Dorzopt and Dorzopt Plus are eye drops that are used in the treatment of glaucoma. The drug belongs to carbonate hydrolysis inhibitors. The medication does not cause myopia or pupil constriction .
Many patients think about the difference between Dorzopt and Dorzopt Plus. The difference between these drugs is that the second has a more pronounced effect due to the content of two active substances - dorzolamide and timolol.
Pharmacological properties
Dorzopt Plus solution is an antiglaucoma combination drug. Each of its components reduces intraocular pressure, reducing the secretion of aqueous humor inside the eye.
Dorzolamide is a carbonic anhydrase inhibitor. Its action reduces the production of intraocular fluid and slows down the formation of bicarbonate, which subsequently weakens the transfer of sodium and water. It is not capable of causing accommodation spasm, miosis or hemeralopia.
Timolol is a non-selective β-adrenergic receptor blocker. Prevents the effect of catecholamines on β-adrenergic receptors. When applied topically as a solution of eye drops, it reduces intraocular pressure as it reduces the formation of aqueous humor and slightly increases its outflow.
Composition and release form
The drug Dorzopt plus is available in the form of eye drops, a colorless, transparent, somewhat viscous solution. Each milliliter of medicine contains two active substances:
- Dorzolamide (hydrochloride) 20 mg;
- Timolol (maleate) 5 mg.
Auxiliary components include mannitol, benzalkonium chloride, hydroxyethylcellulose, purified water, acidity stabilizers.
5 ml of solution are placed in dropper bottles made of polymer material.
Contraindications
- COPD and bronchial asthma (including indication in medical history);
- Sinus bradycardia;
- Severe heart failure and AV block;
- Cardiogenic shock;
- Severe degrees of renal failure;
- Corneal degeneration;
- Pregnancy;
- Lactation;
- Age up to 18 years;
- Individual hypersensitivity.
The drug should be prescribed with caution in case of liver failure, diabetes mellitus, and in old age.
How are medications similar?
There are the following similarities between the drugs Dorzopt and Dorzopt Plus:
- Both medications are available in eye drops.
- Both drugs are used for open-angle and pseudoexfoliative glaucoma.
- Eye drops are contraindicated if you are allergic to their composition, children under 18 years of age, pregnant women and those supporting breastfeeding, patients with chronic renal failure when the glomerular filtration rate is less than 30 ml per minute. They should be used with caution in diabetes mellitus and liver failure.
- Both medications can cause pinpoint keratitis, lacrimation, irritation and inflammation of the eyelid, iridocyclitis, headache, nausea, impotence, paresthesia, conjunctivitis.
- Dorzopt and Dorzopt plus can be purchased at the pharmacy upon presentation of a prescription.
- To ensure that medications do not lose their therapeutic effect, they must be stored at temperatures up to 25 degrees, in a dry place, protected from light, for 2 years from the date of issue. After opening the bottle, eye drops can be used for a month.
Side effects
- Inflammation, irritation and peeling of the eyelids, iridocyclitis, myopia, which goes away when the drug is discontinued, punctate keratitis, conjunctivitis, keratitis, dry eye syndrome, diplopia, ptosis.
- Headache, asthenia, paresthesia, tinnitus, depression, memory loss.
- Angioedema, bronchospasm, itching, urticaria, alopecia, exacerbation of psoriasis.
- Nosebleeds, dry mouth, throat irritation, rash.
- Arrhythmia, fainting, decreased blood pressure, rhythm disturbances, decreased temperature of the extremities, edema, Raynaud's syndrome.
- Bronchospasm, cough and chest pain.
- Diarrhea, dry mouth, decreased libido, Peyronie's disease.
Dorzopt plus eye drops 5ml bottle
A country
Russia, 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.
Active substance
Dorzolamide + Timolol
Compound
hyethylose - 1 mg, citric acid monohydrate - 4 mg, sodium hydroxide solution 1M - 0.066 ml, mannitol - 20 mg, benzalkonium chloride - 0.075 mg, sodium hydroxide solution 1M/hydrochloric acid solution 1M - to pH 5.6±0.1, purified water - up to 1 ml.
