Instructions for Dorzamed 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; hydroxyethylcellulose; sodium hydroxide; mannitol (E 421); citric acid monohydrate; purified water.
Dosage form
Eye drops, solution.
Main physicochemical properties: clear solution without visible particles.
Pharmacotherapeutic group
Antiglaucoma drugs and miotics. Carbonic anhydrase inhibitors. Dorzolamide. ATX code S01E C03.
Pharmacological properties
Pharmacodynamics
Dorzolamide is a potent inhibitor of human carbonic anhydrase II (CA-II). After topical application, it reduces elevated intraocular pressure, whether associated with or not associated with glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field narrowing.
The reduction in intraocular pressure with dorzolamide is not accompanied by the development of common adverse reactions characteristic of miotics, such as night blindness, accommodation spasm and mydriasis. It has no or negligible effect on blood pressure and pulse rate.
Unlike oral carbonic anhydrase inhibitor preparations, topical dorzolamide acts directly in the eye at significantly lower concentrations, and therefore such use is accompanied by less systemic exposure.
The efficacy of dorzolamide, used in patients with glaucoma or ocular hypertension as monotherapy 3 times a day (initial intraocular pressure ≥ 23 mmHg) or 2 times a day as an adjunct to topical beta-blockers (initial intraocular pressure ≥ 22 mmHg), has been confirmed in clinical studies. When used both as monotherapy and in combination with beta-blockers, dorzolamide reduced intraocular pressure throughout the day, and this effect was maintained over a long period of time. The efficacy of dorzolamide after long-term use as monotherapy was similar to that of betaxolol and only slightly less than that of timolol. When dorzolamide was used as an adjunct to topical beta-blockers, an additional reduction in intraocular pressure was observed, similar to that of pilocarpine 2% 4 times a day.
Pharmacokinetics
When applied topically, dorzolamide enters the systemic circulation.
Moderately bound to plasma proteins (approximately 33%). With prolonged use, dorzolamide accumulates in erythrocytes due to selective binding to CA-II, while extremely low concentrations of free active substance are maintained in plasma. Dorzolamide forms one N-desethylated metabolite, which inhibits CA-II to a lesser extent than the parent compound, but also inhibits the less active isoenzyme CA-I. The metabolite also accumulates in erythrocytes, where it binds predominantly to CA-I.
Excreted in urine mainly unchanged; the metabolite is also excreted in urine. After discontinuation of use, there is a nonlinear washout of dorzolamide from erythrocytes, which initially leads to a rapid decrease in dorzolamide concentrations, followed by a slower elimination phase with a half-life of approximately 4 months.
Indication
Additional therapy in the treatment of topical beta-blockers. Monotherapy when topical beta-blockers are insufficiently effective or contraindicated. Treatment of increased intraocular pressure in: Ocular hypertension; Open-angle glaucoma; Pseudoexfoliative glaucoma.
Contraindication
Hypersensitivity to the active substance or to any of the other components of the drug. Severe renal impairment (creatinine clearance less than 30 ml/minute). Hyperchloremic acidosis.
Interaction with other medicinal products and other types of interactions
No specific studies of the interaction of dorzolamide with other drugs have been conducted.
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.
There is a potential for increased overall effects of carbonic anhydrase inhibitors in patients receiving oral carbonic anhydrase inhibitors and dorzolamide. The concomitant use of dorzolamide and oral carbonic anhydrase inhibitors has not been studied and is not recommended.
The interaction of dorzolamide with miotics and adrenomimetics during the treatment of glaucoma has not been sufficiently studied.
Application features
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.
In case of allergic reactions (such as conjunctivitis, eyelid reactions), discontinuation of the drug should be considered.
Dorzolamide has not been studied in patients with hepatic impairment and should be used with caution in such patients.
Corneal edema and irreversible corneal decompensation have been observed in patients with previously diagnosed chronic corneal defects and/or a history of intraocular surgery during the use of dorzolamide. The drug should be used with caution in such patients.
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.
