Instructions Dorzoptic eye drops solution 20 mg/ml dropper bottle 5 ml
Composition
active ingredient: dorzolamide;
1 ml of solution contains 20 mg of dorzolamide as dorzolamide hydrochloride;
excipients: mannitol (E 421); hydroxyethylcellulose; sodium citrate, dihydrate; sodium hydroxide; benzalkonium chloride, 50% solution; water for injections.
Dosage form
Eye drops, solution.
Main physicochemical properties: transparent, colorless, slightly viscous liquid.
Pharmacotherapeutic group
Antiglaucoma drugs for topical use. Carbonic anhydrase inhibitors. Dorzolamide. ATX code S01E C03.
Pharmacological properties
Pharmacodynamics
Dorzolamide is a carbonic anhydrase inhibitor for topical use in the form of eye drops. Carbonic anhydrase is an enzyme present in many tissues of the body (including the tissues of the eye), which is involved in the process of hydration of carbon dioxide and dehydration of carbonic acid. In humans, this enzyme is represented by various isoenzymes, the most active of which is carbonic anhydrase II, which is primarily found in erythrocytes, and then in cells of other tissues. Inhibition of carbonic anhydrase of the ciliary body of the eye leads to a decrease in the secretion of intraocular fluid (mainly due to a decrease in the formation of bicarbonate ions with a subsequent decrease in the transport of sodium ions and fluid).
After topical application, the drug reduces intraocular pressure, regardless of whether its increase is associated with glaucoma.
Dorzolamide reduces intraocular pressure without the development of side effects characteristic of miotic agents, such as night blindness, accommodation spasm, and pupil constriction.
Pharmacokinetics
When applied topically as a 2% ophthalmic solution, dorzolamide reduces elevated intraocular pressure, which is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual impairment (visual field loss).
When administered orally, the effect of dorzolamide occurs within 60-90 minutes and lasts for 8-12 hours. Dorzolamide enters the systemic circulation. In the case of continuous oral administration, dorzolamide accumulates in erythrocytes through selective binding to carbonic anhydrase type II. Very low concentrations of this drug are maintained in plasma in free form.
Dorzolamide is metabolized to N-desyl-dorzolamide, which inhibits carbonic anhydrase II less strongly, but at the same time inhibits the less active isoenzyme - carbonic anhydrase I. This metabolite accumulates in red blood cells, where it mainly binds to carbonic anhydrase I.
Dorzolamide is moderately bound to plasma proteins (approximately 33%). It is excreted in the urine both as unchanged drug (80%) and as metabolites (20%). Release from erythrocytes follows nonlinear kinetics, resulting in an initial rapid decline in concentration followed by a very slow elimination phase with a mean elimination half-life of 4 months. At steady state, renal excretion is approximately 1.3 mg/day at a dose of 4 mg, assuming a renal clearance of 90 ml/min.
When dorzolamide is administered orally to simulate the maximum systemic effect during prolonged topical administration, steady-state concentrations are reached after approximately 13 weeks. At steady state, no free drug or metabolites were detected in plasma. The degree of inhibition of carbonic anhydrase in erythrocytes was below that required to produce a pharmacological effect on the respiratory system or renal function.
In elderly patients with renal insufficiency (creatinine clearance 30-60 ml/min), higher concentrations of the metabolite in erythrocytes were found, but no significant difference in carbonic anhydrase inhibition and no significant clinical side effects were observed.
Unlike oral administration, ophthalmic administration allows for a local effect at lower doses.
When administered intraconjunctivally, the enzymatic activity of carbonic anhydrase is inhibited in corneal endothelial cells, ciliary body, lenticular epithelial cells and cornea within 1-8 hours after application. In the cornea and lenticular epithelial cells, the enzymatic activity is inhibited even 10 hours after instillation.
Dorzolamide is rapidly distributed in ocular tissues. Significant concentrations of dorzolamide appear in the bloodstream within 15 minutes after instillation (in the cornea, tear fluid, iris, ciliary body) and reach maximum levels approximately 1 hour after application.
Indication
Treatment of elevated intraocular pressure in patients with:
ocular hypertension; open-angle glaucoma; pseudoexfoliative glaucoma; as adjunctive therapy to beta-blocker treatment or as monotherapy when beta-blocker treatment has not been successful or beta-blockers are contraindicated.
Contraindication
Hypersensitivity to dorzolamide or to any of the components of the drug.
Severe renal failure (creatinine clearance less than 30 ml/min).
Hyperchloremic acidosis.
Interaction with other medicinal products and other types of interactions
In clinical studies, dorzolamide was used concomitantly with timolol and betaxolol in the form of eye drops, with systemic drugs: angiotensin-converting enzyme (ACE) inhibitors, calcium channel blockers, diuretics and non-steroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid, as well as with hormonal agents (e.g. estrogens, insulin, thyroxine), which was not accompanied by the development of drug interactions.
The interaction of dorzolamide with miotics and adrenomimetics during the treatment of glaucoma has not been sufficiently studied.
Application features
The specifics of the use of Dorzoptic in patients with significant liver dysfunction have not been determined (should be used with caution).
In the treatment of patients with acute angle-closure glaucoma, other therapeutic measures should be used in addition to the use of drugs that reduce intraocular pressure. The use of dorzolamide in patients with acute angle-closure glaucoma has not been studied.
Dorzolamide contains a sulfonamide group and, although applied topically, is subject to systemic absorption. Therefore, when used in the form of eye drops, adverse reactions characteristic of sulfonamides may occur, including Stevens-Johnson syndrome and toxic epidermal necrolysis (Lyell's syndrome). In the event of serious adverse reactions or signs of hypersensitivity, the drug should be discontinued.
