Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Ophthalmic, as tartrate:
Alphagan P: 0.1% (5 mL, 10 mL, 15 mL); 0.15% (5 mL, 10 mL, 15 mL)
Lumify: 0.025% (2.5 mL, 7.5 mL) [contains benzalkonium chloride]
Generic: 0.15% (5 mL, 10 mL, 15 mL); 0.2% (5 mL, 10 mL, 15 mL)
Pharmacology
Mechanism of Action
A relatively selective alpha-2 adrenergic agonist; causes reduction of aqueous humor formation and increased uveoscleral outflow
Pharmacokinetics/Pharmacodynamics
Metabolism
Hepatic (extensive)
Excretion
Urine (74%)
Time to Peak
Plasma: 1 to 4 hours
Half-Life Elimination
~3 hours
Use: Labeled Indications
Elevated intraocular pressure: Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension
Ocular redness (OTC only): Relief of redness of the eye due to minor eye irritations
Contraindications
Hypersensitivity to brimonidine or any component of the formulation; neonates and infants <2 years; concomitant MAO inhibitor therapy
Dosage and Administration
Dosing: Adult
Elevated intraocular pressure:
US labeling: Ophthalmic (0.1%, 0.15%, 0.2% solution): Instill 1 drop in affected eye(s) 3 times/day (approximately every 8 hours)
Canadian labeling: Ophthalmic:
Solution 0.15%: Instill 1 drop in affected eye(s) 3 times/day (approximately every 8 hours)
Solution 0.2%: Instill 1 drop in affected eye(s) 2 times/day (approximately every 12 hours)
Ocular redness (OTC): Ophthalmic (0.025% solution): Instill 1 drop in affected eye(s) every 6 to 8 hours up to 4 times daily
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Glaucoma, ocular hypertension: Children ≥2 years and Adolescents: Ophthalmic solution (0.1%, 0.15%, or 0.2%): Ophthalmic: Instill 1 drop into lower conjunctival sac of affected eye(s) 3 times daily (approximately every 8 hours)
Ocular redness: Children ≥5 years: Ophthalmic solution (0.025%): Ophthalmic: Instill 1 drop info affected eye(s) every 6 to 8 hours as needed up to 4 times daily
Administration
Ophthalmic: Remove contact lenses prior to administration; wait 15 minutes before reinserting if using products containing benzalkonium chloride. Separate administration of other ophthalmic agents by at least 5 minutes. Do not touch tip of container to any surface, the eyelids, or the surrounding area.
Storage
Store at 15°C to 25°C (59°F to 77°F).
Drug Interactions
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Monitor therapy
Alizapride: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). Avoid combination
Beta-Blockers: Alpha2-Agonists may enhance the AV-blocking effect of Beta-Blockers. Sinus node dysfunction may also be enhanced. Beta-Blockers may enhance the rebound hypertensive effect of Alpha2-Agonists. This effect can occur when the Alpha2-Agonist is abruptly withdrawn. Management: Closely monitor heart rate during treatment with a beta blocker and clonidine. Withdraw beta blockers several days before clonidine withdrawal when possible, and monitor blood pressure closely. Recommendations for other alpha2-agonists are unavailable. Exceptions: Levobunolol; Metipranolol. Consider therapy modification
Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Consider therapy modification
Brexanolone: CNS Depressants may enhance the CNS depressant effect of Brexanolone. Monitor therapy
Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Bromopride: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Bromperidol: May enhance the CNS depressant effect of CNS Depressants. Avoid combination
Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine at lower doses in patients already receiving CNS depressants. Consider therapy modification
Cannabidiol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Cannabis: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Chlormethiazole: May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used. Consider therapy modification
Chlorphenesin Carbamate: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Monitor therapy
Dimethindene (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Monitor therapy
Dronabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Consider therapy modification
Esketamine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Consider therapy modification
HYDROcodone: CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Consider therapy modification
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy
Lemborexant: May enhance the CNS depressant effect of CNS Depressants. Management: Dosage adjustments of lemborexant and of concomitant CNS depressants may be necessary when administered together because of potentially additive CNS depressant effects. Close monitoring for CNS depressant effects is necessary. Consider therapy modification
Lofexidine: May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs. Monitor therapy
Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Consider therapy modification
MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Monitor therapy
Mianserin: May diminish the therapeutic effect of Alpha2-Agonists (Ophthalmic). Avoid combination
Minocycline (Systemic): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Mirtazapine: May diminish the antihypertensive effect of Alpha2-Agonists. Management: Consider avoiding concurrent use. If the combination cannot be avoided, monitor for decreased effects of alpha2-agonists if mirtazapine is initiated/dose increased, or increased effects if mirtazapine is discontinued/dose decreased. Consider therapy modification
Monoamine Oxidase Inhibitors: May enhance the adverse/toxic effect of Brimonidine (Ophthalmic). Monoamine Oxidase Inhibitors may increase the serum concentration of Brimonidine (Ophthalmic). Monitor therapy
Nabilone: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Opioid Agonists: CNS Depressants may enhance the CNS depressant effect of Opioid Agonists. Management: Avoid concomitant use of opioid agonists and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Consider therapy modification
Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Avoid combination
Oxomemazine: May enhance the CNS depressant effect of CNS Depressants. Avoid combination
OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Consider therapy modification
Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Avoid combination
Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Consider therapy modification
Piribedil: CNS Depressants may enhance the CNS depressant effect of Piribedil. Monitor therapy
Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Monitor therapy
ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Monitor therapy
Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Monitor therapy
Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Monitor therapy
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Monitor therapy
Serotonin/Norepinephrine Reuptake Inhibitors: May diminish the antihypertensive effect of Alpha2-Agonists. Monitor therapy
Sodium Oxybate: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. Consider therapy modification
Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Consider therapy modification
Tapentadol: May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug. Consider therapy modification
Tetrahydrocannabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Tetrahydrocannabinol and Cannabidiol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Avoid combination
Tricyclic Antidepressants: May diminish the therapeutic effect of Alpha2-Agonists (Ophthalmic). Monitor therapy
Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy
Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Consider therapy modification
Adverse Reactions
Actual frequency of adverse reactions may be formulation dependent; percentages reported with Alphagan P:
>10%:
Central nervous system: Drowsiness (children 25% to 83%; adults 1% to 4%)
Ophthalmic: Allergic conjunctivitis, conjunctival hyperemia, eye pruritus
1% to 10% (unless otherwise noted 1% to 4%):
Cardiovascular: Hypertension (5% to 9%), hypotension
Central nervous system: Dizziness, fatigue, foreign body sensation of eye, headache, impaired consciousness (children), insomnia
Dermatologic: Erythema of eyelid, skin rash
Endocrine & metabolic: Hypercholesterolemia
Gastrointestinal: Xerostomia (5% to 9%), dyspepsia
Hypersensitivity: Local ocular hypersensitivity reaction (5% to 9%), hypersensitivity reaction
Infection: Infection
Neuromuscular & skeletal: Weakness
Ophthalmic: Burning sensation of eyes (5% to 9%), follicular conjunctivitis (5% to 9%), visual disturbance (5% to 9%), blepharitis, blepharoconjunctivitis, blurred vision, cataract, conjunctival edema, conjunctival hemorrhage, conjunctivitis, decreased visual acuity, dry eye syndrome, epiphora, eye discharge, eye irritation, eyelid disease, eyelid edema, eye pain, keratitis, photophobia, stinging of eyes, superficial punctate keratitis, visual field defect, vitreous detachment, vitreous opacity, watery eyes
Respiratory: Bronchitis, cough, dyspnea, flu-like symptoms, pharyngitis, rhinitis, sinus infection, sinusitis
<1%, postmarketing, and/or case reports: Anterior uveitis, apnea (infants), bradycardia, corneal erosion, depression, dermatological reaction (erythema, eyelid pruritus, vasodilation), dry nose, dysgeusia, hordeolum, hypothermia (infants), hypotonia (infants), iritis, keratoconjunctivitis sicca, miosis, nausea, tachycardia
Warnings/Precautions
Concerns related to adverse effects:
- Bacterial keratitis: Inadvertent contamination of multiple-dose ophthalmic solutions has caused bacterial keratitis.
- CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns:
- Cardiovascular disease: Use with caution in patients with severe cardiovascular disease or coronary insufficiency.
- Cerebrovascular insufficiency: Use with caution in patients with cerebral insufficiency.
- Hepatic impairment: Use with caution in patients with hepatic impairment (has not been studied).
- Orthostatic hypotension: Use with caution in patients with orthostatic hypotension.
- Raynaud phenomenon: Use with caution in patients with Raynaud phenomenon.
- Renal impairment: Use with caution in patients with renal impairment (has not been studied).
- Thromboangiitis obliterans: Use with caution in patients with thromboangiitis obliterans.
Concurrent drug therapy issues:
- Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed.
Special populations:
- Contact lens wearers: Some formulations may contain benzalkonium chloride which may be adsorbed by soft contact lenses; remove contacts prior to administration and wait 15 minutes before reinserting.
- Pediatric: Systemic absorption has been reported; children are at higher risk of systemic adverse events (Levy, 2004). Use is contraindicated in children <2 years of age.
Other warnings/precautions:
- Self-medication (OTC use): Discontinue use and contact health care provider if eye pain or changes in vision occur; redness or irritation of the eye continues, or condition worsens or persists for >3 days. Do not use if solution changes color or becomes cloudy.
Monitoring Parameters
IOP routinely (first month of therapy may not reflect long-term level of IOP reduction)
Pregnancy
Pregnancy Risk Factor
B
Pregnancy Considerations
Teratogenic effects were not observed in animal reproduction studies.
Patient Education
What is this drug used for?
- It is used to lower high eye pressure.
- It is used to treat glaucoma.
- Some products are used to treat eye redness.
Frequently reported side effects of this drug
- Burning
- Stinging
- Blurred vision
- Foreign body sensation in eye
- Headache
- Loss of strength and energy
- Fatigue
- Dry mouth
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
- Vision changes
- Eye pain
- Severe eye irritation
- Eyelid swelling
- Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