Cases of choroid detachment have been observed while taking agents that inhibit the production of aqueous humor after filtration procedures.
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.
The product contains the preservative benzalkonium chloride, which may cause eye irritation and discolouration of soft contact lenses. Contact lenses should be removed before using the product and reinserted no earlier than 15 minutes after instillation.
Ability to influence reaction speed when driving vehicles or other mechanisms
Studies on the effect of dorzolamide on the ability to drive or use machines have not been conducted. During the use of the drug, side effects such as dizziness and visual disturbances may develop, which may affect the ability to drive or use machines.
Use during pregnancy or breastfeeding
There are no adequate and well-controlled studies of dorzolamide in pregnant women. The drug is not recommended for use during pregnancy.
It is not known whether dorzolamide passes into breast milk. If necessary, breastfeeding should be discontinued.
Method of administration and doses
The drug is intended for ophthalmic use only.
As monotherapy.
Apply 1 drop of the drug into the affected eye(s) 3 times a day.
As an additional therapy.
Apply 1 drop of the drug into the affected eye(s) 2 times a day.
If it is necessary to replace another topical antiglaucoma agent with dorzolamide, treatment with that agent should be discontinued and the drug should be started the next day.
When using multiple topical ophthalmic agents, they should be instilled at least 10 minutes apart.
Wash your hands before using the medicine and avoid any contact of the dropper tip with the eye or skin when instilling the drops. If handled improperly, eye drops can become contaminated with common bacteria that cause eye infections. Using contaminated eye drops can lead to serious eye damage and loss of vision.
Children
Clinical data on the use of dorzolamide in children are limited. The drug should not be used in children.
Overdose
Symptoms.
Data on overdose with dorzolamide in humans are limited. The following symptoms have been observed: after oral administration - drowsiness; after topical application - nausea, dizziness, headache, fatigue, abnormal dreams and dysphagia. Electrolyte disturbances, asthenia and central nervous system symptoms may occur.
Treatment.
In case of overdose, symptomatic and supportive therapy should be carried out. Plasma electrolyte concentrations (especially potassium) should be checked and blood pH determined.
Adverse reactions
The following adverse reactions have been reported with dorzolamide during clinical trials and post-marketing surveillance.
Adverse reactions are classified according to frequency as follows: very common (≥ 1/10); common (≥ 1/100,
From the nervous system:
often - headache; rarely - paresthesia, dizziness.
very often - burning and tingling; often - superficial punctate keratitis, lacrimation, conjunctivitis, blepharitis, itching in the eyes, eye irritation, blurred vision; infrequently - iridocyclitis; rarely - irritation, including redness, pain, eyelid adhesion, transient myopia (reversible after discontinuation of treatment), corneal edema, ocular hypotension, choroid detachment after filtration procedures; unknown - sensation of a foreign body in the eye.
From the respiratory system, chest organs and mediastinum:
Rare: epistaxis; unknown: dyspnea.
From the heart:
unknown – palpitations.
From the digestive tract:
often - nausea, bitter taste in the mouth; rarely - throat irritation, dry mouth.
Skin and subcutaneous tissue disorders:
rarely - contact dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).
From the kidneys and urinary tract:
rarely - urolithiasis.
General violations:
often - asthenia/fatigue; rarely - hypersensitivity reactions, including palpebral reactions,
angioedema, urticaria, itching, rash, shortness of breath, bronchospasm.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions that occur after the marketing authorisation of a medicinal product is very important. This allows the benefit/risk balance of the medicinal product to be continuously monitored. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system.
Expiration date
2 years.
After opening the bottle, eye drops should be used within 4 weeks.
Storage conditions
Store at a temperature not exceeding 25 ºС in a place inaccessible to children.
Packaging
5 ml in a dropper bottle, 1 dropper bottle in a cardboard box.
Vacation category
According to the recipe.
Producer
JSC "Rompharm Company SRL".
Location of the manufacturer and its business address
Otopeni city, Eroilor str. № 1A, 075100, jud. Ilfov, Romania.
