Brinzolamide

Generic Name

Brinzolamide ophthalmic suspension

Brand Names

Azopt

Generic formulations available in several regions

Drug Class

Carbonic anhydrase inhibitor (topical ophthalmic)

Intraocular pressure-lowering agent

Mechanism of Action

Brinzolamide inhibits carbonic anhydrase II, an enzyme found in the ciliary processes of the eye

By inhibiting this enzyme, it reduces the formation of bicarbonate ions which are necessary for aqueous humour production

The result is decreased secretion of aqueous humour from the ciliary epithelium

This leads to a reduction in intraocular pressure (IOP)

The effect occurs without significant impact on pupil size or accommodation

Indications

Approved Uses

Ocular hypertension

Open-angle glaucoma

Adjunctive therapy in patients not adequately controlled with beta-blockers or prostaglandin analogues

Off-label/Investigational

Used as part of combination therapy in pseudoexfoliative glaucoma

Secondary glaucoma (with specialist supervision)

Post-surgical IOP control in select cases

Dosing and Administration

Adults (including elderly)

Instill one drop into the affected eye(s) twice daily

In some cases, three times daily may be used under specialist advice

If used with other topical ophthalmic drugs, administer at least 5 minutes apart

Shake the bottle well before each use

Avoid contact of the dropper tip with the eye or any surface

Close the eye gently and apply nasolacrimal occlusion for 1–2 minutes to reduce systemic absorption

Pediatric Use

Safety and efficacy not established in children

Not commonly used in pediatric glaucoma

Contraindications

Hypersensitivity to brinzolamide or any component of the formulation

Hypersensitivity to sulfonamides (risk of cross-reactivity)

Severe renal impairment (CrCl <30 mL/min) due to potential for systemic accumulation

Hyperchloremic acidosis

Precautions

Use with caution in patients with mild to moderate renal impairment

Contains benzalkonium chloride which may be absorbed by soft contact lenses—remove lenses before administration and wait at least 15 minutes before reinsertion

Use caution in patients with corneal abnormalities or chronic ocular surface disease

May cause transient blurred vision after instillation

Not for injection or oral use

Adverse Effects

Ocular Effects

Blurred vision

Eye discomfort

Foreign body sensation

Eye pain or stinging

Conjunctivitis

Dry eye

Photophobia

Discharge

Systemic Effects (rare)

Bitter taste

Headache

Nausea

Fatigue

Dizziness

Allergic reactions (rash, pruritus, urticaria)

Serious Reactions

Stevens-Johnson syndrome (rare, hypersensitivity-related)

Severe dermatologic or respiratory hypersensitivity (extremely rare)

Metabolic acidosis in those with renal impairment or other risk factors

Pregnancy and Lactation

Pregnancy

Limited human data available

Animal studies have shown embryotoxic effects at high doses

Use only if clearly needed and prescribed by a specialist

Avoid during pregnancy unless the benefits outweigh risks

Lactation

Unknown whether brinzolamide is excreted in human milk

Systemic exposure is minimal via ophthalmic route

Use with caution in breastfeeding women

Use in Special Populations

Elderly

No specific dose adjustments required

Similar efficacy and safety as in younger adults

Renal Impairment

Avoid in severe renal dysfunction

Caution in moderate impairment due to risk of systemic accumulation

Hepatic Impairment

No specific dose adjustments

Limited data; use with caution

Drug Interactions

Oral Carbonic Anhydrase Inhibitors (e.g. acetazolamide)

Additive effects may increase risk of systemic acidosis

Avoid concomitant use unless under specialist monitoring

High-dose salicylates (e.g. aspirin)

Potential risk of toxicity with concurrent use

Contact Lenses

Wait 15 minutes before reinsertion after instillation

Other Ophthalmic Medications

Separate administration by at least 5 minutes

Administer gels or ointments last

Monitoring Parameters

Intraocular pressure (baseline and regular follow-up)

Signs of allergic reactions or hypersensitivity

Renal function in prolonged therapy

Corneal health in long-term users

Vision changes

Patient Counseling Points

Shake the bottle well before each use

Wash hands before using the drops

Tilt head back, pull down lower eyelid, and instill one drop

Do not touch dropper tip to the eye

Close eye and gently press on the inner corner of the eye for 1–2 minutes

If using other eye medications, space them 5 minutes apart

Remove contact lenses before use and wait 15 minutes to reinsert

Expect mild temporary blurred vision after use

Report eye pain, severe irritation, skin rash, or signs of allergy immediately

Store at room temperature and protect from light

Use within 4 weeks of opening the bottle

Keep out of reach of children