Glaucopt (Drops) Instructions for Use

Marketing Authorization Holder

Scan Biotech LLC (India)

Manufactured By

Dalkhimpharm, JSC (Russia)

ATC Code

S01EC03 (Dorzolamide)

Active Substance

Dorzolamide (Rec.INN registered by WHO)

Dosage Form

Glaucopt

Eye drops 2%: bottle 5 ml with dropper cap

Dosage Form, Packaging, and Composition

Eye drops in the form of a transparent, colorless solution.

Excipients: benzalkonium chloride – 0.1 mg, anhydrous citric acid – 18.3 mg, mannitol – 20 mg, hypromellose – 1 mg, hydrochloric acid – q.s. to adjust pH, sodium hydroxide – q.s. to adjust pH, water for injections – up to 1 ml.

5 ml – low-density polyethylene bottles (1) with dropper cap – cardboard packs.

Clinical-Pharmacological Group

Antiglaucoma drug – topical carbonic anhydrase inhibitor

Pharmacotherapeutic Group

Antiglaucoma agent – carbonic anhydrase inhibitor

Pharmacological Action

Antiglaucoma agent, a selective inhibitor of human carbonic anhydrase II. Inhibition of carbonic anhydrase in the ciliary processes of the eye leads to a decrease in the secretion of aqueous humor, resulting in a decrease in intraocular pressure (IOP). Dorzolamide has minimal or practically no effect on heart rate or blood pressure.

Pharmacokinetics

When applied topically, Dorzolamide penetrates into the systemic circulation. With course use, due to selective binding with carbonic anhydrase II, it accumulates in erythrocytes. At the same time, very low concentrations of the unchanged active substance are determined in the blood plasma. Dorzolamide is metabolized to form a single N-desethyl metabolite, which also accumulates in erythrocytes. The binding of dorzolamide to plasma proteins is about 33%. It is excreted mainly in the urine as unchanged substance and metabolite. After the end of dorzolamide administration, the washout process from erythrocytes is non-linear: initially, there is a rapid decrease in the concentration of the active substance, then the elimination slows down, with a T_1/2 of 4 months.

Indications

Ocular hypertension, primary open-angle glaucoma, pseudoexfoliative glaucoma, secondary glaucoma (without anterior chamber angle block); as additional therapy to beta-blockers, as monotherapy when beta-blockers are ineffective or contraindicated.

Treatment of glaucoma in children from the 1st week of life – as monotherapy or as an addition to treatment with beta-blockers.

ICD codes

Dosage Regimen

Instill one drop into the conjunctival sac of the affected eye(s) three times daily when used as monotherapy.

When used as adjunctive therapy with a topical beta-blocker, instill one drop two times daily.

Administer doses approximately eight hours apart to maintain consistent therapeutic effect.

If using more than one topical ophthalmic product, space administrations at least five minutes apart.

To minimize systemic absorption, apply gentle pressure to the lacrimal sac at the inner corner of the eye for one to two minutes immediately after instillation.

Avoid allowing the dropper tip to contact the eye, eyelids, or any other surface to prevent contamination of the solution.

For pediatric patients from one week of age, follow the same dosing frequency as for adults, adjusting only the number of drops per instillation if specifically directed by a physician.

Dosage adjustment is not typically required for elderly patients or those with mild to moderate hepatic impairment; use is contraindicated in patients with severe renal impairment (creatinine clearance less than 30 ml/min).

Adverse Reactions

From the organ of vision very common – burning, pain; common – superficial punctate keratitis, lacrimation, conjunctivitis, eyelid inflammation, itching, eyelid irritation and swelling, blurred vision; uncommon – iridocyclitis; rare – eye redness, pain, eyelid hyperkeratosis, transient myopia disappearing after drug withdrawal, corneal edema, ocular hypotension, retinal detachment in patients after surgical interventions to restore intraocular fluid outflow.

From the nervous system common – headache; rare – dizziness, paresthesia.

From the respiratory system rare – epistaxis, throat irritation; frequency unknown – dyspnea.

From the digestive system common – nausea, bitter taste in mouth; rare – dry mouth.

From the cardiovascular system frequency unknown – palpitation

From the skin and subcutaneous tissues rare – contact dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the urinary tract rare – urolithiasis.

From the immune system rare – allergic reactions of the eyelids, symptoms of systemic allergic reactions – including angioedema, urticaria, itching, rash, difficulty breathing, less commonly – bronchospasm.

General reactions common – asthenia, fatigue.

Contraindications

Hypersensitivity to dorzolamide, severe renal failure, hyperchloremic acidosis, pregnancy, breastfeeding period, children under 1 week of age.

Use in Pregnancy and Lactation

The use of dorzolamide is contraindicated during pregnancy and breastfeeding.

Use in Hepatic Impairment

Use with caution in patients with impaired liver function.

Use in Renal Impairment

Contraindicated in severe renal failure (creatinine clearance less than 30 ml/min).

Pediatric Use

Used for the treatment of glaucoma in children from the 1st week of life – as monotherapy or as an addition to treatment with beta-blockers.

Geriatric Use

Elderly patients may have increased sensitivity to dorzolamide.

Special Precautions

Use with caution in patients with a history of recurrent corneal erosions and/or surgical interventions with violation of the integrity of the eyeball; the likelihood of corneal edema increases.

Elderly patients may have increased sensitivity to dorzolamide.

If allergic reactions develop, the use of dorzolamide should be discontinued.

Effect on ability to drive vehicles and mechanisms

Since Dorzolamide may cause dizziness and nausea, potentially hazardous activities requiring concentration and increased speed of psychomotor reactions should be avoided during treatment.

Drug Interactions

There is a possibility of an additive effect regarding the known systemic effects of carbonic anhydrase inhibition in patients receiving an oral carbonic anhydrase inhibitor and Dorzolamide.

Possible increased toxicity when taking acetylsalicylic acid in high doses.

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.