Oral carbonic anhydrase inhibitors have been associated with urinary tract stones due to fluid and electrolyte disturbances, particularly in patients with a history of nephrolithiasis. Although fluid and electrolyte disturbances have not been observed with dorzolamide, rare cases of ureterolithiasis have been reported. Since dorzolamide is a locally acting carbonic anhydrase inhibitor that enters the systemic circulation, patients with a history of nephrolithiasis are at increased risk of developing ureterolithiasis with dorzolamide.
In patients receiving oral carbonic anhydrase inhibitors and dorzolamide, there is a potential risk of additive systemic effects of these drugs. The concomitant use of dorzolamide and oral carbonic anhydrase inhibitors is not recommended.
If allergic reactions occur (e.g. conjunctivitis and eyelid reactions), the use of the drug should be discontinued and a doctor should be consulted.
Corneal edema and irreversible corneal decompensation have been reported with dorzolamide in patients with pre-existing chronic corneal defects and/or a history of intraocular surgery. Corneal edema is more likely to occur in patients with low endothelial cell counts. Caution should be exercised when prescribing dorzolamide to such patients.
Cases of choroid detachment have been observed while taking agents that inhibit the production of aqueous humor after filtration procedures.
Dorzoptic contains a preservative (benzalkonium chloride) which may cause irritation. Contact with soft contact lenses should be avoided (remove contact lenses before using the drug and reinsert them 15 minutes after using the drug). Discolors soft contact lenses.
Ability to influence reaction speed when driving vehicles or other mechanisms
No studies of the effect of the drug on the ability to drive or operate machinery have been conducted. Adverse reactions such as dizziness and blurred vision are possible, therefore, during the treatment period, potentially hazardous activities that require concentration of attention and increased speed of psychomotor reactions should be avoided, especially at the beginning of treatment with the drug.
Use during pregnancy or breastfeeding
Clinical trials on the safety of dorzolamide during pregnancy have not been conducted, therefore the use of the drug during this period is not recommended.
It is not known whether dorzolamide is excreted in breast milk, therefore it should not be used during breastfeeding.
Method of administration and doses
When used as monotherapy, 1 drop is prescribed in the affected eye 3 times a day.
In combination with beta-blockers for topical use, 1 drop is prescribed in the affected eye 2 times a day.
If several topical ophthalmic agents are used in the treatment, the administration of the agents should be carried out with an interval of 10 minutes. If switching from treatment with other ophthalmic agents to the use of Dorzoptic, this drug is canceled after the usual daily dosage and the treatment with Dorzoptic is started the next day.
The patient should be warned to wash their hands before use and not to touch the eye and surrounding surfaces with the pipette.
Patients should also be informed that if eye drops are handled improperly, these solutions can become contaminated with bacteria that cause eye infections. If a contaminated solution is used, serious damage with subsequent loss of vision is possible.
Instructions for use:
2. Unscrew the cap on the bottle.
3. It is necessary to tilt the head back and pull the lower eyelid down in order to form a space between the eyelid and the eyeball.
4. Turn the bottle upside down, press lightly with your index finger and thumb on the walls and squeeze 1 drop into the conjunctival sac. Do not touch the tip of the dropper to the surface of the eye or surrounding tissues. If the drop does not reach the conjunctival sac, another drop should be instilled.
5. If the doctor has prescribed the use of the medicine in the conjunctival sac of the other eye, it is necessary to repeat points 3-4.
6. The dispenser tip is designed to accurately dispense 1 drop, so the hole in the dispenser should not be enlarged.
7. After instillation, the bottle cap must be screwed on tightly, but not too tightly.
Children
Not used.
Overdose
There are limited data on overdose in humans following accidental or intentional ingestion of dorzolamide hydrochloride.
Symptoms
Drowsiness has been reported after oral administration. Nausea, dizziness, headache, weakness, unusual dreams, and dysphagia (difficulty swallowing) have been reported with topical administration.
Treatment
Treatment is symptomatic and supportive. Electrolyte imbalance, acidosis, and central nervous system disorders are not excluded. Serum electrolyte levels (especially potassium) and blood pH should be monitored.
Adverse reactions
From the nervous system: headache; dizziness, paresthesia.
Cardiovascular system: palpitations.
On the part of the organs of vision: tingling and burning, superficial punctate keratitis, lacrimation, conjunctivitis, eyelid inflammation, eye itching, eyelid irritation, blurred vision, blepharitis, iridocyclitis, irritation and redness, pain, eyelid peeling, temporary myopia (which disappears after discontinuation of treatment), corneal edema, ocular hypotony, uveitis after filtration surgery.
Frequency unknown: foreign body sensation in the eyes.
From the respiratory system, chest organs and mediastinum: epistaxis, sinusitis, rhinitis.
Frequency unknown: shortness of breath.
On the part of the digestive system: nausea, bitter taste in the mouth, throat irritation, dry mouth.
Skin and subcutaneous tissue disorders: contact dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.
From the kidneys and urinary system: urolithiasis.
General disorders and administration site conditions: asthenia/fatigue, symptoms of hypersensitivity: local palpebral reactions, systemic angioedema, urticaria, pruritus, rash, anaphylaxis, rarely bronchospasm.
Laboratory test results: Dorzolamide was not associated with clinically significant electrolyte abnormalities.
Expiration date
2 years. Do not use after the expiry date stated on the packaging.
The shelf life of the drug after first opening is 4 weeks.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children.
Packaging
5 ml of the drug in a 5 ml polyethylene dropper bottle with a cap with a warranty ring. 1 bottle in a cardboard box.
Vacation category
According to the recipe.
Producer
Warsaw Pharmaceutical Plant Polfa JSC.
Location of the manufacturer and its business address
Karolkova St. 22/24, 01-207 Warsaw, Poland.
