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Pronunciation
(bri MOE ni deen)
Generic Available (U.S.)
Yes
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Lowering of intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension
Pregnancy Risk Factor
B
Pregnancy Considerations
Teratogenic effects were not observed in animal studies. There are no adequate and well-controlled studies in pregnant women.
Lactation
Excretion in breast milk unknown/not recommended
Contraindications
Hypersensitivity to brimonidine tartrate or any component of the formulation; during or within 14 days of MAO inhibitor therapy
Warnings/Precautions
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns:
• Cardiovascular disease: Use with caution in patients with severe cardiovascular disease.
• Cerebrovascular insufficiency: Use with caution in patients with cerebral insufficiency.
• Depression: Use with caution in patients with depression.
• Hepatic impairment: Use with caution in patients with hepatic impairment; not studied.
• Orthostatic hypotension: Use with caution in patients with orthostatic hypotension.
• Raynaud's phenomenon: Use with caution in patients with Raynaud's phenomenon.
• Renal impairment: Use with caution in patients with renal impairment; not studied.
• Thromboangiitis obliterans: Use with caution in patients with thromboangiitis obliterans.
Special populations:
• Contact lens wearers: Some formulations may contain benzalkonium chloride which may be adsorbed by soft contact lenses; remove contacts prior to administration and wait 15 minutes before reinserting.
• Pediatrics: Systemic absorption has been reported; children are at higher risk of systemic adverse events (Levy, 2004).
Other warnings/precautions:
• Monitoring efficacy: The IOP-lowering efficacy observed during the first month of therapy may not always reflect the long-term level of IOP reduction; routinely monitor IOP.
Adverse Reactions
Actual frequency of adverse reactions may be formulation dependent; percentages reported with Alphagan® P:
>10%:
Central nervous system: Somnolence (adults 1% to 4%; children 25% to 83%)
Ocular: Allergic conjunctivitis, conjunctival hyperemia, eye pruritus
1% to 10% (unless otherwise noted 1% to 4%):
Cardiovascular: Hypertension (5% to 9%), hypotension
Central nervous system: Alertness decreased (children), dizziness, fatigue, headache, insomnia
Dermatologic: Rash
Endocrine & metabolic: Hypercholesterolemia
Gastrointestinal: Xerostomia (5% to 9%), dyspepsia
Neuromuscular & skeletal: Weakness
Ocular: Burning sensation (5% to 9%), conjunctival folliculosis (5% to 9%), ocular allergic reaction (5% to 9%), visual disturbance (5% to 9%), blepharitis, blepharoconjunctivitis, blurred vision, cataract, conjunctival edema, conjunctival hemorrhage, conjunctivitis, dry eye, epiphora, eye discharge, eyelid disorder, eyelid edema, eyelid erythema, follicular conjunctivitis, foreign body sensation, irritation, keratitis, pain, photophobia, stinging, superficial punctate keratopathy, visual acuity worsened, visual field defect, vitreous detachment, vitreous floaters, watery eyes
Respiratory: Bronchitis, cough, dyspnea, pharyngitis, rhinitis, sinus infection, sinusitis
Miscellaneous: Allergic reaction, flu-like syndrome, infection
<1%: Corneal erosion, hordeolum, nasal dryness, taste perversion
Postmarketing and/or case reports: Anterior uveitis, bradycardia, depression, iritis, keratoconjunctivitis sicca, miosis, nausea, skin reactions (erythema, eyelid pruritus, vasodilation), tachycardia; apnea, bradycardia, hypothermia, and hypotonia have been reported in infants
Metabolism/Transport Effects
None known.
