Dorzial, eye drops 20 mg/ml 10 ml

Pharmacotherapeutic group

A carboangidrase inhibitor antiglaucoma drug.

The ATX code: S01EC03

Pharmacological properties

Pharmacodynamics

Dorzolamide hydrochloride is a carboanhydrase II inhibitor.

The inhibition of carboanhydrase (CA) in the ciliary body of the eyeball reduces intraocular fluid production, presumably by slowing the synthesis of bicarbonate ions with their subsequent reduction to sodium and fluid excretion. The result is a decrease in intraocular pressure (IOP).

Pharmacokinetics

. With prolonged use, it selectively accumulates in erythrocytes as a result of selective binding to carboanhydrase II (CA-II), while the plasma concentration of free dorzolamide remains extremely low. Dorzolamide forms a single metabolite, N-dezethyl-dorzolamide, which inhibits to a lesser extent than dorzolamide the KA-II enzyme as well as the KA-I enzyme. The metabolite accumulates in erythrocytes, binding mainly to KA-I. Dorzolamide binds moderately to plasma proteins (about 33%). Dorzolamide and its metabolite are excreted mainly unchanged through the kidneys. After the end of treatment, dorzolamide is eliminated from erythrocytes unevenly, i.e. very intensively in the beginning, resulting in a rapid and significant decrease in concentration, followed by a phase of slow elimination with a half-life of about 4 months.

Indications

The drug is indicated for adult patients with:

• ophthalmohypertension;
• primary open-angle glaucoma;
• pseudoexfoliative glaucoma;
• secondary glaucoma (without block of the anterior chamber angle).

The drug is indicated for children:

• for the treatment of glaucoma in children from 1 week of age in monotherapy or as an adjunct to treatment with beta-adrenoblockers.

Active ingredient

Dorzolamide

Composition

Active ingredient:

Dorzolamide hydrochloride 22.26 mg converted to dorzolamide 20.0 mg

Excipients:

Sodium citrate dihydrate 2.94 mg
Sodium hyaluronate 1.80 mg
Mannitol 23.0 mg
Sodium hydroxide solution 1 M to pH 5.6
Water for injection to 1.0 ml

How to take, the dosage

When using Dorzial, the usual dosage is 1 drop in the affected eye (or both eyes) in the morning, afternoon and evening.

If any anti-glaucoma drug is replaced with Dorsial, treatment with Dorsial should be started the day after the previous drug has been withdrawn.

If Dorsial is used concomitantly with other eye drops, they should be injected at least 10 minutes apart.

Principles for use with a bottle fitted with a dropper dispenser:

1. Remove the safety ring before using the bottle for the first time. Without touching the pipette, turn the bottle with the pipette downwards and lock it between your thumb and forefinger.
   We recommend that the pipette is pumped until the first drop of the product appears by pressing the top of the bottle with your index finger several times before use.
   The bottle must not be mechanically damaged!
2. Tilt your head back, place the dispenser over your eye and use the index finger of one hand to pull down your lower eyelid. Press the vial gently down and drip the desired amount of solution into the conjunctival sac of the eye.
   The tip of the open bottle should never come into contact with the eye surface or hands.
3. Place the cap back on the vial after use.

After opening the vial, the drug may be used for its entire shelf life. After the expiry date the drug should be destroyed. If the vial is visibly damaged, do not use the drug Dorzial.

Interaction

Special studies on the study of interaction of the drug Dorzial with other medicinal products have not been conducted. In clinical trials the drug with dorzolamide in form of eye drops was administered in combination with other medicinal agents without negative manifestations of interdrug interaction, including: timolol and betaxolol eye drops as well as systemic drugs: Angiotensin-converting enzyme (ACE) inhibitors, calcium channel blockers, diuretics, nonsteroidal anti-inflammatory drugs (including acetylsalicylic acid), hormones (estrogen, insulin, thyroxine).

The possibility of mutual enhancement of the systemic effects of carboangiradrase inhibitors for internal use and the drug Dorzial when using them simultaneously is not excluded. Combined treatment with drugs with systemic effects and topical carboangiidrase inhibitors has not been studied in clinical trials.

