Brimonidine Tartrate eent

Contraindications

• Concomitant use with an MAO inhibitor.1 19

• Known hypersensitivity to brimonidine or any ingredient in the formulation.1 19

Warnings/Precautions

Sensitivity Reactions

Ocular hypersensitivity reactions (e.g., allergic conjunctivitis, conjunctival hyperemia, ocular pruritus) reported.1 If sensitivity reaction occurs, discontinue brimonidine.17

Possible partial cross-sensitivity between brimonidine and apraclonidine;18 use with caution in patients with a history of hypersensitivity to apraclonidine.17

General Precautions

Minimal effects on blood pressure in clinical studies; use with caution in patients with severe cardiovascular conditions, depression, orthostatic hypotension, cerebral or coronary insufficiency, Raynaud’s phenomenon, or thromboangiitis obliterans.1 19

IOP-lowering effect of 0.2% brimonidine tartrate ophthalmic solution may diminish over time; routinely monitor IOP.19

Specific Populations

Category B.1 19

Distributed into milk in rats;1 17 discontinue nursing or the drug.1 19

Potentially serious adverse CNS effects, including apnea8 19 and lethargy reported in infants;8 19 not recommended for children < 2 years of age.1 6 19

No substantial differences in safety and efficacy relative to younger adults.1 19

Common Adverse Effects

With brimonidine tartrate 0.15% ophthalmic solution in adults, allergic conjunctivitis,1 conjunctival hyperemia,1 ocular pruritus,1 burning sensation,1 conjunctival folliculosis,1 hypertension,1 xerostomia,1 and visual disturbances.1

With brimonidine tartrate 0.2% ophthalmic solution in adults, oral dryness, ocular hyperemia, burning and stinging, headache, blurring, foreign body sensation, fatigue/drowsiness, conjunctival follicles, ocular allergic reactions, ocular pruritus.19

Age- and weight-related somnolence and decreased mental alertness reported in children 2–7 years of age with glaucoma receiving brimonidine tartrate 0.2% ophthalmic solution.1 6 19

No formal drug interaction studies have been performed.1 19

Specific Drugs

Absorption

Bioavailability

Peak plasma concentrations occurred within 0.5–4 hours after ocular administration of brimonidine tartrate 0.1 or 0.2% ophthalmic solution.1 19

Onset

Peak ocular hypotensive effects occur 2–3 hours following topical administration of brimonidine.1 3 19

Distribution

Extent

Distributed into milk in animals; not known whether the drug distributes into milk in humans.1 19

Elimination

Metabolism

Extensively metabolized in the liver.1 19

Elimination Route

Brimonidine and its metabolites are excreted principally in urine.1 19

Half-life

2–3 hours.1 19

• Reduces IOP by decreasing aqueous humor production and increasing uveoscleral outflow.1 3 4 11 19

• Selectivity for α2- versus α1-adrenergic receptors at least 10 or 28 times greater than that of clonidine or apraclonidine, respectively;3 9 11 may result in reduction in adverse pulmonary and cardiovascular effects.1 11

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name