Brimonidine

ALPHAGAN

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Pronunciation: bri-MOE-ni-deen

Brimonidine ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Brimonidine ballicule

Brimonidine mascot mnemonic cartoon — Visual mnemonic: Brimonidine mascot
**“Brimo, needy Alpha agonist”**
orange plus signs → alpha-2 agonist

What it isTopical alpha-2 agonist that reduces aqueous production or constricts cutaneous vessels; glaucoma and rosacea.

Why this oneIt lowers intraocular pressure without beta blockade and its facial gel directly blanches persistent rosacea erythema.

What limits itSomnolence and apnea can occur in small children; ocular allergy and rebound facial redness can end treatment.

Brimonidine molecular structure (skeletal formula) — Molecular structure: Brimonidine

FDA-approved for

glaucoma (1996)
rosacea (2013)

FDA label

Read the full label on DailyMed ↗

FDA dosing	Population	Start	Target	Max
Reduction of elevated IOP in open-angle glaucoma or ocular hypertension	adults & children ≥2 y	1 drop affected eye(s) TID (~8 h apart)	1 drop TID	1 drop TID

Renal Undefined

Hepatic Undefined

Instructions

Instill 1 drop in affected eye(s) three times daily, ~8 hours apart
May be used with other topical ophthalmic IOP-lowering products; instill different products ≥5 minutes apart
Do not touch dispenser tip to eye (contamination/bacterial keratitis risk)

Available strengths

drops 0.025, 0.1, 0.15, 0.2 %
sol 1.5, 2 mg/mL
gel 0.33 %

Contraindications

Neonates and infants (younger than 2 years)

Cautions

May potentiate vascular insufficiency — caution in depression, cerebral or coronary insufficiency, Raynaud's phenomenon, orthostatic hypotension, thromboangiitis obliterans
Caution in severe cardiovascular disease
Contaminated multi-dose containers have caused bacterial keratitis
Pediatric ≥2 y: somnolence and decreased alertness common (less frequent ≥7 y/>20 kg)

Adverse reactions

Allergic conjunctivitis
Conjunctival hyperemia
Eye pruritus
Burning sensation
Conjunctival folliculosis
Hypertension
Ocular allergic reaction
Oral dryness
Visual disturbance

Pregnancy No adequate human studies; crosses placenta in animals; use only if benefit justifies fetal risk

Lactation Unknown if in human milk (present in rat milk); not recommended during lactation — risk of CNS depression and apnea in nursing infants

Cost

Brimonidine (ALPHAGAN)

Strength		#/mo	CostPlus
0.025 %	drops	per unit	not offered
0.1 %	drops	per unit	not offered
0.15 %	drops	per unit	not offered
0.2 %	drops	per unit	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Brimonidine is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Generic entry2003

NO BOXED WARNINGS

Principal riskSomnolence, marked in small children

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability1 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk1 / 4

Legacy pregnancy categoryUnknown / historical label unavailable

Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.

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