Brimonidine Ophthalmic Advanced Patient Information

Brimonidine Ophthalmic Advanced Patient Information

Brimonidine Ophthalmic Advanced Patient Information/Brimonidine Tartrate is the tartrate salt form of brimonidine, an imidazole derivative, and a selective alpha-2 adrenergic receptor agonist. Upon ocular administration, brimonidine tartrate acts on the blood vessels causing them to constrict which leads to a decrease in the production of aqueous humor. Brimonidine tartrate also enhances the outflow of aqueous humor. This drug is used in the treatment of glaucoma to reduce intraocular pressure.
Brimonidine is an imidazole derivative and a selective alpha-2 adrenergic receptor agonist. Upon ocular administration, brimonidine acts on the blood vessels causing them to constrict which leads to a decrease in the production of aqueous humor. Brimonidine also enhances the uveoscleral outflow of aqueous humor. This reduces intraocular pressure.

Brimonidine is a quinoxaline derivative, a secondary amine and a member of imidazoles. It has a role as an adrenergic agonist, an antihypertensive agent, and an alpha-adrenergic agonist.

Synonyms

  • 5-Bromo-6-(2-imidazolin-2-ylamino)quinoxaline
  • Brimonidina
  • Brimonidine
  • Brimonidinum
  • Bromoxidine

Mechanism of Action of Brimonidine Tartrate

In the eye, alpha-1 adrenoceptors play a role in vasoconstriction, mydriasis, eyelid retraction, and elevation of intraocular pressure (IOP) whereas alpha-2 adrenoceptors are responsible for IOP reduction via a complex Gi-coupled signaling cascade pathway. Activation of alpha-2 receptors leads to inhibition of adenylyl cyclase and reduction of cyclic AMP levels. As a result, there is a decrease in norepinephrine (NE) release at the synaptic junction, NE-induced stimulation of beta-2 adrenoceptors, and production of aqueous humor by the ciliary epithelium. An elevated IOP is the most significant risk factor for developing glaucomatous optic neuropathy, which is associated with progressive visual field loss and functional disability if left untreated. Regardless of the etiology of the disease, the aim of current therapies for glaucoma is to reduce IOP, as reduction of IOP significantly reduces the risk of progression of vision loss even when IOP is already within the normal range. When administered ophthalmically, brimonidine is rapidly absorbed into the eye, acts as an agonist at ocular alpha-2 adrenoceptors and lowers IOP via a dual mechanism of action. It is proposed that the initial dosing of the drug causes a reduction in aqueous humor production and chronic dosing leads to an increase in uveoscleral outflow. Brimonidine does not affect episcleral venous pressure. By reducing IOP, brimonidine aims to reduce the likelihood of glaucomatous visual field loss in ocular hypertension and slow the progression of visual field defects in established open-angle glaucoma. When applied topically on the skin, brimonidine reduces erythema through direct vasoconstriction of small arteries and veins. As brimonidine mediates a potent peripheral vasoconstrictive activity by selectively working on the alpha-2 adrenoceptors, the use of brimonidine is thought to be efficacious for the treatment of facial erythema of rosacea, which is thought to arise from vasomotor instability and abnormal vasodilation of the superficial cutaneous vasculature of the face.

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Indications of Brimonidine Tartrate

  • Indicated for lowering intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension as monotherapy or combination product with.
  • Indicated for the treatment of persistent (non-transient) facial erythema of rosacea in adults 18 years of age or older
  • It is indicated for the symptomatic treatment of facial erythema of rosacea in adult patients.
  • Decrease of elevated intraocular pressure (IOP) in adult patients with open-angle glaucoma or ocular hypertension for whom monotherapy provides insufficient IOP reduction.
  • Treatment of rosacea
  • Ocular Hypertension, Glaucoma, Open-Angle
  • Eye Redness

Contraindications of Brimonidine Tartrate

  • Cardiac disease, cerebrovascular disease, coronary artery disease
  • Depression
  • A disorder of the blood vessels of the brain
  • Raynaud’s phenomenon
  • A condition where blood vessels constrict too much with coldness or stress
  • Depression, orthostatic hypotension, Raynaud’s phenomenon, scleroderma, Sjogren’s syndrome, thromboangiitis obliterans (Buerger’s disease)
  • Contact lenses
  • Buerger’s Disease
  • Orthostatic hypotension
  • A form of low blood pressure
  • Allergies to Alpha 2 Adrenergic Agonist

Dosage of Brimonidine Tartrate

Strengths: 0.2%; 0.15%; 0.1%; 0.025%

Intraocular Hypertension

  • 1 drop in the affected eye(s) 3 times per day, approximately 8 hours apart

Glaucoma (Open Angle)

  • 1 drop in the affected eye(s) 3 times per day, approximately 8 hours apart

Pediatric Dose

Intraocular Hypertension

2 years or older

  • 1 drop in the affected eye(s) 3 times per day, approximately 8 hours apart

Glaucoma (Open Angle)

2 years or older

  • 1 drop in the affected eye(s) 3 times per day, approximately 8 hours apart

Maximum Dosage

Adults
  • 3 drops/day/affected eye 0.1%, 0.15%, or 0.2% ophthalmic solution; 4 drops/day/affected eye 0.025% ophthalmic solution; 1 application/day topically brimonidine gel.
Geriatric
  • 3 drops/day/affected 0.1%, 0.15%, or 0.2% ophthalmic solution; 4 drops/day/affected eye 0.025% ophthalmic solution; 1 application/day topically brimonidine gel.
Adolescents
  • 3 drops/day/affected eye 0.1%, 0.15%, or 0.2% ophthalmic solution; 4 drops/day/affected eye 0.025% ophthalmic solution; safety and efficacy of brimonidine topical gel have not been established.
Children
  • 5 years and older – 3 drops/day/affected eye 0.1%, 0.15%, or 0.2% ophthalmic solution; 4 drops/day/affected eye 0.025% ophthalmic solution; safety and efficacy of brimonidine topical gel have not been established.
  • 2 to 4 years – 3 drops/day/affected eye 0.1%, 0.15%, or 0.2% ophthalmic solution; safety and efficacy of brimonidine topical gel or 0.025% ophthalmic solution have not been established.
  • less than 2 years – Use of ophthalmic solution not recommended; safety and efficacy of brimonidine topical gel have not been established.

