Pharmacodynamics and pharmacokinetics
The drug is a local carbonic anhydrase . The mechanism of action is based on inhibition of the secretion of intraocular fluid and slowing down the formation of bicarbonate with a subsequent weakening of the transfer of sodium and water.
The drug does not cause spasm of accommodation, as well as miosis or hemeralopia.
Pharmacokinetic information
- Absorption occurs through the cornea, and also, to a lesser extent, through the sclera and limbus. Systemic absorption rates are low. Once in the blood stream, it quickly penetrates into red blood cells with a significant content of carbonic anhydrase II.
- Binding to plasma proteins occurs by 33%. Converts to an N-desethylated metabolite , which is less active towards carbonic anhydrase II , but is capable of blocking carbonic anhydrase I. Long-term use leads to accumulation in red blood cells.
- Excreted through the kidneys. Withdrawal of the drug has two phases of elimination: fast and subsequent slow, due to the gradual release of the substance from red blood cells.
- Half-life: approximately 4 months.
Contraindications
- increased or hypersensitivity to the components of eye drops;
- severe renal dysfunction;
- hyperchloremic acidosis;
- age group: under 18 years old;
- lactation period.
Use with caution
- patients with low density of corneal endothelial cells, due to an increased likelihood of corneal edema;
- patients with liver failure ;
- for diabetes mellitus .
Dorzopt Plus, 1 piece, 5 ml, 20 mg/ml+5 mg/ml, eye drops
The drug Dorzopt Plus, like other ophthalmic drugs used topically, can penetrate the systemic circulation. Since timolol, which is part of the drug, is a beta-blocker, adverse reactions that develop with the systemic use of beta-blockers may occur with topical use of the drug Dorzopt Plus.
Reactions from the cardiovascular and respiratory systems
Before starting to use the drug Dorzopt Plus, it is necessary to ensure adequate monitoring of the state of the cardiovascular system.
Patients with a history of cardiovascular disease, including heart failure, should be closely monitored for signs of worsening of these diseases (monitoring heart rate and blood pressure).
Cases of fatal heart failure have been reported with the use of timolol eye drops.
When the first signs or symptoms of heart failure appear, the use of Dorzopt Plus should be discontinued.
Patients with first-degree heart block should be prescribed beta-blockers with caution due to their ability to slow impulse conduction.
There have been reports of cases of fatal bronchospasm in patients with bronchial asthma during the use of timolol in the form of eye drops.
In patients with mild to moderate COPD, Dorzopt Plus should be used with caution and only if the expected benefit of treatment outweighs the potential risk.
The drug should be used with caution in patients with severe peripheral circulatory disorders (severe forms of Raynaud's disease or syndrome).
Diabetes
The drug should be used with caution in patients with spontaneous hypoglycemia or in patients with diabetes mellitus (especially with a labile course) while using insulin or oral hypoglycemic drugs, since beta-blockers may mask the symptoms of hypoglycemia.
Hyperthyroidism
Beta blockers may mask some clinical signs of hyperthyroidism (eg tachycardia). If hyperthyroidism is suspected, patients should be closely monitored. Abrupt withdrawal of beta-blockers should be avoided due to the risk of developing thyrotoxic crisis.
Anesthesia in surgery
The need to discontinue beta-blockers in the event of upcoming major surgery has not been proven. The effects of beta-blockers during surgery, if necessary, can be eliminated by using sufficient doses of adrenergic agonists.
Liver dysfunction
Studies of the use of Dorzopt Plus in patients with liver failure have not been conducted, so the drug should be used with caution in such patients.
Allergies and hypersensitivity reactions
Like other ophthalmic drugs for topical use, Dorzopt Plus can penetrate into the systemic circulation. Dorzolamide, which is part of the drug, is a sulfanilamide. Adverse reactions identified with systemic use of sulfonamides may occur with topical use of the drug (Stevens-Johnson syndrome and toxic epidermal necrolysis). If signs of serious hypersensitivity reactions occur, the drug should be discontinued.
When treating patients with atopy or a history of severe anaphylactic reactions to various allergens with running blockers, the response may be enhanced upon repeated exposure to these allergens. In this group of patients, the use of epinephrine at a standard therapeutic dose to relieve allergic reactions may not be effective.
Concomitant therapy
When using the drug Dorzopt Plus in patients taking systemic beta-blockers, it is necessary to take into account the possible mutual enhancement of the pharmacological action of the drugs, both in relation to the known systemic effects of beta-blockers and in relation to the reduction of intraocular pressure. The combined use of Dorzopt Plus with other beta-blockers is not recommended.
Discontinuation of therapy
If it is necessary to discontinue topical use of timolol, as in the case of discontinuation of systemic beta-blockers, discontinuation of therapy in patients with coronary heart disease should be carried out gradually.
Corneal disorders
Beta-blockers used in ophthalmology can cause dryness of the eye mucosa. In patients with corneal disorders, the drug should be used with caution. Patients with low endothelial cell counts have an increased risk of developing corneal edema.
Urolithiasis disease
The use of systemic carbonic anhydrase inhibitors can lead to acid-base imbalance and be accompanied by urolithiasis, especially in patients with a history of urolithiasis.
Dorzopt Plus contains a carbonic anhydrase inhibitor, which, when applied topically, can be absorbed and penetrate into the systemic circulation, so the risk of developing urolithiasis in patients with a history of urolithiasis when treated with Dorzopt Plus may increase.
Use in the elderly
In clinical studies, no difference in the effectiveness and safety of dorzolamide + timolol was found in patients over 65 years of age compared with younger patients. However, the possibility of higher sensitivity to the drug in some elderly patients should not be excluded.
