BRIMONIDINE TARTRATE

AbsorptionAfter ocular administration of a 0.2% solution, plasma concentrations peaked within 1 to 4 hours and declined with a systemic half-life of approximately 3 hours.

DistributionThe protein binding of brimonidine has not been studied.

MetabolismIn humans, brimonidine is extensively metabolized by the liver.

ExcretionUrinary excretion is the major route of elimination of brimonidine and its metabolites. Approximately 87% of an orally-administered radioactive dose of brimonidine was elim...

Elevated IOP presents a major risk factor in glaucomatous field loss. The higher the level of IOP, the greater the likelihood of optic nerve damage and visual field loss. Brimonidine tartrate has the action of lowering intraocular pressure with minimal effect on cardiovascular and pulmonary parameters. In comparative clinical studies with timolol 0.5%, lasting up to one year, the IOP lowering effect of Brimonidine tartrate ophthalmic solution, 0.2% was approximately 4 to 6 mm Hg compared with approximately 6 mm Hg for timolol. In these studies, both patient groups were dosed BID; however, due ...

The following serious adverse reactions are described elsewhere in the labeling: Potentiation of Vascular Insufficiency [see Warnings and Precautions ( 5.1 )] Severe Cardiovascular Disease [see Warnings and Precautions ( 5.2 )] Contamination of Topical Ophthalmic Products after Use [see Warnings and Precautions ( 5.3 )] Neonates and Infants (under the age of 2 years) [see Contraindications ( 4.1 )] Most common adverse reactions occurring in approximately 10 to 30% of patients receiving brimon...

Brimonidine Tartrate Ophthalmic Solution, 0.2% is contraindicated in patients with hypersensitivity to brimonidine tartrate or any component of this medication. It is also contraindicated in patients receiving monoamine oxidase (MAO) inhibitor therapy. Neonates and infants (under the age of 2 years). ( 4.1 ) 4.1 Neonates and Infants (under the age of 2 years) Brimonidine tartrate ophthalmic soluti...

Potentiation of vascular insufficiency. ( 5.1 ) 5.1 Potentiation of Vascular Insufficiency Brimonidine tartrate ophthalmic solution, 0.2% may potentiate syndromes associated with vascular insufficiency. Brimonidine tartrate ophthalmic solution, 0.2% should be used with caution in patients with depression, cerebral or coronary insufficiency, Raynaud’s phenomenon, orthostatic hypotension, or thromboangiitis obliterans 5.2 Severe Cardiovascular Disease Although brimonidine tartrate ophthalmic solut...

7 DRUG INTERACTIONS

• Antihypertensives/cardiac glycosides may lower blood pressure. ( 7.1 )
• Use with CNS depressants may result in an additive or potentiating effect. ( 7.2 )
• Tricyclic antidepressants may potentially blunt the hypotensive effect of systemic clonidine. ( 7.3 )
• Monoamine oxidase inhibitors may result in increased hypotension. ( 7.4 ) 7.1 Antihypertensive/Cardiac Glycosides Be...