Azopt

Although no human data are available, electrolyte imbalance, development of an acidotic state, and possible nervous system effects may occur following oral administration of an overdose. Serum electrolyte levels (particularly potassium) and blood pH levels should be monitored.

Use the medication as soon as you remember. If it is almost time for the next dose, skip the missed dose and use the medicine at the next regularly scheduled time. Do not use extra medicine to make up the missed dose.

Storage

Ophthalmic

4–30°C.1

• Potent ocular hypotensive agent; can produce mean IOP reductions of about 16–19% in patients with elevated IOP.1 3 8

• Highly specific inhibitor of CA-II, the main carbonic anhydrase isoenzyme involved in aqueous humor secretion.1 2 3 Inhibition of carbonic anhydrase in the ciliary process of the eye decreases the rate of aqueous humor secretion and IOP by slowing bicarbonate formation and reducing sodium and fluid transport.1 2

• Accumulates in erythrocytes as a result of CA-II binding; however, sufficient CA-II activity remains so that adverse effects resulting from systemic carbonic anhydrase inhibition are not observed.1 5

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

In the U.S.

• Azopt

In Canada

• Azopt 1%

Available Dosage Forms:

• Suspension

Therapeutic Class: Antiglaucoma

Pharmacologic Class: Carbonic Anhydrase Inhibitor

• It is used to treat glaucoma.
• It is used to lower high eye pressure.

• Tell all of your health care providers that you take Azopt. This includes your doctors, nurses, pharmacists, and dentists.
• Avoid driving and doing other tasks or actions that call for you to be alert or have clear eyesight until you see how this medicine affects you.
• If you have a sulfa (sulfonamide) allergy, talk with your doctor.
• Have your eye pressure and eyesight checked as you have been told by the doctor.
• Tell your doctor if you have an eye infection, eye injury, or will be having eye surgery.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using Azopt while you are pregnant.

Sulfonamide Hypersensitivity Reactions

Azopt® (brinzolamide ophthalmic suspension) 1% is a sulfonamide and although administered topically it is absorbed systemically. Therefore, the same types of adverse reactions that are attributable to sulfonamides may occur with topical administration of Azopt® (brinzolamide ophthalmic suspension) 1%. Fatalities have occurred, although rarely, due to severe reactions to sulfonamides including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias. Sensitization may recur when a sulfonamide is re-administered irrespective of the route of administration. If signs of serious reactions or hypersensitivity occur, discontinue the use of this preparation. 

 Corneal Endothelium

Carbonic anhydrase activity has been observed in both the cytoplasm and around the plasma membranes of the corneal endothelium. There is an increased potential for developing corneal edema in patients with low endothelial cell counts. Caution should be used when prescribing Azopt® (brinzolamide ophthalmic suspension) 1% to this group of patients. 

Severe Renal Impairment

Azopt® (brinzolamide ophthalmic suspension) 1% has not been studied in patients with severe renal impairment (CrCl < 30 mL/min). Because Azopt® (brinzolamide ophthalmic suspension) 1% and its metabolite are excreted predominantly by the kidney, Azopt® (brinzolamide ophthalmic suspension) 1% is not recommended in such patients.

Acute Angle-Closure Glaucoma

The management of patients with acute angle-closure glaucoma requires therapeutic interventions in addition to ocular hypotensive agents. Azopt® (brinzolamide ophthalmic suspension) 1% has not been studied in patients with acute angle-closure glaucoma.

Contact Lens Wear

The preservative in Azopt® (brinzolamide ophthalmic suspension) 1%, benzalkonium chloride, may be absorbed by soft contact lenses. Contact lenses should be removed during instillation of Azopt® (brinzolamide ophthalmic suspension) 1%, but may be reinserted 15 minutes after instillation.

Clinical Studies Experience

Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to the rates in the clinical studies of another drug and may not reflect the rates observed in practice. 

In clinical studies of Azopt® (brinzolamide ophthalmic suspension) 1%, the most frequently reported adverse reactions reported in 5 to 10% of patients were blurred vision and bitter, sour or unusual taste. Adverse reactions occurring in 1 to 5% of patients were blepharitis, dermatitis, dry eye, foreign body sensation, headache, hyperemia, ocular discharge, ocular discomfort, ocular keratitis, ocular pain, ocular pruritus and rhinitis. 

The following adverse reactions were reported at an incidence below 1%: allergic reactions, alopecia, chest pain, conjunctivitis, diarrhea, diplopia, dizziness, dry mouth, dyspnea, dyspepsia, eye fatigue, hypertonia, keratoconjunctivitis, keratopathy, kidney pain, lid margin crusting or sticky sensation, nausea, pharyngitis, tearing and urticaria.

Oral Carbonic Anhydrase Inhibitors

There is a potential for an additive effect on the known systemic effects of carbonic anhydrase inhibition in patients receiving an oral carbonic anhydrase inhibitor and Azopt® (brinzolamide ophthalmic suspension) 1%. The concomitant administration of Azopt® (brinzolamide ophthalmic suspension) 1% and oral carbonic anhydrase inhibitors is not recommended.

High-Dose Salicylate Therapy

Carbonic anhydrase inhibitors may produce acid-base and electrolyte alterations. These alterations were not reported in the clinical trials with brinzolamide. However, in patients treated with oral carbonic anhydrase inhibitors, rare instances of acid-base alterations have occurred with high-dose salicylate therapy. Therefore, the potential for such drug interactions should be considered in patients receiving Azopt® (brinzolamide ophthalmic suspension) 1%.