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|Brinzolamide

Brinzolamide

Trade Names:
Azopt
- Ophthalmic suspension 1%

Mechanism of Action

Pharmacology

Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, resulting in a reduction in IOP.

Pharmacokinetics

Absorption

Following ocular administration, absorbed into the systemic circulation.

Distribution

Distributes extensively into RBCs. Protein binding is about 60%.

Metabolism

Metabolite is N-desethylbrinzolamide.

Elimination

Eliminated predominantly unchanged in the urine. Metabolites also found in the urine.

Indications and Usage

Treatment of elevated IOP in patients with ocular hypertension or open-angle glaucoma.

Contraindications

Standard considerations.

Dosage and Administration

Ophthalmic 1 gtt in affected eye(s) 3 times daily.

General Advice

• Shake dropper bottle well before instilling eye drops.
• If using other topical ophthalmic drugs, separate each medication by at least 10 min.

Storage/Stability

Store below 86°F. Keep dropper bottle tightly closed.

Drug Interactions

None well documented.

Laboratory Test Interactions

None well documented.

Adverse Reactions

CNS

Headache (1% to 5%).

Dermatologic

Dermatitis (1% to 5%).

EENT

Blurred vision (5% to 10%); blepharitis, dry eye, foreign body sensation, hyperemia, ocular discharge, ocular discomfort, ocular keratitis, ocular pain, ocular pruritus, rhinitis (1% to 5%).

GI

Bitter, sour, or unusual taste (5% to 10%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Use not recommended.

Hepatic Function

Use with caution.

Sulfonamides

Brinzolamide is a sulfonamide and adverse reactions attributable to sulfonamides may occur (eg, Stevens-Johnson syndrome, toxic epidermal necrolysis, aplastic anemia, death).

Overdosage

Symptoms

Electrolyte imbalance, acidotic state, possible nervous system effects.

Patient Information

• Advise patient that usual dose is 1 gtt instilled into the affected eye(s) 3 times daily.
• Teach patient proper technique for instilling eye drops: wash hands; shake well; do not allow dropper tip to touch eye. Tilt head back, look up; pull lower eyelid down; instill prescribed number of drops. Close eye for 1 to 2 min and apply gentle pressure to bridge of nose for 3 to 5 min. Do not rub eye.
• Advise patient that if more than 1 topical ophthalmic drug is being used, administer the drugs at least 10 min apart.
• Advise patients who wear contact lenses to remove lenses before instilling this medicine and to wait at least 15 min after instilling eye drops before reinserting lenses.
• Inform patient that blurred vision and taste abnormalities (bitter, sour, or unusual taste) are the most common side effects and to contact health care provider if they occur and are bothersome.
• Advise patient that medication may cause temporary blurring of vision and to use caution driving or performing other tasks requiring good vision until tolerance is determined.
• Advise patient to discontinue therapy and immediately notify health care provider if serious or unusual reactions occur in the eye (eg, eye or eyelid inflammation) or if experiencing any signs or symptoms of an allergic reaction (eg, rash, hives, itching).
• Advise patient to contact the eye doctor if eye injury occurs or eye surgery is forthcoming.
• Remind patient that eye examinations and measurement of IOP will be necessary while using this medication and to keep appointments.