Dorzopt (Drops) Instructions for Use

Marketing Authorization Holder

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

ATC Code

S01EC03 (Dorzolamide)

Active Substance

Dorzolamide (Rec.INN registered by WHO)

Dosage Form

Dorzopt

Eye drops 20 mg/1 ml: bottle 5 ml 1 or 3 pcs. with dropper cap

Dosage Form, Packaging, and Composition

Eye drops in the form of a clear, slightly viscous yellowish-brown solution.

Excipients: hydroxyethyl cellulose – 1 mg, mannitol – 20 mg, citric acid monohydrate – 4 mg, sodium hydroxide – 2.426 mg, benzalkonium chloride – 0.1 mg, purified water – up to 1 ml.

5 ml – polyethylene bottles (1) with dropper cap – cardboard boxes.
5 ml – polyethylene bottles (3) with dropper cap – cardboard boxes.

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, 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 to 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 an 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 angle closure of the anterior chamber of the eye); as an additional therapy to beta-blockers, as monotherapy in case of ineffectiveness of beta-blockers or contraindications to them.

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 droptwo times daily.

Administer drops approximately every 8 hours for the three-times-daily regimen and approximately every 12 hours for the twice-daily regimen.

To prevent contamination of the solution, avoid contact between the dropper tip and the eye, eyelids, or any other surface.

If more than one topical ophthalmic drug is being used, administer them at least 10 minutes apart.

In pediatric patients from the first week of life, apply the same dosage regimen as for adults.

If a dose is missed, administer it as soon as possible. However, if it is almost time for the next dose, skip the missed dose and continue with the regular dosing schedule.

Do not use while wearing soft contact lenses; remove lenses prior to instillation and wait at least 15 minutes before reinsertion.

Adverse Reactions

From the organ of vision very common – burning, pain; common – superficial punctate keratitis, lacrimation, conjunctivitis, eyelid inflammation, itching, irritation and swelling of the eyelids, 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 the outflow of intraocular fluid.

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 the 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 from the eyelids, symptoms of systemic allergic reactions – including angioedema, urticaria, itching, rash, difficulty breathing, less often – 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 operate machinery

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.

Increased toxicity is possible 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.