Alphagan (brimonidine tartrate ophthalmic solution) 0.1% and 0.15% is a prescription alpha-2 adrenergic agonist indicated for the lowering of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. As a first-line therapeutic option, it offers a well-established mechanism of action with a favorable safety profile. This medication works by reducing aqueous humor production and increasing uveoscleral outflow, providing dual-action pressure control critical for preserving optic nerve health. Alphagan represents a cornerstone in glaucoma management protocols, particularly suitable for patients requiring adjunctive therapy or those intolerant to beta-blockers.

Features

• Contains brimonidine tartrate 0.1% or 0.15% as active pharmaceutical ingredient
• Preservative-free formulation available (Alphagan P) utilizing Purite® preservative system
• Clear, isotonic ophthalmic solution with pH range of 6.3-7.3
• Multi-dose plastic dispenser bottle with controlled drop tip
• Refrigeration not required after opening
• Compatible with most contact lens materials (wait 15 minutes after instillation)

Benefits

• Provides consistent 20-27% reduction in intraocular pressure from baseline
• Dual mechanism of action reduces aqueous production and enhances uveoscleral outflow
• Demonstrates neuroprotective properties potentially preserving retinal ganglion cells
• Lower incidence of cardiovascular effects compared to beta-blockers
• Minimal impact on pulmonary function, making it suitable for asthmatic patients
• Preservative-free option reduces risk of ocular surface disease with long-term use

Common use

Alphagan is primarily prescribed for the management of open-angle glaucoma, the most prevalent form of glaucoma characterized by impaired aqueous outflow through the trabecular meshwork. It is also indicated for ocular hypertension, where elevated intraocular pressure exists without detectable optic nerve damage or visual field loss. Clinicians frequently employ Alphagan as monotherapy in patients contraindicated for beta-blockers or as adjunctive therapy when single-agent treatment provides insufficient IOP control. The medication has shown particular utility in normal-tension glaucoma cases where additional pressure reduction is desired despite statistically normal IOP measurements. Off-label uses include prevention of intraocular pressure spikes following laser procedures and management of pediatric glaucoma in patients over two years of age.

Dosage and direction

The recommended dosage is one drop in the affected eye(s) three times daily, approximately eight hours apart. Patients should wash hands thoroughly before administration. To instill: tilt head backward, pull down the lower eyelid to form a pouch, place one drop into the conjunctival sac, and close eyes gently. Apply gentle pressure to the lacrimal sac (inner corner of eye) for 1-2 minutes to minimize systemic absorption. Wait at least five minutes between instilling different ophthalmic medications if using multiple therapies. Do not touch the dropper tip to any surface to avoid contamination. The prescribed concentration (0.1% or 0.15%) should be maintained consistently unless directed otherwise by the prescribing physician.

Precautions

Patients should be advised that Alphagan may cause drowsiness, dizziness, or blurred vision that could impair physical coordination and mental alertness. Caution should be exercised when driving, operating machinery, or performing hazardous activities requiring clear vision. Contact lens wearers should remove lenses prior to administration and wait at least 15 minutes before reinsertion. Systemic absorption may occur through nasolacrimal drainage, potentially exacerbating cardiovascular conditions. Regular monitoring of IOP, visual fields, and optic nerve head morphology is essential throughout treatment. Pediatric patients may experience heightened sensitivity to brimonidine’s effects, requiring careful dose titration. Elderly patients may exhibit increased susceptibility to hypotensive effects and should be monitored for orthostatic changes.

Contraindications

Alphagan is contraindicated in patients with known hypersensitivity to brimonidine tartrate or any component of the formulation. It should not be used in patients receiving monoamine oxidase inhibitor (MAOI) therapy due to potential hypertensive crisis. The medication is contraindicated in infants and children under 2 years of age due to risk of severe central nervous system depression, apnea, and bradycardia. Patients with untreated angle-closure glaucoma should not receive Alphagan until appropriate iridotomy has been performed. Those with severe cardiovascular disease, including uncontrolled hypertension or hypotension, may require alternative therapies. Concurrent use with central alpha-2 agonists for systemic hypertension is generally contraindicated.

