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Uses

Ocular Hypertension and Glaucoma

Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.

Dosage and Administration

General

• IOP should be determined after about 4 weeks of therapy with the drug; thereafter, IOP should be determined as necessary.

Administration

Topical Administration

Apply topically to the affected eye(s).

If more than one topical ophthalmic drug is used, administer the drugs at least 5 minutes apart.

Dosage

Pediatric Patients

Ocular Hypertension and Glaucoma

Ophthalmic

The manufacturer makes no specific dosage recommendations for children ≥2 years of age.

Adults

Ocular Hypertension and Glaucoma

Ophthalmic

One drop in the affected eye(s) 3 times daily, approximately 8 hours apart.

Cautions

Contraindications

• Concomitant use with an MAO inhibitor.
• Known hypersensitivity to brimonidine or any ingredient in the formulation.

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity Reactions

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

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

General Precautions

Systemic Effects

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.

IOP Monitoring

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

Specific Populations

Pregnancy

Category B.

Lactation

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

Pediatric Use

Potentially serious adverse CNS effects, including apnea and lethargy reported in infants; not recommended for children < 2 years of age.

Geriatric Use

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

Common Adverse Effects

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

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.

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.

Interactions

No formal drug interaction studies have been performed.

Specific Drugs

Pharmacokinetics

Absorption

Bioavailability

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

Onset

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

Distribution

Extent

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

Elimination

Metabolism

Extensively metabolized in the liver.

Elimination Route

Brimonidine and its metabolites are excreted principally in urine.

Half-life

2–3 hours.

Stability

Storage

Ophthalmic

Solution

15–25°C.

Actions

• Reduces IOP by decreasing aqueous humor production and increasing uveoscleral outflow.

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