Dorzamed (dorzolamide) eye drops 2% 5 ml. vial

Description

Dorzamed Composition
active substance: dorzolamide;

1 ml of the drug contains 22.3 mg dorzolamide hydrochloride, which is equivalent to 20 mg dorzolamide;

Dorzamed excipients: benzalkonium chloride, hydroxyethyl cellulose; sodium hydroxide beckons (E 421) citric acid monohydrate, purified water.

Dorzamed Dosage form
Eye drops, solution.

Basic physical and chemical properties: transparent solution without visible particles.

Pharmacotherapeutic group
Antiglaucoma drugs and miotics. Carbonic anhydrase inhibitors. Dorzolamide. ATX code S01E C03.

Pharmacodynamics
Dorzolamide is a strong inhibitor of human carbonic anhydrase II (CA-II). After topical application, it reduces the increased intraocular pressure, associated or not associated with glaucoma. Increased intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous narrowing of the visual field.

A decrease in intraocular pressure with the use of dorzolamide is not accompanied by the development of common adverse reactions characteristic of miotics, such as night blindness, accommodative spasm and pupil constriction. Does not affect or has little effect on blood pressure and heart rate.

Unlike oral preparations of carbonic anhydrase inhibitors, when applied topically, dorzolamide acts directly in the eye at significantly lower concentrations, and therefore such use is accompanied by a lesser systemic effect.

The efficacy of dorzolamide, which was used in patients with glaucoma or ocular hypertension as monotherapy 3 times a day (primary intraocular pressure ≥ 23 mm Hg) or 2 times a day as an adjunctive therapy in the treatment of local beta-blockers (primary intraocular pressure ≥ 22 mmHg), has been confirmed in clinical studies. When used as monotherapy and in combination with beta-blockers, dorzolamide reduced intraocular pressure throughout the day, and this effect persisted for a long time. The effectiveness of dorzolamide after long-term use as monotherapy was similar to that of betaxolol and only slightly less than that of timolol. When using dorzolamide as an adjunctive therapy in the treatment of local beta-blockers, an additional decrease in intraocular pressure was noted, similar to that when using pilocarpine 2% 4 times a day.

Pharmacokinetics
When applied topically, dorzolamide enters the systemic circulation.

Moderately binds to blood plasma proteins (approximately 33%). With long-term use, dorzolamide is accumulated in erythrocytes as a result of selective binding to CA-II, while a very low concentration of the free active substance is maintained in the blood plasma. Dorzolamide forms one N-desetilation metabolite that inhibits CA-II to a lesser extent than the parent compound, but also inhibits the less active CA-I isoenzyme. The metabolite also accumulates in erythrocytes, where it binds predominantly to CA-I.

It is excreted in the urine mainly unchanged; the metabolite is also excreted in the urine. After withdrawal, nonlinear leaching of dorzolamide from erythrocytes occurs, which first leads to a rapid decrease in the concentration of dorzolamide, after which a slower withdrawal phase occurs with a half-life of about 4 months.

Indications
Adjunctive therapy with topical beta-blockers.
Monotherapy when treatment with local beta-blockers is not effective enough or is contraindicated.
Therapy for increased eye pressure with:
With intramural hypertension;
With open-angle glaucoma;
With pseudoexfoliative glaucoma.

Contraindications
Hypersensitivity to the active substance or other components of the drug. Severe renal dysfunction (CC less than 30 ml / min). Hyperchloremic acidosis.

Interaction with other medicinal products and other types of interactions
Special studies of the interaction of dorzolamide with other drugs have not been conducted.

In clinical studies, dorzolamide was used simultaneously with timolol and betaxolol in the form of eye drops, with drugs of systemic action, ACE inhibitors (ACE), calcium channel blockers, diuretics and non-steroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid, as well as hormonal agents ( for example, estrogens, insulin, thyroxine), was not accompanied by the development of drug interactions.

It is possible to increase the overall effect of carbonic anhydrase inhibitors in patients who simultaneously take an oral carbonic anhydrase inhibitor and dorzolamide. The simultaneous use of dorzolamide and oral administration of carbonic anhydrase inhibitors has not been investigated and is not recommended.

The interaction of dorzolamide with miotics and adrenomimetics in the treatment of glaucoma has been insufficiently studied.