Alphagan-P®
Brimonidine 0.1%, 0.15%, 0.2% B&L · ophthalmic solution
Antiglaucoma
Approved uses
Elevated IOP in open-angle glaucoma or ocular hypertension
1 drop in the affected eye(s) TID, approximately 8 hours apart
IOP control equals brimonidine 0.2% with 41% less allergic conjunctivitis over 12 months.
Adjunctive IOP lowering added to a prostaglandin analog
1 drop TID added to latanoprost 0.005% QHS; instill at least 5 minutes apart from the other drop
Added to latanoprost, mean diurnal IOP fell from 19.6 to 16.3 mm Hg at 3 months.
OFF-LABELNot in the FDA label for this product
IOP spike prophylaxis for Nd:YAG posterior capsulotomy
1 drop 1 hour before the laser and 1 drop immediately after
RCT · n=106 · single-site
Prospective, double-masked, randomized trial, 106 eyes, comparing 0.15% Purite, 0.2%, and vehicle: both active arms fell 2.2 to 2.7 mm Hg below baseline while vehicle rose. Elevations under 5 mm Hg occurred in 27.8% of the 0.15% Purite arm, 22.9% of the 0.2% arm, and 48.6% of vehicle; spikes above 10 mm Hg in 2.8%, 2.9%, and 8.6%. Single-center, and the two strengths did not differ from each other.
Low-pressure (normal-tension) glaucoma, visual field preservation
Trial dose was brimonidine 0.2% BID, not the 0.1% or 0.15% strengths and not the labeled TID frequency
RCT · very low certainty
LoGTS randomized, double-masked, multicenter trial, 178 patients with untreated IOP 21 mm Hg or lower: field progression by pointwise linear regression in 9.1% on brimonidine 0.2% BID versus 39.2% on timolol 0.5% BID (p=0.001) at equivalent treated IOP, but 28.3% versus 11.4% withdrew for drug-related adverse events. A Cochrane review graded the finding very low certainty because 40.5% never completed 4 years and attrition was unbalanced (55% brimonidine versus 29% timolol), and concluded no reliable inference could be drawn.
Contraindications
- Neonates and infants younger than 2 years old.
- Hypersensitivity to any component of the formulation.
0.1% (1 mg/mL) and 0.15% (1.5 mg/mL) Purite-preserved solution, 5 mL, 10 mL, and 15 mL bottles in each strength
Relatively selective alpha-2 adrenergic agonist with a dual mechanism, reducing aqueous humor production and increasing uveoscleral outflow. Peak ocular hypotensive effect occurs about 2 hours after instillation.
Warnings & Precautions
- Infant CNS and respiratory depression: Apnea, bradycardia, hypotension, hypothermia, hypotonia, lethargy, pallor, respiratory depression, and somnolence reported in infants; contraindicated under 2 years.
- Vascular insufficiency: May potentiate syndromes associated with vascular insufficiency; caution in depression, cerebral or coronary insufficiency, Raynaud's phenomenon, orthostatic hypotension, or thromboangiitis obliterans.
- Severe cardiovascular disease: Minimal blood pressure effect in clinical studies, but caution in severe cardiovascular disease.
- Delayed-onset ocular allergy: Follicular conjunctivitis and contact dermatoconjunctivitis accrue steadily over months rather than peaking early, reaching a cumulative rate near 26% in a practice-based cohort of the 0.2% concentration; a mean onset near 8 months comes from 5 reactors in a small apraclonidine-allergic subgroup and should not be read as a general time course.
- Sedation and reduced alertness: Fatigue and drowsiness occur; relevant for drivers and patients in hazardous occupations.
- Systemic drug interactions: Additive blood pressure lowering with antihypertensives or cardiac glycosides; additive sedation with CNS depressants; MAO inhibitors may increase systemic hypotension; caution with tricyclic antidepressants.
- Tip contamination: Bacterial keratitis has followed use of contaminated multidose containers; keep the tip off the eye and adnexa.
Common Side Effects
- Ocular: Allergic conjunctivitis, conjunctival hyperemia, and eye pruritus in 10% to 20%; burning, conjunctival folliculosis, ocular allergic reaction, and visual disturbance in 5% to 9%; blepharitis, follicular conjunctivitis, keratitis, superficial punctate keratopathy, dry eye, blurred vision, and foreign body sensation in 1% to 4%.
- Systemic: Hypertension and oral dryness in 5% to 9%; headache, somnolence, fatigue, dizziness, insomnia, hypotension, altered taste, and upper respiratory symptoms in 1% to 4%.
- Postmarketing: Bradycardia, tachycardia, syncope, depression, iritis, miosis, and keratoconjunctivitis sicca; frequency not estimable.
Pregnancy: No adequate and well-controlled studies in pregnant women and human data are insufficient; oral dosing in rabbits caused miscarriage at 5 mg/kg/day (about 50 to 70 times the ophthalmic dose by AUC) with no treatment-related malformations in rabbits or rats. Use only if benefit justifies fetal risk.
Lactation: Not recommended during lactation given the risk of CNS depression and apnea in nursing infants; human milk excretion unknown, present in rat milk.
Contraindicated under 2 years; somnolence 50% to 83% at ages 2 to 6 and 25% at 7 and older on the 0.2% concentration TID.