pharmachologic effect
An antiglaucoma drug that contains two active ingredients: dorzolamide and timolol, each of which reduces increased intraocular pressure by reducing the secretion of intraocular fluid. The combined effect of these substances in the combined drug Dorzopt Plus leads to a more pronounced decrease in intraocular pressure. Dorzolamide is a selective inhibitor of type II carbonic anhydrase. Inhibition of carbonic anhydrase of the ciliary body leads to a decrease in the secretion of intraocular fluid, presumably due to a decrease in the formation of bicarbonate ions, which in turn leads to a slowdown in the transport of sodium and intraocular fluid. Timolol is a non-selective beta-blocker. Although the exact mechanism of action of timolol in reducing intraocular pressure has not yet been established, a number of studies have shown a predominant decrease in the formation of intraocular fluid, as well as a slight increase in its outflow. The decrease in intraocular pressure occurs 20 minutes after instillation, reaches a maximum after 2 hours and continues for at least 24 hours
Indications for use
- increased intraocular pressure in open-angle glaucoma and pseudoexfoliative glaucoma with insufficient effectiveness of monotherapy.
Mode of application
The drug Dorzopt Plus is recommended to instill 1 drop into the conjunctival sac of the eye (or both eyes) 2 times a day. If the drug Dorzopt Plus is prescribed as a replacement for another ophthalmic drug for the treatment of glaucoma, the latter must be discontinued 1 day before the start of therapy with Dorzopt Plus. In the case of combined use with other local ophthalmic drugs, the drug Dorzopt Plus should be administered at intervals of 10 minutes. With nasolacrimal occlusion (closing of the eyelids) for 2 minutes after instillation of the drug, its systemic absorption decreases, which can lead to increased local action. The drug Dorzopt Plus is a sterile solution, so patients must be instructed how to use the bottle correctly. The duration of treatment is determined by the doctor depending on the clinical condition of the patient. Dorzopt Plus is contraindicated for use during pregnancy and lactation (breastfeeding). Dorzolamide Data on the use of dorzolamide not enough during pregnancy. Studies on rats have revealed the teratogenic effect of dorzolamide in doses toxic to pregnant females. It is not known whether dorzolamide passes into the breast milk of nursing women. A decrease in body weight gain was found in the offspring of lactating female rats treated with dorzolamide. Timolol There is insufficient data on the use of timolol during pregnancy. Epidemiological studies have not found the effect of beta-blockers when taken orally on the formation of congenital malformations, but intrauterine growth retardation has been identified. In addition, signs and symptoms of β-adrenergic receptor blockade (bradycardia, hypotension, respiratory failure, hypoglycemia) were found in newborns when beta-blockers were used before birth. Beta-blockers pass into breast milk. During the period of breastfeeding, it is necessary to discontinue use of the drug Dorzopt Plus or stop breastfeeding. Contraindicated in children and adolescents under the age of 18 years.
Interaction
There have been no studies of the interaction of the drug Dorzopt Plus with other drugs. However, there is a possibility of enhancing the hypotensive effect and/or developing severe bradycardia when timolol ophthalmic solution is used together with slow calcium channel blockers, sympatholytics, beta-blockers, antiarrhythmic drugs (including amiodarone ), cardiac glycosides, parasympathomimetics, opioid analgesics and MAO inhibitors. With the combined use of timolol and inhibitors of the CYP2D6 isoenzyme (for example, quinidine or selective serotonin reuptake inhibitors), a potentiated effect of systemic blockade of β-adrenergic receptors (for example, decreased heart rate, depression) has been reported. Despite the fact that the carbonic anhydrase inhibitor dorzolamide, which is part of Dorzopt Plus, is used topically, it can penetrate into the systemic circulation. In clinical studies of the use of dorzolamide ophthalmic solution, no acid-base balance disorders were identified. However, with systemic use of carbonic anhydrase inhibitors, these disorders are known, and in some cases they may affect interactions with other drugs (for example, enhance toxic reactions when using salicylates in high doses). Systemic beta-blockers may enhance the effect of hypoglycemic drugs. Systemic beta-blockers can increase the severity of arterial hypertension, which is the effect of clonidine withdrawal. There is isolated data on the development of mydriasis with the combined use of timolol and adrenaline. There is a possibility of enhancing the known systemic effects of carbonic anhydrase inhibition with the combined use of local and systemic carbonic anhydrase inhibitors. Because There are no data on the use of such a combination; the combined use of Dorzopt Plus and systemic carbonic anhydrase inhibitors is not recommended.
