Brinzolamide/brimonidine

What is Brinzolamide/brimonidine?

• Brinzolamide/brimonidine (Simbrinza) is a fixed combination of a carbonic anhydrase inhibitor and an alpha 2 adrenergic receptor agonist used for the reduction of elevated intraocular pressure (IOP).

Brinzolamide

Brinzolamide Structural Formula V1

Brimonidine

Brimonidine structure

What are the uses of this medicine?

• Brinzolamide/brimonidine (Simbrinza) used for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.

How does this medicine work?

• Simbrinza is comprised of two components: brinzolamide (carbonic anhydrase inhibitor) and brimonidine tartrate (alpha 2 adrenergic receptor agonist).

Brinzolamide:

• Brinzolamide is an inhibitor of carbonic anhydrase II (CA-II).
• Carbonic anhydrase (CA) is an enzyme found in many tissues of the body including the eye.
• It catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid.
• In humans, carbonic anhydrase exists as a number of isoenzymes, the most active being carbonic anhydrase II (CA-II), found primarily in red blood cells (RBCs), but also in other tissues.
• Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport.
• The result is a reduction in intraocular pressure (IOP).
• Following topical ocular administration, brinzolamide inhibits aqueous humor formation and reduces elevated intraocular pressure.

Brimonidine:

• Brinzolamide has a peak ocular hypotensive effect occurring at 2 to 3 hours post-dosing.
• Fluorophotometric studies in animals and humans suggest that brimonidine tartrate has a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow.
• Brimonidine tartrate has a peak ocular hypotensive effect occurring at two hours post-dosing.

• Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss.
• The higher the level of intraocular pressure, the greater the likelihood of glaucomatous field loss and optic nerve damage.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• who are hypersensitive to any component of this product.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention the following:

• especially acetazolamide (Diamox), dichlorphenamide (Daranide), eye medications, methazolamide (Neptazane), products that contain aspirin
• monoamine oxidase (MAO) inhibitor such as isocarboxazid (Marplan), phenelzine (Nardil), selegiline (Eldepryl), or tranylcypromine (Parnate)
• antidepressants such as amitriptyline (Elavil), amoxapine (Asendin), clomipramine (Anafranil), desipramine (Norpramin), doxepin (Adapin, Sinequan), imipramine (Tofranil), nortriptyline (Aventyl, Pamelor), protriptyline (Vivactil), and trimipramine (Surmontil)
• barbiturates such as phenobarbital and secobarbital (Seconal)
• digoxin (Lanoxin)
• medications for anxiety, high blood pressure, mental illness, pain, or seizures
• sedatives
• sleeping pills
• tranquilizers

Is this medicine FDA approved?

• Brinzolamide/brimonidine was approved for medical use in the United States in April 2013, and in the European Union in July 2014.

How should this medicine be used?

Recommended dosage:

• The recommended dose is one drop of Simbrinza in the affected eye(s) three times daily.
• Simbrinza ophthalmic suspension may be used concomitantly with other topical ophthalmic drug products to lower intraocular pressure.
• If more than one topical ophthalmic drug is being used, the drugs should be administered at least five minutes apart.

Administration:

• Shake well before use.
• Instill one drop in the affected eye three times daily.
• Instruct patients that ocular solutions, if handled improperly or if the tip of the dispensing container contacts the eye or surrounding structures, can become contaminated by common bacteria known to cause ocular infections.
• Contact lenses should be removed during instillation of Simbrinza, but may be reinserted 15 minutes after instillation.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Suspension containing 10 mg/mL brinzolamide and 2 mg/mL brimonidine tartrate.

This medicine is available in fallowing brand namesː

• Simbrinza

What side effects can this medication cause?

The most common side effects of this medicine include:

• blurred vision, eye irritation, dysgeusia (bad taste), dry mouth, eye allergy.

Less common side effects may include:

• bradycardia, hypersensitivity, iritis, keratoconjunctivitis sicca, miosis, nausea, skin reactions (including erythema, eyelid pruritus, rash, and vasodilation), and tachycardia.

• Apnea, bradycardia, coma, hypotension, hypothermia, hypotonia, lethargy, pallor, respiratory depression, and somnolence have been reported in infants receiving brimonidine tartrate ophthalmic solutions.

What special precautions should I follow?

• Simbrinza contains brinzolamide, a sulfonamide and although administered topically is absorbed systemically. Advise patients that if serious or unusual ocular or systemic reactions or signs of hypersensitivity occur, they should discontinue the use of the product and consult their physician.
• Vision may be temporarily blurred following dosing with Simbrinza. Care should be exercised in operating machinery or driving a motor vehicle.
• As with other drugs in this class, Simbrinza may cause fatigue and/or drowsiness in some patients. Caution patients who engage in hazardous activities of the potential for a decrease in mental alertness.
• Instruct patients that ocular solutions, if handled improperly or if the tip of the dispensing container contacts the eye or surrounding structures, can become contaminated by common bacteria known to cause ocular infections. Always replace the cap after using. If solution changes color or becomes cloudy, do not use. Do not use the product after the expiration date marked on the bottle.
• Advise patients that if they have ocular surgery or develop an intercurrent ocular condition (e.g., trauma or infection), they should immediately seek their physician's advice concerning the continued use of the present multidose container.
• If more than one topical ophthalmic drug is being used, the drugs should be administered at least five minutes apart
• The preservative in Simbrinza, benzalkonium chloride, may be absorbed by soft contact lenses. Contact lenses should be removed during instillation of Simbrinza, but may be reinserted 15 minutes after instillation.

What to do in case of emergency/overdose?

Symptoms of overdosage may include: Brinzolamide overdose:

• electrolyte imbalance, development of an acidotic state, and possible nervous system effects may occur following an oral overdose of brinzolamide.

Brimonidine overdose:

• the only adverse event reported to date has been hypotension.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Treatment of an oral overdose includes supportive and symptomatic therapy; a patent airway should be maintained.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies in pregnant women.
• Simbrinza should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• The individual component, brinzolamide, has been studied in pediatric glaucoma patients 4 weeks to 5 years of age.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• Brinzolamide
• Brimonidine Tartrate

Inactive ingredients:

• Benzalkonium Chloride
• Boric Acid
• Carbomer Homopolymer Type B (allyl Pentaerythritol Crosslinked)
• Mannitol
• Propylene Glycol
• Water
• Sodium Chloride
• Tyloxapol
• Hydrochloric Acid
• Sodium Hydroxide

Who manufactures and distributes this medicine?

Distributed by:

• ALCON LABORATORIES, INC.
• Fort Worth, Texas USA

What should I know about storage and disposal of this medication?

• Store Simbrinza at 2 - 25°C (36 - 77°F).

• Dailymed label info on Brinzolamide/brimonidine
• FDA Brinzolamide/brimonidine

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