Instructions for Dorzol eye drops 2% dropper bottle 5 ml
Composition
active ingredient: dorzolamide;
1 ml of the drug contains 22.3 mg of dorzolamide hydrochloride, which is equivalent to 20 mg of dorzolamide;
excipients: benzalkonium chloride, mannitol (E 421), sodium citrate, sodium hydroxide, hydroxyethylcellulose, purified water.
Dosage form
Eye drops, solution.
Main physicochemical properties: transparent and colorless or almost colorless liquid.
Pharmacotherapeutic group
Ophthalmological agents. Antiglaucoma drugs and miotics. Carbonic anhydrase inhibitors. Dorzolamide.
ATX code S01E C03.
Pharmacological properties
Pharmacodynamics
Carbonic anhydrase (CA) is an enzyme found in many tissues, including the eye. In humans, CA exists in several isoenzymes, the most active of which is CA II. CA II is predominantly found in red blood cells, but is also found in other tissues. Inhibition of CA in the ciliary processes of the eye reduces tear production, primarily by slowing the formation of bicarbonate ions, with subsequent reductions in sodium and fluid concentration. This results in a decrease in intraocular pressure.
Dorzolamide is a potent inhibitor of CA II in humans. After administration, it reduces intraocular pressure, whether or not associated with glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and visual field loss in glaucoma. Intraocular pressure is reduced without the usual side effects of miotics such as night blindness, accommodation spasm, and pupillary constriction. Dorzolamide has no or minimal effects on pulse or blood pressure.
Topical beta-blockers also reduce intraocular pressure by reducing tear production and by other mechanisms of action. Studies have shown that the use of dorzolamide in combination with a topical beta-blocker provides an additional reduction in intraocular pressure. This finding supports the previously known additive effect of beta-blockers and carbonic anhydrase inhibitors.
Pharmacokinetics
Unlike oral carbonic anhydrase inhibitors, topical application of dorzolamide allows the active substance to act directly on the eye, even at low doses, which also reduces its systemic effect. In this way, it is possible to reduce intraocular pressure without disturbing the acid-base and electrolyte balance that accompany the use of carbonic anhydrase inhibitors.
Dorzolamide enters the peripheral circulation even when applied topically. To assess the systemic inhibition of carbonic anhydrase with topical application of the drug, the concentration of the active substance and metabolites in plasma and erythrocytes was determined, as well as the inhibition of carbonic anhydrase activity in erythrocytes. Dorzolamide accumulates in erythrocytes during prolonged use due to selective binding to CA II, while in plasma it is stored in free form in very low concentrations. One N-diethyl metabolite is formed from the active substance, which inhibits the activity of CA II less than the active substance, but also inhibits the activity of the less active isoenzyme (CA I). The metabolite also accumulates in erythrocytes, where it binds first to CA I. Dorzolamide binds to plasma proteins (about 33%). It is excreted first with urine, and in unchanged form. The metabolite is also excreted in the urine. After discontinuation of the drug, dorzolamide is eliminated non-linearly from erythrocytes, with an initial rapid decline in concentration and a subsequent phase of slow elimination with a half-life of approximately 4 months.
Similar pharmacokinetic results have also been obtained with long-term topical use of dorzolamide. In some elderly patients with impaired renal function with creatinine clearance (CrCl) of 30–60 mL/min, increased concentrations of metabolites in erythrocytes are observed, but there is no difference in the degree of carbonic anhydrase inhibition and clinically significant systemic adverse events.
Indication
Dorzol® is used to treat 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 the active substances or to any of the excipients; severe renal impairment (CrCl < 30 ml/min); hyperchloremic acidosis.
Interaction with other medicinal products and other types of interactions
The possibility of interaction of Dorzol® drops with other drugs has not been studied.
No undesirable interactions were observed when dorzolamide was used concomitantly with the following drugs: timolol and betaxolol eye drops, drugs with systemic effects - angiotensin-converting enzyme (ACE) inhibitors, calcium channel blockers, diuretics, nonsteroidal anti-inflammatory drugs, including acetylsalicylic acid, and hormones (e.g. estrogen, insulin, and thyroxine).
The interaction of dorzolamide, a miotic and a β-adrenergic agonist during the treatment of glaucoma has not been fully studied.
Taking it internally increases the risk of developing systemic side effects of dorzolamide.
The effect of acetylcholinesterase inhibitors such as physostigmine, galantamine, neostigmine or pyridostigmine (which are often used in myasthenia gravis) may be reduced by dorzolamide.
When used together with diuretics, significant potassium loss is possible.
Concomitant administration with phenytoin may worsen the course of osteoporosis.
Salicylic acid, when used with dorzolamide, may cause acidosis. In addition, the preservative in dorzolamide drops (benzalkonium chloride) may interact with soft contact lenses.
Application features
Patients with acute angle-closure glaucoma also need to use other medications along with those that lower intraocular pressure. The use of Dorzol® drops in patients with acute angle-closure glaucoma has not been studied.