Side effect
In clinical studies, the drug was generally well tolerated. Adverse reactions were limited to known adverse reactions with dorzolamide and timolol. Systemic adverse reactions were mild and did not lead to drug discontinuation. In approximately 1.2% of patients, the drug was discontinued due to local allergic reactions. Among the most common adverse local reactions were a burning sensation or itching in the eyes, corneal erosions, injection of the vessels of the conjunctiva of the sclera, blurred vision, lacrimation, distortion of taste. In the post-registration period, when using the combination of dorzolamide + timolol, the following adverse reactions were noted: shortness of breath, respiratory failure, bradycardia , AV block, choroidal detachment, nausea, contact dermatitis, Stevens-Johnson syndrome and toxic epidermal necrolysis. Cases of edema and irreversible destruction of the cornea have been reported in patients with chronic corneal defects and/or those who have undergone intraocular surgery. The following possible adverse reactions of the active components of the drug are known. Dorzolamide From the nervous system: headache, dizziness, asthenia/fatigue, paresthesia. From the organ of vision : inflammation of the eyelid, lacrimation, irritation and peeling of the eyelid, iridocyclitis, punctate keratitis, transient myopia (passing after discontinuation of the drug). Allergic reactions: angioedema, bronchospasm, urticaria, itching, rash. From the respiratory system: nosebleeds. Timolol (local application) Mental disorders: depression. From the immune system: anaphylaxis, angioedema, urticaria, local or generalized rash. From the nervous system: tinnitus, paresthesia, headache, asthenia, fatigue, dizziness, insomnia, nightmares, decreased memory, increasing symptoms of myasthenia gravis. From the respiratory system: bronchospasm (mainly in patients with previous broncho-obstructive pathology), cough, chest pain. From the organ of vision: conjunctivitis, blepharitis, keratitis, decreased sensitivity of the cornea, dry eye syndrome; visual disturbances, including changes in the refractive power of the eye (in some cases due to the withdrawal of miotics), diplopia, ptosis. From the cardiovascular system: arrhythmia, cardiac arrest, decreased blood pressure, fainting, Raynaud's syndrome, decreased temperature of the hands and feet. from the digestive system: diarrhea, dyspepsia, dry mouth, pharyngeal irritation, abdominal pain. From the skin and subcutaneous tissues: alopecia, psoriasis-like rash or exacerbation of psoriasis. From the musculoskeletal system and connective tissue: lameness, systemic lupus erythematosus. From the reproductive system: decreased libido, Peyronie's disease. General disorders and disorders at the injection site: edema. Timolol (systemic use) From the blood and lymphatic system: non-thrombocytopenic purpura. From the nervous system: weakness, dizziness, increased drowsiness, decreased concentration attention. From the endocrine system: hyperglycemia, hypoglycemia. From the respiratory system: pulmonary edema, wheezing. From the cardiovascular system: decreased tolerance to physical exercise, AV blockade II-III degree, sinotrial blockade, decompensation of heart failure, progression angina pectoris, vasodilation. From the digestive system: vomiting. From the skin and subcutaneous tissues: exfoliative dermatitis, skin itching, increased sweating. From the kidneys and urinary tract: urinary disorders. From the musculoskeletal system: pain in the extremities, arthralgia. From the reproductive system: impotence. Laboratory and instrumental data: rarely - a slight increase in the concentration of residual nitrogen, potassium, uric acid and triglycerides in the blood plasma; a slight decrease in the concentration of hemoglobin, hematocrit, cholesterol, HDL. These changes were not clinically manifested and did not progress.
Contraindications
- hyperreactivity of the respiratory tract; - bronchial asthma (including a history); - severe chronic obstructive pulmonary disease (COPD); - sinus bradycardia; - SSSS; - sinoatrial block; - AV block II-III degree; - severe heart failure;—cardiogenic shock;—severe renal failure (creatinine clearance less than 30 ml/min);—hyperchloremic acidosis;—dystrophic processes in the cornea;—pregnancy;—lactation (breastfeeding);—childhood and adolescence up to 18 years ( because the effectiveness and safety have not been sufficiently studied); - hypersensitivity to the components of the drug. The drug should be prescribed with caution if there is a history of cardiovascular diseases, including heart failure; AV blockade of the first degree; mild to moderate COPD; severe peripheral circulatory disorders (severe forms of Raynaud's disease or Raynaud's syndrome); liver failure; diabetes mellitus; urolithiasis (including history); hyperthyroidism; corneal disorders; elderly patients.