Possible side effects

Ocular adverse reactions occur in approximately 10-30% of patients and include allergic conjunctivitis (15%), conjunctival hyperemia (10%), burning and stinging (10%), blurring (5%), foreign body sensation (5%), conjunctival folliculosis (5%), and ocular pruritus (5%). Dry mouth occurs in up to 30% of patients, typically diminishing with continued therapy. Systemic effects may include fatigue/drowsiness (15%), headache (10%), dizziness (5%), and nasal dryness (3%). Less common reactions include corneal erosion/ulceration, photophobia, eyelid erythema, and visual disturbance. Serious but rare adverse events include syncope, hypotension, bradycardia, and apnea. Allergic reactions may manifest as ocular itching, redness, and swelling that typically resolve upon discontinuation.

Drug interaction

Concomitant use with CNS depressants (alcohol, barbiturates, opioids) may potentiate sedative effects. Tricyclic antidepressants may antagonize Alphagan’s IOP-lowering effects. Beta-blockers, calcium channel blockers, and digitalis may enhance cardiovascular effects including bradycardia and hypotension. MAO inhibitors may precipitate hypertensive crisis. Antihypertensive agents may have additive hypotensive effects. Topical non-steroidal anti-inflammatory drugs may reduce Alphagan’s efficacy. Anesthetics that affect cardiovascular regulation may have synergistic effects. Patients using other ocular medications should administer them at least 5 minutes apart to avoid wash-out effects.

Missed dose

If a dose is missed, administer it as soon as possible. However, if it is nearly time for the next scheduled dose, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed administration. Maintain the recommended eight-hour interval between doses whenever possible. Consistent dosing is important for maintaining stable intraocular pressure control, but occasional missed doses are unlikely to significantly affect long-term pressure management. Patients should maintain a regular dosing schedule and consider using reminder systems if missed doses occur frequently.

Overdose

Ocular overdose may result in increased local adverse effects including conjunctival blanching, rebound hyperemia, and ocular irritation. Systemic overdose symptoms may include hypotension, bradycardia, hypothermia, apnea, sedation, lethargy, and coma. Management involves supportive care with monitoring of vital signs. Activated charcoal may be considered if recent ingestion occurs. Atropine may reverse bradycardia, while intravenous fluids and vasopressors may address hypotension. Hemodialysis is unlikely to be effective due to brimonidine’s protein binding and volume of distribution. Patients should seek immediate medical attention if accidental ingestion occurs or if systemic symptoms develop.

Storage

Store at controlled room temperature between 15-30°C (59-86°F). Protect from light and excessive heat. Keep the bottle tightly closed when not in use. Do not freeze the solution. Discard any unused solution 28 days after opening the bottle, even if medication remains. Do not use if the solution changes color or becomes cloudy. Keep out of reach of children and pets. Do not transfer the solution to any other container. Store upright to prevent leakage and contamination.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Individual patient responses may vary. The prescribing physician should be consulted for specific medical advice, diagnosis, and treatment. Always follow the instructions provided by your healthcare professional and the medication guide accompanying the product. Do not discontinue or modify treatment without consulting your physician. Report any adverse reactions to your healthcare provider promptly.

Reviews

Clinical studies demonstrate Alphagan’s efficacy in numerous randomized controlled trials. The Brimonidine Study Group reported mean IOP reduction of 22-27% from baseline with three-times-daily dosing. Long-term extension studies show maintained efficacy over 12 months with consistent safety profile. Patient satisfaction surveys indicate high tolerability compared to beta-blockers, particularly regarding respiratory and cardiovascular parameters. Real-world evidence from glaucoma registries supports its position as preferred adjunctive therapy. The medication receives consistently high marks from clinicians for its predictable efficacy and manageable side effect profile, though some note the need for TID dosing compared to newer once-daily alternatives.