Overview
11 DESCRIPTION Brimonidine tartrate/timolol maleate ophthalmic solution 0.2%/0.5%, sterile, is a relatively selective alpha-2 adrenergic receptor agonist with a non-selective beta-adrenergic receptor inhibitor (topical intraocular pressure lowering agent). The structural formulae are: Brimonidine tartrate: 5-bromo-6-(2-imidazolidinylideneamino) quinoxaline L-tartrate; MW= 442.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Brimonidine tartrate/timolol maleate ophthalmic solution 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. Brimonidine tartrate/timolol maleate ophthalmic solution is a relatively selective alpha-2 adrenergic receptor agonist with a non-selective beta-adrenergic receptor inhibitor.
Indications
- 1 INDICATIONS AND USAGE Brimonidine tartrate/timolol maleate ophthalmic solution 0.2%/0.5% is an alpha adrenergic receptor agonist with 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 brimonidine tartrate/timolol maleate ophthalmic solution dosed twice a day was slightly less than that seen with the concomitant administration of 0.
Common Doses
- Refer to label
Dosage
2 DOSAGE AND ADMINISTRATION The recommended dose is one drop of brimonidine tartrate/timolol maleate ophthalmic solution in the affected eye(s) twice daily approximately 12 hours apart. If more than one topical ophthalmic product is to be used, the different products should be instilled at least 5 minutes apart. One drop in the affected eye(s), twice daily approximately 12 hours apart. ( 2 )
Contraindications
- 4 CONTRAINDICATIONS Bronchial asthma, a history of bronchial asthma, severe chronic obstructive pulmonary disease. ( 4.1 , 5.1 , 5.3 ) Sinus bradycardia, atrioventricular block, overt cardiac failure, cardiogenic shock. ( 4.2 , 5.2 ) Neonates and infants (under the age of 2 years). ( 4.3 ) Hypersensitivity to any component of this product. ( 4.4 ) 4.1 Reactive Airway Disease Including Asthma, COPD Brimonidine tartrate/timolol maleate ophthalmic solution is contraindicated in patients with reactive airway disease including bronchial asthma; a history of bronchial asthma; severe chronic...
Side Effects
- 6 ADVERSE REACTIONS Most common adverse reactions occurring in approximately 5 to 15% of patients included allergic conjunctivitis, conjunctival folliculosis, conjunctival hyperemia, eye pruritus, ocular burning, and stinging. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Sentiss at 1-855-473-6847 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Studies Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of...
Interactions
- 7 DRUG INTERACTIONS Antihypertensives/cardiac glycosides may lower blood pressure. ( 7.1 ) Concomitant use with systemic beta-blockers may potentiate systemic beta-blockade. ( 7.2 ) Oral or intravenous calcium antagonists may cause atrioventricular conduction disturbances, left ventricular failure, and hypotension. ( 7.3 ) Catecholamine-depleting drugs may have additive effects and produce hypotension and/or marked bradycardia. ( 7.4 ) Use with CNS depressants may result in an additive or potentiating effect. ( 7.