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Brimonidine (Ophthalmic)

Pronunciation

(bri MOE ni deen)

Index Terms

  • Alphagan
  • Brimonidine Tartrate

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) [contains carboxymethylcellulose sodium]

Generic: 0.15% (5 mL, 10 mL, 15 mL); 0.2% (5 mL, 10 mL, 15 mL)

Brand Names: U.S.

  • Alphagan P

Pharmacologic Category

  • Alpha2 Agonist, Ophthalmic
  • Ophthalmic Agent, Antiglaucoma

Pharmacology

A relatively selective alpha-2 adrenergic agonist; causes reduction of aqueous humor formation and increased uveoscleral outflow

Metabolism

Hepatic (extensive)

Excretion

Urine (74%)

Time to Peak

Plasma: 0.5 to 4 hours

Half-Life Elimination

~2 to 3 hours

Use: Labeled Indications

Elevated intraocular pressure: Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension

Contraindications

Hypersensitivity to brimonidine or any component of the formulation; neonates and infants <2 years; concomitant MAO inhibitor therapy

Dosing: Adult

Elevated intraocular pressure:

US labeling: Ophthalmic: 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)

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

US labeling: Children ≥2 years and Adolescents: Refer to adult dosing.

Canadian labeling: Children ≥2 years and Adolescents: Use is not recommended.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).

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.

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

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

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

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 patches (Butrans brand) at 5 mcg/hr in adults when used with other CNS depressants. Consider therapy modification

Cannabis: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Monitor therapy

Dimethindene: 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 (e.g., opioids, barbiturates) with concomitant use. Consider therapy modification

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: Consider starting with a 20% to 30% lower hydrocodone dose when using together with any other CNS depressant. Dose reductions in the other CNS depressant may also be warranted. Consider therapy modification

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Iobenguane I 123: Alpha2-Agonists may diminish the therapeutic effect of Iobenguane I 123. Avoid combination

Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

MAO Inhibitors: May enhance the adverse/toxic effect of Brimonidine (Ophthalmic). MAO Inhibitors may increase the serum concentration of Brimonidine (Ophthalmic). 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: 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

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Avoid combination

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: When oxycodone is combined with another CNS depressant, a dose reduction of one or both agents should be considered. The extended release oxycodone starting dose should be reduced 50% to 67% when initiated in patients already receiving CNS depressants. 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 [INT]: CNS Depressants may enhance the CNS depressant effect of Piribedil [INT]. 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: Start tapentadol at a dose of one-third to one-half of the normal dose if being initiated in a patient who is taking another drug with CNS depressant effects. Monitor closely for evidence of excessive CNS depression. Consider therapy modification

Tetrahydrocannabinol: 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% (Limited to important or life-threatening): Anterior uveitis, apnea (infants), bradycardia, corneal erosion, depression, dermatological reaction (erythema, eyelid pruritus, vasodilatation), 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.

• Depression: Use with caution in patients with depression.

• 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's phenomenon: Use with caution in patients with Raynaud's 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.

Monitoring Parameters

IOP routinely (first month of therapy may not reflect long-term level of IOP reduction)

Pregnancy Risk Factor

B

Pregnancy Considerations

Teratogenic effects were not observed in animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience burning, stinging, blurred vision, foreign body sensation in eye, headache, loss of strength and energy, fatigue, or dry mouth. Have patient report immediately to prescriber vision changes, eye pain, severe eye irritation, or eyelid edema (HCAHPS).

• Educate patient about signs of a significant reaction (eg, 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. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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