechanisms, these components can be responsible for symptoms associated with allergic responses such as itching, redness, lid swelling, vasodilation and chemosis.

Antihistamines are compounds which are administered to prevent histamines, released from mast cells in response to the presence of allergens, from binding to, for example, nerves and smooth muscle cells of the conjunctival blood vessels causing redness, itching and swelling. They serve to prevent or alleviate many of the symptoms which can result from degranulation of mast cells.

It is an object of the present invention to provide improved ophthalmic compositions comprising an antiallergic and an antihistamine, for treating existing symptoms of mast cell degranulation caused by the release of histamines and preventing further allergic and inflammatory symptoms by stabilizing the mast cells of the eye, or by inhibitng the allergic reaction which results in mast cell degranulation and ocular irritation.


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