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Dorzolamide (Drops) Instructions for Use

ATC Code

S01EC03 (Dorzolamide)

Active Substance

Dorzolamide (Rec.INN registered by WHO)

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 reduction of 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 detected 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 nonlinear: initially, there is a rapid decrease in the concentration of the active substance, then the elimination slows down, with a T1/2 of 4 months.

Indications

Ocular hypertension, primary open-angle glaucoma, pseudoexfoliative glaucoma, secondary glaucoma (without angle closure); as an 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

ICD-10 code Indication
H40.0 Glaucoma suspect (ocular hypertension)
H40.1 Primary open-angle glaucoma
H40.3 Secondary post-traumatic glaucoma
H40.4 Glaucoma secondary to inflammatory eye disease
H40.5 Glaucoma secondary to other eye disorders
ICD-11 code Indication
9C60 Glaucoma suspect
9C61.0Z Primary open-angle glaucoma, unspecified
9C61.24 Glaucoma due to ocular inflammation
9C61.29 Traumatic glaucoma
9C61.2Z Secondary open-angle glaucoma, unspecified

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

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

When used concomitantly with other topical ophthalmic agents, administer Dorzolamide two times daily.

Maintain an interval of at least ten minutes between instillations of different eye drop preparations.

For pediatric patients from the first week of life, apply the same dosage: one drop, two to three times daily, based on the treatment regimen.

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 any surface, including the eye, to prevent contamination of the solution.

If more than one type of ophthalmic drop is prescribed, always instill eye gels or ointments last.

Do not wear soft contact lenses during treatment with Dorzolamide; the preservative benzalkonium chloride may be absorbed by the lenses.

Adhere strictly to the prescribed administration schedule to ensure consistent intraocular pressure control.

Adverse Reactions

Ophthalmic 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, which disappears after drug withdrawal, corneal edema, ocular hypotension, retinal detachment in patients after surgical interventions to restore intraocular fluid outflow.

Nervous system common – headache; rare – dizziness, paresthesia.

Respiratory system rare – epistaxis, throat irritation; frequency unknown – dyspnea.

Digestive system common – nausea, bitter taste in mouth; rare – dry mouth.

Cardiovascular system frequency unknown – palpitation.

Skin and subcutaneous tissue rare – contact dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Urinary tract rare – urolithiasis.

Immune system rare – allergic reactions of the eyelids, symptoms of systemic allergic reactions – including angioedema, urticaria, pruritus, 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 operate machinery

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

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 may occur 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.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Marketing Authorization Holder

Kosmofarm, LLC (Russia)

Manufactured By

Slavic Pharmacy, LLC (Russia)

Dosage Form

Bottle Rx Icon Dorzolamide Eye drops 20 mg/1 ml: bottle 5 ml or 10 ml

Dosage Form, Packaging, and Composition

Eye drops as a clear, colorless or almost colorless, slightly viscous solution.

1 ml
Dorzolamide hydrochloride (calculated as Dorzolamide) 22.26 mg (20 mg)

Excipients : mannitol, hyetellose, sodium citrate, benzalkonium chloride, sodium hydroxide solution 1M, water for injections.

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

Marketing Authorization Holder

Medical Leasing-Consulting, LLC (Russia)

Manufactured By

Dalkhimpharm, JSC (Russia)

Dosage Form

Bottle Rx Icon Dorzolamide Eye drops 2%: bottle or dropper bottle 5 ml 1 pc.

Dosage Form, Packaging, and Composition

Eye drops as a clear, colorless solution.

1 ml
Dorzolamide hydrochloride 22.3 mg,
   Equivalent to dorzolamide content 20 mg

Excipients : benzalkonium chloride – 0.1 mg, citric acid – 18.3 mg, mannitol – 20 mg, hypromellose – 1 mg, hydrochloric acid solution 1M or sodium hydroxide solution 1M – to pH 5.0-6.5, water for injections – to 1 ml.

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

Marketing Authorization Holder

Jadran-Galenski Laboratorij, D.D. (Croatia)

Dosage Form

Bottle Rx Icon Dorzolamide hydrochloride Eye drops 20 mg/1 ml: bottle 5 ml 1 pc.

Dosage Form, Packaging, and Composition

Eye drops as a clear, colorless or almost colorless, slightly viscous solution.

1 ml
Dorzolamide hydrochloride 22.3 mg,
   Equivalent to dorzolamide content 20 mg

Excipients : mannitol, hydroxyethylcellulose, sodium citrate, benzalkonium chloride solution 50%, purified water.

5 ml – bottles (1) – cardboard boxes.

Marketing Authorization Holder

Grotex, LLC (Russia)

Dosage Form

Bottle Rx Icon Dorzolamide solopharm Eye drops 20 mg/1 ml: bottle 5 ml 1 or 3 pcs.

Dosage Form, Packaging, and Composition

Eye drops as a clear, colorless or almost colorless, slightly viscous solution.

1 ml
Dorzolamide hydrochloride 22.26 mg,
   Equivalent to dorzolamide content 20 mg

Excipients : sodium citrate dihydrate – 2.94 mg, sodium hyaluronate – 1.8 mg, mannitol – 23 mg, sodium benzoate – 2 mg, 1M sodium hydroxide solution or 1M hydrochloric acid solution – to pH 5.0-6.0, water for injections – to 1 ml.

5 ml – bottles made of low-density polyethylene (1) with a dropper – cardboard boxes.
5 ml – bottles made of low-density polyethylene (3) with a dropper – cardboard boxes.

Marketing Authorization Holder

Lekko, CJS (Russia)

Dosage Form

Bottle Rx Icon Dorzolamide-Optic Eye drops 20 mg/1 ml: bottle 5 ml or 10 ml

Dosage Form, Packaging, and Composition

Eye drops as a clear, colorless or with a brownish-yellow tint, slightly viscous liquid.

1 ml
Dorzolamide hydrochloride 22.26 mg,
   Equivalent to dorzolamide content 20 mg

Excipients : mannitol – 23 mg, hypromellose (hydroxypropyl methylcellulose) – 8.5 mg, sodium citrate dihydrate – 2.94 mg, benzalkonium chloride (calculated as anhydrous substance) – 0.075 mg, sodium hydroxide 1M – to pH 5.5-5.8, purified water – to 1 ml.

5 ml – polymer bottles (1) with a dropper cap – cardboard boxes.
5 ml – polymer bottles (1) with a dropper attachment – cardboard boxes.
10 ml – polymer bottles (1) with a dropper cap – cardboard boxes.
10 ml – polymer bottles (1) with a dropper attachment – cardboard boxes.

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