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 oneLowers 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.

Pearls

Contraindicated under age 2; caution ages 2–6.
Rosacea gel fades redness only; papules and pustules unaffected.
Systemic absorption: fatigue and drowsiness even in adults.

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

Brimonidine prescription history

Animated chart of estimated U.S. prescriptions per year, Glaucoma medicines (1900–2026). Brimonidine enters in 1996 (estimated).

FDA-approved for

glaucoma (1996)
rosacea (2013)

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.

FDA label

Read the full label on DailyMed ↗

NO BOXED WARNINGS

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

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Self-check

What serious effects can brimonidine cause in small children?
Somnolence and apnea.
What does brimonidine facial gel directly blanch?
Persistent rosacea erythema.