Brimonidine (brimonidine tartrate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Brimonidine tartrate is a relatively selective alpha2-adrenergic agonist.
Brimonidine, a relatively selective alpha2-adrenergic agonist, is structurally and pharmacologically related to apraclonidine and clonidine. In vitro pharmacologic studies indicate that the selectivity of brimonidine for alpha2- versus alpha1-adrenergic receptors is at least 10 or 28 times greater than that of clonidine or apraclonidine, respectively. Such selectivity of brimonidine for the alpha2-receptor may result in a reduced incidence of adverse pulmonary and cardiovascular effects.
Following topical application to the eye, brimonidine tartrate 0.2% reduces both elevated and normal intraocular pressure (IOP) in patients with or without glaucoma. Fluorophotometric studies in animals and humans suggest that brimonidine tartrate ophthalmic solution reduces IOP by decreasing aqueous humor production and increasing uveoscleral outflow. Peak ocular hypotensive effects occur 2-3 hours following topical administration of brimonidine tartrate ophthalmic solution.
Controlled studies in patients with primary open-angle glaucoma or ocular hypertension have demonstrated that the ocular hypotensive effect of brimonidine tartrate 0.1 or 0.15% ophthalmic solution is comparable to that of the 0.2% solution. When used at low dosages (i.e., brimonidine tartrate 0.025%) in individuals with normal IOP, the vasoconstrictive effects of the drug relieve ocular redness without altering IOP.
USES: This medication is used to treat open-angle glaucoma or high fluid pressure in the eye. Lowering high fluid pressure in the eye reduces the risk of vision loss, nerve damage, or blindness. This medication lowers pressure by allowing better fluid drainage from within the eye and also by reducing the amount of fluid formed in the eye.
It is known as an alpha agonist. This drug is not recommended for use in children less than 2 years of age due to an increased risk of serious side effects such as very slowed breathing. Ask the doctor or pharmacist for details.
Generic name: brimonidine tartrate
Pronunciation: (bri-MOE-ni-deen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Brimonidine
Indications
The following indications are listed for Brimonidine:
- Ocular Hypertension
- Open Angle Glaucoma
Also known as: Chronic Glaucoma, Compensated Glaucoma, Glaucoma Simplex, Increased Intraocular Pressure, Increased Iop, Open-Angle Glaucoma, Raised Intraocular Pressure, Simple Glaucoma.
Dosing
No dosing information is available for this tab.
Brimonidine tartrate is applied topically to the eye as an ophthalmic solution. Brimonidine tartrate also is commercially available in fixed combination with brinzolamide (as an ophthalmic suspension) and in fixed combination with timolol (as an ophthalmic solution) for topical application to the eye.
Although topical brimonidine has been administered twice daily as an ocular hypotensive agent in certain clinical studies, reductions in intraocular pressure (IOP) induced by the drug appear to diminish 8 hours following administration. Therefore, the manufacturers recommend administering brimonidine tartrate 0.1, 0.15, or 0.2% ophthalmic solution 3 times daily at intervals of approximately 8 hours. The fixed-combination ophthalmic suspension containing brinzolamide and brimonidine tartrate also is administered 3 times daily. However, when used in fixed combination with timolol, brimonidine is administered twice daily at intervals of approximately 12 hours. For self-medication for temporary relief of ocular redness, brimonidine tartrate 0.025% may be administered up to 4 times daily.
The fixed-combination ophthalmic suspension containing brinzolamide and brimonidine tartrate should be shaken well prior to use.
Care should be taken to avoid contamination of the dispensing container. (See Bacterial Keratitis under Cautions: Warnings/Precautions.)
Some brimonidine ophthalmic preparations contain benzalkonium chloride, which may be absorbed by soft contact lenses. Contact lenses should be removed prior to administration of each dose of these preparations, but may be reinserted 15 minutes after the dose. The manufacturer of brimonidine tartrate 0.025% ophthalmic solution states that contact lenses may be reinserted 10 minutes after the dose.
