Composition and methods for treating allergic response
The invention generally relates to compositions and methods for treating and/or preventing an allergic response with reduced rebound hyperemia, comprising highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume, and histamine antagonists. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.
1 . A composition formulated for treating and/or preventing an allergic response with reduced rebound hyperemia, comprising a selective a-2 adrenergic receptor agonist having a binding affinity of 100 fold or greater for a-2 over a-1 adrenergic receptors, or a pharmaceutically acceptable salt thereof, and a histamine antagonist, wherein said selective a-2 adrenergic receptor agonist is present at a concentration below about 0.025% weight by volume.
2 . The composition of claim 1 , wherein said binding affinity is about 500 fold or greater for a-2 over a-1 adrenergic receptors.
3 . The composition of claim 1 , wherein said first selective a-2 adrenergic receptor agonist is present at a concentration from between about 0.001% to about 0.025% weight by volume.
4 . The composition of claim 1 , wherein said selective selective a-2 adrenergic receptor agonist is selected from the group consisting of apraclonidine, mivazerol, clonidine, brimonidine, alpha methyl dopa, guanfacine, dexemeditomidine, (+)-(S)-4-[1-(2,3-dimethyl-phenyl)-ethyl]-1,3-dihydro-imidazole-2-thione, 1-[(imidazolidin-2-yl)imino]indazole, and mixtures of these compounds.
5 . A composition comprising brimonidine and a histamine antagonist, wherein said brimonidine concentration is from between about 0.001% to about 0.025% weight by volume.
6 . A method of treating and/or preventing an allergic response with reduced rebound hyperemia comprising administering to a patient in need thereof a composition of claim 1 .
7 . A method of treating and/or preventing an allergic response with reduced rebound hyperemia comprising administering to a patient in need thereof a composition of claim 5 .
8 . A composition consisting essentially of brimonidine and a nonsedating antihistamine, wherein said brimonidine concentration is from between about 0.001% to about 0.025% weight by volume, wherein pH of said composition is between about 5.5 and about 6.5, and wherein said composition is formulated as an aerosolized composition.
9 . The composition of claim 8 wherein said nonsedating antihistamine is selected from the group consisting of loratadine, desloratadine, cetirizine, fexofenadine, acrivastine, ebastine, norastemizole, levocetirizine, and mizolastine.
10 . The composition of claim 8 , wherein the nonsedating antihistamine is pheniramine maleate.