Like all topically applied ophthalmic drugs, the drug can also be absorbed systemically. Dorzolamide, like sulfonamides, contains a sulfonamide group. Therefore, with topical use, side effects are possible that are also observed with systemic use of sulfonamide drugs, including such severe reactions as Stevens-Johnson syndrome and toxic epidermal necrolysis. If signs of acute reactions or hypersensitivity appear, the drug should be discontinued.
If signs of an allergic reaction appear (conjunctivitis, eyelid reactions), the possibility of discontinuing the use of Dorzol® drops should be considered.
Treatment with oral carbonic anhydrase inhibitors has been associated with urolithiasis as a result of acid-base disturbances, particularly in patients with a history of renal calculi. Although acid-base disturbances have not been observed with Dorzol® eye drops, there have been rare reports of urolithiasis. Dorzolamide is a topical carbonic anhydrase inhibitor that may be systemically absorbed, and patients with a history of renal calculi are at increased risk of urolithiasis.
In patients taking an oral carbonic anhydrase inhibitor and dorzolamide, there is an increased risk of additive systemic effects, therefore concomitant use is not recommended.
There are cases of corneal edema and irreversible corneal decompensation in patients with a history of chronic corneal defects and/or ocular surgery. Dorzolamide should be used with caution in such patients.
Patients taking medications to prevent tearing may experience uveitis with concomitant ocular hypotension after filtration surgery.
Liver dysfunction.
The use of Dorzol® in patients with impaired liver function has not been studied, therefore it should be used with caution in such patients.
The drops contain benzalkonium chloride, which may cause eye irritation.
Direct contact with soft contact lenses should be avoided.
Contact lenses should be removed before instillation of the drug and put back on approximately 15 minutes later.
The drug changes the color of soft contact lenses.
Elderly patients
The indicated dosage also applies to elderly patients.
Ability to influence reaction speed when driving vehicles or other mechanisms
The medicine may cause side effects, such as blurred vision, dizziness, nausea, which may affect the ability to drive and operate other mechanisms.
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
Dorzol® drops are not recommended for use during pregnancy.
Breastfeeding is not recommended when using Dorzol® drops.
Method of administration and doses
It is recommended to instill 1 drop of Dorzol® into the conjunctival sac of the affected eye 3 times a day in the case of monotherapy.
Instill 1 drop into the medial canthus of each eye. Press lightly on the lacrimal sac area immediately after instillation to reduce the possibility of systemic absorption of Dorzol®.
If the drug is used as an adjunctive therapy, together with a topical beta-blocker, instill 1 drop of Dorzol® into the conjunctival sac of the affected eye twice daily.
When one glaucoma medication is replaced with Dorzol® drops, the use of this medication is discontinued by taking the appropriate daily dose and Dorzol® drops should be started the next day.
In the case of topical application of multiple ophthalmic drugs, they should be taken at intervals of 10 minutes.
Patients should be advised to wash their hands before using the medication and not to touch the eye or surrounding surfaces with the pipette.
Patients should also be informed that if eye drops are handled improperly, they may become contaminated with bacteria that can cause eye infections. Using a contaminated solution can cause serious damage and loss of vision.
Children
Data on the use of the drug in children are limited, so it is not used in children.
Overdose
There are no reports of accidental or intentional overdose of dorzolamide taken orally.
Symptoms
When used internally, drowsiness is observed.
With topical application, nausea, dizziness, headache, fatigue, abnormal dreams, and dysphagia have been reported.
Treatment
Treatment of overdose should be symptomatic and supportive.
Electrolyte disturbances, acidosis, and nervous system side effects are possible. Electrolyte levels should be monitored.
Adverse reactions
From the nervous system: headache, dizziness, paresthesia.
On the part of the organs of vision: tingling and burning, superficial punctate keratitis, tearing, 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, foreign body sensation in the eye.
Respiratory, thoracic and mediastinal disorders: epistaxis, sinusitis, rhinitis, shortness of breath.
On the part of the digestive system: nausea and bitter taste in the mouth, throat irritation, dry mouth.
Skin and subcutaneous tissue disorders: contact dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
From the cardiovascular system:
Strong heartbeat, which may be rapid or irregular (palpitations) – frequency cannot be estimated from available data.
On the part of the kidneys and urinary system: urolithiasis (urolithiasis).
General disorders and administration site conditions: asthenia/fatigue, signs and symptoms of hypersensitivity: local palpebral reactions, angioedema, urticaria, pruritus, rash, anaphylaxis and rarely bronchospasm.
Laboratory test results: Dorzolamide was not associated with clinically significant electrolyte abnormalities.
Expiration date
2 years.
Storage conditions
Store out of the reach of children at a temperature not exceeding 30 ° C. After opening the bottle, eye drops should be used within 4 weeks.
Packaging
5 ml of solution in a dropper bottle; 1 dropper bottle in a cardboard box.
Vacation category
According to the recipe.
Producer
Jadran-Galenski Laboratorij dd/Jadran-Galenski Laboratorij dd
Location of the manufacturer and its business address
Svilno 20, 51000 Rijeka, Croatia/Svilno 20, 51000 Rijeka, Croatia