Overdose
There are no data on accidental or intentional overdose of the drug. Cases of unintentional overdose of timolol in the form of eye drops with the development of systemic symptoms of beta-blocker overdose with systemic use have been described: dizziness, headache, shortness of breath, bradycardia, bronchospasm, cardiac arrest. The most expected symptoms of dorzolamide overdose are electrolyte imbalance, development of acidosis, headache, asthenia/fatigue, paresthesia. Treatment: symptomatic and supportive therapy. The concentration of electrolytes (primarily potassium) and blood plasma pH should be monitored. Timolol is not excreted during dialysis.
special instructions
Dorzopt Plus, like other ophthalmic drugs for topical use, can penetrate into the systemic circulation. Since timolol, which is part of the drug, is a beta-blocker, undesirable reactions that develop with the systemic use of beta-blockers may be observed with topical use of the drug Dorzopt Plus. Reactions from the cardiovascular and respiratory systems Before starting the use of the drug Dorzopt Plus, it is necessary to ensure adequate monitoring of the condition 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 in the form of eye drops. When the first signs or symptoms of heart failure appear, the use of the drug 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. Cases of bronchospasm with fatal outcome in patients have been reported with bronchial asthma while using 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 Raynaud's syndrome). Diabetes mellitus 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 can mask symptoms of hypoglycemia. Hyperthyroidism Beta-blockers may mask some clinical signs of hyperthyroidism (for example, tachycardia). If hyperthyroidism is suspected, patients should be closely monitored. Abrupt withdrawal of beta-blockers should be avoided due to the risk of developing a thyrotoxic crisis. Anesthesia in surgery The need to discontinue beta-blockers in the event of an upcoming major surgical intervention has not been proven. The effects of beta-blockers during surgery, if necessary, can be eliminated by using sufficient doses of adrenergic agonists. Impaired liver function. Studies on the use of the drug Dorzopt Plus in patients with liver failure have not been conducted, so the drug should be used with caution in such patients. Allergy and hypersensitivity reactions Like others ophthalmic preparations for topical use, the drug 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 appear, the drug should be discontinued. When treating patients with atopy or severe anaphylactic reactions to various allergens in history, the response may be enhanced upon repeated contact with these allergens. In this group of patients, the use of epinephrine in a standard therapeutic dose to relieve allergic reactions may be ineffective. 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, as in relation to the known systemic effects of beta-blockers , and in relation to reducing 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 artery disease should be carried out gradually. Corneal disorders Beta-blockers used in ophthalmology may cause dryness of the eye mucosa. In patients with corneal disorders, the drug should be used with caution. Patients with a low number of endothelial cells have an increased risk of developing corneal edema. Urolithiasis 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, it can be absorbed and penetrate into the systemic circulation, therefore the risk of developing urolithiasis in patients with a history of urolithiasis during treatment with Dorzopt Plus may increase. Use in elderly patients In clinical studies of the difference in the effectiveness and safety of the combination of dorzolamide + timolol in patients over the age of 65 years of age compared with younger patients was not identified. However, the possibility of higher sensitivity to the drug in some elderly patients should not be excluded. Use of 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. Effect 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.
Dispensing conditions in pharmacies
On prescription
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.
Instructions for use
The medicine is indicated for use one drop at a time . Instillation is carried out into the conjunctival sac three times a day. For Dorzopt plus, the instructions for use indicate that it is necessary to apply drops 2 times a day. If several ophthalmic agents are used, they are administered at intervals of 20 minutes. The duration of therapy should be determined by a specialist. It depends on the patient's condition.
The drug has quite a large number of side effects. Systemic reactions include skin rashes, aplastic anemia, bitterness in the mouth, Stevens-Johnson syndrome, asthenia, headache. Local reactions include ocular hypotension, retinal detachment after surgery, itching, irritation, keratitis, and photophobia.
In case of overdose, acidosis and central nervous system pathologies may appear..
If such symptoms occur, you should consult your doctor as soon as possible. Symptomatic therapy may be prescribed.
Interactions
No special studies have been conducted regarding the interaction of Dorzopt plus with other medications.
Increased hypotension, bradycardia and cardiac depression are possible with simultaneous use of systemic beta-blockers, antiarrhythmics, calcium blockers, glycosides, opioid analgesics, parasympathomimetics, MAO inhibitors.
With simultaneous administration of CYP2D6 inhibitors, the systemic effects of beta blockers (depression, bradycardia, etc.) may be enhanced.
Since Dorzopt plus can penetrate into the systemic circulation in some quantities, it may increase the toxic effects of large doses of salicylates.
It is not recommended to combine Dorzopt Plus with systemic carbonic anhydrase inhibitors.
