Small molecule drug with a maximum clinical stage of Approval (across all indications), with 7 approved and 9 investigational indications.
targets Adrenergic receptor alpha-2
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trade names
Alphagan, Alphagan p, Brimonidine tartrate, Brimonidine tartrate component of combigan, Brimonidine tartrate component of simbrinza, Brymont
generic
BRIMONIDINE TARTRATE
MOA
12.1 Mechanism of Action COMBIGAN is comprised of two components: brimonidine tartrate and timolol. Each of these two components decreases elevated intraocular pressure, whether or not associated with glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss. The higher the level of intraocular pressure, the greater the likelihood of glaucomatous field loss and optic nerve damage. COMBIGAN is a relatively selective alpha-2 adrenergic receptor agonist with a non-selective beta-adrenergic receptor inhibitor. Both brimonidine and timolol have a rapid onset of action, with peak ocular hypotensive effect seen at two hours post-dosing for brimonidine and one to two hours for timolol. Fluorophotometric studies in animals and humans suggest that brimonidine tartrate has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow. Timolol maleate is a beta 1 and beta 2 adrenergic receptor inhibitor that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity.
indication
1 INDICATIONS AND USAGE COMBIGAN ® is indicated for the reduction of elevated intraocular pressure (IOP) in patients with glaucoma or ocular hypertension who require adjunctive or replacement therapy due to inadequately controlled IOP. The IOP-lowering of COMBIGAN dosed twice a day was slightly less than that seen with the concomitant administration of 0.5% timolol maleate ophthalmic solution dosed twice a day and 0.2% brimonidine tartrate ophthalmic solution dosed three times per day. COMBIGAN is a combination of brimonidine tartrate, an alpha-adrenergic receptor agonist, and timolol maleate, a beta-adrenergic receptor inhibitor, indicated for the reduction of elevated intraocular pressure (IOP) in patients with glaucoma or ocular hypertension who require adjunctive or replacement therapy due to inadequately controlled IOP. The IOP-lowering of COMBIGAN dosed twice a day was slightly less than that seen with the concomitant administration of timolol maleate ophthalmic solution, 0.5% dosed twice a day and brimonidine tartrate ophthalmic solution, 0.2% dosed three times per day. ( 1 )
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