Vasoconstriction compositions and methods of use

Abstract

The invention generally relates to compositions for inducing vasoconstriction. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5.

1 . A composition for inducing vasoconstriction 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 wherein said selective a-2 adrenergic receptor agonist is present at a concentration below about 0.05% 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 a-2 adrenergic receptor agonist is present at a concentration between about 0.001% and about 0.025% weight by volume. 
     
     
         4 . The composition of  claim 1 , wherein said selective a-2 adrenergic receptor agonist is selected from the group consisting of apraclonidine, mivazerol, clonidine, brimonidine, alpha methyl dopa, guanfacine, dexemeditomidine, (+HS)-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 . The composition of  claim 1 , wherein said composition is formulated for treating a nasal congestion or a pulmonary condition. 
     
     
         6 . The composition of  claim 1 , wherein the composition is formulated for treating an ocular condition. 
     
     
         7 . A composition for inducing vasoconstriction comprising brimonidine wherein said brimonidine concentration is between about 0.001% and about 0.025% weight by volume. 
     
     
         8 . A composition for inducing vasoconstriction comprising a selective a-2 adrenergic receptor agonist having a binding affinity of 100 fold or greater for a-2b and/or a-2c receptors over a-1 adrenergic receptors, or a pharmaceutically acceptable salt thereof, and wherein said selective a-2 adrenergic receptor agonist is present at a concentration below about 0.05% weight by volume 
     
     
         9 . A composition for inducing vasoconstriction consisting essentially of brimonidine, wherein said brimonidine concentration is between about 0.01% and about 0.02% 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 ocular drop. 
     
     
         10 . A composition for inducing vasoconstriction consisting essentially of brimonidine and potassium, wherein said brimonidine concentration is from between about 0.01% to about 0.02% 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 eye drop. 
     
     
         11 . The composition of  claim 10 , wherein potassium is in the form of potassium chloride, and wherein said potassium chloride concentration is between about 0.2% to about 0.9% weight by volume. 
     
     
         12 . A method of treating a disease or condition comprising topically administering to a patient in need thereof the composition of  claim 1 . 
     
     
         13 . The method of  claim 12  wherein said disease or condition is selected from the group consisting of nasal congestion, pulmonary condition, and ocular condition.