Drug Interactions
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Risk C: Monitor therapy
Hypotensive Agents: May enhance the adverse/toxic effect of other Hypotensive Agents. Risk C: Monitor therapy
MAO Inhibitors: May enhance the hypertensive effect of Alpha2-Agonists (Ophthalmic). Risk X: Avoid combination
MAO Inhibitors: May enhance the orthostatic hypotensive effect of Orthostatic Hypotension Producing Agents. Risk C: Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Herb/Nutraceutical: Avoid herbs with hypertensive properties (bayberry, blue cohosh, cayenne, ephedra, ginger, ginseng, gotu kola, licorice); may diminish antihypertensive effect. Avoid herbs with hypotensive properties (black cohosh, California poppy, coleus, golden seal, hawthorn, mistletoe, periwinkle, quinine, shepherd's purse); may enhance hypotensive effect.
Storage
Store between 15°C to 25°C (59°F to 77°F).
Mechanism of Action
Selective agonism for alpha2-receptors; causes reduction of aqueous humor formation and increased uveoscleral outflow
Pharmacodynamics/Kinetics
Onset of action: Peak effect: 2 hours
Metabolism: Hepatic
Half-life elimination: ~2 hours
Time to peak, plasma: 0.5-2.5 hours
Excretion: Urine (74%)
Dosage
Ophthalmic: Children ≥2 years and Adults: Glaucoma, ocular hypertension: Instill 1 drop in affected eye(s) 3 times/day (approximately every 8 hours)
Administration: Other
Remove contact lenses prior to administration; wait 15 minutes before reinserting if using products containing benzalkonium chloride. Separate administration of other ophthalmic agents by 5 minutes.
Monitoring Parameters
Closely monitor patients who develop fatigue or drowsiness; IOP
Patient Education
For use in eyes only. Wash hands before instilling. Remove contacts prior to administration and wait 15 minutes before reinserting. Sit or lie down to instill. Open eye, look at ceiling, and instill prescribed amount of solution. Apply gentle pressure to inner corner of eye. Do not let tip of applicator touch eyes; do not contaminate tip of applicator (may cause eye infection, eye damage, or vision loss). Brimonidine tartrate may cause fatigue or drowsiness in some patients. Avoid engaging in hazardous activities due to potential for decreased mental alertness until response known. Wait at least 15 minutes after instilling brimonidine tartrate before reinserting soft contact lenses.
Geriatric Considerations
Evaluate the patient's or caregiver's ability to safely administer the correct dose of ophthalmic medication.
Additional Information
The use of Purite® as a preservative in Alphagan® P has lead to a reduced incidence of certain adverse effects associated with products using benzalkonium chloride as a preservative. The 0.1% and 0.15% solutions are comparable to the 0.2% solution in lowering intraocular pressure.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Drowsiness is common
Mental Health: Effects on Psychiatric Treatment
Contraindicated with MAO inhibitors; concurrent use with psychotropics may produce additive sedation
Nursing: Physical Assessment/Monitoring
Monitor intraocular pressure periodically.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, ophthalmic, as tartrate [drops]: 0.15% (5 mL, 10 mL, 15 mL); 0.2% (5 mL, 10 mL, 15 mL)
Alphagan® P: 0.1% (5 mL, 10 mL, 15 mL); 0.15% (5 mL, 10 mL, 15 mL) [contains Purite®]
Pricing: U.S. (www.drugstore.com)
Solution (Alphagan P)
0.1% (5): $76.99
0.1% (10): $154.95
0.1% (15): $232.95
0.15% (5): $88.55
0.15% (10): $168.99
0.15% (15): $259.99
Solution (Brimonidine Tartrate)
0.15% (5): $70.99
0.15% (10): $134.99
0.15% (15): $174.99
0.2% (5): $25.99
0.2% (10): $51.99
0.2% (15): $51.96
References
Byles DB, Frith P, and Salmon JF, “Anterior Uveitis as a Side Effect of Topical Brimonidine,” Am J Ophthalmol, 2000, 130(3):287-91.
Levy Y and Zadok D, “Systemic Side Effects of Ophthalmic Drops,” Clin Pediatr (Phila), 2004, 43(1):99-101.
International Brand Names
Lexi-Comp.com
Last full review/revision October 2011
Content last modified October 2011
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