Brinzopt (Drops) Instructions for Use

Marketing Authorization Holder

S.C. Rompharm Company S.R.L. (Romania)

ATC Code

S01EC04 (Brinzolamide)

Active Substance

Brinzolamide (Rec.INN registered by WHO)

Dosage Form

Brinzopt

Eye drops 10 mg/1 ml: bottle 5 ml with dropper applicator

Dosage Form, Packaging, and Composition

Eye drops as a white or almost white suspension.

Excipients: tyloxapol – 0.25 mg, carbomer 974R – 4 mg, mannitol (E421) – 33 mg, sodium chloride – 2.5 mg, disodium edetate dihydrate – 0.1 mg, benzalkonium chloride – 0.15 mg, sodium hydroxide or hydrochloric acid – to adjust pH to 7.5±0.1, purified water – up to 1 ml.

5 ml – polyethylene bottles with a capacity of 5 ml (1) with a dropper applicator – cardboard packs.

Clinical-Pharmacological Group

Antiglaucoma drug – topical carbonic anhydrase inhibitor

Pharmacotherapeutic Group

Drugs used in ophthalmology; antiglaucoma drugs and miotic agents; carbonic anhydrase inhibitors

Pharmacological Action

Antiglaucoma agent, carbonic anhydrase II inhibitor. Inhibition of carbonic anhydrase II slows the formation of bicarbonate ions with a subsequent reduction in sodium and fluid transport, which leads to a decrease in the production of intraocular fluid in the ciliary body of the eye. As a result, intraocular pressure is reduced.

Pharmacokinetics

When applied topically, it penetrates into the systemic circulation. With prolonged use, it accumulates in erythrocytes due to binding to carbonic anhydrase II. The metabolite N-desethyl also accumulates in erythrocytes, but due to binding to carbonic anhydrase I. Plasma protein binding is 60%. The plasma concentration during continuous use is below 10 ng/ml. It is metabolized to form N-desethyl brinzolamide, N-desmethoxypropyl, and O-desmethyl. Characterized by a long T_1/2. Excreted in the urine (mainly unchanged).

Indications

Ocular hypertension, open-angle glaucoma.

ICD codes

Dosage Regimen

Instill one drop into the lower conjunctival sac of the affected eye(s) two times daily, approximately every 12 hours.

Do not allow the dropper tip to contact any surface to avoid contamination of the suspension.

If using more than one topical ophthalmic product, administer them at least 10 minutes apart.

Shake the bottle well before each use to ensure uniform suspension.

Wash hands before and after application.

Remove contact lenses prior to application; you may reinsert them 15 minutes after instillation.

Immediately after application, temporary blurred vision may occur; wait until clear vision is restored before driving or operating machinery.

Do not exceed the prescribed dosage. If a dose is missed, apply it as soon as possible. If it is almost time for the next dose, skip the missed dose and continue with the regular schedule.

Discontinue use and consult your physician immediately if you experience severe skin rashes, eye pain, vision changes, or signs of systemic reactions.

Adverse Reactions

From the organ of vision frequently – blurred vision; blepharitis, keratitis, dermatitis, dry eye, hyperemia, foreign body sensation in the eye, eye discharge, discomfort, pain, eye itching are possible; conjunctivitis, keratoconjunctivitis, keratopathy, initial symptoms of blepharitis (eyelid sticking or crusting on the eyelid margins), lacrimation, diplopia, asthenopia are possible.

From the digestive system frequently – bitter, sour taste in the mouth, dry mouth, dyspepsia, nausea, diarrhea; rarely – hepatonecrosis.

From the respiratory system rhinitis, dyspnea, pharyngitis.

From the cardiovascular system arterial hypertension, chest pain.

From the hematopoietic system rarely – agranulocytosis, aplastic anemia.

Allergic reactions urticaria; rarely – Stevens-Johnson syndrome, toxic epidermal necrolysis.

Other headache, kidney pain, alopecia, dizziness.

Contraindications

Hypersensitivity to brinzolamide.

Use in Pregnancy and Lactation

There are no reliable data regarding the use of brinzolamide in pregnant women. Animal studies have shown reproductive toxicity after systemic administration. Brinzolamide is not recommended for use during pregnancy and by women of childbearing potential not using contraception.

It is not known whether Brinzolamide is excreted in breast milk. If it is necessary to use brinzolamide during lactation, the issue of discontinuing breastfeeding should be considered.

Use in Hepatic Impairment

Brinzolamide should be used with caution in severe hepatic impairment.

Use in Renal Impairment

It is not recommended to prescribe to patients with severe renal impairment (CrCl<30 ml/min) because Brinzolamide and its metabolites are excreted in the urine.

Pediatric Use

The efficacy and safety of brinzolamide use in children have not been established.

Special Precautions

Brinzolamide should be used with caution in severe hepatic impairment.

The safety and efficacy of brinzolamide in patients with acute angle-closure glaucoma have not been studied.

It is not recommended to prescribe to patients with severe renal impairment (CrCl<30 ml/min) because Brinzolamide and its metabolites are excreted in the urine.

If severe adverse reactions develop (Stevens-Johnson syndrome, toxic epidermal necrolysis, hepatonecrosis, agranulocytosis, aplastic anemia), the use of brinzolamide should be discontinued.

The efficacy and safety of brinzolamide use in children have not been established.

Effect on ability to drive vehicles and operate machinery

Immediately after the application of brinzolamide, temporary blurred vision is possible, so the patient should be cautious when driving vehicles and operating machinery.

Drug Interactions

With the simultaneous use of brinzolamide and systemic carbonic anhydrase inhibitors, an increase in systemic reactions associated with enzyme inhibition is possible (the combination is not recommended).

With the simultaneous use of brinzolamide and high doses of salicylates, acid-base and electrolyte balance disorders are possible.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.