Side Effects of Brimonidine Tartrate

More common

  • burning, stinging, or irritated eyes upon instillation of eye drops
  • discoloration of white part of the eye
  • drowsiness or tiredness
  • dry eyes
  • dry mouth
  • Blurred or loss of vision
  • burning, dry, or itching eyes
  • discharge or excessive tearing
  • disturbed color perception
  • double vision
  • halos around lights
  • headache
  • itching of the eye
  • night blindness
  • the overbright appearance of lights
  • redness of the eye or inner lining of the eyelid
  • swelling of the eyelid
  • tearing of the eye
  • tunnel vision
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Less common

  • Ache or pain in the eye
  • cold-like symptoms (e.g., sore throat, tiredness, nasal congestion or runny nose)
  • dizziness
  • lightheaded feeling or dizziness when rising from a sitting or lying position
  • red, swollen, or itchy eyelid
  • redness of the eye or inner lining of the eyelid
  • the sensitivity of the eye to light
  • signs of an eye infection (e.g., pain, irritation, redness of the eye; increased sensitivity to light)slowed heartbeat
  • vision problems (e.g., decrease acuity)
  • blindness
  • bloody eye
  • blurred vision or other change in vision
  • change in color vision
  • confusion
  • decreased vision
  • difficult or labored breathing
  • difficulty seeing at night
  • dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
  • drainage from the eye
  • fast heartbeat
  • the feeling of something in the eye
  • gradual blurring or loss of vision
  • increased blood pressure

Rare

  • symptoms of an allergic reaction such as difficulty breathing, hives, or itchy skin rash
  • Bluish lips or skin
  • chest pain or discomfort
  • confusion
  • fast, pounding, or irregular heartbeat or pulse
  • feeling of warmth or heat
  • flushing or redness of the skin, especially on the face and neck
  • irregular, fast, slow, or shallow breathing
  • low body temperature
  • muscle aches or weakness
  • shivering
  • slow or irregular heartbeat
  • weak or feeble pulse
  • weight gain

Drug Interactions of Brimonidine Tartrate Eye Drops

may interact with following drugs, supplements & may change the efficacy of drugs

  • alcohol
  • alpha agonists (e.g., clonidine, methyldopa)
  • alpha-blockers (e.g., alfuzosin, doxazosin, tamsulosin)
  • angiotensin-converting enzyme inhibitors (ACEIs; e.g., captopril, enalapril, ramipril)
  • angiotensin receptor blockers (ARBs; e.g., candesartan, irbesartan, losartan)
  • antihistamines (e.g. cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
  • antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
  • aripiprazole
  • baclofen
  • barbiturates (e.g., butalbital, phenobarbital)
  • beta-blockers (e.g., atenolol, metoprolol, propranolol)
  • benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
  • calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
  • carbamazepine
  • diuretics (e.g., hydrochlorothiazide, furosemide)
  • gabapentin
  • hydralazine
  • mirtazapine
  • monoamine oxidase inhibitors (MAOIs; e.g, phenelzine, rasagiline, selegiline,  rasagiline, tranylcypromine)
  • selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, paroxetine, sertraline, fluoxetineparoxetine, fluvoxamine,
  • muscle relaxants (e.g., cyclobenzaprine, methocarbamol, orphenadrine)
  • narcotic pain relievers (e.g., codeine, fentanyl, morphine, oxycodone)
  • nitrates(e.g., nitroglycerin, isosorbide dinitrate)
  • phenytoin
  • tapentadol
  • tramadol
  • tricyclic antidepressants (e.g., amitriptyline, imipramine)


Pregnancy Category of Brimonidine Tartrate Eye Drops

FDA Pregnancy Category – B

Pregnancy

This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while using this medication, contact your doctor immediately. It is not known whether brimonidine is distributed into human breast milk. However, brimonidine was detected in breast milk in animal studies.

Lactation

It is not known if brimonidine passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding.

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Children

This medication is not recommended for children, as serious side effects have been reported in people less than 18 years of age. Do not use this medication for children less than 2 years old. No information is available on the relationship of age to the effects of brimonidine in pediatric patients. Safety and efficacy have not been established.

To use the eye drops

  • Wash your hands before using the eye drops.
  • Remove the cap and place it in a clean location. To avoid possible contamination, keep the tip of the container away from contact with any surface.
  • Tilt the head back and look towards the ceiling.
  • With your index finger, gently pull the lower eyelid down and away from the eye to form a pouch.
  • Apply one drop into the pouch but do not allow the tip of the container to touch the eye or areas around the eye.
  • Gently apply pressure to the inner corner of the eye (at the bridge of the nose) for about 30 seconds (this is called nasolacrimal occlusion). This prevents the medication from dripping down through the tear duct and entering the bloodstream, which could cause you to experience some side effects.
  • Repeat with the other eye, if prescribed by your physician.
  • Wash your hands again to remove any medication.

Do not allow the dropper tip of the bottle to touch the eye or other surrounding structures. This can contaminate the tip with common bacteria known to cause eye infections. Serious damage to the eye may result if you use eye drop solutions that have become contaminated.

References

 

Brimonidine Ophthalmic Eye Drops


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