Dorzial is a carboangiidrase inhibitor, and although used topically, it is partially absorbed and may have a systemic effect. In clinical studies, the use of drugs with dorzolamide in the form of eye drops was not accompanied by a violation of the acid-base balance. However, such phenomena have been observed when using carboanhydrase inhibitors, including as a result of interdrug interaction with other drugs (as a manifestation of toxicity against the background of taking high doses of salicylates). Thus when prescribing Dorzial the possibility of such drug-drug interactions should not be forgotten.

Patients need to tell their physician about all the medications they are using or plan to use, including over-the-counter medications.

Particular caution should be exercised when taking high doses of acetylsalicylic acid, because of the potential for increased toxicity.

Special Instructions

In the elderly, dorzolamide sensitivity may increase (dose reduction required).

There are no data available to study the use of the drug in patients with acute attack of closed angle glaucoma. Discontinuation of the drug in case of allergic reactions should be considered.

In improper use, ophthalmic medications may become contaminated with ocular pathogenic bacteria, which may cause serious damage to the eye and subsequent loss of vision.

Impact on driving and operating ability

When using the drug, it is not recommended to drive vehicles and engage in potentially dangerous activities requiring increased concentration and quick psychomotor reactions.

Synopsis

Transparent colorless or nearly colorless slightly viscous liquid.

Contraindications

• Aged less than 1 week;
• hypersensitivity to the drug components;
• chronic renal failure;
• pregnancy;
• breastfeeding period.

Cautions

The drug has not been studied in patients with severe hepatic impairment and therefore should be used with caution in this category of patients.

Side effects

In clinical trials, dorzolamide in the form of eye drops was administered to 1108 patients as monotherapy or adjunctive therapy to treatment with beta-adrenoblockers. In approximately 3% of patients, the drug was withdrawn due to local ocular adverse reactions, the most common of which were conjunctivitis and eyelid reactions.

The side effects reported in the studies and during the post-registration period are classified by frequency (very common (≥1/10); common (≥1/100, < 1/10); infrequent (≥1/1000, < 1/100); rare (≥1/10000, < 1/1000)).

Nervous system disorders
Often: headache.
Rarely: dizziness, paresthesias.

Sight organ
Very common: burning and pain.
Often: superficial pitting keratitis, lacrimation, conjunctivitis, eyelid inflammation, itching, eyelid irritation, blurred vision.
Infrequent: iridocyclitis.
Rare: red eyes, pain, eyelid hyperkeratosis, transient myopia (disappearing after drug withdrawal), corneal edema, eye hypotony, choroidal detachment after surgical interventions to restore outflow of intraocular fluid.

In the respiratory system, chest and mediastinum
Rarely: nasal bleeding.

Gastrointestinal tract
Often: nausea, bitter taste in the mouth.
Rarely: pharyngitis, dry mouth.

Urinary tract disorders
Rarely: urolithiasis.

Skin and subcutaneous tissue
Rare: contact dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.

General disorders and disorders at the site of administration
Often: asthenia, fatigue.
Rarely: allergic reactions – signs and symptoms of local reactions (on the eyelids) and systemic allergic reactions including angioedema, urticaria, itching, rash, difficulty breathing, rarely – bronchospasm.

Children

In a 3-month, double-blind, multicenter, active-drug comparison study involving 184 children younger than 6 years of age, the adverse reaction profile of dorzolamide in eye-drop form was comparable to the adverse reaction profile in adult patients. Conjunctival injection (5.4%) and ocular discharge (3.6%) were the most common adverse reactions associated with the use of dorzolamide in the form of eye drops in children younger than 2 years of age. In children 2 to 6 years of age, the most common adverse reactions were burning sensation in the eye (12.1%), conjunctival injection (7.6%), pain in the eye (3%). eyelid inflammation (3%).

Overdose

Symptoms

Possible electrolyte disturbances, development of metabolic acidosis and the occurrence of drowsiness, nausea, dizziness, headache, weakness, unusual dreams, dysphagia.

Treatment

Symptomatic therapy is given to maintain vital body functions. Plasma concentrations of electrolytes (especially potassium) and blood pH values should be monitored.

Pregnancy use

The drug is contraindicated in pregnancy and during breast-feeding.

Similarities

Trusopt, Dorzopt, Dorzolamide-Solofarm