Brimonidine

Pronunciation

(bri MOE ni deen)

U.S. Brand Names

Alphagan® P

Synonyms

Brimonidine Tartrate

Generic Available

Yes

Canadian Brand Names

Alphagan®; PMS-Brimonidine Tartrate; ratio-Brimonidine

Use

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

Pregnancy Risk Factor

Lactation

Excretion in breast milk unknown/contraindicated

Contraindications

Hypersensitivity to brimonidine tartrate or any component of the formulation; patients receiving MAO-inhibitor therapy

Warnings/Precautions

Exercise caution in treating patients with severe cardiovascular disease. Use with caution in patients with depression, cerebral or coronary insufficiency, Raynaud's phenomenon, orthostatic hypotension or thromboangiitis obliterans. Use with caution in patients with hepatic or renal impairment. Safety and efficacy in children <2 years of age have not been established.

Alphagan® contains benzalkonium chloride which may be absorbed by contact lenses; remove contacts prior to administration and wait 15 minutes before reinserting. The IOP-lowering efficacy observed with brimonidine tartrate during the first of month of therapy may not always reflect the long term level of IOP reduction. Routinely monitor IOP.

Adverse Reactions

Alphagan®:

>10%:

Central nervous system: Drowsiness, fatigue, headache

Gastrointestinal: Xerostomia

Ocular: Allergic reactions, blurring, burning, follicular conjunctivitis, foreign body sensation, hyperemia, pruritus, stinging

1% to 10% (unless otherwise noted 3% to 9%):

Cardiovascular: Arrhythmias (<3%), hypertension (<3%), palpitation (<3%), syncope (<3%)

Central nervous system: Dizziness, anxiety (<3%), depression (<3%), insomnia (<3%)

Gastrointestinal: Abnormal taste, nasal dryness (<3%)

Neuromuscular & skeletal: Muscular pain, weakness

Ocular: Corneal staining, corneal erosion, photophobia, eyelid erythema, ocular ache/pain, ocular dryness, tearing, eyelid edema, conjunctival edema, blepharitis, ocular irritation, conjunctival blanching, abnormal vision, lid crusting, conjunctival hemorrhage, conjunctival discharge

Respiratory: Upper respiratory symptoms

Pediatric use: Somnolence and lethargy were reported in up to 83% of patients 2-6 years of age. Children 7 years of age experienced somnolence less frequently (25%).

Alphagan® P:

>10%: Ocular: Allergic conjunctivitis, conjunctival hyperemia, eye pruritus

1% to 10% (unless otherwise noted 1% to 4%):

Cardiovascular: Hypertension (5% to 9%)

Central nervous system: Dizziness, headache

Dermatologic: Rash

Gastrointestinal: Xerostomia (5% to 9%), dyspepsia

Ocular: Burning sensation (5% to 9%), conjunctival folliculosis (5% to 9%), visual disturbance (5% to 9%), blepharitis, conjunctival edema, conjunctival hemorrhage, conjunctivitis, eye discharge, irritation, eyelid edema, eyelid erythema, follicular conjunctivitis, foreign body sensation, pain, photophobia, stinging, superficial punctate keratopathy, visual field defect, vitreous floaters, watery eyes, worsened visual acuity

Respiratory: Bronchitis, cough, dyspnea, pharyngitis, rhinitis, sinus infection

Miscellaneous: Allergic reaction, flu-like syndrome

<1%: Corneal erosion, insomnia, nasal dryness, somnolence, taste perversion

Postmarketing and/or case reports (Alphagan® and Alphagan® P): Agitation, apnea, bradycardia, convulsions, cyanosis, depression, dyspnea, emotional instability, hypotension, hypothermia, hypotonia, hypoventilation, irritability, lethargy, somnolence, and stupor have been reported when used in pediatric patients

Overdosage/Toxicology

No information is available on overdosage in humans. Treatment is supportive and symptomatic.

Drug Interactions

Antihypertensives: Concomitant use may have additive effects

Cardiac glycosides: May increase effects

CNS depressants (eg, ethanol, barbiturates, opiates, sedatives, anesthetics): Concomitant use may have additive or potentiating effects.

Pilocarpine: Additive decrease in intraocular pressure

Topical beta-blockers: Additive decreased intraocular pressure

Tricyclic antidepressants: Can affect the metabolism and uptake of circulating amines, resulting in decreased IOP-lowering effect of brimonidine.

Stability

Store between 15°C to 25°C (59°F to 77°F)

Mechanism of Action

Selective for alpha2-receptors; appears to result in reduction of aqueous humor formation and increase uveoscleral outflow

Pharmacodynamics/Kinetics

Onset of action: Peak effect: 2 hours

Metabolism: Hepatic

Half-life elimination: 2-3 hours

Time to peak, plasma: Alphagan®: 1-4 hours; Alphagan® P: 0.5-2.5 hours

Excretion: Urine (74%)

Dosage

Ophthalmic: Children

2 years of age and Adults: Glaucoma (Alphagan®, Alphagan® P): Instill 1 drop in affected eye(s) 3 times/day (approximately every 8 hours)

Administration

Alphagan®: Remove contact lenses prior to administration; wait 15 minutes before reinserting

Monitoring Parameters

Closely monitor patients who develop fatigue or drowsiness; IOP

Patient Education

For use in eyes only. Wash hands before instilling. 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. Wait at least 15 minutes after instilling brimonidine tartrate before reinserting soft contact lenses. Breast-feeding precaution: Do not breast-feed.

Additional Information

The use of Purite® as a preservative in Alphagan® P has lead to a reduced incidence of certain adverse effects associated with Alphagan®, which uses benzalkonium chloride as a preservative.

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

Dosage Forms

Solution, ophthalmic, as tartrate:

Alphagan® P: 0.15% (5 mL, 10 mL, 15 mL) [contains Purite® 0.005% as preservative]

International Brand Names

Agglad ofteno® (MX); Alphagan® (AR, AT, AU, BE, BR); Alphagan™ (CA); Alphagan® (CH, CL, CO, CR, CZ, DE, DK, ES, FI, FR, GB, GT, HR, HU, IE, IL, IT, MX, NL, NO, NZ, PA, PL, PT, SE, SG, SV, TH, TR, ZA); Oftalmotonil® (AR); PMS-Brimonidine Tartrate (CA); ratio-Brimonidine (CA)

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