If the patient is receiving more than one topical ophthalmic preparation, the preparations should be administered at least 5 minutes apart.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
No formal drug interaction studies have been performed.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Brimonidine is contraindicated in neonates and infants younger than 2 years of age. (See Pediatric Use under Warnings/Precautions: Specific Populations, in Cautions.) Brimonidine also is contraindicated in patients with known hypersensitivity to the drug or any ingredient in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in approximately 10-30% of patients receiving brimonidine tartrate 0.1-0.2% ophthalmic solution include oral dryness, ocular or conjunctival hyperemia, burning and stinging, allergic conjunctivitis, headache, blurring, foreign body sensation, fatigue/drowsiness, conjunctival follicles, ocular allergic reactions, and ocular pruritus. In addition, corneal staining/erosion, photophobia, eyelid erythema, ocular ache/pain, ocular dryness, tearing, upper respiratory symptoms, eyelid edema, conjunctival edema, dizziness, blepharitis, ocular irritation, GI symptoms, hypertension, asthenia, conjunctival blanching, abnormal vision, visual disturbances, and muscular pain have been reported in approximately 3-9% of patients receiving brimonidine tartrate 0.1-0.2% ophthalmic solution.
Adverse effects reported in approximately 1-4% of patients receiving brimonidine tartrate 0.025% ophthalmic solution include decreased visual acuity, conjunctival or ocular hyperemia, dry eye, instillation site pain, and headache.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Safety and efficacy of topical brimonidine tartrate for the treatment of open-angle glaucoma or ocular hypertension in pediatric patients younger than 2 years of age have not been established. Because potentially serious adverse effects, including apnea, bradycardia, coma, hypotension, hypothermia, hypotonia, lethargy, pallor, respiratory depression, and somnolence, have been reported in infants treated with topical brimonidine tartrate, use of the drug is contraindicated in infants younger than 2 years of age. In a well-controlled clinical study in children 2-7 years of age with glaucoma who received brimonidine tartrate 0.2% ophthalmic solution 3 times daily, the most commonly observed adverse effects were somnolence and decreased mental alertness; approximately 16% of these children discontinued therapy because of somnolence. The incidence of somnolence generally appeared to be age and weight related, occurring in 50-83% of children 2-6 years of age and 25% of those 7 years of age who weighed more than 20 kg.
The individual components of brinzolamide and brimonidine tartrate fixed-combination ophthalmic suspension have been studied in pediatric patients 4 weeks to 5 years of age (brinzolamide) and 2-7 years of age (brimonidine).
Safety and efficacy of brimonidine tartrate and timolol fixed-combination ophthalmic solution in pediatric patients 2-16 years of age have been established based on evidence from adequate and well-controlled studies of the fixed combination in adults and additional data from a study evaluating the individually administered drugs (brimonidine tartrate 0.2% administered 3 times daily as an adjunct to timolol therapy) in children 2-7 years of age with glaucoma.
Safety and efficacy of brimonidine tartrate 0.025% ophthalmic solution for self-medication for relief of ocular redness due to minor irritation have not been established in children younger than 5 years of age. Safety and efficacy in pediatric patients 5 years of age or older are supported by evidence from controlled clinical trials in adults and additional data from a safety study that included both adults and pediatric patients 5 years of age or older.
In studies in animals, brimonidine crossed the placenta and entered the fetal circulation to a limited extent; no evidence of teratogenicity was observed. There are no adequate and well-controlled studies of brimonidine to date in pregnant women. Brimonidine should be used during pregnancy only if potential benefits to the woman justify the potential risk to the fetus.
Brimonidine is distributed into milk in animals. It is not known whether brimonidine is distributed into human milk following topical application to the eye. A decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
No substantial differences in safety and efficacy have been observed between geriatric patients and younger adults.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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