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
Drug
Interaction
Comment
β-Adrenergic blocking agents (topical or systemic)
Additive IOP-lowering and cardiovascular effects
Use with caution
Cardiac glycosides
Additive cardiovascular effects
Use with caution
CNS depressants (e.g., alcohol, barbiturates, general anesthetics, opiates, sedatives)
TCAs that affect the metabolism and uptake of circulating amines may interfere with IOP-lowering effect of brimonidine
Use with caution
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.
Advice to Patients
Importance of advising patients that brimonidine tartrate may cause fatigue and/or drowsiness and to exercise caution when engaged in hazardous activities requiring mental alertness.
Importance of informing patients to administer other ophthalmic drugs at least 5 minutes apart.
Importance of delaying insertion of soft contact lenses for at least 15 minutes after 0.2% brimonidine tartrate instillation, since benzalkonium chloride preservative in the solution may be absorbed by soft lenses.
Importance of learning and adhering to proper administration techniques to avoid contamination of the solution container.
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs as well as any concomitant illnesses.
Importance of informing patients of other important precautionary information. (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Comparative Pricing
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 09/2009. For the most current and up-to-date pricing information, please visit www.drugstore.com. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
Remember, keep this and all other medicines out of the reach of children,
never share your medicines with others, and use this medication only for the indication prescribed.
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