Using contact lenses
Dorzopt Plus contains the preservative benzalkonium chloride, which may cause eye irritation. Therefore, before using the drug, patients should remove soft contact lenses and put them back no earlier than 15 minutes after instillation of the drug. Benzalkonium chloride can discolor soft contact lenses.
Impact on the ability to drive vehicles and machinery
During the period of use of the drug Dorzopt Plus, it is necessary to refrain from driving vehicles and machinery and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Side effects
Local
- burning and itching in the eye area, swelling of the eyelids, paresthesia , lacrimation, impaired visual clarity, conjunctivitis , blepharitis , superficial punctate keratitis , photophobia ;
- Rare cases of iridocyclitis , allergic reactions, increased corneal thickness, hypotonia , and retinal detachment after AGO ( anti-glaucomatous operations ) are rare.
System
- a feeling of bitterness in the mouth, nausea, development of asthenia , nephrourolithiasis , malignant exudative erythema, migraine, toxic epidermal necrolysis, agranulocytosis , aplastic anemia , skin rashes.
Dorzopt 2% eye drops dropper bottle 5ml No. 3
A country
Romania
The country of production may vary depending on the batch of goods. Please check with the operator for detailed information when confirming your order.
Compound
Bottle 5 ml Dorzolamide (in the form of hydrochloride) 20 mg per 1 ml. Excipients: hyethylose - 1 mg, mannitol - 20 mg, citric acid monohydrate - 4 mg, sodium hydroxide - 2.4 mg, benzalkonium chloride - 0.1 mg, purified water - up to 1 ml. Eye drops 2% transparent, colorless.
pharmachologic effect
Antiglaucoma drug, local carbonic anhydrase inhibitor. Reduces the secretion of intraocular fluid, slowing down the formation of bicarbonate with a subsequent weakening of the transfer of sodium and water. Does not cause spasm of accommodation, miosis, hemeralopia.
Indications for use
- open-angle (including secondary) glaucoma; - pseudoexfoliative glaucoma; - ocular hypertension.
Mode of application
Instill 1 drop into the conjunctival sac of the affected eye 3 times a day. In combination with beta-blockers for local use - 1 drop 2 times a day. If several local ophthalmic drugs are used during treatment, they are administered at intervals of 10 minutes.
Interaction
Antiglaucoma drugs (beta-blockers, pilocarpine, dipivefrin, carbachol) enhance the effect of dorzolamide. When used simultaneously with acetazolamide, the risk of developing systemic side effects increases. Increased toxicity is possible when taking large doses of acetylsalicylic acid.
Side effect
Local reactions: burning, paresthesia, itching in the eyes, lacrimation, blurred vision, irritation and swelling of the eyelids, conjunctivitis, superficial punctate keratitis, blepharitis, photophobia. Rarely - iridocyclitis, increased corneal thickness, allergic reactions, eye hypotonia, retinal detachment in patients after antiglaucomatous operations. Systemic reactions: bitterness in the mouth, nausea, headache, asthenia, nephrourolithiasis, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), agranulocytosis, aplastic anemia, skin rashes.
Contraindications
- chronic renal failure (creatinine clearance less than 30 ml/min); - hyperchloremic acidosis; - childhood and adolescence under 18 years of age; - pregnancy; - lactation period (breastfeeding); - simultaneous oral administration of carbonic anhydrase inhibitors; - increased sensitivity to any or a component of the drug. The drug is prescribed with caution for diabetes mellitus, liver failure, corneal diseases, and use in patients after antiglaucomatous operations (risk of eye hypotony, retinal detachment).
Overdose
Symptoms: impaired water-electrolyte metabolism, acidosis, central nervous system disorders. Treatment: symptomatic therapy. Electrolyte levels (especially potassium) and blood pH levels need to be monitored.
special instructions
The preservative benzalkonium chloride contained in the drug can be adsorbed by soft contact lenses, causing eye irritation and toxic effects. The drug is used only after removing contact lenses. Contact lenses should be installed no earlier than 15 minutes after instillation. Monitoring of the content of potassium, electrolytes in the blood serum and its pH is necessary. Elderly patients may increase sensitivity to dorzolamide, so this category of patients may require a dose reduction. Impact on the ability to drive vehicles and operating machinery During treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Dispensing conditions in pharmacies
On prescription
Interaction
- Combination with antiglaucoma drugs ( β-blockers , Pilocarpine , Dipivefrin , Carbachol ) causes an increase in the action of Dorzolamide .
- With Acetazolamide - increased risk of systemic adverse reactions.
- With large doses of Acetylsalicylic acid , increased toxicity is likely.
special instructions
The use of Dorzopt Plus solution requires adequate control of the cardiovascular system.
Dorzopt Plus contains benzalkonium chloride, a preservative that can precipitate in hydrophilic contact lenses, causing a damaging effect on the tissues of the organ of vision. Therefore, patients using soft contact lenses should remove them before applying drops, and install them back after instillation approximately 20 minutes later.
When prescribing a planned surgical operation, Dorzopt Plus solution is canceled 48 hours before general anesthesia, due to the enhanced effect of muscle relaxants, as well as general anesthesia.
During the treatment period, there is a need to refrain from driving vehicles and not engage in activities associated with dangerous mechanisms.
Store Dorzopt Plus solution at room temperature. Keep away from children.
Shelf life – 2 years. Shelf life after opening is one month.
Dorzopt price, where to buy
Average price per eye. Dorzopt drops 2% (5 ml bottle) – 360-370 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
ZdravCity
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RUR 869 order
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Pharmacy24
- Dorzoptik 20 mg/ml 5 ml No. 1 eye drops Warsaw FZ, Polfa AT, Poland
153 UAH.order
